Journal of Biomedical and Pharmaceutical Research, Oct 30, 2012
In this study core in coat tablets containing enteric coated Pantaprazole (PP) core and Cefuroxim... more In this study core in coat tablets containing enteric coated Pantaprazole (PP) core and Cefuroxime axetil (CA) floating type coat formulation as single unit prepared by compression coating method. The tablets were evaluated for their various pre-compression, compression characteristics, in vitro drug release kinetics and stability studies. The analytical estimation of drugs was found to be accurate and precise. The results of rheological characteristics indicated that, the powder beds of both core formulations of PP are freely flowable and easily compressible. Acryl EZE coating over the core tablets protects PP from GI fluids and helps in release of drug in intestinal pH. These studies on coat granules indicated that, the granule beds of all the coat formulations of CA are easily compressible and that flow increases with the addition of glidants. The release rate of CA from HPMC K4M formulations is majorly by burst effect, since HPMCK4M (p<0.05) is relatively more hydrophilic and when swells it forms weaker gel. Also, the release of CA from guar gum and xanthan gum formulations follows zero order release (p<0.05). The guar gum when it swells forms thicker gels hence the release rate 'k' is small of the three diluents. Stability studies at 40°C / 75% RH indicated that there is no significant change in CA content for a period of 3 months. Therefore it could be concluded that the combination of PP and CA would be useful for improved ulcer therapy associated with symptomatic relief to the patient.
Current investigation was aimed to study bioequivalence of two felodipine formulations and pharma... more Current investigation was aimed to study bioequivalence of two felodipine formulations and pharmacokinetic studies of human plasma were conducted. Pharmacokinetic parameters such as C max, T max , AUC (0-t), AUC (0-∞), K eli and t ½ were calculated and the blood plasma level data of the reference product and the test product were compared. Plasma onset of drug for both was 0.5 hr. The C max for reference product was 10.72 1.15 ng/ml with T max of 3.17 0.70 hr. The C max and T max of the Felodipine test product were 10.70 1.17 ng/ml and 3.75 0.44 hr. The AUC (0-t) for reference product was 216.24 33.66 ng.h / ml and 196.50 30.28 ng.h / ml for the test product. The K eli for the reference product was 0.03 0.00 h-1 and 0.03 0.03 h-1 for the test product. The t ½ of reference product was 24.22 0.88 h and for test product it was found to be 25.01 0.99 h. The AUC (0-∞) for the reference product was 240.87±34.56 ng.h/ml and for test product it was found to be 221.26±33.05 ng.h/ml. No subject developed any adverse experience during the study protocol. Based on the above observations after oral administration of tablets containing 10 mg of Felodipine it could conclude that the test product is bioequivalent of that of the reference product of felodipine and both are well tolerated. Further the results of the present investigation shown that there is scope for further studies on felodipine metabolism with respect to efficacy and pharmacokinetics.
Journal of Biomedical and Pharmaceutical Research, Nov 24, 2012
The present investigation was planned to formulate effervescent floating, gastroretentive guar gu... more The present investigation was planned to formulate effervescent floating, gastroretentive guar gum tablets containing famotidine, which can be useful in the treatment of gastric ulcer. The investigations carried out on various formulations resulted in totally four formulations obeying zero order kinetics. The study on rheological characteristics of powder bed indicated that, all the granules were freely flowing and compressible; density of all the tablets was less than 1, thereby assisting in floating of the dosage form on the surface of the simulated gastric fluids in vitro. Studies on compression characteristics indicated that, the tablets float over the surface and remain over the surface for a period of more than 10 h, except FS and FS1, which stay over the surface little lesser time than other tablets. Drug content was fairly uniform and consistent. The floating guar gum tablets containing HPMC K4M and Xanthan gum as binders follow zero order drug release kinetics. The increasing the amounts of magnesium stearate does not significantly alter the drug release kinetics; it improves the flowability of the granule bed. Tablets swell when in contact with water and the swelling index is highest with xanthan gum gel followed by the order, followed by FH> FX1> FC>FH1> FC1>FS>FS1. Stability studies at 45ºC and 75 % RH indicates that there is decrease in drug content, amounting to 30%, when observed for a period of 3 months.
Osteoarthritis predominantly affects the large weight bearing joints and the clinical characteris... more Osteoarthritis predominantly affects the large weight bearing joints and the clinical characteristics include morning stiffness of short duration, stiffness or gelling on rest, pain on use, joint inflammation and bone deformity. Microcapsules of aceclofenac were formulated with methyl cellulose, sodium CMC and hydroxyl propyl methyl cellulose by technique. The microcapsules showed excellent rheological properties for all batches. The formulations showed drug content uniformity with high drug entrapment efficiency. The in vitro wash off test revealed the mucoadhesive ability of the micro capsules. Scanning electron microscopy indicated structural and surface morphology uniformity. The in vitro release studies indicated sustained release of aceclofenac from the formulations. Kinetic study of the release data indicated the zero order release and non fickian sustained release mode of drug release. The microcapsules showed the correlation between wall thickness and drug release pattern.
The current investigation was aimed to study the minimization of the effect of Rifampicin induced... more The current investigation was aimed to study the minimization of the effect of Rifampicin induced hepatotoxicity by the use of Racemethionine molecule which is an anti dote for paracetamol over dosage in humans. Racemethionine, a drug used for the treatment of toxic effects of paracetamol, was studied for its hepatoprotective activity against anti tubercular drug (Rifampicin) induced hepatotoxicity in wistar albino rats. The serum samples collected were estimated for various biochemical parameters. Racemethionine showed normalization of bio chemical parameters like serum glutamyl oxaloacetate transaminase (ASAT), serum glutamyl pyruvate transaminase (ALAT), alkaline phosphatase (ALP). Total cholesterol (TC) levels were found to be slightly raised in the Racemethionine treated group as compared to the anti tubercular drug treated group. The results indicated that Racemethionine showed to be a more potent hepatoprotective drug against Rifampicin induced hepatic injury in experimental animals. Hence racemethionine could be used for hepatoprotective study models in albino rats indicated by its reduction ability of ASAT, ALAT, ALP and TC in serum.
Journal of Biomedical and Pharmaceutical Research, Dec 12, 2012
A simple, rapid, specific, precise and accurate HPLC method has been developed for the estimation... more A simple, rapid, specific, precise and accurate HPLC method has been developed for the estimation of Pregabalin in bulk drugs and in capsule dosage forms. The mobile phase consisted of 80: 10: 10 (v/v/v) of Disodium Hydrogen Phosphate Buffer: Acetonitrile: Methanol. The flow rate is 1 ml/min. Chromatographic determination of Pregabalin was performed on Inertsil ODS-3V, C18 (250 X 4.6 mm Id, 5μm) column. The wavelength of detection is 210 nm. The injection volume is 20μL. The retention time of Pregabalin is 4.7 minutes. The developed method was validated in terms of specificity, accuracy, precision, linearity, solution stability, ruggedness, robustness and system suitability. The influence of Acid, Alkaline, Oxidative Stress, Photolytic stress, Thermal stress, and Humidity stress conditions on pregabalin was studied. Results indicated that Pregabalin is stable under the experimental conditions. The proposed method has been successfully used for the routine analysis of pregabalin in capsule dosage forms.
journal of applied pharmaceutical science, Nov 29, 2012
Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method usi... more Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method using Hydroxy propyl methyl cellulose as matrix materials with or without xanthan gum and carbopol, and combination of xanthan gum and carbopol and propylene glycol as plasticizer. The prepared mini matrices were further evaluated for surface texture, uniformity of diameter, thickness, weight, moisture content, drug content uniformity, drug-excipients interaction, relative swelling, mucoadhesive test, in vitro drug release pattern. All the HPMC mini matrices showed good swelling which is proportional to concentration of polymer. The In vitro release of drug was in the range of 64.83% to 93.66%. Formulation H1 prepared with a drug-polymer ratio of 1:0.5 (LSP:HPMC) and 5% propylene glycol by weight of polymer as plasticizer showed promising results as a controlled release dosage form and released approximately 93.66% of the drug in 12 h. This study proves that extrusion method can be used for designing controlled release drug delivery systems providing nearly zero-order drug release over a period of 12 h.
The objective of this study is to formulate and evaluate sustained release tablets of Pioglitazon... more The objective of this study is to formulate and evaluate sustained release tablets of Pioglitazone HCl, which were developed to prolong the action leading to an increase in drug bioavailability and reduced dosing frequency. Sustained release (SR) drug delivery systems are developed to modulate the release of drug, in order to achieve specific clinical objectives that cannot be attained with conventional dosage forms. Possible therapeutic benefits of a properly designed SR dosage form include low cost, simple processing, improved efficacy, reduced adverse events and flexibility in terms of the range of release profiles attainable. Two different grades of HPMC K 100M, HPMC K15M and PEO, carbopol, Xanthum gum, MCC, Magnesium stearate and talc were used as variants along with pioglitazone HCl as active pharmaceutical ingredient. All these polymers are used in different concentrations to sustain the action. The tablets were prepared by direct compression method and are evaluated for pre compressional studies like bulk density, tapped density, compressibility index, Hausner ratio and angle of repose; all the values were found within limits of standard. In vitro release studies were carried out by USP type II paddle apparatus. The interaction of polymer and drug ruled out by FTIR studies. The FTIR studies confirmed that there is no interaction between the drug and polymer. Data of in-vitro release of tablets were fit in different equations and kinetic models to explain release kinetics the models used were zero order and first order equations. Higuchi and Korsmeyer peppas models based on physiochemical properties and in vitro release studies. The results showed that HPMC K15M produce sustained release of drug. The formulation F10 (HPMCK15M) with 1:3 ratio produced 99% drug release at 12 h.
The current work evaluate directly compressible esomeprazole magnesium trihydrate enteric coated ... more The current work evaluate directly compressible esomeprazole magnesium trihydrate enteric coated tablets were prepared to deliver drug in upper GIT. Different tablets were prepared with super disintegrants like Ac-Di-Sol, Crospovidone, sodium starch glycolate and diluents like Pharmatose DCL11, Mannogem EZ. Tablets were enteric coated using Acryl-EZE. The tablets were evaluated for hardness, disintegration time and in vitro drug release. The powder bed showed good rheological properties and enteric coated tablets showed acid uptake value <5 indicates significant protection of acid liable drug. The compressional parameters were within the limits, the drug content in all formulations was found to be uniform and consistent. In vitro dissolution studies indicated there is no drug loss during gastric phase. The tablets with Pharmatose DCL11 released higher than Mannogem EZ which colud be due to its hydrophilicity and due to swelling of the super disintegrant. Stability studies indicated that the prepared formulations were stable for a period of four months of all formulations showed comparable dissolution profiles with similarity factor more than fifty at p<0.05. From the above findings it can conclude that an Esomeprazole magnesium trihydrate enteric coated tablet could be developed to deliver the drug in to proximal small intestine.
Pharmacological studies indicate that pioglitazone improves glycemic control while reducing circu... more Pharmacological studies indicate that pioglitazone improves glycemic control while reducing circulating insulin level. [1] Pioglitazone has short biological half-life of 3-5 hours and is eliminated rapidly. [4] Therefore control release (CR) products are needed for pioglitazone to prolong its duration of action and to improve patience compliance; there are few reports [5] on the formulation of pioglitazone employing coated granules and matrix tablets. Microencapsulation has been accepted as a process to achieve controlled release and drug targeting. Mucoadhesion has been a topic of interest in the design of drug delivery system to prolong the residence time of the dosage form at the site of application or the absorption and to facilitate intimate contact dosage form with the underlying absorption surface to improve and enhance the bioavailability of drugs.
Journal of Biomedical and Pharmaceutical Research, Nov 24, 2012
Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method usi... more Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method using Hydroxy propyl methyl cellulose as matrix materials with or without xanthan gum and carbopol, and combination of xanthan gum and carbopol and propylene glycol as plasticizer. The prepared mini matrices were further evaluated for surface texture, uniformity of diameter, thickness, weight, moisture content, drug content uniformity, drug-excipients interaction, relative swelling, mucoadhesive test, in vitro drug release pattern. All the HPMC mini matrices showed good swelling which is proportional to concentration of polymer. The In vitro release of drug was in the range of 64.83% to 93.66%. Formulation H1 prepared with a drug-polymer ratio of 1:0.5 (LSP:HPMC) and 5% propylene glycol by weight of polymer as plasticizer showed promising results as a controlled release dosage form and released approximately 93.66% of the drug in 12 h. This study proves that extrusion method can be used for designing controlled release drug delivery systems providing nearly zero-order drug release over a period of 12 h.
Journal of Biomedical and Pharmaceutical Research, Nov 24, 2012
Aim of the present work was to formulate and evaluate pulsatile drug delivery system to achieve t... more Aim of the present work was to formulate and evaluate pulsatile drug delivery system to achieve time release of Verapamil HCl, based on pulsincap approach for the treatment of anti hypertensive drug. As fat production takes place in night time is more than day time. Pulsatile delivery system is capable of delivering drug when and where it required most. Time-delayed tablets, designed to release drug after a predictable lag time. The basic design consists of an insoluble hard gelatin capsule body filled with physical mixture of Verapamil HCl with HPMC and Guar gum, lactose as channeling agent and sealed with a Sodium alginate and xanthan gum plug. The Verapamil HCl pulsincaps were prepared by physical mixture method with lactose by varying drug to polymer ratio and evaluated for the micromeretic property, percentage yield, drug content, IR and in vitro release study. A hydrogel polymer Sodium alginate and Xanthan gum was used as plugs to maintain a suitable lag period. The in vitro release study were carried out using pH 1.2 buffer for a period of 2 h then 7.4 pH phosphate buffer for a period of 10 h. The cumulative % release for HPMC formulations were found to be in the range of 82.87% to 90.28% and for Guar gum were found to be75.28 to 98.08% at the end of 12 h. From the obtained result formulation GS3 showing 94.5% drug release at 12 h with 3h lag time was selected as an optimized formulation for designing pulsatile device. The programmable pulsatile release has been achieved from prepared formulation over a 12 h period, consistent with the demands of Pulsincap drug delivery. KEY WORDS: Pulsatile drug delivery; Verapamil HCl; Xanthan gum; Guar gum; In vitro study.
Purpose: A simple reverse phase liquid chromatographic and mass spectroscopic analytical method h... more Purpose: A simple reverse phase liquid chromatographic and mass spectroscopic analytical method has been developed and validated for estimation of felodipine in plasma. Methods: The separation was carried out on Princeton SPHER C18 (150 x 4.6 mm i.d. of 5) as Stationary phase, Mobile Phase: Acetonitrile : 2mM ammonium acetate Elution mode : Isocratic A: B= 80:20% v/v Flow rate: 0.8 ml/min using SPD M-10AVP photo diode array detector at 38.10 nm. Results: The described LC MS method was linear over a concentration range of 0.8-13.0ng/ml. Pantaprazole was used as internal standard. The felodipine and pantaprazole showed retention factor of 2.97 respectively. The limit of detection (LOD) and the limit of quantification (LOQ) for felodipine was 0.10 ng/ml, 0.50 ng/ml and for pantaprazole 0.06, 0.21 ng/ml respectively. The stability of the drug spiked human plasma samples during three freeze thaw cycles were stable in plasma for about one month when stored at frozen state. Conclusions: The results of the study showed that the proposed LC MS method is simple, rapid, precise and accurate, which is useful for the estimation of felodipine in bulk fluids and biological plasma sample analyte with accuracy and reproducibility.
Diltiazem hydrochloride has poor oral bioavailability, easily undergo first passage effect in the... more Diltiazem hydrochloride has poor oral bioavailability, easily undergo first passage effect in the liver. Hence, an attempt was made to prepare and evaluate mucoadhesive buccal films containing diltiazem hydrochloride by employing HPMC, eudragit, ethyl cellulose alone and in combination with PVP. The I.R and DSC studies showed that there was no interaction between drug and the utilized polymer. The prepared mucoadhesive buccal films showed uniform thickness, weight, folding endurance, surface pH, drug content and swelling index. The drug content of all the formulation was found to be uniform. In vitro drug release studies indicated that the films prepared with HPMC (3%) and ethyl cellulose (4%) has shown fast and slow release respectively. The formulations incorporated with SLS and sodium glycocholate indicated significant drug release from F11 and F15. Later the in-situ diffusion studies using goat cheek pouch showed faster drug release from film with 1% (SLS). About 93.04% and 91.83% of drug release profile were observed during in situ diffusion studies at the end of 9hrs and 18 hrs respectively. The formulated films were stable during stability studies at 45ºC and 75%RH with respect to drug content.
Esomeprazole magnesium trihydrate tablets were formulated by directly compression and enteric coa... more Esomeprazole magnesium trihydrate tablets were formulated by directly compression and enteric coated with Acryl EZE. The rheological characteristics of powder beds were freely flowable and easily compressible. The Compressional parameters after enteric coating were found to be uniform and consistent. The hardness (Kg/cm2) was found in the range of 4.133±0.321 to 4.833±0.153. The enteric coated tablets were not disintegrated in simulated gastric fluid. The drug content in all formulations was found to be uniform and consistent. Accuracy and precision studies indicated drug content uniformity in tablet formulations. The acid uptake studies showed less than 5% acid uptake for all tablets indicated that the drug could be protected from degradation in gastric environment by acryl EZE enteric coating. In the In vitro drug release studies there is no loss during gastric phase. Later the study showed that tablets with lactose DC released higher than mannitol probably owing to its hydrophilicity and due to swelling of the super disintegrant. From the above findings it can conclude that an enteric coated Esomeprazole magnesium trihydrate tablet dosage form could be developed to deliver the drug in to proximal small intestine for more bio availability and to treat peptic ulcer.
The present study was aimed to develop a gastroretentive tablet that could deliver antibiotic in ... more The present study was aimed to develop a gastroretentive tablet that could deliver antibiotic in stomach from the coat tablet for localized action and acid liable anti secretory agent in duodenum from the enteric coated core. During tablet formulation Studies on rheological characteristics of Clarithromycin coat granular blends showed their free flowing nature and ease for compression to tablet. The compressed tablets exhibited uniform post compressional characteristics. Evaluation of floating parameters indicated results suits for the tablets to formulate core in coat tablets for release of Clarithromycin in gastric pH and esomeprazole in alkaline pH to treat peptic ulcer disease associated with h pylori bacteria. The formulations exhibited uniform rheological and post compressional properties. The drug content was found to be uniform and consistent in all formulations. The tablet showed density < 1 facilitated tablets floating ability over 0.1N HCl with minimum floating lag time. In vitro release studies showed that T6C6 formulation exhibited better release for both the drugs in simulated gastric and intestinal fluids for 12 h. The study revealed the role of porous carriers, cellulosic polymers and natural gums on drug release profiles of esomeprazole core in clarithromycin coat gastroretentive tablets in duodenal ulcer treatment.
Current investigation was aimed to study bioequivalence of two felodipine formulations and pharma... more Current investigation was aimed to study bioequivalence of two felodipine formulations and pharmacokinetic studies of human plasma were conducted. Pharmacokinetic parameters such as Cmax, Tmax, AUC(0-t), AUC(0-∞), Keli and t½ were calculated and the blood plasma level data of the reference product and the test product were compared. Plasma onset of drug for both was 0.5 hr. The Cmax for reference product was 10.72 1.15 ng/ml with Tmax of 3.17 0.70 hr. The Cmax and Tmax of the Felodipine test product were 10.70 1.17 ng/ml and 3.75 0.44 hr. The AUC(0-t) for reference product was 216.24 33.66 ng.h / ml and 196.50 30.28 ng.h / ml for the test product. The Keli for the reference product was 0.03 0.00 h-1 and 0.03 0.03 h-1for the test product. The t½ of reference product was 24.22 0.88 h and for test product it was found to be 25.01 0.99 h. The AUC(0-∞) for the reference product was 240.87±34.56 ng.h/ml and for test product it was found to be 221.26±33.05 ng.h/ml. No subject developed any...
The current investigation was aimed to study the minimization of the effect of Rifampicin induced... more The current investigation was aimed to study the minimization of the effect of Rifampicin induced hepatotoxicity by the use of Racemethionine molecule which is an anti dote for paracetamol over dosage in humans. Racemethionine, a drug used for the treatment of toxic effects of paracetamol, was studied for its hepatoprotective activity against anti tubercular drug (Rifampicin) induced hepatotoxicity in wistar albino rats. The serum samples collected were estimated for various biochemical parameters. Racemethionine showed normalization of bio chemical parameters like serum glutamyl oxaloacetate transaminase (ASAT), serum glutamyl pyruvate transaminase (ALAT), alkaline phosphatase (ALP). Total cholesterol (TC) levels were found to be slightly raised in the Racemethionine treated group as compared to the anti tubercular drug treated group. The results indicated that Racemethionine showed to be a more potent hepatoprotective drug against Rifampicin induced hepatic injury in experimental ...
Matrix colon tablet formulation of Ciprofloxacin hydrochloride containing matrix carrier granules... more Matrix colon tablet formulation of Ciprofloxacin hydrochloride containing matrix carrier granules were prepared by wet granulation technology. The granular bed were evaluated for rheological properties indicated that, the granules were freely flowable and easily compressible. Granules were compressed in 10 station tablet punching machine and evaluated for post compressional characteristics of weight variation, thickness test, diameter test, hardness test, friability. The results showed that the pre formulation batches of tablets showed uniform and reproducible compressional characteristics. The drug content of tablet revealed that the drug is accurately and fairly distributed. The hardness (Kg/cm2) was found in the range of 4.5 ± 0.090 – 5.6 ± 0.201 Kg/cm2 with minimum friability. The colon targeted tablets were not disintegrated in 0.1N HCl. The in vitro drug release studies indicated that sterculia and almond gum could be used for development of colon matrix tablets of ciprofloxac...
Journal of Biomedical and Pharmaceutical Research, Oct 30, 2012
In this study core in coat tablets containing enteric coated Pantaprazole (PP) core and Cefuroxim... more In this study core in coat tablets containing enteric coated Pantaprazole (PP) core and Cefuroxime axetil (CA) floating type coat formulation as single unit prepared by compression coating method. The tablets were evaluated for their various pre-compression, compression characteristics, in vitro drug release kinetics and stability studies. The analytical estimation of drugs was found to be accurate and precise. The results of rheological characteristics indicated that, the powder beds of both core formulations of PP are freely flowable and easily compressible. Acryl EZE coating over the core tablets protects PP from GI fluids and helps in release of drug in intestinal pH. These studies on coat granules indicated that, the granule beds of all the coat formulations of CA are easily compressible and that flow increases with the addition of glidants. The release rate of CA from HPMC K4M formulations is majorly by burst effect, since HPMCK4M (p<0.05) is relatively more hydrophilic and when swells it forms weaker gel. Also, the release of CA from guar gum and xanthan gum formulations follows zero order release (p<0.05). The guar gum when it swells forms thicker gels hence the release rate 'k' is small of the three diluents. Stability studies at 40°C / 75% RH indicated that there is no significant change in CA content for a period of 3 months. Therefore it could be concluded that the combination of PP and CA would be useful for improved ulcer therapy associated with symptomatic relief to the patient.
Current investigation was aimed to study bioequivalence of two felodipine formulations and pharma... more Current investigation was aimed to study bioequivalence of two felodipine formulations and pharmacokinetic studies of human plasma were conducted. Pharmacokinetic parameters such as C max, T max , AUC (0-t), AUC (0-∞), K eli and t ½ were calculated and the blood plasma level data of the reference product and the test product were compared. Plasma onset of drug for both was 0.5 hr. The C max for reference product was 10.72 1.15 ng/ml with T max of 3.17 0.70 hr. The C max and T max of the Felodipine test product were 10.70 1.17 ng/ml and 3.75 0.44 hr. The AUC (0-t) for reference product was 216.24 33.66 ng.h / ml and 196.50 30.28 ng.h / ml for the test product. The K eli for the reference product was 0.03 0.00 h-1 and 0.03 0.03 h-1 for the test product. The t ½ of reference product was 24.22 0.88 h and for test product it was found to be 25.01 0.99 h. The AUC (0-∞) for the reference product was 240.87±34.56 ng.h/ml and for test product it was found to be 221.26±33.05 ng.h/ml. No subject developed any adverse experience during the study protocol. Based on the above observations after oral administration of tablets containing 10 mg of Felodipine it could conclude that the test product is bioequivalent of that of the reference product of felodipine and both are well tolerated. Further the results of the present investigation shown that there is scope for further studies on felodipine metabolism with respect to efficacy and pharmacokinetics.
Journal of Biomedical and Pharmaceutical Research, Nov 24, 2012
The present investigation was planned to formulate effervescent floating, gastroretentive guar gu... more The present investigation was planned to formulate effervescent floating, gastroretentive guar gum tablets containing famotidine, which can be useful in the treatment of gastric ulcer. The investigations carried out on various formulations resulted in totally four formulations obeying zero order kinetics. The study on rheological characteristics of powder bed indicated that, all the granules were freely flowing and compressible; density of all the tablets was less than 1, thereby assisting in floating of the dosage form on the surface of the simulated gastric fluids in vitro. Studies on compression characteristics indicated that, the tablets float over the surface and remain over the surface for a period of more than 10 h, except FS and FS1, which stay over the surface little lesser time than other tablets. Drug content was fairly uniform and consistent. The floating guar gum tablets containing HPMC K4M and Xanthan gum as binders follow zero order drug release kinetics. The increasing the amounts of magnesium stearate does not significantly alter the drug release kinetics; it improves the flowability of the granule bed. Tablets swell when in contact with water and the swelling index is highest with xanthan gum gel followed by the order, followed by FH> FX1> FC>FH1> FC1>FS>FS1. Stability studies at 45ºC and 75 % RH indicates that there is decrease in drug content, amounting to 30%, when observed for a period of 3 months.
Osteoarthritis predominantly affects the large weight bearing joints and the clinical characteris... more Osteoarthritis predominantly affects the large weight bearing joints and the clinical characteristics include morning stiffness of short duration, stiffness or gelling on rest, pain on use, joint inflammation and bone deformity. Microcapsules of aceclofenac were formulated with methyl cellulose, sodium CMC and hydroxyl propyl methyl cellulose by technique. The microcapsules showed excellent rheological properties for all batches. The formulations showed drug content uniformity with high drug entrapment efficiency. The in vitro wash off test revealed the mucoadhesive ability of the micro capsules. Scanning electron microscopy indicated structural and surface morphology uniformity. The in vitro release studies indicated sustained release of aceclofenac from the formulations. Kinetic study of the release data indicated the zero order release and non fickian sustained release mode of drug release. The microcapsules showed the correlation between wall thickness and drug release pattern.
The current investigation was aimed to study the minimization of the effect of Rifampicin induced... more The current investigation was aimed to study the minimization of the effect of Rifampicin induced hepatotoxicity by the use of Racemethionine molecule which is an anti dote for paracetamol over dosage in humans. Racemethionine, a drug used for the treatment of toxic effects of paracetamol, was studied for its hepatoprotective activity against anti tubercular drug (Rifampicin) induced hepatotoxicity in wistar albino rats. The serum samples collected were estimated for various biochemical parameters. Racemethionine showed normalization of bio chemical parameters like serum glutamyl oxaloacetate transaminase (ASAT), serum glutamyl pyruvate transaminase (ALAT), alkaline phosphatase (ALP). Total cholesterol (TC) levels were found to be slightly raised in the Racemethionine treated group as compared to the anti tubercular drug treated group. The results indicated that Racemethionine showed to be a more potent hepatoprotective drug against Rifampicin induced hepatic injury in experimental animals. Hence racemethionine could be used for hepatoprotective study models in albino rats indicated by its reduction ability of ASAT, ALAT, ALP and TC in serum.
Journal of Biomedical and Pharmaceutical Research, Dec 12, 2012
A simple, rapid, specific, precise and accurate HPLC method has been developed for the estimation... more A simple, rapid, specific, precise and accurate HPLC method has been developed for the estimation of Pregabalin in bulk drugs and in capsule dosage forms. The mobile phase consisted of 80: 10: 10 (v/v/v) of Disodium Hydrogen Phosphate Buffer: Acetonitrile: Methanol. The flow rate is 1 ml/min. Chromatographic determination of Pregabalin was performed on Inertsil ODS-3V, C18 (250 X 4.6 mm Id, 5μm) column. The wavelength of detection is 210 nm. The injection volume is 20μL. The retention time of Pregabalin is 4.7 minutes. The developed method was validated in terms of specificity, accuracy, precision, linearity, solution stability, ruggedness, robustness and system suitability. The influence of Acid, Alkaline, Oxidative Stress, Photolytic stress, Thermal stress, and Humidity stress conditions on pregabalin was studied. Results indicated that Pregabalin is stable under the experimental conditions. The proposed method has been successfully used for the routine analysis of pregabalin in capsule dosage forms.
journal of applied pharmaceutical science, Nov 29, 2012
Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method usi... more Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method using Hydroxy propyl methyl cellulose as matrix materials with or without xanthan gum and carbopol, and combination of xanthan gum and carbopol and propylene glycol as plasticizer. The prepared mini matrices were further evaluated for surface texture, uniformity of diameter, thickness, weight, moisture content, drug content uniformity, drug-excipients interaction, relative swelling, mucoadhesive test, in vitro drug release pattern. All the HPMC mini matrices showed good swelling which is proportional to concentration of polymer. The In vitro release of drug was in the range of 64.83% to 93.66%. Formulation H1 prepared with a drug-polymer ratio of 1:0.5 (LSP:HPMC) and 5% propylene glycol by weight of polymer as plasticizer showed promising results as a controlled release dosage form and released approximately 93.66% of the drug in 12 h. This study proves that extrusion method can be used for designing controlled release drug delivery systems providing nearly zero-order drug release over a period of 12 h.
The objective of this study is to formulate and evaluate sustained release tablets of Pioglitazon... more The objective of this study is to formulate and evaluate sustained release tablets of Pioglitazone HCl, which were developed to prolong the action leading to an increase in drug bioavailability and reduced dosing frequency. Sustained release (SR) drug delivery systems are developed to modulate the release of drug, in order to achieve specific clinical objectives that cannot be attained with conventional dosage forms. Possible therapeutic benefits of a properly designed SR dosage form include low cost, simple processing, improved efficacy, reduced adverse events and flexibility in terms of the range of release profiles attainable. Two different grades of HPMC K 100M, HPMC K15M and PEO, carbopol, Xanthum gum, MCC, Magnesium stearate and talc were used as variants along with pioglitazone HCl as active pharmaceutical ingredient. All these polymers are used in different concentrations to sustain the action. The tablets were prepared by direct compression method and are evaluated for pre compressional studies like bulk density, tapped density, compressibility index, Hausner ratio and angle of repose; all the values were found within limits of standard. In vitro release studies were carried out by USP type II paddle apparatus. The interaction of polymer and drug ruled out by FTIR studies. The FTIR studies confirmed that there is no interaction between the drug and polymer. Data of in-vitro release of tablets were fit in different equations and kinetic models to explain release kinetics the models used were zero order and first order equations. Higuchi and Korsmeyer peppas models based on physiochemical properties and in vitro release studies. The results showed that HPMC K15M produce sustained release of drug. The formulation F10 (HPMCK15M) with 1:3 ratio produced 99% drug release at 12 h.
The current work evaluate directly compressible esomeprazole magnesium trihydrate enteric coated ... more The current work evaluate directly compressible esomeprazole magnesium trihydrate enteric coated tablets were prepared to deliver drug in upper GIT. Different tablets were prepared with super disintegrants like Ac-Di-Sol, Crospovidone, sodium starch glycolate and diluents like Pharmatose DCL11, Mannogem EZ. Tablets were enteric coated using Acryl-EZE. The tablets were evaluated for hardness, disintegration time and in vitro drug release. The powder bed showed good rheological properties and enteric coated tablets showed acid uptake value <5 indicates significant protection of acid liable drug. The compressional parameters were within the limits, the drug content in all formulations was found to be uniform and consistent. In vitro dissolution studies indicated there is no drug loss during gastric phase. The tablets with Pharmatose DCL11 released higher than Mannogem EZ which colud be due to its hydrophilicity and due to swelling of the super disintegrant. Stability studies indicated that the prepared formulations were stable for a period of four months of all formulations showed comparable dissolution profiles with similarity factor more than fifty at p<0.05. From the above findings it can conclude that an Esomeprazole magnesium trihydrate enteric coated tablet could be developed to deliver the drug in to proximal small intestine.
Pharmacological studies indicate that pioglitazone improves glycemic control while reducing circu... more Pharmacological studies indicate that pioglitazone improves glycemic control while reducing circulating insulin level. [1] Pioglitazone has short biological half-life of 3-5 hours and is eliminated rapidly. [4] Therefore control release (CR) products are needed for pioglitazone to prolong its duration of action and to improve patience compliance; there are few reports [5] on the formulation of pioglitazone employing coated granules and matrix tablets. Microencapsulation has been accepted as a process to achieve controlled release and drug targeting. Mucoadhesion has been a topic of interest in the design of drug delivery system to prolong the residence time of the dosage form at the site of application or the absorption and to facilitate intimate contact dosage form with the underlying absorption surface to improve and enhance the bioavailability of drugs.
Journal of Biomedical and Pharmaceutical Research, Nov 24, 2012
Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method usi... more Mini matrices containing Losartan potassium as a model drug were prepared by extrusion method using Hydroxy propyl methyl cellulose as matrix materials with or without xanthan gum and carbopol, and combination of xanthan gum and carbopol and propylene glycol as plasticizer. The prepared mini matrices were further evaluated for surface texture, uniformity of diameter, thickness, weight, moisture content, drug content uniformity, drug-excipients interaction, relative swelling, mucoadhesive test, in vitro drug release pattern. All the HPMC mini matrices showed good swelling which is proportional to concentration of polymer. The In vitro release of drug was in the range of 64.83% to 93.66%. Formulation H1 prepared with a drug-polymer ratio of 1:0.5 (LSP:HPMC) and 5% propylene glycol by weight of polymer as plasticizer showed promising results as a controlled release dosage form and released approximately 93.66% of the drug in 12 h. This study proves that extrusion method can be used for designing controlled release drug delivery systems providing nearly zero-order drug release over a period of 12 h.
Journal of Biomedical and Pharmaceutical Research, Nov 24, 2012
Aim of the present work was to formulate and evaluate pulsatile drug delivery system to achieve t... more Aim of the present work was to formulate and evaluate pulsatile drug delivery system to achieve time release of Verapamil HCl, based on pulsincap approach for the treatment of anti hypertensive drug. As fat production takes place in night time is more than day time. Pulsatile delivery system is capable of delivering drug when and where it required most. Time-delayed tablets, designed to release drug after a predictable lag time. The basic design consists of an insoluble hard gelatin capsule body filled with physical mixture of Verapamil HCl with HPMC and Guar gum, lactose as channeling agent and sealed with a Sodium alginate and xanthan gum plug. The Verapamil HCl pulsincaps were prepared by physical mixture method with lactose by varying drug to polymer ratio and evaluated for the micromeretic property, percentage yield, drug content, IR and in vitro release study. A hydrogel polymer Sodium alginate and Xanthan gum was used as plugs to maintain a suitable lag period. The in vitro release study were carried out using pH 1.2 buffer for a period of 2 h then 7.4 pH phosphate buffer for a period of 10 h. The cumulative % release for HPMC formulations were found to be in the range of 82.87% to 90.28% and for Guar gum were found to be75.28 to 98.08% at the end of 12 h. From the obtained result formulation GS3 showing 94.5% drug release at 12 h with 3h lag time was selected as an optimized formulation for designing pulsatile device. The programmable pulsatile release has been achieved from prepared formulation over a 12 h period, consistent with the demands of Pulsincap drug delivery. KEY WORDS: Pulsatile drug delivery; Verapamil HCl; Xanthan gum; Guar gum; In vitro study.
Purpose: A simple reverse phase liquid chromatographic and mass spectroscopic analytical method h... more Purpose: A simple reverse phase liquid chromatographic and mass spectroscopic analytical method has been developed and validated for estimation of felodipine in plasma. Methods: The separation was carried out on Princeton SPHER C18 (150 x 4.6 mm i.d. of 5) as Stationary phase, Mobile Phase: Acetonitrile : 2mM ammonium acetate Elution mode : Isocratic A: B= 80:20% v/v Flow rate: 0.8 ml/min using SPD M-10AVP photo diode array detector at 38.10 nm. Results: The described LC MS method was linear over a concentration range of 0.8-13.0ng/ml. Pantaprazole was used as internal standard. The felodipine and pantaprazole showed retention factor of 2.97 respectively. The limit of detection (LOD) and the limit of quantification (LOQ) for felodipine was 0.10 ng/ml, 0.50 ng/ml and for pantaprazole 0.06, 0.21 ng/ml respectively. The stability of the drug spiked human plasma samples during three freeze thaw cycles were stable in plasma for about one month when stored at frozen state. Conclusions: The results of the study showed that the proposed LC MS method is simple, rapid, precise and accurate, which is useful for the estimation of felodipine in bulk fluids and biological plasma sample analyte with accuracy and reproducibility.
Diltiazem hydrochloride has poor oral bioavailability, easily undergo first passage effect in the... more Diltiazem hydrochloride has poor oral bioavailability, easily undergo first passage effect in the liver. Hence, an attempt was made to prepare and evaluate mucoadhesive buccal films containing diltiazem hydrochloride by employing HPMC, eudragit, ethyl cellulose alone and in combination with PVP. The I.R and DSC studies showed that there was no interaction between drug and the utilized polymer. The prepared mucoadhesive buccal films showed uniform thickness, weight, folding endurance, surface pH, drug content and swelling index. The drug content of all the formulation was found to be uniform. In vitro drug release studies indicated that the films prepared with HPMC (3%) and ethyl cellulose (4%) has shown fast and slow release respectively. The formulations incorporated with SLS and sodium glycocholate indicated significant drug release from F11 and F15. Later the in-situ diffusion studies using goat cheek pouch showed faster drug release from film with 1% (SLS). About 93.04% and 91.83% of drug release profile were observed during in situ diffusion studies at the end of 9hrs and 18 hrs respectively. The formulated films were stable during stability studies at 45ºC and 75%RH with respect to drug content.
Esomeprazole magnesium trihydrate tablets were formulated by directly compression and enteric coa... more Esomeprazole magnesium trihydrate tablets were formulated by directly compression and enteric coated with Acryl EZE. The rheological characteristics of powder beds were freely flowable and easily compressible. The Compressional parameters after enteric coating were found to be uniform and consistent. The hardness (Kg/cm2) was found in the range of 4.133±0.321 to 4.833±0.153. The enteric coated tablets were not disintegrated in simulated gastric fluid. The drug content in all formulations was found to be uniform and consistent. Accuracy and precision studies indicated drug content uniformity in tablet formulations. The acid uptake studies showed less than 5% acid uptake for all tablets indicated that the drug could be protected from degradation in gastric environment by acryl EZE enteric coating. In the In vitro drug release studies there is no loss during gastric phase. Later the study showed that tablets with lactose DC released higher than mannitol probably owing to its hydrophilicity and due to swelling of the super disintegrant. From the above findings it can conclude that an enteric coated Esomeprazole magnesium trihydrate tablet dosage form could be developed to deliver the drug in to proximal small intestine for more bio availability and to treat peptic ulcer.
The present study was aimed to develop a gastroretentive tablet that could deliver antibiotic in ... more The present study was aimed to develop a gastroretentive tablet that could deliver antibiotic in stomach from the coat tablet for localized action and acid liable anti secretory agent in duodenum from the enteric coated core. During tablet formulation Studies on rheological characteristics of Clarithromycin coat granular blends showed their free flowing nature and ease for compression to tablet. The compressed tablets exhibited uniform post compressional characteristics. Evaluation of floating parameters indicated results suits for the tablets to formulate core in coat tablets for release of Clarithromycin in gastric pH and esomeprazole in alkaline pH to treat peptic ulcer disease associated with h pylori bacteria. The formulations exhibited uniform rheological and post compressional properties. The drug content was found to be uniform and consistent in all formulations. The tablet showed density < 1 facilitated tablets floating ability over 0.1N HCl with minimum floating lag time. In vitro release studies showed that T6C6 formulation exhibited better release for both the drugs in simulated gastric and intestinal fluids for 12 h. The study revealed the role of porous carriers, cellulosic polymers and natural gums on drug release profiles of esomeprazole core in clarithromycin coat gastroretentive tablets in duodenal ulcer treatment.
Current investigation was aimed to study bioequivalence of two felodipine formulations and pharma... more Current investigation was aimed to study bioequivalence of two felodipine formulations and pharmacokinetic studies of human plasma were conducted. Pharmacokinetic parameters such as Cmax, Tmax, AUC(0-t), AUC(0-∞), Keli and t½ were calculated and the blood plasma level data of the reference product and the test product were compared. Plasma onset of drug for both was 0.5 hr. The Cmax for reference product was 10.72 1.15 ng/ml with Tmax of 3.17 0.70 hr. The Cmax and Tmax of the Felodipine test product were 10.70 1.17 ng/ml and 3.75 0.44 hr. The AUC(0-t) for reference product was 216.24 33.66 ng.h / ml and 196.50 30.28 ng.h / ml for the test product. The Keli for the reference product was 0.03 0.00 h-1 and 0.03 0.03 h-1for the test product. The t½ of reference product was 24.22 0.88 h and for test product it was found to be 25.01 0.99 h. The AUC(0-∞) for the reference product was 240.87±34.56 ng.h/ml and for test product it was found to be 221.26±33.05 ng.h/ml. No subject developed any...
The current investigation was aimed to study the minimization of the effect of Rifampicin induced... more The current investigation was aimed to study the minimization of the effect of Rifampicin induced hepatotoxicity by the use of Racemethionine molecule which is an anti dote for paracetamol over dosage in humans. Racemethionine, a drug used for the treatment of toxic effects of paracetamol, was studied for its hepatoprotective activity against anti tubercular drug (Rifampicin) induced hepatotoxicity in wistar albino rats. The serum samples collected were estimated for various biochemical parameters. Racemethionine showed normalization of bio chemical parameters like serum glutamyl oxaloacetate transaminase (ASAT), serum glutamyl pyruvate transaminase (ALAT), alkaline phosphatase (ALP). Total cholesterol (TC) levels were found to be slightly raised in the Racemethionine treated group as compared to the anti tubercular drug treated group. The results indicated that Racemethionine showed to be a more potent hepatoprotective drug against Rifampicin induced hepatic injury in experimental ...
Matrix colon tablet formulation of Ciprofloxacin hydrochloride containing matrix carrier granules... more Matrix colon tablet formulation of Ciprofloxacin hydrochloride containing matrix carrier granules were prepared by wet granulation technology. The granular bed were evaluated for rheological properties indicated that, the granules were freely flowable and easily compressible. Granules were compressed in 10 station tablet punching machine and evaluated for post compressional characteristics of weight variation, thickness test, diameter test, hardness test, friability. The results showed that the pre formulation batches of tablets showed uniform and reproducible compressional characteristics. The drug content of tablet revealed that the drug is accurately and fairly distributed. The hardness (Kg/cm2) was found in the range of 4.5 ± 0.090 – 5.6 ± 0.201 Kg/cm2 with minimum friability. The colon targeted tablets were not disintegrated in 0.1N HCl. The in vitro drug release studies indicated that sterculia and almond gum could be used for development of colon matrix tablets of ciprofloxac...
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