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含有10-羟基喜树碱固体分散体的单室渗透片

Monolithic osmotic tablet containing solid dispersion of 10-hydroxycamptothecin.

作者信息

Chen Huanhuan, Jiang Guoqiang, Ding Fuxin

机构信息

Depatment of Chemical Engineering, Tsinghua University, Beijing, China.

出版信息

Drug Dev Ind Pharm. 2009 Feb;35(2):131-7. doi: 10.1080/03639040701657388.

DOI:10.1080/03639040701657388
PMID:19169941
Abstract

A novel monolithic osmotic tablet composed of solid dispersion of water-insoluble 10-hydroxycamptothecin (HCPT) was prepared. The tablet core was made of a suspending agent, polyethylene oxide, an osmotic agent, sodium chloride, and a solid dispersion consisting of polyethylene glycol 6000 and HCPT. Optimized formulation was able to deliver HCPT at the constant rate of 1.21 mg/hour for 12 hours with cumulative release above 90% in vitro, independent of environmental media and stirring rate, and the release rate is co-controlled by osmotic pressure, suspending effect, and drug solubility in solid dispersion. The monolithic osmotic tablet containing solid dispersion has great potential in the controlled delivery of water-insoluble drugs.

摘要

制备了一种由水不溶性10-羟基喜树碱(HCPT)固体分散体组成的新型整体式渗透片。片芯由悬浮剂聚环氧乙烷、渗透剂氯化钠以及由聚乙二醇6000和HCPT组成的固体分散体制成。优化后的制剂能够以1.21毫克/小时的恒定速率释放HCPT达12小时,体外累积释放率超过90%,且不受环境介质和搅拌速率的影响,释放速率由渗透压、悬浮作用以及药物在固体分散体中的溶解度共同控制。含有固体分散体的整体式渗透片在水不溶性药物的控释方面具有巨大潜力。

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