Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam, India.
Int J Biol Macromol. 2012 Mar 1;50(2):362-8. doi: 10.1016/j.ijbiomac.2011.12.011. Epub 2011 Dec 21.
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.
本研究致力于开发使用乙酰化豇豆淀粉的拉米夫定控释片。采用乙酸酐在吡啶介质中合成乙酰化淀粉。对乙酰化豇豆淀粉进行了急性毒性和药物辅料相容性研究。对制剂的物理特性(如硬度、脆碎度、%药物含量和重量变化)进行了评估。体外释放研究表明,优化的制剂在 Higuchi 动力学模型中表现出最高的相关性(R)值,释放机制研究表明,该制剂表现出扩散和侵蚀过程的结合。与市售的传统片剂 Lamivir(®)相比,优化制剂的药代动力学参数(T(max)、C(max)、AUC、V(d)、T(1/2)和 MDT)有显著差异,这证明了乙酰化豇豆淀粉具有控制释放的潜力。