采用32因子设计方法对氯沙坦钾微颗粒持续给药系统的研制进行统计研究

Gokul Khairnar, Jitendra Naik, Vinod Mokale
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引用次数: 21

摘要

研究聚合物和表面活性剂浓度对氯沙坦钾(LST)微颗粒给药系统载药和体外释药的影响。采用O/O溶剂乳化法制备微颗粒。采用32全因子设计推导统计方程并构建等高线图来预测反应。自变量为聚合物浓度(A)、表面活性剂浓度(B),因变量为载药量百分比(Y1)和12 h释药百分比(Y2)。将制备的微颗粒与市售片剂进行了体外释放谱比较。与市场上销售的制剂相比,发现微颗粒的释放曲线是持续的。载药量在15.32% (F6) ~ 22.27% (F5)之间。FT-IR分析显示无药物赋形剂干扰。在−1级时,微颗粒的形貌为球形和光滑的,而在更高的+1级时,微颗粒的形貌为粗糙、不规则,表面有侵蚀、裂纹和皱纹。在XRD分析中,纯LST转化为微粒后,其晶型转变为非晶型。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
A statistical study on the development of micro particulate sustained drug delivery system for Losartan potassium by 32 factorial design approach

The purpose of this study was to investigate the effect of polymer and surfactant concentration on drug loading and in vitro drug release of micro particulate drug delivery system of Losartan potassium (LST). Microparticles were prepared by O/O solvent emulsification method. A 32 full factorial design was used to derive statistical equation and construct contour plots to predict responses. The independent variables selected were polymer concentration (A), surfactant concentration (B). Dependent variables were percentage drug loading (Y1) and percentage drug release at 12 h (Y2). The in vitro drug release profile of prepared microparticles was compared with marketed tablet formulation. The release profile of microparticles was found to be sustained as compared to the marketed formulation. The drug loading was found to be in the range of 15.32% (F6) to 22.27% (F5). FT-IR analysis revealed no drug excipient interference. The morphology of evaluated microparticles at −1 level was found to be spherical and smooth in nature while at higher level +1 it was found to be rough, irregular, with erosion, cracks and wrinkles on the surface. In XRD analysis crystalline pattern of pure LST was changed to amorphous pattern when converted to microparticles.

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