Papers by Mohammed Gulzar Ahmed
Indexed in Index Copernicus Chemical Abstract Indian Citation Index (ICI)
Objective: The oral bioavailability of Candesartan cilexetil is less (<15%), so in this study an ... more Objective: The oral bioavailability of Candesartan cilexetil is less (<15%), so in this study an approach has been made to increase its bioavailability by proniosomal gel formulation. Methods: The proniosomal formulation of Candesartan cilexetil was prepared by slurry method, using span 60 and Tween 60 as non-ionic surfactants, maltodextrin as carrier and cholesterol and soya lecithin as stabilizers. Prepared gel formulations were evaluated for compatibility study, entrapment efficiency, vesicle size, surface morphology, in-vitro diffusion studies, in-vitro skin permeation studies, in-vivo pharmacokinetics studies, various release kinetic studies and stability studies. Results: FT-IR study showed no interaction between drugs and other excipients, drugs and excipients are compatible. Mean vesicles size of proniosome derived niosome was found in the range of 16.34 µm-32.48 µm and 7.25-16.45 µm before and after shaking. An optimized formulation A3 containing a 2:1 ratio of span 60 and cholesterol showed maximum entrapment (86.17%) and in-vitro drug release (93.8%) compared to other formulations. In-vitro skin permeation studies were carried out using Albino rat skin and results showed that formulation A3 exhibited 88.65% drug permeation in a steady-state manner over a period of 24 h with a flux value of 1.94 µg/cm 2 /h and enhancement ratio of 3.73. In-vivo pharmacokinetics studies of proniosomal gel formulation A3 showed a significant increase in bioavailability (1.425 folds) compared with an oral formulation of Candesartan cilexetil. Stability studies showed that proniosomal gel formulation was stable throughout its study period. Conclusion: Physiochemically stable Candesartan cilexetil proniosomal gel was formulated, which could deliver significant amount of the drug across the skin in a steady-state manner for the prolong period of time in the treatment of hypertension.
Abstract:
Periodontitis is an inflammatory disease of the supporting tissues of the teeth caused ... more Abstract:
Periodontitis is an inflammatory disease of the supporting tissues of the teeth caused by groups of specific
microorganisms. Local delivery of tetracycline antibiotics has been investigated for the possibility of
overcoming the limitations of conventional therapy. The goal of this research work is to prepare nanoparticles
and microspheres containing minocycline hydrochloride, these tiny particles are formulated into in-situ gels as
a local drug delivery system within the periodontal pockets for the effective treatment of periodontitis. FT-IR
studies indicated that there was no chemical interaction between drug and polymer and stability of the drug.
The microspheres were prepared by emulsion cross linking method using chitosan as a polymer. Nanoparticles
containing Minocycline hydrochloride were developed by using eudragit RL 100 as polymer. Microspheres
and nanoparticles were evaluated for drug content, particle size analysis and stability studies. The physicochemical
parameters reveal that microspheres have a discrete spherical structure without aggregation. The
average particle size of minocycline nanoparticles and microspheres were within the range. On the other hand
optimized formulations ofin-situ gels containing nanoparticles, microspheres and pure drug were prepared by
using gellan gum (0.6 % w/v) and comparative in-vitro diffusion study have done for these in-situ gel
formulations. No appreciable difference was observed in the extent of degradation of product during 60 days
in which nanoparticles and microspheres were stored at 40°C/ 75% RH.
Key words: periodontitis,minocycline hydrochloride, nanoparticles, microspheres and In-situ gels.
ABSTRACT
The main aim of present work was to formulate and evaluate sustain release matrix tablet... more ABSTRACT
The main aim of present work was to formulate and evaluate sustain release matrix tablets of Valsartan, an angiotensin II Receptor type 1 antagonist. Sustain release formulation are those which delivers the drug locally or systemically at a predetermined rate for a fixed period of time. The matrix table was prepared by direct compression method using by various concentration of chitosan and sodium alginate with combination of various release retardant polymer. The powder mixtures were subjected to various pre-compression and post compression parameters. In-vitro dissolution studies were carried out for 24 hours using 0.1 N HCL for first 2 hours and pH 6.8 phosphate buffer for 24 hours and the result indicates that formulations F4 and F7 showed good dissolution profile compare to other formulations. The
compatibility of the drug, polymers and other excipients were determined by FT-IR Spectroscopy. Results showed that the drug was compatible with polymers and other
Objective: The main objective of present study was to formulate and evaluate methyl cellulose bas... more Objective: The main objective of present study was to formulate and evaluate methyl cellulose based in
situ gel of rosuvastatin for the treatment of periodontal diseases.
Methods: The rosuvastatin in situ gel was prepared by using different concentration of methyl cellulose as
gel base and gel was evaluated for pH, viscosity, rheology, drug content, syringeability, spreadability, drug
release and drug release kinetics studies.
Results: Compatibility study was performed using FT-IR and results showed there was no interaction
between drug and other excipients. Viscosity of all formulations was found in the range of 320-590
centipoise and all formulations exhibited shear thinning pseudoplastic behaviour. Gelation time and
temperature was found in the range of 2-15 min and 26oC-39oC respectively. All the formulation except
formulation F6, F7 and G8 passed syringeabilitytest, as these formulations easily gets expelled from the
syringe. An in vitro release study was conducted using 1.2 pH buffer for 8 hours and results showed that
formulation F5 containing 0.9% methyl cellulose was considered as optimum formulation as it released
54.33% drug at the end 8 hours. In vitro release study revealed that release rate of drug from the in situ gel
was concentration dependent; as concentration of methyl cellulose increased the drug release rate was
retarded. Conclusion:Thus, it can be concluded that formulation F5 containing 0.9%w/v of methyl
cellulose as gel base was considered as an optimized formulation, as it release drug in sustain manner in
the treatment of periodontal diseases.
Candesartan is an angiotensin II receptor antagonist and is widely used in the management of hype... more Candesartan is an angiotensin II receptor antagonist and is widely used in the management of hypertension to reduce cardiovascular mortality in patients with left ventricular dysfunction following myocardial infarction, and in the management of heart failure. The Mucoadhesive buccal tablets were prepared by direct compression method using carbopol 934, HPMC K4M, sodium CMC as mucoadhesive polymer. The compatibility studies of drug and excipients were performed by FT-IR spectroscopy. After examining the flow properties of the powder blends the results are found to be within prescribed limits and indicated good flowing property, hence it was subjected to tablet compression. The tablets were evaluated for post-compression parameters like weight variation, hardness, thickness, friability, drug content uniformity, Surface pH, in-vitro studies like swelling, mucoadhesive strength and drug release. Formulation (F6) containing Carbopol-934 and Sodium CMC in the ratio of (2: 3) showed good mucoadhesive strength (36.14) and maximum drug release of 98.15% in 8 hrs. Swelling increases with increase in concentration of Sodium CMC in tablets. The drug content of shown highest of 99.15 %, Surface pH was found to be 6.42. All the evaluation parameters given the positive results and comply with the standards. Stability studies were carried out on the developed formulations indicated that the formulations were stable during the study period. The results indicate that the mucoadhesive buccal tablets of Candesartan may be good choice to bypass the extensive hepatic first pass metabolism with an improvement in the bioavailability of candesartan through buccal mucosa.
Key Words: Mucoadhesive buccal tablets, direct compression, Hypertension, Candesartan cilexetil,
The aim of the present work was to develop sustained release matrix
tablets of Lornoxicam using p... more The aim of the present work was to develop sustained release matrix
tablets of Lornoxicam using polymers such as carbopol, Eudragit
RS100, polyvinylpyrrolidone, ethyl cellulose, pectin as carriers in
various concentrations. Matrix tablets were prepared by direct
compression method. Prepared formulations were subjected to various
evaluation parameters like hardness, friability, thickness, % drug
content, weight variation etc. In-vitro dissolution studies were carried
out for 12 hrs. The tablets were subjected to in-vitro drug release in 1.2
pH for first 2 hrs then followed by 6.8 pH phosphate buffer for next 10
hrs and the results showed that among the ten formulations F2 and F4
showed good dissolution profile to control the drug release
respectively. Combination of polymers shows greater retarding of drug
release. The compatibility of the drug and polymer were determined by FT-IR spectroscopy.
Results showed that the drug was compatible with all polymers. The release data was fitted to
various mathematical models such as Higuchi, Korsmeyer-peppas, Hixson crowell, Zero
order and first order to evaluate the kinetics of drug release. The drug release follows mixed
order kinetics and mechanism was found to be non-fickian diffusion. The stability studies
were carried out according to the ICH guideline which indicates the selected formulation (F2
& F4) was stable. In conclusion, the results suggest that the developed matrix tablets of
Lornoxicam shows to improved efficacy and better patient compliance.
ABSTRACT
Dimenhydrinate is a salt of Diphenhydramine and 8-
chlorotheophylline. Diphenhydramine i... more ABSTRACT
Dimenhydrinate is a salt of Diphenhydramine and 8-
chlorotheophylline. Diphenhydramine is an Antihistaminic drug that is
antagonistic at the H1receptor in order to prevent and treat nausea and
motion sickness. 8-chlorotheophylline is added to counteract
drowsiness triggered by diphenhydramine. Dimenhydrinate mouth
dissolving tablets were prepared by direct compression technique by
using mannitol as a diluent, crospovidoneand sodium starch glycolate
as a superdisintegrants, Aspartame as a sweetening agent which is
suitable for diabetic patients. Drug compatibility with excipients was
checked by FTIR studies. After examining the flow properties of the
powder blends, the results are found to bewithin prescribed limits and indicated good flow
property, it was subjected to tablet compression. All the formulations were subjected to post
compression parameters such ashardness and friability (≤1%), indicated that tablets had a
good mechanical strength and resistance.Percentage cumulative drug release was found to be
in the range of 87.08 to 94.35 %. The wetting time was found to be in the range of 15.9±0.62
to 32.4±0.47 seconds. Among all the designed formulations, formulation MDF2 was found to
be promising and displayed an in-vitro disintegration time, in-vitro dispersion time of
10.57±0.93 and 25.87±1.29 seconds respectively, which facilitates its faster disintegration
and dispersion in the mouth.Depend upon percentage cumulative drug release, in-vitro
disintegration time, in-vitro dispersion time, wetting time results, oneformulationMDF2 were
selected for stability studies and subjected at 400C/75%RH for 2 months. Formulations
MDF2 found tobe stable after performing physical and chemical parameters at suitable
intervals.
ABSTRACT
The objective of the research project is to enhance of the solubility of
Glimepiride by ... more ABSTRACT
The objective of the research project is to enhance of the solubility of
Glimepiride by using solid dispersion technique and the production of
GMP tablets showing prolonged effect. The polymers used were β-
Cyclodextrin (β-CD) and Poloxamer 188 (PLX-188) and solid
dispersions were prepared by physical mixture (PHY) and Solvent
evaporation (SE) method. Solid dispersions with different ratios 1:1,
1:3, 1:5 (using physical mixture and solvent evaporation method were
prepared). The prepared solid dispersions were characterized by
Physical appearance, FT-IR, % Drug content were evaluated. F1 to
F19 tablet formulations were prepared by dry granulation technique,
lactose monohydrate used as a filler, HPMC as a binder, ethyl alcohol
used as a granulating agent, ethyl cellulose used as a granules coating
polymer and each formulation GMP containing; a) GMP alone, b)
GMP : β-CD (1:1, 1:3,1:5) PHY and SE, c) GMP : PLX-188 (1:1, 1:3,1:5) PHY and SE and,
d) GMP: β-CD: PLX-188 (1:1:1, 1:2:2,1:3:3) PHY and SE. The solvent evaporation method
showed more enhancement of GMP solubility than the Physical mixture. Finally, optimized
coated granules were evaluated for their micromeritic properties such as true density, tapped
density, Carr's index, and flow properties show satisfactory results. Tablet formulations were
evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight
variation, drug content, in-vitro dissolution profiles. The dissolution results revealed that
formulations F12 showed 96.15%, F15 showed 94.93% and F18 showed 97.67% of drug
release at the end of 12 hrs. The drug release follows mixed order kinetics and the mechanism
was found to be diffusion and non-fickian release. Based on the results of in-vitro and
ABSTRACT
The aim of the study was to improve the solubility and dissolution rate
of the drug Vera... more ABSTRACT
The aim of the study was to improve the solubility and dissolution rate
of the drug Verapamil HCL using solid-dispersion-Sustained release
matrix tablets by direct compression method. Solid dispersions were
prepared by solvent evaporation technique using PEG 6000 poloxamer
188 and Urea as carriers. The solid dispersions were characterized by
using FTIR and confirmed that no chemical interaction during
entrapment process. The prepared solid dispersions were formulated in
matrix tablets evaluated for pre-compression and post-compression
parameters. The post compression parameters were evaluated for
hardness, friability, weight variation and drug content which were
within the acceptable official limits. The drug content was found to be
high and uniformly distributed in all formulations. It was shown that
with the developed formulations, the release and dissolution of drug
from the tablets can be increased by formulating it as solid dispersion tablets. It was
concluded that development of sustained release solid-dispersion tablets using poloxamer 188
[97%] with HPMC K4m results highest increase in dissolution rate and optimum rate of drug
and reduced crystallinity of Verapamil HCL can account for the faster dissolution of the
released drug from the polymer matrix.
ABSTRACT
Background and purpose of the study: Osteoarthritis (OA) is the
most common joint disord... more ABSTRACT
Background and purpose of the study: Osteoarthritis (OA) is the
most common joint disorder worldwide. Generally, oral dosage forms
are used for the treatment of OA but they have some disadvantages like
slow absorption and thus, onset of action is prolong. This can be
overcome by administrating the drug in liquid form but, many APIs
have limited level of stability in liquid form. Recently, effervescent
drug delivery systems have started gaining popularity, because they are
easy to administer and lead to better compliance. The aim of this study
is to formulate effervescent tablet with sufficient mechanical integrity
and to achieve faster disintegration in water. Method: They are
intended to be dissolved or dispersed in water before use. The study was designed to assess
the treatment for osteoarthritis by using combination of drugs such as Ibuprofen,
Glucosamine and Vitamin E in an effective way. The dosage of Ibuprofen is reduced by
addition of glucosamine sulphate (nutraceutical) on an assumption that the activity of
ibuprofen may be enhanced by nutraceutical. The formulations were subjected to various
evaluation tests. Results: All the formulations have shown good effervescence when placed
in 100 ml of water. The resultant solution appeared clear indicating the solubility of
ingredients in water. The friability and hardness of formulations are in the acceptable range.
The Angle of Repose (θ), Hausner’s Ratio and Carr’s Compressibility Index (%) revealed
that the formulations have good flow property. The solution time, CO2 and moisture content
of all the formulations are in the acceptable range. Conclusion: All the results concluded that
effervescent tablet preparation containing ibuprofen in combination with glucosamine
Indian J Pharm Educ Res, 2008
, the neglected group of enzymes possess panoramic utility in biotechnology processes and therapy... more , the neglected group of enzymes possess panoramic utility in biotechnology processes and therapy. Hyaluronidase is a general term used to describe enzymes that are able to break down primarily hyaluronan and other glucoseaminoglycans which facilitates the invasion of the host tissues, by bacterial pathogen, mostly Gram-positive. Hyaluronic acid (HA) is the most abundant glucoseaminoglycan of the extracellular matrix (ECM) of connective tissues responsible for cellular attachment and locomotion. The present work encompasses therapeutic, pathophysiological, physiological and biological importance of the enzyme which aids in production of pure, potent, stable microbial hyaluronidases with its specific and selective inhibitors, as an alternative approach in designing and development of targeted drugs, potent vaccines and pharmaceuticals.
The main objective of present study is to formulate and evaluate hydrogel contact lenses
of sparf... more The main objective of present study is to formulate and evaluate hydrogel contact lenses
of sparfloxacin and diclofenac sodium by using HEMA (hydroxyl ethyl methacrylate)
and 4- Vinyl pyridine (monomers) for the treatment of ocular infections. Sparfloxacin
has in vitro activity against a wide range of gram-negative and gram-positive
microorganisms. The incorporation of ionic/hydrophobic monomer would increase
the interaction between hydrogel and drugs so that drugs will take long time to diffuse
from the hydrogel. The developed formulations were evaluated for water content,
center thickness, in–vitro drug release and stability studies. Compatibility study performed
by FT-IR method showed no interaction between drug and other excipients.
Water content of formulations S1, S2 and S3 were found be 4.2, 3.2 and 4.1% respectively.
Centre thickness of the formulations S1, S2 and S3 was found to be 6.6, 6.5 and
6.4μm respectively. Drugs are delivered by soaking the contact lenses in drug solution
to load the drugs. In-vitro release study revealed that release rate of drug from hydrogel
contact lenses dependent on concentration of 4-polyvinyl pyridine. The antimicrobial
studies against p.aureginus were performed for the formulation S2 which showed
more drug release compared other formulations. All the results were found that pure
drug has more bacterial inhibition activity initially compared to formulation S2. Thus,
it can be concluded that formulation S2 containing 0.5% w/v of 4-poly vinyl pyridine
as monomer was considered as an optimized formulation, as it provided sustained
release of the drug for the treatment of ocular infections.
Aim and Background: The purpose of present investigation was to develop proniosomal formulation o... more Aim and Background: The purpose of present investigation was to develop proniosomal formulation of Diclofenac Sodium by
slurry method based on non-ionic surfactants (tween 60), cholesterol and maltodextrin as a carrier. Materials and Methods:Four
formulations were prepared using maltodextrin as a carrier, cholesterol, tween 60, carbopol 934P as polymers. Proniosomal
formulations were prepared using slurry method. The proniosomal formulation was evaluated for FT-IR study, scanning electron
microscopy, stability study, In-vitro release study respectively. Further stability studies were carried out for 12 weeks in
accelerated conditions at 25 C and 60% RH. Results:The result from scanning electron microscopy analyses was con?rmed that 0
the surface of proniosomewas smooth. The formulation F4 which showed higher entrapment ef?ciency of 77.23% with tween 60
respectively and in-vitro releases of 77.01% at the end of 24 hrs was found to be best among the all 4 formulations. The drug
release follows Higuchi and Korsmeyer peppas model (mixed order). Kinetic analysis shows that the drug release follows ?ckian
release mechanism. FT-IR spectroscopic studies revealed no interaction between drug and polymer. The stability studies
indicated that F4 formulations were stable for 12 weeks. Conclusion: Proniosomal formulation could be a promising delivery
system for Diclofenac Sodium with improved bioavailability and better controlled drug release.
Purpose: The main objective of present study is to formulate and evaluate methyl cellulose based ... more Purpose: The main objective of present study is to formulate and evaluate methyl cellulose based in situ periodontal gel of Atorvastatin. Approach: The in situ gel was prepared by using different concentration of methyl cellulose and gel was evaluated for pH, viscosity and rheology, syringeability, drug content, in vitro drug release, and drug release kinetics. Findings: Compatibility study was performed using FTIR and results showed there was no interaction between drug and other excipients. Viscosity of all formulations was found in the range of 320-570 centipoise and all formulations exhibited pseudoplastic behaviour. Gelation time and temperature was found in the range of 6-17 min and 29o-39o respectively. All the formulation except formulation G6 and G7 showed satisfactory syringeability due to lower concentration of polymer. Based on the results of release study, formulation G5 was found to be optimum formulation as it released 96.87% drug at the end of 24 h. In vitro release study revealed that release rate of drug from the in situ gel was concentration dependent; as concentration of methyl cellulose increased the drug release rate was retarded. Conclusion: It can be concluded that formulation containing 0.9%w/v of methyl cellulose gave optimized formulation.
Olmesartan medoxomil (OLM) is a prodrug of Olmesartan, a selective AT1 subtype angiotensin-II rec... more Olmesartan medoxomil (OLM) is a prodrug of Olmesartan, a selective AT1 subtype angiotensin-II receptor antagonist for the treatment of hypertension. The purpose of the study was to enhance the aqueous solubility of OLM by three different approaches; solid dispersion (SD), complexation and selfemulsification. The SD was prepared by solvent evaporation method using poloxamer188 as a carrier. In complexation technique, inclusion complex of drug and β-cyclodextrin was formulated following solvent evaporation technique. In selfemulsification method soya bean oil, tween 80 and PEG 400 were used as oil, surfactants and co-surfactant respectively. The prepared formulations were characterized for compatibility, drug content, saturation solubility,dissolution studies and stability studies. FT-IR study revealed no interaction between drug and excipients. Among all methods solid dispersion (SD3) containing drug: poloxamer188 in the ratio of 1:4 showed rapid and higher drug release (88.36% within 45 min). The in-vitro drug release data was fitted to various kinetic models and all the formulations showed first order kinetics following super case II mechanism. The increase in dissolution rate of Olmesartan medoxomil from solid dispersion of poloxamer 188 might be due to reduction of crystal size of the drug, conversion of
Epilepsy is abnormal, high frequency electrical discharge in brain characterized by transient epi... more Epilepsy is abnormal, high frequency electrical discharge in brain characterized by transient episode (seizure)
with or without loss of consciousness and characteristic body movement (convulsion). Among many drug of
antiepileptic drug, Divalproex sodium is considered as the most important antiepileptic drug and widely used for
treatment of epilepsy. The present work has been done to formulate sustained release tablets of divalproex
sodium containing HPMC K4M and HPMC K100M as release retarding agent. The FTIR study revealed that
there was no interaction between drug and polymer and combination can be safely prepared. The tablets were
prepared by wet granulation technique using PVP K30 solution as binding agent. Tablets were evaluated for
hardness, thickness, weight variation, disintegration time, drug content and in vitro drug release. All the physical
parameters were in acceptable limit of pharmacopeial specification. The in vitro release of sustained release
tablet was carried out for 18 hours using USP type-II apparatus (DS-1800) at 100 rpm for the first 45 minute in
900 ml 0.1N HCL maintaining at 37 ± 0.50C and then at phosphate buffer pH 6.8 in 900ml for another 18 hour.
The optimized formulation (F8) was found to exhibit more than 90% after 18 hours. Further the drug release of
sustained release tablets was compared with the conventional tablet which was prepared by using 5% micro
crystalline cellulose (MCC) as disintegrating agent. The stability studies, shown the optimized tablets of
immediate release formulation were stable at 400C / 75% RH for a period of 3 months.
The main aim of present work was to formulate and evaluate
controlled release matrix tablets of p... more The main aim of present work was to formulate and evaluate
controlled release matrix tablets of pregabalin; an antiepileptic drug.
Controlled release formulation is such drug delivery system that
delivers the drug locally or systemically at a predetermined rate for a
fixed period of time. The matrix tablet were prepared by direct
compression method using by various concentration of chitosan with
combination of various release retardant polymers like HPMC K100M,
carbopol 934P, xanthan gum and trisodium citrate as cross-linking
agent. Compatibility of the drug with the polymers was studied using
Fourier transform infrared spectroscopy and result showed no possible
interaction between drug and excipients. The powder mixtures were
subjected to pre-compression studies and obtained results were found
to be satisfactory. The compressed tablets were evaluated for postcompression
parameters such as weight variation, hardness, drug content, swelling study, invitro
drug release and stability studies. Swelling studies were carried out using water uptake
method and results revealed that formulation F3 containing higher concentration of carbopol
and chitosan showed highest swelling capacity. In-vitro dissolution studies were carried out
for 24 hours using 0.06N HCL for first 2 hours and pH 6.8 phosphate buffer for remaining 22
hours. Formulation F3 was able to release 99.45% drug at the end of 24 hours. The release
data were fitted to various mathematical models and it was found that formulation batches
followed first order release kinetics indicating drug release was concentration dependent.
Formulation F3 and F9 were subjected to short term stability studies and were
physiochemically stable throughout the study period.
Divalproex sodium is considered as the most important antiepileptic drug and widely used for trea... more Divalproex sodium is considered as the most important antiepileptic drug and widely used for treatment of epilepsy,
bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate immediate release
tablets of divalproex sodium containing sodium starch glycolate (SSG) and croscarmellose as super disintegrating
agents. The FTIR study revealed that there was no interaction between drug and polymer and combination can be
safely prepared. The tablets were prepared by wet granulation technique as poor flow property exhibited by pure
drug. Tablets were evaluated for hardness, thickness, weight variation, disintegration time, drug content and in vitro
drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. In vitro drug
release studies were performed using USP type II apparatus (paddle method) in 900 ml of phosphate buffer pH 6.8
at 100 rpm. The optimized formulation (F6) was found to exhibit the highest in- vitrodrug release of 98.11percent at
the end of 20 minutes. Further the drug release of immediate release tablets was compared with the drug release
profile of conventional tablet which was prepared by using 5% micro crystalline cellulose (MCC) as disintegrating
agent. The stability studies, shown the optimized tablets of immediate release formulation were stable at 400C / 75%
RH for a period of 3 months.
Uploads
Papers by Mohammed Gulzar Ahmed
Periodontitis is an inflammatory disease of the supporting tissues of the teeth caused by groups of specific
microorganisms. Local delivery of tetracycline antibiotics has been investigated for the possibility of
overcoming the limitations of conventional therapy. The goal of this research work is to prepare nanoparticles
and microspheres containing minocycline hydrochloride, these tiny particles are formulated into in-situ gels as
a local drug delivery system within the periodontal pockets for the effective treatment of periodontitis. FT-IR
studies indicated that there was no chemical interaction between drug and polymer and stability of the drug.
The microspheres were prepared by emulsion cross linking method using chitosan as a polymer. Nanoparticles
containing Minocycline hydrochloride were developed by using eudragit RL 100 as polymer. Microspheres
and nanoparticles were evaluated for drug content, particle size analysis and stability studies. The physicochemical
parameters reveal that microspheres have a discrete spherical structure without aggregation. The
average particle size of minocycline nanoparticles and microspheres were within the range. On the other hand
optimized formulations ofin-situ gels containing nanoparticles, microspheres and pure drug were prepared by
using gellan gum (0.6 % w/v) and comparative in-vitro diffusion study have done for these in-situ gel
formulations. No appreciable difference was observed in the extent of degradation of product during 60 days
in which nanoparticles and microspheres were stored at 40°C/ 75% RH.
Key words: periodontitis,minocycline hydrochloride, nanoparticles, microspheres and In-situ gels.
The main aim of present work was to formulate and evaluate sustain release matrix tablets of Valsartan, an angiotensin II Receptor type 1 antagonist. Sustain release formulation are those which delivers the drug locally or systemically at a predetermined rate for a fixed period of time. The matrix table was prepared by direct compression method using by various concentration of chitosan and sodium alginate with combination of various release retardant polymer. The powder mixtures were subjected to various pre-compression and post compression parameters. In-vitro dissolution studies were carried out for 24 hours using 0.1 N HCL for first 2 hours and pH 6.8 phosphate buffer for 24 hours and the result indicates that formulations F4 and F7 showed good dissolution profile compare to other formulations. The
compatibility of the drug, polymers and other excipients were determined by FT-IR Spectroscopy. Results showed that the drug was compatible with polymers and other
situ gel of rosuvastatin for the treatment of periodontal diseases.
Methods: The rosuvastatin in situ gel was prepared by using different concentration of methyl cellulose as
gel base and gel was evaluated for pH, viscosity, rheology, drug content, syringeability, spreadability, drug
release and drug release kinetics studies.
Results: Compatibility study was performed using FT-IR and results showed there was no interaction
between drug and other excipients. Viscosity of all formulations was found in the range of 320-590
centipoise and all formulations exhibited shear thinning pseudoplastic behaviour. Gelation time and
temperature was found in the range of 2-15 min and 26oC-39oC respectively. All the formulation except
formulation F6, F7 and G8 passed syringeabilitytest, as these formulations easily gets expelled from the
syringe. An in vitro release study was conducted using 1.2 pH buffer for 8 hours and results showed that
formulation F5 containing 0.9% methyl cellulose was considered as optimum formulation as it released
54.33% drug at the end 8 hours. In vitro release study revealed that release rate of drug from the in situ gel
was concentration dependent; as concentration of methyl cellulose increased the drug release rate was
retarded. Conclusion:Thus, it can be concluded that formulation F5 containing 0.9%w/v of methyl
cellulose as gel base was considered as an optimized formulation, as it release drug in sustain manner in
the treatment of periodontal diseases.
Key Words: Mucoadhesive buccal tablets, direct compression, Hypertension, Candesartan cilexetil,
tablets of Lornoxicam using polymers such as carbopol, Eudragit
RS100, polyvinylpyrrolidone, ethyl cellulose, pectin as carriers in
various concentrations. Matrix tablets were prepared by direct
compression method. Prepared formulations were subjected to various
evaluation parameters like hardness, friability, thickness, % drug
content, weight variation etc. In-vitro dissolution studies were carried
out for 12 hrs. The tablets were subjected to in-vitro drug release in 1.2
pH for first 2 hrs then followed by 6.8 pH phosphate buffer for next 10
hrs and the results showed that among the ten formulations F2 and F4
showed good dissolution profile to control the drug release
respectively. Combination of polymers shows greater retarding of drug
release. The compatibility of the drug and polymer were determined by FT-IR spectroscopy.
Results showed that the drug was compatible with all polymers. The release data was fitted to
various mathematical models such as Higuchi, Korsmeyer-peppas, Hixson crowell, Zero
order and first order to evaluate the kinetics of drug release. The drug release follows mixed
order kinetics and mechanism was found to be non-fickian diffusion. The stability studies
were carried out according to the ICH guideline which indicates the selected formulation (F2
& F4) was stable. In conclusion, the results suggest that the developed matrix tablets of
Lornoxicam shows to improved efficacy and better patient compliance.
Dimenhydrinate is a salt of Diphenhydramine and 8-
chlorotheophylline. Diphenhydramine is an Antihistaminic drug that is
antagonistic at the H1receptor in order to prevent and treat nausea and
motion sickness. 8-chlorotheophylline is added to counteract
drowsiness triggered by diphenhydramine. Dimenhydrinate mouth
dissolving tablets were prepared by direct compression technique by
using mannitol as a diluent, crospovidoneand sodium starch glycolate
as a superdisintegrants, Aspartame as a sweetening agent which is
suitable for diabetic patients. Drug compatibility with excipients was
checked by FTIR studies. After examining the flow properties of the
powder blends, the results are found to bewithin prescribed limits and indicated good flow
property, it was subjected to tablet compression. All the formulations were subjected to post
compression parameters such ashardness and friability (≤1%), indicated that tablets had a
good mechanical strength and resistance.Percentage cumulative drug release was found to be
in the range of 87.08 to 94.35 %. The wetting time was found to be in the range of 15.9±0.62
to 32.4±0.47 seconds. Among all the designed formulations, formulation MDF2 was found to
be promising and displayed an in-vitro disintegration time, in-vitro dispersion time of
10.57±0.93 and 25.87±1.29 seconds respectively, which facilitates its faster disintegration
and dispersion in the mouth.Depend upon percentage cumulative drug release, in-vitro
disintegration time, in-vitro dispersion time, wetting time results, oneformulationMDF2 were
selected for stability studies and subjected at 400C/75%RH for 2 months. Formulations
MDF2 found tobe stable after performing physical and chemical parameters at suitable
intervals.
The objective of the research project is to enhance of the solubility of
Glimepiride by using solid dispersion technique and the production of
GMP tablets showing prolonged effect. The polymers used were β-
Cyclodextrin (β-CD) and Poloxamer 188 (PLX-188) and solid
dispersions were prepared by physical mixture (PHY) and Solvent
evaporation (SE) method. Solid dispersions with different ratios 1:1,
1:3, 1:5 (using physical mixture and solvent evaporation method were
prepared). The prepared solid dispersions were characterized by
Physical appearance, FT-IR, % Drug content were evaluated. F1 to
F19 tablet formulations were prepared by dry granulation technique,
lactose monohydrate used as a filler, HPMC as a binder, ethyl alcohol
used as a granulating agent, ethyl cellulose used as a granules coating
polymer and each formulation GMP containing; a) GMP alone, b)
GMP : β-CD (1:1, 1:3,1:5) PHY and SE, c) GMP : PLX-188 (1:1, 1:3,1:5) PHY and SE and,
d) GMP: β-CD: PLX-188 (1:1:1, 1:2:2,1:3:3) PHY and SE. The solvent evaporation method
showed more enhancement of GMP solubility than the Physical mixture. Finally, optimized
coated granules were evaluated for their micromeritic properties such as true density, tapped
density, Carr's index, and flow properties show satisfactory results. Tablet formulations were
evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight
variation, drug content, in-vitro dissolution profiles. The dissolution results revealed that
formulations F12 showed 96.15%, F15 showed 94.93% and F18 showed 97.67% of drug
release at the end of 12 hrs. The drug release follows mixed order kinetics and the mechanism
was found to be diffusion and non-fickian release. Based on the results of in-vitro and
The aim of the study was to improve the solubility and dissolution rate
of the drug Verapamil HCL using solid-dispersion-Sustained release
matrix tablets by direct compression method. Solid dispersions were
prepared by solvent evaporation technique using PEG 6000 poloxamer
188 and Urea as carriers. The solid dispersions were characterized by
using FTIR and confirmed that no chemical interaction during
entrapment process. The prepared solid dispersions were formulated in
matrix tablets evaluated for pre-compression and post-compression
parameters. The post compression parameters were evaluated for
hardness, friability, weight variation and drug content which were
within the acceptable official limits. The drug content was found to be
high and uniformly distributed in all formulations. It was shown that
with the developed formulations, the release and dissolution of drug
from the tablets can be increased by formulating it as solid dispersion tablets. It was
concluded that development of sustained release solid-dispersion tablets using poloxamer 188
[97%] with HPMC K4m results highest increase in dissolution rate and optimum rate of drug
and reduced crystallinity of Verapamil HCL can account for the faster dissolution of the
released drug from the polymer matrix.
Background and purpose of the study: Osteoarthritis (OA) is the
most common joint disorder worldwide. Generally, oral dosage forms
are used for the treatment of OA but they have some disadvantages like
slow absorption and thus, onset of action is prolong. This can be
overcome by administrating the drug in liquid form but, many APIs
have limited level of stability in liquid form. Recently, effervescent
drug delivery systems have started gaining popularity, because they are
easy to administer and lead to better compliance. The aim of this study
is to formulate effervescent tablet with sufficient mechanical integrity
and to achieve faster disintegration in water. Method: They are
intended to be dissolved or dispersed in water before use. The study was designed to assess
the treatment for osteoarthritis by using combination of drugs such as Ibuprofen,
Glucosamine and Vitamin E in an effective way. The dosage of Ibuprofen is reduced by
addition of glucosamine sulphate (nutraceutical) on an assumption that the activity of
ibuprofen may be enhanced by nutraceutical. The formulations were subjected to various
evaluation tests. Results: All the formulations have shown good effervescence when placed
in 100 ml of water. The resultant solution appeared clear indicating the solubility of
ingredients in water. The friability and hardness of formulations are in the acceptable range.
The Angle of Repose (θ), Hausner’s Ratio and Carr’s Compressibility Index (%) revealed
that the formulations have good flow property. The solution time, CO2 and moisture content
of all the formulations are in the acceptable range. Conclusion: All the results concluded that
effervescent tablet preparation containing ibuprofen in combination with glucosamine
of sparfloxacin and diclofenac sodium by using HEMA (hydroxyl ethyl methacrylate)
and 4- Vinyl pyridine (monomers) for the treatment of ocular infections. Sparfloxacin
has in vitro activity against a wide range of gram-negative and gram-positive
microorganisms. The incorporation of ionic/hydrophobic monomer would increase
the interaction between hydrogel and drugs so that drugs will take long time to diffuse
from the hydrogel. The developed formulations were evaluated for water content,
center thickness, in–vitro drug release and stability studies. Compatibility study performed
by FT-IR method showed no interaction between drug and other excipients.
Water content of formulations S1, S2 and S3 were found be 4.2, 3.2 and 4.1% respectively.
Centre thickness of the formulations S1, S2 and S3 was found to be 6.6, 6.5 and
6.4μm respectively. Drugs are delivered by soaking the contact lenses in drug solution
to load the drugs. In-vitro release study revealed that release rate of drug from hydrogel
contact lenses dependent on concentration of 4-polyvinyl pyridine. The antimicrobial
studies against p.aureginus were performed for the formulation S2 which showed
more drug release compared other formulations. All the results were found that pure
drug has more bacterial inhibition activity initially compared to formulation S2. Thus,
it can be concluded that formulation S2 containing 0.5% w/v of 4-poly vinyl pyridine
as monomer was considered as an optimized formulation, as it provided sustained
release of the drug for the treatment of ocular infections.
slurry method based on non-ionic surfactants (tween 60), cholesterol and maltodextrin as a carrier. Materials and Methods:Four
formulations were prepared using maltodextrin as a carrier, cholesterol, tween 60, carbopol 934P as polymers. Proniosomal
formulations were prepared using slurry method. The proniosomal formulation was evaluated for FT-IR study, scanning electron
microscopy, stability study, In-vitro release study respectively. Further stability studies were carried out for 12 weeks in
accelerated conditions at 25 C and 60% RH. Results:The result from scanning electron microscopy analyses was con?rmed that 0
the surface of proniosomewas smooth. The formulation F4 which showed higher entrapment ef?ciency of 77.23% with tween 60
respectively and in-vitro releases of 77.01% at the end of 24 hrs was found to be best among the all 4 formulations. The drug
release follows Higuchi and Korsmeyer peppas model (mixed order). Kinetic analysis shows that the drug release follows ?ckian
release mechanism. FT-IR spectroscopic studies revealed no interaction between drug and polymer. The stability studies
indicated that F4 formulations were stable for 12 weeks. Conclusion: Proniosomal formulation could be a promising delivery
system for Diclofenac Sodium with improved bioavailability and better controlled drug release.
with or without loss of consciousness and characteristic body movement (convulsion). Among many drug of
antiepileptic drug, Divalproex sodium is considered as the most important antiepileptic drug and widely used for
treatment of epilepsy. The present work has been done to formulate sustained release tablets of divalproex
sodium containing HPMC K4M and HPMC K100M as release retarding agent. The FTIR study revealed that
there was no interaction between drug and polymer and combination can be safely prepared. The tablets were
prepared by wet granulation technique using PVP K30 solution as binding agent. Tablets were evaluated for
hardness, thickness, weight variation, disintegration time, drug content and in vitro drug release. All the physical
parameters were in acceptable limit of pharmacopeial specification. The in vitro release of sustained release
tablet was carried out for 18 hours using USP type-II apparatus (DS-1800) at 100 rpm for the first 45 minute in
900 ml 0.1N HCL maintaining at 37 ± 0.50C and then at phosphate buffer pH 6.8 in 900ml for another 18 hour.
The optimized formulation (F8) was found to exhibit more than 90% after 18 hours. Further the drug release of
sustained release tablets was compared with the conventional tablet which was prepared by using 5% micro
crystalline cellulose (MCC) as disintegrating agent. The stability studies, shown the optimized tablets of
immediate release formulation were stable at 400C / 75% RH for a period of 3 months.
controlled release matrix tablets of pregabalin; an antiepileptic drug.
Controlled release formulation is such drug delivery system that
delivers the drug locally or systemically at a predetermined rate for a
fixed period of time. The matrix tablet were prepared by direct
compression method using by various concentration of chitosan with
combination of various release retardant polymers like HPMC K100M,
carbopol 934P, xanthan gum and trisodium citrate as cross-linking
agent. Compatibility of the drug with the polymers was studied using
Fourier transform infrared spectroscopy and result showed no possible
interaction between drug and excipients. The powder mixtures were
subjected to pre-compression studies and obtained results were found
to be satisfactory. The compressed tablets were evaluated for postcompression
parameters such as weight variation, hardness, drug content, swelling study, invitro
drug release and stability studies. Swelling studies were carried out using water uptake
method and results revealed that formulation F3 containing higher concentration of carbopol
and chitosan showed highest swelling capacity. In-vitro dissolution studies were carried out
for 24 hours using 0.06N HCL for first 2 hours and pH 6.8 phosphate buffer for remaining 22
hours. Formulation F3 was able to release 99.45% drug at the end of 24 hours. The release
data were fitted to various mathematical models and it was found that formulation batches
followed first order release kinetics indicating drug release was concentration dependent.
Formulation F3 and F9 were subjected to short term stability studies and were
physiochemically stable throughout the study period.
bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate immediate release
tablets of divalproex sodium containing sodium starch glycolate (SSG) and croscarmellose as super disintegrating
agents. The FTIR study revealed that there was no interaction between drug and polymer and combination can be
safely prepared. The tablets were prepared by wet granulation technique as poor flow property exhibited by pure
drug. Tablets were evaluated for hardness, thickness, weight variation, disintegration time, drug content and in vitro
drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. In vitro drug
release studies were performed using USP type II apparatus (paddle method) in 900 ml of phosphate buffer pH 6.8
at 100 rpm. The optimized formulation (F6) was found to exhibit the highest in- vitrodrug release of 98.11percent at
the end of 20 minutes. Further the drug release of immediate release tablets was compared with the drug release
profile of conventional tablet which was prepared by using 5% micro crystalline cellulose (MCC) as disintegrating
agent. The stability studies, shown the optimized tablets of immediate release formulation were stable at 400C / 75%
RH for a period of 3 months.
Periodontitis is an inflammatory disease of the supporting tissues of the teeth caused by groups of specific
microorganisms. Local delivery of tetracycline antibiotics has been investigated for the possibility of
overcoming the limitations of conventional therapy. The goal of this research work is to prepare nanoparticles
and microspheres containing minocycline hydrochloride, these tiny particles are formulated into in-situ gels as
a local drug delivery system within the periodontal pockets for the effective treatment of periodontitis. FT-IR
studies indicated that there was no chemical interaction between drug and polymer and stability of the drug.
The microspheres were prepared by emulsion cross linking method using chitosan as a polymer. Nanoparticles
containing Minocycline hydrochloride were developed by using eudragit RL 100 as polymer. Microspheres
and nanoparticles were evaluated for drug content, particle size analysis and stability studies. The physicochemical
parameters reveal that microspheres have a discrete spherical structure without aggregation. The
average particle size of minocycline nanoparticles and microspheres were within the range. On the other hand
optimized formulations ofin-situ gels containing nanoparticles, microspheres and pure drug were prepared by
using gellan gum (0.6 % w/v) and comparative in-vitro diffusion study have done for these in-situ gel
formulations. No appreciable difference was observed in the extent of degradation of product during 60 days
in which nanoparticles and microspheres were stored at 40°C/ 75% RH.
Key words: periodontitis,minocycline hydrochloride, nanoparticles, microspheres and In-situ gels.
The main aim of present work was to formulate and evaluate sustain release matrix tablets of Valsartan, an angiotensin II Receptor type 1 antagonist. Sustain release formulation are those which delivers the drug locally or systemically at a predetermined rate for a fixed period of time. The matrix table was prepared by direct compression method using by various concentration of chitosan and sodium alginate with combination of various release retardant polymer. The powder mixtures were subjected to various pre-compression and post compression parameters. In-vitro dissolution studies were carried out for 24 hours using 0.1 N HCL for first 2 hours and pH 6.8 phosphate buffer for 24 hours and the result indicates that formulations F4 and F7 showed good dissolution profile compare to other formulations. The
compatibility of the drug, polymers and other excipients were determined by FT-IR Spectroscopy. Results showed that the drug was compatible with polymers and other
situ gel of rosuvastatin for the treatment of periodontal diseases.
Methods: The rosuvastatin in situ gel was prepared by using different concentration of methyl cellulose as
gel base and gel was evaluated for pH, viscosity, rheology, drug content, syringeability, spreadability, drug
release and drug release kinetics studies.
Results: Compatibility study was performed using FT-IR and results showed there was no interaction
between drug and other excipients. Viscosity of all formulations was found in the range of 320-590
centipoise and all formulations exhibited shear thinning pseudoplastic behaviour. Gelation time and
temperature was found in the range of 2-15 min and 26oC-39oC respectively. All the formulation except
formulation F6, F7 and G8 passed syringeabilitytest, as these formulations easily gets expelled from the
syringe. An in vitro release study was conducted using 1.2 pH buffer for 8 hours and results showed that
formulation F5 containing 0.9% methyl cellulose was considered as optimum formulation as it released
54.33% drug at the end 8 hours. In vitro release study revealed that release rate of drug from the in situ gel
was concentration dependent; as concentration of methyl cellulose increased the drug release rate was
retarded. Conclusion:Thus, it can be concluded that formulation F5 containing 0.9%w/v of methyl
cellulose as gel base was considered as an optimized formulation, as it release drug in sustain manner in
the treatment of periodontal diseases.
Key Words: Mucoadhesive buccal tablets, direct compression, Hypertension, Candesartan cilexetil,
tablets of Lornoxicam using polymers such as carbopol, Eudragit
RS100, polyvinylpyrrolidone, ethyl cellulose, pectin as carriers in
various concentrations. Matrix tablets were prepared by direct
compression method. Prepared formulations were subjected to various
evaluation parameters like hardness, friability, thickness, % drug
content, weight variation etc. In-vitro dissolution studies were carried
out for 12 hrs. The tablets were subjected to in-vitro drug release in 1.2
pH for first 2 hrs then followed by 6.8 pH phosphate buffer for next 10
hrs and the results showed that among the ten formulations F2 and F4
showed good dissolution profile to control the drug release
respectively. Combination of polymers shows greater retarding of drug
release. The compatibility of the drug and polymer were determined by FT-IR spectroscopy.
Results showed that the drug was compatible with all polymers. The release data was fitted to
various mathematical models such as Higuchi, Korsmeyer-peppas, Hixson crowell, Zero
order and first order to evaluate the kinetics of drug release. The drug release follows mixed
order kinetics and mechanism was found to be non-fickian diffusion. The stability studies
were carried out according to the ICH guideline which indicates the selected formulation (F2
& F4) was stable. In conclusion, the results suggest that the developed matrix tablets of
Lornoxicam shows to improved efficacy and better patient compliance.
Dimenhydrinate is a salt of Diphenhydramine and 8-
chlorotheophylline. Diphenhydramine is an Antihistaminic drug that is
antagonistic at the H1receptor in order to prevent and treat nausea and
motion sickness. 8-chlorotheophylline is added to counteract
drowsiness triggered by diphenhydramine. Dimenhydrinate mouth
dissolving tablets were prepared by direct compression technique by
using mannitol as a diluent, crospovidoneand sodium starch glycolate
as a superdisintegrants, Aspartame as a sweetening agent which is
suitable for diabetic patients. Drug compatibility with excipients was
checked by FTIR studies. After examining the flow properties of the
powder blends, the results are found to bewithin prescribed limits and indicated good flow
property, it was subjected to tablet compression. All the formulations were subjected to post
compression parameters such ashardness and friability (≤1%), indicated that tablets had a
good mechanical strength and resistance.Percentage cumulative drug release was found to be
in the range of 87.08 to 94.35 %. The wetting time was found to be in the range of 15.9±0.62
to 32.4±0.47 seconds. Among all the designed formulations, formulation MDF2 was found to
be promising and displayed an in-vitro disintegration time, in-vitro dispersion time of
10.57±0.93 and 25.87±1.29 seconds respectively, which facilitates its faster disintegration
and dispersion in the mouth.Depend upon percentage cumulative drug release, in-vitro
disintegration time, in-vitro dispersion time, wetting time results, oneformulationMDF2 were
selected for stability studies and subjected at 400C/75%RH for 2 months. Formulations
MDF2 found tobe stable after performing physical and chemical parameters at suitable
intervals.
The objective of the research project is to enhance of the solubility of
Glimepiride by using solid dispersion technique and the production of
GMP tablets showing prolonged effect. The polymers used were β-
Cyclodextrin (β-CD) and Poloxamer 188 (PLX-188) and solid
dispersions were prepared by physical mixture (PHY) and Solvent
evaporation (SE) method. Solid dispersions with different ratios 1:1,
1:3, 1:5 (using physical mixture and solvent evaporation method were
prepared). The prepared solid dispersions were characterized by
Physical appearance, FT-IR, % Drug content were evaluated. F1 to
F19 tablet formulations were prepared by dry granulation technique,
lactose monohydrate used as a filler, HPMC as a binder, ethyl alcohol
used as a granulating agent, ethyl cellulose used as a granules coating
polymer and each formulation GMP containing; a) GMP alone, b)
GMP : β-CD (1:1, 1:3,1:5) PHY and SE, c) GMP : PLX-188 (1:1, 1:3,1:5) PHY and SE and,
d) GMP: β-CD: PLX-188 (1:1:1, 1:2:2,1:3:3) PHY and SE. The solvent evaporation method
showed more enhancement of GMP solubility than the Physical mixture. Finally, optimized
coated granules were evaluated for their micromeritic properties such as true density, tapped
density, Carr's index, and flow properties show satisfactory results. Tablet formulations were
evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight
variation, drug content, in-vitro dissolution profiles. The dissolution results revealed that
formulations F12 showed 96.15%, F15 showed 94.93% and F18 showed 97.67% of drug
release at the end of 12 hrs. The drug release follows mixed order kinetics and the mechanism
was found to be diffusion and non-fickian release. Based on the results of in-vitro and
The aim of the study was to improve the solubility and dissolution rate
of the drug Verapamil HCL using solid-dispersion-Sustained release
matrix tablets by direct compression method. Solid dispersions were
prepared by solvent evaporation technique using PEG 6000 poloxamer
188 and Urea as carriers. The solid dispersions were characterized by
using FTIR and confirmed that no chemical interaction during
entrapment process. The prepared solid dispersions were formulated in
matrix tablets evaluated for pre-compression and post-compression
parameters. The post compression parameters were evaluated for
hardness, friability, weight variation and drug content which were
within the acceptable official limits. The drug content was found to be
high and uniformly distributed in all formulations. It was shown that
with the developed formulations, the release and dissolution of drug
from the tablets can be increased by formulating it as solid dispersion tablets. It was
concluded that development of sustained release solid-dispersion tablets using poloxamer 188
[97%] with HPMC K4m results highest increase in dissolution rate and optimum rate of drug
and reduced crystallinity of Verapamil HCL can account for the faster dissolution of the
released drug from the polymer matrix.
Background and purpose of the study: Osteoarthritis (OA) is the
most common joint disorder worldwide. Generally, oral dosage forms
are used for the treatment of OA but they have some disadvantages like
slow absorption and thus, onset of action is prolong. This can be
overcome by administrating the drug in liquid form but, many APIs
have limited level of stability in liquid form. Recently, effervescent
drug delivery systems have started gaining popularity, because they are
easy to administer and lead to better compliance. The aim of this study
is to formulate effervescent tablet with sufficient mechanical integrity
and to achieve faster disintegration in water. Method: They are
intended to be dissolved or dispersed in water before use. The study was designed to assess
the treatment for osteoarthritis by using combination of drugs such as Ibuprofen,
Glucosamine and Vitamin E in an effective way. The dosage of Ibuprofen is reduced by
addition of glucosamine sulphate (nutraceutical) on an assumption that the activity of
ibuprofen may be enhanced by nutraceutical. The formulations were subjected to various
evaluation tests. Results: All the formulations have shown good effervescence when placed
in 100 ml of water. The resultant solution appeared clear indicating the solubility of
ingredients in water. The friability and hardness of formulations are in the acceptable range.
The Angle of Repose (θ), Hausner’s Ratio and Carr’s Compressibility Index (%) revealed
that the formulations have good flow property. The solution time, CO2 and moisture content
of all the formulations are in the acceptable range. Conclusion: All the results concluded that
effervescent tablet preparation containing ibuprofen in combination with glucosamine
of sparfloxacin and diclofenac sodium by using HEMA (hydroxyl ethyl methacrylate)
and 4- Vinyl pyridine (monomers) for the treatment of ocular infections. Sparfloxacin
has in vitro activity against a wide range of gram-negative and gram-positive
microorganisms. The incorporation of ionic/hydrophobic monomer would increase
the interaction between hydrogel and drugs so that drugs will take long time to diffuse
from the hydrogel. The developed formulations were evaluated for water content,
center thickness, in–vitro drug release and stability studies. Compatibility study performed
by FT-IR method showed no interaction between drug and other excipients.
Water content of formulations S1, S2 and S3 were found be 4.2, 3.2 and 4.1% respectively.
Centre thickness of the formulations S1, S2 and S3 was found to be 6.6, 6.5 and
6.4μm respectively. Drugs are delivered by soaking the contact lenses in drug solution
to load the drugs. In-vitro release study revealed that release rate of drug from hydrogel
contact lenses dependent on concentration of 4-polyvinyl pyridine. The antimicrobial
studies against p.aureginus were performed for the formulation S2 which showed
more drug release compared other formulations. All the results were found that pure
drug has more bacterial inhibition activity initially compared to formulation S2. Thus,
it can be concluded that formulation S2 containing 0.5% w/v of 4-poly vinyl pyridine
as monomer was considered as an optimized formulation, as it provided sustained
release of the drug for the treatment of ocular infections.
slurry method based on non-ionic surfactants (tween 60), cholesterol and maltodextrin as a carrier. Materials and Methods:Four
formulations were prepared using maltodextrin as a carrier, cholesterol, tween 60, carbopol 934P as polymers. Proniosomal
formulations were prepared using slurry method. The proniosomal formulation was evaluated for FT-IR study, scanning electron
microscopy, stability study, In-vitro release study respectively. Further stability studies were carried out for 12 weeks in
accelerated conditions at 25 C and 60% RH. Results:The result from scanning electron microscopy analyses was con?rmed that 0
the surface of proniosomewas smooth. The formulation F4 which showed higher entrapment ef?ciency of 77.23% with tween 60
respectively and in-vitro releases of 77.01% at the end of 24 hrs was found to be best among the all 4 formulations. The drug
release follows Higuchi and Korsmeyer peppas model (mixed order). Kinetic analysis shows that the drug release follows ?ckian
release mechanism. FT-IR spectroscopic studies revealed no interaction between drug and polymer. The stability studies
indicated that F4 formulations were stable for 12 weeks. Conclusion: Proniosomal formulation could be a promising delivery
system for Diclofenac Sodium with improved bioavailability and better controlled drug release.
with or without loss of consciousness and characteristic body movement (convulsion). Among many drug of
antiepileptic drug, Divalproex sodium is considered as the most important antiepileptic drug and widely used for
treatment of epilepsy. The present work has been done to formulate sustained release tablets of divalproex
sodium containing HPMC K4M and HPMC K100M as release retarding agent. The FTIR study revealed that
there was no interaction between drug and polymer and combination can be safely prepared. The tablets were
prepared by wet granulation technique using PVP K30 solution as binding agent. Tablets were evaluated for
hardness, thickness, weight variation, disintegration time, drug content and in vitro drug release. All the physical
parameters were in acceptable limit of pharmacopeial specification. The in vitro release of sustained release
tablet was carried out for 18 hours using USP type-II apparatus (DS-1800) at 100 rpm for the first 45 minute in
900 ml 0.1N HCL maintaining at 37 ± 0.50C and then at phosphate buffer pH 6.8 in 900ml for another 18 hour.
The optimized formulation (F8) was found to exhibit more than 90% after 18 hours. Further the drug release of
sustained release tablets was compared with the conventional tablet which was prepared by using 5% micro
crystalline cellulose (MCC) as disintegrating agent. The stability studies, shown the optimized tablets of
immediate release formulation were stable at 400C / 75% RH for a period of 3 months.
controlled release matrix tablets of pregabalin; an antiepileptic drug.
Controlled release formulation is such drug delivery system that
delivers the drug locally or systemically at a predetermined rate for a
fixed period of time. The matrix tablet were prepared by direct
compression method using by various concentration of chitosan with
combination of various release retardant polymers like HPMC K100M,
carbopol 934P, xanthan gum and trisodium citrate as cross-linking
agent. Compatibility of the drug with the polymers was studied using
Fourier transform infrared spectroscopy and result showed no possible
interaction between drug and excipients. The powder mixtures were
subjected to pre-compression studies and obtained results were found
to be satisfactory. The compressed tablets were evaluated for postcompression
parameters such as weight variation, hardness, drug content, swelling study, invitro
drug release and stability studies. Swelling studies were carried out using water uptake
method and results revealed that formulation F3 containing higher concentration of carbopol
and chitosan showed highest swelling capacity. In-vitro dissolution studies were carried out
for 24 hours using 0.06N HCL for first 2 hours and pH 6.8 phosphate buffer for remaining 22
hours. Formulation F3 was able to release 99.45% drug at the end of 24 hours. The release
data were fitted to various mathematical models and it was found that formulation batches
followed first order release kinetics indicating drug release was concentration dependent.
Formulation F3 and F9 were subjected to short term stability studies and were
physiochemically stable throughout the study period.
bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate immediate release
tablets of divalproex sodium containing sodium starch glycolate (SSG) and croscarmellose as super disintegrating
agents. The FTIR study revealed that there was no interaction between drug and polymer and combination can be
safely prepared. The tablets were prepared by wet granulation technique as poor flow property exhibited by pure
drug. Tablets were evaluated for hardness, thickness, weight variation, disintegration time, drug content and in vitro
drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. In vitro drug
release studies were performed using USP type II apparatus (paddle method) in 900 ml of phosphate buffer pH 6.8
at 100 rpm. The optimized formulation (F6) was found to exhibit the highest in- vitrodrug release of 98.11percent at
the end of 20 minutes. Further the drug release of immediate release tablets was compared with the drug release
profile of conventional tablet which was prepared by using 5% micro crystalline cellulose (MCC) as disintegrating
agent. The stability studies, shown the optimized tablets of immediate release formulation were stable at 400C / 75%
RH for a period of 3 months.