ABSTRACT
The present investigation concerns with the development of controlled release tablets of lamivudine using acetylated moth bean starch. The acetylated starch was synthesized with acetic anhydride in pyridine medium. The acetylated moth bean starch was tested for acute toxicity and drug-excipient compatibility study. The formulations were evaluated for physical characteristics like hardness, friability, % drug content and weight variations. The in vitro release study showed that the optimized formulation exhibited highest correlation (R) value in case of Higuchi kinetic model and the release mechanism study proved that the formulation showed a combination of diffusion and erosion process. There was a significant difference in the pharmacokinetic parameters (T(max), C(max), AUC, V(d), T(1/2) and MDT) of the optimized formulation as compared to the marketed conventional tablet Lamivir(®), which proved controlled release potential of acetylated moth bean starch.
Subject(s)
Anti-HIV Agents/administration & dosage , Drug Carriers/chemistry , Lamivudine/administration & dosage , Starch/chemistry , Acetylation , Animals , Anti-HIV Agents/pharmacokinetics , Anti-HIV Agents/pharmacology , Biological Availability , Chemistry, Pharmaceutical , Delayed-Action Preparations/administration & dosage , Delayed-Action Preparations/pharmacology , Drug Carriers/chemical synthesis , Drug Carriers/toxicity , Drug Stability , Excipients/chemistry , Female , Kinetics , Lamivudine/pharmacokinetics , Lamivudine/pharmacology , Male , Rabbits , Starch/chemical synthesis , Starch/toxicityABSTRACT
Highly substituted sago starch phosphate was synthesized using POCl(3) as cross-linking reagent. Titrimetric and Fourier transform infra red (FT-IR) spectral analysis were used to characterize the substitution. Studying the different factors affecting the reaction parameters showed that the optimal conditions for starch phosphorylation were: 4h reaction time and reagent concentration 1.5% (w/w). The physicochemical properties of cross-linked sago starch (CLSS) were done using Scanning electron micrograph (SEM), X-ray powder diffractometer (XRD and Thermogravimetric analysis (TGA). The results revealed that crystalline nature of native sago starch was transformed after cross-linking. TGA report exhibited higher thermal stability, which makes it suitable for various industrial applications. Swelling behavior showed high swelling at low temperature (30 and 60°C) as compared to high temperature (90°C).
Subject(s)
Cross-Linking Reagents/chemistry , Starch/chemistry , Starch/chemical synthesis , Chemistry, Physical/methods , Cross-Linking Reagents/pharmacology , Cycadopsida , Hot Temperature , Macromolecular Substances/chemistry , Microscopy, Electron, Scanning/methods , Models, Chemical , Spectroscopy, Fourier Transform Infrared/methods , Temperature , Thermogravimetry/methods , Time Factors , X-Ray Diffraction/methodsABSTRACT
In the present study, cross linked sodium carboxymethylated pea starch (SCPS) was synthesized and evaluated as tablet superdisintegrant in diclofenac sodium based tablets. SCPS was synthesized using native pea starch with monochloroacetic acid and NaOH in microwave radiation environment. Finally the dried product was cross-linked with phosphorous oxychloride, which produced granular highly swellable starch. SCPS with degree of substitution of 0.34 was formed and it was further evaluated as superdisintegrant in diclofenac sodium based tablets. Diclofenac sodium tablets were prepared by direct compression method with 2, 4, 6 and 8%w/w of SCPS as superdisintegrant and further comparatively evaluated for in vitro disintegration and dissolution study with Sodium starch glycolate containing tablets as reference. The results revealed that SCPS could be a promising superdisintegrant for immediate release tablets in concentration dependant manner.
