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采用析因设计研究羟丙甲纤维素和卡波姆对胃漂浮给药系统释放度和漂浮性能的影响。

Effect of HPMC and Carbopol on the release and floating properties of Gastric Floating Drug Delivery System using factorial design.

作者信息

Li Shoufeng, Lin Senshang, Daggy Bruce P, Mirchandani Haresh L, Chien Yie W

机构信息

Controlled Drug-Delivery Research Center, College of Pharmacy, Rutgers-The State University of New Jersey, Piscataway, NJ 08854, USA.

出版信息

Int J Pharm. 2003 Mar 6;253(1-2):13-22. doi: 10.1016/s0378-5173(02)00642-7.

Abstract

The purpose of this study is to investigate the effect of formulation variables on drug release and floating properties of the delivery system. Hydroxypropyl methylcellulose (HPMC) of different viscosity grades and Carbopol 934P (CP934) were used in formulating the Gastric Floating Drug Delivery System (GFDDS) employing 2 x 3 full factorial design. Main effects and interaction terms of the formulation variables could be evaluated quantitatively by a mathematical model. It was found that both HPMC viscosity, the presence of Carbopol and their interaction had significant impact on the release and floating properties of the delivery system. The decrease in the release rate was observed with an increase in the viscosity of the polymeric system. Polymer with lower viscosity (HPMC K100LV) was shown to be beneficial than higher viscosity polymer (K4M) in improving the floating properties of GFDDS. Incorporation of Carbopol, however, was found to compromise the floating capacity of GFDDS and release rate of calcium. The observed difference in the drug release and the floating properties of GFDDS could be attributed to the difference in the basic properties of three polymers (HPMC K4M, K100LV and CP934) due to their water uptake potential and functional group substitution.

摘要

本研究的目的是考察处方变量对给药系统药物释放及漂浮性能的影响。采用2×3全因子设计,使用不同黏度等级的羟丙基甲基纤维素(HPMC)和卡波姆934P(CP934)来制备胃漂浮给药系统(GFDDS)。通过数学模型可定量评估处方变量的主效应和交互项。结果发现,HPMC黏度、卡波姆的存在及其相互作用对给药系统的释放和漂浮性能均有显著影响。随着聚合物体系黏度的增加,释放速率降低。低黏度聚合物(HPMC K100LV)在改善GFDDS漂浮性能方面比高黏度聚合物(K4M)更具优势。然而,加入卡波姆会损害GFDDS的漂浮能力和钙的释放速率。GFDDS在药物释放和漂浮性能上观察到的差异可能归因于三种聚合物(HPMC K4M、K100LV和CP934)由于其吸水潜力和官能团取代而导致的基本性质差异。

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