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不同载药量对用纤维素酯制备的盐酸维拉帕米微球粒径分布和药物释放动力学的影响。

Effect of varying drug loading on particle size distribution and drug release kinetics of verapamil hydrochloride microspheres prepared with cellulose esters.

作者信息

Bhardwaj S B, Shukla A J, Collins C C

机构信息

SmithKline Beecham, Parsippanny, NJ 07054-3884, USA.

出版信息

J Microencapsul. 1995 Jan-Feb;12(1):71-81. doi: 10.3109/02652049509051128.

Abstract

Microspheres containing two different drug loadings of a calcium channel blocker, verapamil hydrochloride, were prepared with three different cellulose esters namely cellulose acetate (CA), cellulose acetate propionate (CAP) and cellulose acetate butyrate (CAB) of approximately similar molecular weights using the emulsion-solvent evaporation method. Increasing the drug loading from 33.3 to 50% w/w increased the geometric mean diameter of the microspheres as well as the T50% values, i.e. time required to release 50% of the drug from microspheres prepared with all the three cellulose esters. Drug release from the microspheres was affected by the nature of polymer. Mathematical modelling of drug release data by fitting the data to various equations revealed that the data did not fit the conventional Higuchi's and Baker-Lonsdale's models for drug release from spherical matrices. Instead, the data fitted the log-probability and the Weibull models quite well.

摘要

采用乳液-溶剂蒸发法,使用三种分子量近似的不同纤维素酯,即醋酸纤维素(CA)、醋酸丙酸纤维素(CAP)和醋酸丁酸纤维素(CAB),制备了含有两种不同载药量的钙通道阻滞剂盐酸维拉帕米的微球。将载药量从33.3% w/w提高到50% w/w,会增加微球的几何平均直径以及T50%值,即从用所有三种纤维素酯制备的微球中释放50%药物所需的时间。微球的药物释放受聚合物性质的影响。通过将药物释放数据拟合到各种方程进行数学建模表明,这些数据不符合传统的Higuchi模型和Baker-Lonsdale模型中关于球形基质药物释放的情况。相反,这些数据与对数概率模型和威布尔模型拟合得相当好。

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