FORMULATION AND EVALUATION OF ACYCLOVIR MATRIX TABLET USING MUCOADHESIVE POLYMER

ABSTRACT Mucoadhesive polymer owing to its binding capacity with gastric mucin prolongs the gastric residence time and thereby increases bioavailablity. In the present research work an attempt was made to formulate and evaluate sustain release mucoadhesive matrix tablet of acyclovir. Matrix tablets were prepared by direct compression technology using different types and levels of polymers viz. HPMC K15M, carbopol 934P, ethyl cellulose etc alone and in combinations. Compressed tablets were evaluated for thickness, friability, hardness, uniformity of weight, content of active ingredient, swelling and in vitro dissolution studies. The studies indicated that the drug release can be modulated by varying the concentrations of polymers. It was observed that combination of both the polymers in equal concentration exhibited the best release profile and able to sustain the drug release for 10 h. Kinetic studies were also carried out on different formulations which showed that formulation F1, F2, F3, F7, F8 and F10 followed zero order while F4, F5, F6 and F10 followed first order release kinetics. According to Korsmeyer Peppas, F1, F2, F3, F7, F8, F9 and F10 showed non fickian diffusion. While F4, F5 and F6 followed fickian diffusion. Stability studies revealed that all the formulation was found to be stable under accelerated stability studies. KEYWORDS:  Acyclovir Mucoadhesive Matrix Tablet, Carbopol 934P, HPMC K15M, Ethyl Cellulose, Gastric Residence Time

EFFET OF COMBINATION OF HPMC AND CARBOPOL 934P ON THE PROPERTIES OF THE GASTRIC FLOATING TABETS OF TIMOLOL MALEATE

The purpose of the present research wasto evaluate the effect of carbopol 934P on gastroretentive drug delivery system.Floating tablet containing timolol maleate were prepared by direct compressionmethod, using three grades of polymer HPMC [K15M, K4M, K100M] and carbopol934P. Sodium bicarbonate and citric acid was incorporated as a gas-generatingagent. The floating tablets were evaluated on the basis of pre-compression andpost-compression characteristics. The pre-compression characteristics such asangle of repose, bulk density, tapered density and compressibility index showedsatisfactory results for all the nine formulations. The results ofpost-compression such as weight variation, hardness, friability and drugcontent estimation showed that all the nine formulations complied with theofficial requirement of IP. The buoyancy lag time indicated that theformulation F1, F4 and F7 without carbopol 934P were less than 8 sec, where asformulation containing carbopol 934P had greater lag time. Formulationcontaining only HPMC grade polymers floated less than 8 h as compared to the formulationcontaining HPMC with carbopol 934P floated more than 12 h. The in vitro dissolution studies indicated94.2% drug release in 12 h by the formulations F2, F3, F5, F6, F8 and F9containing different concentration of carbopol 934P with different grades ofHPMC, when compared to 100% drug release within 9 h by the formulation F1, F4and F7 containing only different grades of HPMC polymers. All formulationfollowed the Higuchi release model. The drug release from the tablets wassufficiently sustained and non-Fickian transport of the drug from tablets wasconfirmed. Hence it can be inferred that the inclusion of carbopol 934P canresult in sustained drug delivery over 12 h, enhances the gastric floating timeand also increases buoyancy lag time. KEYWORDS:Timololmaleate, HPMC, carbopol 934P, Floating tablets, direct compressio

IMPROVEMENT OF THE SOLUBILITY AND DISSOLUTION OF TOLFENAMIC ACID USING LYOPHILIZATION TECHNIQUE

Abstract: The aim of the present study was to prepare freeze dried crystals (FD) of Tolfenamic acid (TA) by freeze drying technique. Crystallization medium used for freeze drying of Tolfenamic acid consisted of N,N-dimethylformamide (DMF) and Water as solvent systems. The presence of solvents residuals in FD was determined by Gas chromatography and particles were characterized by DSC, FT-IR, XRD and SEM. The respective solubility study and dissolution behaviour studies were carried out. The samples were stored in stability chamber to investigate their physical stabilities. Residual Solvents in FDs were found to be within the limit and exhibited decreased crystallinity as well solubility and dissolution of the Freeze dried crystals was improved than commercial sample of Tolfenamic acid. In stability study, it was found that physical properties and release profile of the freeze dried crystals was unaffected for 3 months. Hence this technique can be used to obtain modified drug raw material for formulation of tablets of Tolfenamic acid by direct compression with directly compressible tablet excipients

A pseudo-randomised clinical trial of in situ gels of fluconazole for the treatment of oropharngeal candidiasis

<p>Abstract</p> <p>Background</p> <p>Oropharyngeal candidasis is a common opportunistic infection seen in immunocompromised patients. Fluconazole has a broad spectrum antifungal activity including a wide variety of <it>candida </it>species. Aim of the present investigation was to formulate and find out the relative efficacy of <it>in situ </it>gels of fluconazole.</p> <p>Method</p> <p>The <it>in situ </it>gels were prepared using polymers which exhibited sol-to-gel phase transition due to change in specific physico-chemical parameters, such as ion triggered system using gellan gum (0.5% w/v) along with sodium carboxylmethylcellulose (0.35%w/v). The study design was bicenter, 'pseudo-randomised, single blind trial conducted in Mangalore., India, which includes 15 HIV positive patients, 15 patients with partial or completes dentures, and 15 patients who were treated with (active control) fluconazole tablets 100 mg/day for 14 days. Severity of disease was scored clinically before treatment and at clinical evaluations on day 3, 7, 14, 18, 21, 35, and 42. Semiquantitative microbiological cultures of oral swabs were also obtained on same days.</p> <p>Results</p> <p>All patients had mycological documented oropharyngeal candidiasis and were treated with fluconazole (0.5%w/v) <it>in situ </it>gels for 14 days Severity of disease was scored clinically before treatment and at different predetermined time intervals along with semi quantitative culture of oral swabs. The clinical response rate showed 97% cure after 14 days in the treated with <it>in situ </it>gel. In comparison, the control group treated with fluconazole tablets showed 85% improvement in symptoms of oral candidiasis. The patients suffering from HIV infection showed relapse in oral candidiasis at the end of 21 days. The patients having oral candidiasis due to partial or complete dentures showed complete recovery and were free from signs and symptoms of oral candidiasis.</p> <p>Conclusions</p> <p>The <it>in situ </it>gel formulation of fluconazole was well tolerated with no severe adverse reaction and offers a better alternative to tablet formulation in the treatment of oropharyngeal candidasis.</p> <p>Trial registration</p> <p>Current Controlled Trails <a href="http://www.controlled-trials.com/ISRCTN90634047">ISRCTN90634047</a></p

Transfersomes as a Surfactant-based Ultradeformable Liposome

In the modern era, there are numerous ways for drug delivery. The change in time has led to the progress of drug delivery systems gaining significant development. Even though most of the drugs are administered orally i.e., in conventional dosage form it has its limitations too like poor patient compliance, metabolism in the liver's first passage, poor absorption, and fluctuations in plasma level.Because our skin is indeed the largest organ, transdermal medication administration has received increased attention in recent years. Many lipids nanovesicles like Liposomes, Niosome, Ethosome, and Transfersomes have been developed as a carrier for transdermal drug delivery. But out of them, Transfersomes are the ones which are of great interest as they show better permeation among all as most of the other carriers cannot pass through the stratum corneum. The method of transdermal medication administration has been used to provide controlled and targeted action and can act as topical and dermal preparation. This review provides basic information about Transfersomes, their mechanism of action, applications, and comparison with other lipid nanocarriers

PREPARATION AND CHARACTERIZATION OF MICROPARTICLES OF TENOXICAM

Abstract: The aim of the present study was to improve the solubility and dissolution rate of Tenoxicam by preparing microparticles by spray drying technique using chloroform and water as solvents systems. Tenoxicam microparticles were prepared by spray drying using chloroform and water as solvents systems to improve solubility and dissolution rate. The prepared microparticles were evaluated for solubility and in-vitro dissolution. The prepared microparticles were characterized by DSC, FT-IR, XRD and SEM. Dissolution profile of the prepared microparticles was compared with its recrystallized and commercialized sample. Prepared microparticles exhibited decreased in crystallinity. The solubility of microparticles exhibited one and half fold increases than the commercial Tenoxicam and dissolution showed 63 % release in 60 min. Consequently, from the above result it can be concluded that spray dried technique is a useful technique to improve the solubility and dissolution of poor water soluble drug like Tenoxicam

Formulation of chitosan-based ciprofloxacin and diclofenac film for periodontitis therapy

Purpose: This study was designed to develop and evaluate chitosan films containing ciprofloxacin and diclofenac sodium for the topical treatment of periodontitis. Methods: Chitosan films containing ciprofloxacin alone and in combination with diclofenac sodium were prepared by solvent casting method. Some of the drug-loaded films were crosslinked with 2% gluteraldehyde for 2 and 4 h, respectively. The films were then evaluated for their physicochemical properties including weight variation, thickness, tensile strength, in vitro release, stability and antibacterial activity. Results: Mean weight and thickness data showed that the different films were uniform. Tensile strength was maximum for drug-free films and minimum for films containing the highest amount of drug(s). In vitro drug release data indicate that the films showed an initial burst release followed by sustained release of the drug(s). Films stored at refrigerated conditions exhibited slower degradation rate. The drug-loaded films that were crosslinked for 4 h had inhibitory effect on Staph mutans for up to 24 days. Conclusion: The study suggests that crosslinked chitosan film containing ciprofloxacin and diclofenac is a potential drug delivery device for the topical treatment of periodontitis. Good physicochemical properties were shown by the films

Development and evaluation of the effect of ethanol and surfactant in vesicular carriers on Lamivudine permeation through the skin

The skin embodies a relatively large and readily accessible surface area to absorb a drug through a non-invasive procedure. The vesicular carrier systems such as liposomes, ethosomes, and transethosomes have been explored as non-invasive systems for transdermal delivery of drugs. In the present study, different vesicular carriers were prepared by the thin-film hydration method with modification, and various parameters like size, elasticity, and release profiles were evaluated. Ethosomes and transethosomes have shown the smaller size of 362.21 ± 55.76 and 314.34 ± 41.21 nm, with deformity of 19.34% and 25.04%, respectively, compared with liposomes. The FTIR study of the skin before and after the application of vesicular formulation was performed. The ethosomes and transethosomes changed the orthorhombic phase to the liquid crystalline phase to move the vesicular carrier with the drug to cross the stratum corneum (SC) of the skin. The thermotropic behaviour of drug and vesicular carrier ingredients was studied using differential scanning calorimetry (DSC). Fluorescence images of vesicular-skin permeation have revealed that ethosome and transethosome formulation have shown deeper penetration across the SC and epidermis. The in vitro drug release from the ethosomes and transethosomes has shown 93.34 ± 1.23% and 95.45 ± 2.67% of drug release using Franz diffusion cell and porcine skin as a membrane. The nanostructured flexible vesicular carrier containing ethanol alone and a combination of ethanol and edge activator is a perfect carrier for drug penetration to the deeper skin layer and maintaining the sustained release of drug for a prolonged time