Current Issue : April - June Volume : 2016 Issue Number : 2 Articles : 4 Articles
The aim of this work was to develop a tablet for the buccal delivery of the poorly water-soluble drug carvedilol. Carvedilol is a non-selective beta blocker indicated in the treatment of mild to moderate congestive heart failure (CHF). HPMC K100 and carbopol were selected as mucoadhesive polymers while ethyl cellulose, as backing material. The complexation was further characterized and studied by FTIR. The mucoadhesive tablets for the delivery of carvedilol were prepared by factorial designs by direct compression of HPMC K100 and carbopol. The tablets were evaluated for their dissolution, surface pH, swelling study and mucoadhesive properties. The surface pH of all formulations was found to be within ±1 units of neutral pH hence these formulations should not cause any irritation in buccal cavity. Carbopol showed superior bioadhesion properties compared to HPMC. The in-vitro release results demonstrated that drug was released by non-fickian diffusion mechanism with first order kinetics. From the drug release data, it was evident that formulation F5 has shown highly satisfactory values for correlation coefficient percentage in-vitro release 0.994, swelling index is 78.4±1.04 (after 6 hours) best formulation with correlation coefficient of 0.994. Hence, formulation F5 may be considered as the optimized buccal tablet containing carvedilol improved bioavailability....
Voriconazole is a new wide spectrum triazole with activity against yeast and molds. It is available as intravenous and oral formulations. No literature was available about solubilizing or formulating voriconazole for ophthalmic route. This study aimed to formulate and evaluate the in-situ gelling ophthalmic delivery systems of voriconazole. Different plain in-situ gel formulations were prepared using three different types of gelling agents, namely, Carbopol®940 (pH sensitive), Sodium alginate (ion sensitive) and Pluronic F127 (temperature sensitive) along with HPMC E50 LV as viscosity enhancing agent. The drug loaded in-situ gels were evaluated for their physical appearance, pH, rheological properties, drug content, stability and microbiological study. All prepared in-situ gel formulations successfully prolonged voriconazole release up to 4 hours. No significant changes in physical properties, drug content and pH were recorded on storage for 6 months at ambient conditions for pluronic F127 based formulations. Voriconazole-loaded in-situ gel showed the same antifungal activity against Candida albicans as voriconazole supersaturated solution. In conclusion, the studied in-situ gel formulations could be promising vehicles for ophthalmic delivery of voriconazole....
Transdermal delivery of drug avoids the first pass effect and provides greater and more prolonged levels of drug when compared to oral administration. Prochlorperazine blocks the D2 somatodendritic autoreceptor, resulting in the blockade of postsynaptic dopamine receptors in the mesolimbic system and an increased dopamine turnover. It also has anti-emetic effects, which can be attributed to dopamine blockade in the chemoreceptor trigger zone. It also blocks anticholinergic and alpha-adrenergic receptors, the blockade of alpha (1)-adrenergic receptors resulting in sedation, muscle relaxation and hypotension. In this study, matrix-type transdermal patches containing prochlorperazine maleate were prepared using different ratios of methocel E15LV, eudragit RL 100 and polyvinyl pyrolidone by solvent evaporation technique. All transdermal patches were evaluated for thickness, percent flatness, moisture uptake, tensile strength, drug content, weight variation, area variation, folding endurance and drug release studies for 6 hours. Selected patches were studied for in-vitro drug release and diffusion through cellophane membrane for 6 hours. The results indicated that combination of methocel E15LV, Eudragit RL 100 and polyvinyl pyrolidone can be used in the design of transdermal drug delivery system for prochlorperazine maleate....
The objective of the present work was to develop a self-emulsifying drug delivery system (SEDDS) for poorly water-soluble drug – leflunomide, to enhance its dissolution which could improve its oral absorption. The liquid SEDDS consisted of capmul MCM 8 as a vehicle for leflunomide, acrysol K 140 as a surfactant and transcutol P as a co-surfactant. Characterization of the SEDDS was performed by droplet size analysis, zeta potential and turbidity measurement. Ternary phase diagram was constructed to identify the self-emulsifying region after evaluation of leflunomide SEDDS by the visual observation. In-vitro dissolution test carried out for formulated leflunomide SEDDS filled in gelatine capsules. The present study revealed that the SEDDS can increase leflunomide dissolution rate and has the potential to enhance its oral bioavailability....
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