Buccal Drug delivery

Mucoadhesion was employed for improving performance and bioavailability of many drugs. Different dosage forms were developed based on this principle. This study aims to prepare bucco-adhesive tablets of anti-migraine drug zolmitriptan as a suitable candidate for improving its oral bioavailability and therapeutic efficacy and to evaluate them for many pre/post-formulation parameters in-vitro/exvivo. The bucco-adhesive tablets containing 2.5 mg zolmitriptan were prepared using carbopol 934LR as a primary polymer alone or in combination with chitosan or xanthan gum as secondary polymers by direct compression. Drug-excipients compatibility and micromeritics study were carried out. Tablets were evaluated for physico-chemical parameters, surface pH, ex-vivo residence time, in-vitro swelling study, ex-vivo mucoadhesive strength, in-vitro drug release study, ex-vivo permeation study and physical stability in human saliva. No interactions were found between drug and excipients. Tablets had good physico-chemical characters. Formulation containing carbopol 934LR and chitosan in a ratio of 1: 3 approximately was the optimum one. It swelled by only 37.67±0.65% after 5 h and showed a nearly neutral surface pH. Ex-vivo residence time was long enough for delivery of the drug for more than 8 h. Ex-vivo mucoadhesive strength was 32.7±2.1 g. Drug release was 86.93±3.73 % after 7 h following zero order kinetics and permeation flux was 0.045 mg/cm 2 h. Tablets were physically stable W WO OR RL LD D J JO OU UR RN NA AL L O OF F P PH HA AR RM MA AC CY Y A AN ND D P PH HA AR RM MA AC CE EU UT TI IC CA AL L S SC CI IE EN NC CE ES S V Vo ol lu um me e 2 2, , I Is ss su ue e 6 6, , 4 42 22 25 5--4 42 24 48 8. . R Re es se ea ar rc ch h A Ar rt ti ic cl le e I

The main objective of this study was to assess awareness of danger
signs of pregnancy and its associated factors in Mekelle public
hospitals, 2014.
Institutional based cross sectional study was conducted among 422
pregnant mothers. Data was collected using interviewer administered
questionnaire; it was entered and analyzed using SPSS version 16.
The data were presented using texts, graphs and tables.
Out of the total participants of this study 79.6% mothers had
information about danger signs of pregnancy from which 61.9%
mothers had information about vaginal bleeding followed by sudden
gush of fluid before labor which was mentioned by 41.9% of
respondents. Severe unusual abdominal pain was the least known
danger signs as mentioned by 19 % of mothers. The main source of
information for the danger signs was health personnel and
Negligence was the main reason for not having good awareness about
danger signs of pregnancy.
Therefore, health extension workers should strengthen their
awareness creation activities; community mobilization and health
education should be considered with policy makers and other
interested organizations.

oligonucleotides have predominant role in its delivery for various
diseases. Objective: Antisense compounds are biological
molecules consisting of small ribonucleic acid (RNA) or
deoxyribonucleic acid (DNA) segments (Oligonucleotide) which
have enormous potential for the treatment of number of diseases.
Methods: All the methods analyzed were obtained through high
impact articles. Results: Several impediments were made to
Oligonucleotide for its widespread usage as them as drugs to
overcome their lack of stability in physiological fluids and their
poor penetration into cells. Experiments like, association with or
encapsulation within nano-and micro sized drug delivery systems,
lipids and polymers could help to increase the efficiency of
oligonucleotide delivery. This review discusses the use of cationic
lipids, Cell penetrating peptides, nanoparticles, microparticles and
several novel methods that have recently been explored as delivery
vehicles. Conclusion: The use of naked Oligonucleotide given a
clear cut way to new targets for potential therapeutic compounds.
Apart this, antisense therapy represents a promising and evolving
approach to the management of numerous diseases in which a
specific abnormality has been identified as a primary or major
contributing etiologic factor. In near future, authors strongly
believe that antisense therapy will give a positive way for number
of In vitro experiments and break through for many life
threatening diseases.

The present work was aimed to design & characterize an oral dosage form to release Terbutaline sulphate following a programmed time period (pulsed release system). Pulsatile release tablet comprises a drug containing core and pH sensitive polymeric coating capable of delaying drug release and providing gastric resistance .The core tablets of terbutaline sulphate were prepared for the treatment of nocturnal asthma .The core tablets were prepared by direct compression method using different disintegrating agents. The cores were coated with pH sensitive polymers (Eudragit S-100, Eudragit L-100) at different coating levels to develop a suitable dosage form which should show minimum drug release in upper regions of gastrointestinal tract (GIT). Prepared tablets were characterized for various physical parameters such as hardness, thickness, weight variation disintegration test drug content and in-vitro drug release characteristics. All the parameters were found to be in the standard range. The dissolution of best formulation F 4 S 3 , F 7 S 3 and F 11 S 3 have shown the lag phase of 5 hrs at 10% coating level and almost complete drug release was achieved after 11 hrs . The kinetic study data for best formulation followed zero order kinetics. Stability study of the best formulation indicates no significant difference in release profile after a period of 3 months.

The objective of the research was firstly to investigate the behavior of Surelease (release retardant binder) alone and in combination with other hydrophilic polymers on the release of zidovudine from sustained release matrix tablet. Secondly, to compare between the release pattern of polyethylene oxide and Methocel K100M alone and in combination. A randomized surface methodology (RSM) was applied to study the effect of polymers on drug release. The independent variables of the formulation were: the type of polymers (X1), concentration of polymers (X2) in the tablet and dependent variables are the percentage drug release at 2 hours (Y1) and the percentage drug release at 12 hours (Y 2 ). Release kinetics were analyzed using zero-order, first order, higuchi's square root and korsmeyer-peppas empirical equations in terms of r 2 . Results of invitro drug release kinetics study suggests that, all formulations follows zero order kinetics with r 2 value in range of 0.99 and fitting the release data to korsmeyers equation release exponent n ranged from 0.83 to 1.22 and followed non-Fickian diffusion mechanism (anomalous transport) and super case II transport for Surelease formulations. Among all the formulations, F14 matrix tablet containing combination of Surelease and polyoxWSR301 shows 102.37% of drug release at the end of 12 hours.

Objective: To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of pediatric anaphylaxis.
Methods: Four different films have been prepared by solvent casting technique where the percentages of the polymer (Lycoat RS720) were optimized. The polymer percentages were (20%, 25%, 27% and 30%) of the total formulation weighs. The thickness and elastic modulus of the optimized film was evaluated using dynamic mechanical analyzer. Epinephrine content uniformity was assessed using UV at wavelength 280 nm. For the dissolution test, fast dissolving films (FDFs) were evaluated in 500 Simulated Saliva, with 50 rpm. In vivo taste and disintegration evaluation was performed on six healthy volunteers.
Results: Films formed by formulations 1, 2 and 3 were too sticky after drying, while formulation 4 that has 30% polymer content formed smooth, transparent, flexible and uniform film, and therefore, it was selected for further testing. The value of elastic modulus was determined at 1.325 MPa. The thickness of the film at different locations was measured at 0.29 mm. Drug content in film was measured at 93% ±10. More than 90% of epinephrine was released from the film within 7.2 min. Bitterness of epinephrine was masked efficiently according to volunteer’s comments with average disintegration time of 20 s.
Conclusion: This study presents potential proof for using FDFs as a replacement therapy of epinephrine injections for pediatrics.

Febuxostat is a urate lowering drug, an inhibitor of xanthine
oxidase used in the treatment of hyperuricemia and chronic gout. The
drug shows dissolution-rate limited absorption, there by poor and
variable bioavailability. It needs enhancement in bioavailability to
derive maximum therapeutic efficacy. The main objective of the
present research work is to enhance the solubility and dissolution rate
of Febuxostat by preparing the Spherical agglomerates. Spherical
agglomerates were prepared by the quasi emulsion solvent diffusion
method. N, N-dimethyl form amide, chloroform and water were
selected as good solvent, bridging liquid and poor solvents
respectively. Polyethylene glycol, Poloxomer- F68 and Polyvinyl
alcohol were used as a carrier. Among all the formulations prepared,
spherical agglomerates prepared with Febuxostat and Poloxomer-
F68 in 1:1 ratio showed highest drug release in 60 minutes. Spherical
agglomerates prepared with Febuxostat and Poloxomer- F68 in 1:1
ratio was used in the preparation of orodispersible tablets. To study
the influence of superdisintegrants on performance of Febuxostat
Orodispersible Tablets, a set of three formulations (K1, K2, K3) were
prepared using three superdisintegrants sodium starch glycolate,
Croscarmalose sodium and Crospovidone . The orodispersible tablets
of Febuxostat prepared with Crospovidone showed rapid drug release
when compared to pure drug and other tablet formulations.

The present study was aimed to formulate and evaluate fast
dissolving oral films of Zolmitriptan using sodium alginate, xanthan
gum and sodium starch glycolate, guar gum. The suitable plasticizer
and its concentration were selected on the basis of flexibility, tensile
strength and stickiness of the film. The films are prepared by solvent
casting method and characterized by UV, FTIR studies. The films
were evaluated for disintegration time, Folding endurance, Tensile
Strength, Mouth dissolving time, Thickness, content uniformity and
In-vitro dissolution studies. The F5 formulation has given 98.5% drug
release within 6 minutes and has a tensile strength of 1.80 MPa.

The current study was aimed to develop the meclizine hydrochloride
sublimated fast dissolving tablets using different sublimated agents to
enhance the dissolution rate. The prepared fast dissolving tablets
were subjected to pre-compression properties and characterized for
hardness, weight variation, friability, wetting time, water absorption
ratio, and disintegration time. From In vitro dissolution studies, the
formulation F3 containing camphor (10%w/w) as the sublimating
agent showed rapid dissolution of about 98.61% in 30 min, and
disintegration time 43 sec when compared with other sublimating
agents. The percent drug release in 30 min (Q30) and initial
dissolution rate for formulation F3 was 98.61±0.25%, 3.29%/min.
These were very much higher compared to marketed tablets
(65.43±0.57%, 2.18%/min). The dissolution efficiency was found to
be 63.37 and it is increased by 1.4 fold with F3 FDT tablets
compared to marketed tablets. Differential scanning calorimetry and
Fourier transform infrared spectroscopy studies revealed that there
was no possibility of interactions. In conclusion, development of
meclizine hydrochloride fast dissolving tablets by sublimation
method is an appropriate method to enhance the dissolution rate.

Mucoadhesive patches containing 10 mg miconazole nitrate were evaluated. The patches were prepared with ionic polymers, sodium carboxymethyl cellulose (SCMC) and chitosan, or non-ionic polymers, polyvinyl alcohol (PVA), hydroxyethyl cellulose (HEC) and hydroxypropylmethyl cellulose (HPMC). Convenient bioadhesion, acceptable elasticity, swelling and surface pH were obtained. Patches exhibited sustained release over more than 5 h and the addition of polyvinyl pyrrolidone (PVP) generally enhanced the release rate. Optimum release behaviour was shown with patches containing 10% w/v PVA and 5% w/v PVP. Study of the in vivo release from this formulation revealed uniform and effective salivary levels with adequate comfort and compliance during at least 6 h. On the contrary, in vivo release of the commercial oral gel product resulted in a burst and transient release of miconazole, which diminished sharply after the first hour of application. Storage of these patches for 6 months did not affect the elastic properties, however, enhanced release rates were observed due to marked changes in the crystal habit of the drug.

Background : The delivery of drugs through the buccal mucosa has received a great deal of attention over the last two decades, and yet there are not many buccal delivery products available on the market. Objective : This review outlines the advantages and disadvantages of buccal drug delivery, provides a historical perspective and discusses representative developmental and marketed drugs. Methods : The structure of the oral mucosa is briefly described to preface a description of the pathways for drug absorption and a critical discussion of permeation experiments. A brief historical perspective followed by a description of some of the currently marketed products provides a picture of where we are today. An indication is given of likely progress in this area and of the attributes of a successful business entity of the future. Conclusion : The authors provide an assessment of the future potential of buccal and sublingual drugs.

The aim of the present study was to investigate the antioxidant activity of methanolic extract of Michelia champaca flowers. Antioxidant activity was evaluated by using in-vitro assay models like Total antioxidant capacity, Nitric oxide radical scavenging assay, Reducing Power Assay and Hydrogen Peroxide Scavenging Activity. All the antioxidant activities were compared with standard antioxidant such as ascorbic acid. Methanolic extract of the plant showed effective free radical scavenging activity at 300µg concentration. The IC50 values of the ethanolic extract of Michelia champaca flowers were found to be 260 µg in total antioxidant activity, 150 µg in nitric oxide radical assay, 240 µg in reducing power assay and 280 µg in hydrogen peroxide assay. The results obtained in this study showed that the flowers of Michelia champaca have antioxidant properties which provide a basis for the traditional use of the plant.

The current study aimed at development and validation of a simple, accurate, precise, sensitive, robust and specific high performance liquid chromatography (HPLC) method for simultaneous estimation of benzocaine (BZN) with tibezonium iodide (TIB) from combined dosage form as well as from human saliva. Instrumental conditions were developed on an auto-sampler Agilent® 1260 Infinity series RP-HPLC machine. The method was validated in accordance with ICH harmonized guidelines Q2 (R1) by using acetonitrile and phosphate buffer as mobile phase in a volumetric proportion of 70:30 which was flowing through C 18 Agilent® column. Flow of mobile phase was maintained at 1 mL/min at 35 °C and elute was detected 318 nm. The peaks for BZN and TIB were separated at 2.29 and 4.15 min, respectively. Linearity range for such were 0.24-20.16 and 0.14-10.08 μg/mL, respectively. Linear coefficient of regression (R2) for BZN and TIB were 0.9987 and 0.9993, respectively. The relative standard deviation (RSD) values for both drugs were less than 2.0% indicating the accuracy and precision. The limit of detection (LOD) and limit of quantification (LOQ) outcomes for BZN were 56 and 187 ng/mL, respectively. For TIB, it were 38 and 127 ng/mL, respectively. The drugs separation against placebo justified the specificity of the method. It was concluded that the developed and validated method could be potentially for in vitro as well as in human salivary extracts of formulated dosage forms.

The current study was designed to evaluate mucoadhesive buccal tablet containing metronidazole (MTZ) for local action aided by Hydroxypropylmethylcellulose K4M (HPMC) and Carbopol 940® (CP) as mucoadhesive polymers with other ingredients like sodium starch glycolate (SSG), polyvinyl pyrollidone K30 (PVP) as disintegrant and binders respectively. Formulations (F1-F8) were prepared by direct compression method and characterized for different physicochemical parameters. Results showed that the average weight and friability were within USP limits. Maximum mucoadhesive time was observed for F2 (14 hr) containing moderate amount of HPMC and CP used in the study. Up most mucoadhesive strength value was observed with F3 containing highest amount of HPMC used. Results indicated that high amount of HPMC was linked with the moderate to higher mucoadhesive strength and time. Maximum swelling index was observed in F7 (191.3%). Only F1-F3 showed complete in vitro MTZ release within 3 hr. Formulations containing PVP released MTZ incompletely over time while SSG released earlier. Formulation F1 was considered best in terms of MTZ release (100.5%) with diffusion based Korsmeyer-Peppas release kinetics. Therefore, MTZ exhibiting best physicochemical characters in mucoadhesive buccal tablet was found in F1 containing HPMC and CP in amounts of 37.5 mg and 25 mg, respectively, for local action.

Because of their large surface area and immunological competence, mucosal tissues are attractive administration and target sites for vaccination. An important characteristic of mucosal vaccination is its ability to elicit local immune responses, which act against infection at the site of pathogen entry. However, mucosal surfaces are endowed with potent and sophisticated tolerance mechanisms to prevent the immune system from overreacting to the many environmental antigens. Hence, mucosal vaccination may suppress the immune system instead of induce a protective immune response. Therefore, mucosal adjuvants and/or special antigen delivery systems as well as appropriate dosage forms are required in order to develop potent mucosal vaccines. Whereas oral, nasal and pulmonary vaccine delivery strategies have been described extensively, the sublingual and buccal routes have received considerably less attention. In this review, the characteristics of and approaches for sublingual and buccal vaccine delivery are described and compared with other mucosal vaccine delivery sites. We discuss recent progress and highlight promising developments in the search for vaccine formulations, including adjuvants and suitable dosage forms, which are likely critical for designing a successful sublingual or buccal vaccine. Finally, we outline the challenges, hurdles to overcome and formulation issues relevant for sublingual or buccal vaccine delivery.

This work evaluated under accelerated conditions the stability of the
biodegradable gentamicin-glyceryl monooleate water based-gel used
in the treatment of chronic osteomyelitis. Three batches of 600.0 g of
gentamicin -glyceryl monooleate -water based-gel (5/80/15% w/w)
were manufactured. The samples were stored in a climatic test
chamber for stability evaluation according to the standards published
by the International Conference on Harmonisation and the World
Health Oganization (25 ± 2°C / 60 ± 5%RH) for 6 months. Samples
were evaluated at pre-determinate times 0, 3 and 6 months with
regard to their physicochemical properties and In Vitro drug release
characteristics. Gentamicin sulfate present in the freshly prepared
gels was the same after three and six months of storage at 25°C / 60%
RH. However the relative amount of gentamicin sulfate in the freshly
prepared gel that was about 110% decreased by about 11% after six
months of storage. The release profiles of the gels remained similar
despite a partial hydrolysis of glyceryl monooleate and an increase in
the residual amount of water and in the viscosity.

Cetylpyridinium chloride (CPC), a quaternary antiseptic, has been found effective in controlling the accumulation of bacterial plaque and the consequent gingivitis (1). The drug has bactericidal activity against Gram-positive and, at higher concentrations, against Gram-negative organisms. It has a good activity against Candida albicans (2). Lozenges and mouthwashes are available but none of these dosage forms can release the antiseptic drug into the oral cavity for a prolonged period because of their short residence time (3). Multilayered bioadhesive lozenges containing CPC were evaluated (4); they were not erodible and required removal after 3 h. A buccoadhesive erodible disk was designed (1), which showed a controlled and delayed release pattern at the targeted Mucoadhesive patches for delivery of cetylpyridinium chloride (CPC) were prepared using polyvinyl alcohol (PVA), hydroxyethyl cellulose (HEC) and chitosan. Swelling and bioadhesive characteristics were determined for both plain and medicated patches. The results showed a remarkable increase in radial swelling (S D ) after addition of the water-soluble drug (CPC) to the plain formulae. A decrease in the residence time was observed for PVA and chitosan-containing formulae. Higher drug release was obtained from PVA patches compared to HEC ones, while both are non-ionic polymers. A considerable drop in release was observed for chitosan formulae after the addition of water-soluble additives, polyvinyl pyrrolidone (PVP) and gelatin. Ageing was done on PVA formulae; the results showed there was no influence on the chemical stability of CPC, as reflected from the drug content data. Physical characteristics of the studied patches showed an increase in the residence time with storage accompanied with a decrease in drug release. This may be due to changes in the crystal habit of the drug as well as to slight agglomeration of the polymer particles.

Body sensor networks (BSN) promise to enhance quality of life in common human habitats. The very next and natural step towards the improvement of the already valuable applications based on BSN is the incorporation of body actuator devices which adapt its actuation dynamically based on the information provided by the body sensors, thus forming Body Sensor and Actuator Networks (BS&AN). This paper shows how BS&AN can be exploited to create an innovative system to support the treatment of patients affected by Parkinson's Disease (PD). The combination of clinical and technological knowledge in BS&AN allows to significantly improve the quality of life of patients suffering from PD.

Objective: The study aims for the design and evaluation of floating tablets of emtricitabine (EMT), post oral administration to sustain the release and enhance gastric residence time (GRT). Methods: EMT is a nucleoside reverse-transcriptase inhibitor for the prevention and treatment of human immunodeficiency virus (HIV) infection. The investigation was considered to formulate a floating tablet of EMT with various agents. The formulation included with various concentrations of hydroxypropyl methylcellulose (HPMC) k4m, ethylcellulose, microcrystalline cellulose, polyvinylpyrrolidone (PVP) by wet granulation method. Various parameters for the prepared formulations were evaluated for weight variation, thickness, hardness, friability, floating lag time (FLT), total floating time (TFT), swelling index, in vitro drug release, and fourier-transform infrared spectroscopy (FTIR) studies. Results: The best formulation F1 exhibited 88.28% release in 24 h duration, with a floating lag time of 7 min and swelling index of 52.1% and drug content was determined to be 98.27%. The release mechanism was determined to be first order with higuchi release kinetics displaying diffusion along with the dissolution of the EMT from the tablet by non fickian mechanism. Conclusion: EMT tablets showed an increased GRT with a sustained release for 24 h thereby allowing a better window for absorption consequently improve the therapeutic effect of the drug.

The extent of Maillard reaction and the development of 5-(hydroxymethyl)-2-furaldehyde (HMF) were evaluated in two roasted plantain cultivars (French sombre and Dwarf kalapua), at different ripening stages. Roasting at high temperature (210°C) and roasting duration were shown to increase the development of HMF in the roasted samples. Similarly, ripening stage had significant influence on the development of HMF. The colour and fluorescence intensities were significantly (P > 0.05) increased by the roasting conditions and the degree of ripening. In addition, the plantain cultivars showed positive correlations with HMF, fluorescence, colour index and the sugars, respectively.

The conventional formulation of prednisolone is considered to be low in efficacy, primarily on account of their failure in providing and maintaining effective therapeutic drug levels. This study aims to focus on development of a mucoadhesive buccal delivery system with a twofold objective of offering a rapid as well as a prolonged delivery of prednisolone coupled with enhanced therapeutic efficacy. Buccoadhesive films of prednisolone were prepared by solvent-casting method using hydroxyl propyl methyl cellulose (K100), Carbopol 940 and/or Eudragit Õ NE 40 D. Placebo films possessing the most desirable physicomechanical properties were selected for drug loading. The effect of polymer and its content on film properties, i.e. mucoadhesive strength, swelling and hydration, in vitro drug release was studied. Based on these studies, film F7D was selected for ex vivo permeation across porcine cheek mucosa. The steady state flux of prednisolone across the buccal mucosa was found to be 105.33 ± 32.07 mg/cm 2 /h. A comparative pharmacokinetic study of prepared film (F7D) and oral suspension of prednisolone was conducted. In vivo data of buccal film show greater bioavailability (AUC 0-a : 24.26 ± 4.06 mg.h/ml versus 10.65 ± 2.15 mg.h/ml) and higher C max (2.70 ± 0.38 mg/ml versus 2.29 ± 0.32 mg/ml) value when compared to oral suspension. The data observed from this study highlight the feasibility of the buccal route as a viable option for delivery of prednisolone.

To develop a fast dissolving film strip containing epinephrine HCl for the potential treatment of pediatric anaphylaxis. Four different films have been prepared by solvent casting technique where the percentages of the polymer (Lycoat RS720) were optimized. The polymer percentages were (20%, 25%, 27% and 30%) of the total formulation weighs. The thickness and elastic modulus of the optimized film was evaluated using dynamic mechanical analyzer. Epinephrine content uniformity was assessed using UV at wavelength 280 nm. For the dissolution test, fast dissolving films (FDFs) were evaluated in 500 Simulated Saliva, with 50 rpm. In vivo taste and disintegration evaluation was performed on six healthy volunteers. Films formed by formulations 1, 2 and 3 were too sticky after drying, while formulation 4 that has 30% polymer content formed smooth, transparent, flexible and uniform film, and therefore, it was selected for further testing. The value of elastic modulus was determined at 1.325 M...

Mucoadhesion was employed for improving performance and bioavailability of many drugs. Different dosage forms were developed based on this principle. This study aims to prepare bucco-adhesive tablets of anti-migraine drug zolmitriptan as a suitable candidate for improving its oral bioavailability and therapeutic efficacy and to evaluate them for many pre/post-formulation parameters in-vitro/ex-vivo. The bucco-adhesive tablets containing 2.5 mg zolmitriptan were prepared using carbopol 934LR as a primary polymer alone or in combination with chitosan or xanthan gum as secondary polymers by direct compression. Drug-excipients compatibility and micromeritics study were carried out. Tablets were evaluated for physico-chemical parameters, surface pH, ex-vivo residence time, in-vitro swelling study, ex-vivo mucoadhesive strength, in-vitro drug release study, ex-vivo permeation study and physical stability in human saliva. No interactions were found between drug and excipients. Tablets had ...

Kelemahan berupa kesulitan dalam menelan dan metabolisme lintas pertama di hati merupakan keterbatasan penggunaan obat-obatan  oral yang mengakibatkan ketidakpatuhan pasien dan bioavailabilitas yang buruk. Kelemahan ini dapat dihindari dengan pemberian bentuk sediaan alternatif seperti mouth dissolving tablets yang larut ketika kontak dengan air liur yang memungkinkan penyerapan obat sistemik melalui mukosa bukal. Penelitian ini bertujuan untuk mempersiapkan mouth dissolving tablets dengan dasar effervesen sebagai agen pembantu disintegrasi. Bioavailabilitas mouth dissolving tablets dengan dasar effervesen melalui administrasi bukal meningkat yang berarti mouth dissolving tablets dengan dasar effervesen melalui bukal memiliki kemampuan untuk melewati metabolisme lintas pertama. Dengan demikian mouth dissolving tablets melalui rute administrasi bukal dapat digunakan untuk meningkatkan kepatuhan pasien.

Kata kunci: Mouth Dissolving Tablets, dasar effervescent, rute administrasi bukal

From the previous work (Part I), mucoadhesive formulae containing 5% CP/65% HPMC/30% lactose and 2% PC/68% HPMC/30% mannitol as well as formulae based on sodium carboxymethyl cellulose (SCMC) were selected. Medicated tablets were prepared using diltiazem hydrochloride (DZ) and metclopramide hydrochloride (MP) in two different doses (30 and 60 mg). The effect of drug and dose on the mucoadhesive properties and in-vitro drug release was evaluated. All formulae produced extended drug release (over 8 to 12 h). Polyacrylic acid based matrices (PAA) showed Fickian's diffusion release pattern for both drugs. SCMC ensured zero-order release for DZ, which deviated to anomalous behavior in case of MP. Doubling the dose significantly reduced the bioadhesion strength (p<0.05) with a slight improvement in drug release rate. The formulation of bilayer tablets containing drug-free layer and medicated layer enhanced the drug release without affecting the bioadhesive performance. The bilayer tablet formulated with 2% PC/68% HPMC/30% mannitol (PC2) was selected for studying the in-vivo metoclopramide release in four healthy volunteers. The tablet ensured controlled drug release for 12 h, in addition, good correlation (r=0.9398) was observed between in-vitro and in-vivo data. The effect of ageing on selected formulae containing DZ and MP, respectively, was studied. Storage at 40 degrees C and 75% relative humidity for 6 months didn't influence the mucoadhesive performance, however, an enhanced released rate was observed.

The conventional formulation of prednisolone is considered to be low in efficacy, primarily on account of their failure in providing and maintaining effective therapeutic drug levels. This study aims to focus on development of a mucoadhesive buccal delivery system with a twofold objective of offering a rapid as well as a prolonged delivery of prednisolone coupled with enhanced therapeutic efficacy. Buccoadhesive films of prednisolone were prepared by solvent-casting method using hydroxyl propyl methyl cellulose (K100), Carbopol 940 and/or Eudragit Õ NE 40 D. Placebo films possessing the most desirable physicomechanical properties were selected for drug loading. The effect of polymer and its content on film properties, i.e. mucoadhesive strength, swelling and hydration, in vitro drug release was studied. Based on these studies, film F7D was selected for ex vivo permeation across porcine cheek mucosa. The steady state flux of prednisolone across the buccal mucosa was found to be 105.33 ± 32.07 mg/cm 2 /h. A comparative pharmacokinetic study of prepared film (F7D) and oral suspension of prednisolone was conducted. In vivo data of buccal film show greater bioavailability (AUC 0-a : 24.26 ± 4.06 mg.h/ml versus 10.65 ± 2.15 mg.h/ml) and higher C max (2.70 ± 0.38 mg/ml versus 2.29 ± 0.32 mg/ml) value when compared to oral suspension. The data observed from this study highlight the feasibility of the buccal route as a viable option for delivery of prednisolone.

Mucoadhesion was employed for improving performance and bioavailability of many drugs. Different dosage forms were developed based on this principle. This study aims to prepare bucco-adhesive tablets of anti-migraine drug zolmitriptan as a suitable candidate for improving its oral bioavailability and therapeutic efficacy and to evaluate them for many pre/post-formulation parameters in-vitro/exvivo. The bucco-adhesive tablets containing 2.5 mg zolmitriptan were prepared using carbopol 934LR as a primary polymer alone or in combination with chitosan or xanthan gum as secondary polymers by direct compression. Drug-excipients compatibility and micromeritics study were carried out. Tablets were evaluated for physico-chemical parameters, surface pH, ex-vivo residence time, in-vitro swelling study, ex-vivo mucoadhesive strength, in-vitro drug release study, ex-vivo permeation study and physical stability in human saliva. No interactions were found between drug and excipients. Tablets had g...

The aptitude of ropinirole to permeate the buccal tissue was tested using porcine mucosa mounted on Franz-type diffusion cells as ex vivo model. Drug permeation was also evaluated in presence of various penetration enhancers and in iontophoretic conditions. Ropinirole, widely used in treatment of motor fluctuations of Parkinson's disease, passes the buccal mucosa. Flux and permeability coefficient values suggested that the membrane does not appear a limiting step to the drug absorption. Nevertheless, an initial lag time is observed but the input rate can be modulated by permeation enhancement using limonene or by application of electric fields. Absorption improvement was accompanied by the important reduction of the lag time; at once the time required to reach the steady state plasma concentration was drastically decreased. On the basis of these results we could assume that clinical application of ropinirole by buccal delivery is feasible.