阿德福韦酯-PEG6000固体分散体的制备

Dissolution study of adefovir dipivoxil solid dispersion with polyethylene glycol 6000

目的将难溶性药物阿德福韦酯制备成固体分散体,以增加体外溶出度。方法以聚乙二醇6000(polyethylene glycol 6000,PEG6000)为载体,采用熔融法制备阿德福韦酯固体分散体;配合差示扫描量热(differential scanning calorimetry,DSC)与X-射线衍射(X-ray diffraction,XRD)观察药物在载体中的存在状态;考察相对湿度(relative humidity,RH)75%40℃放置3个月固体分散体对溶出度的变化及载体-药物质量比对溶出的影响。结果阿德福韦酯以无定型状态存在于固体分散体中,相对湿度RH75%40℃放置3个月固体分散体对溶出度改善明显,载体-药物质量比不同,药物的溶出度不同。结论将阿德福韦酯制成固体分散体能显著增加阿德福韦酯的体外溶出度。

Objective To prepare adefovir dipivoxil solid dispersion from poorly-soluble adefovir dipivoxil so as to improve its dissolution rate in vitro.Methods The hot melt method,with PEG6000 as carrier material,was used for preparation of adefovir dipivoxil solid dispersion.The status of adefovir dipivoxil in carrier was determined by differential scanning calorimetry（DSC）and X-ray diffracttion（XRD）.The effects of the variable ratio between the carriers and adefovir dipivoxil on dissolution were studied.Different results of dissolution of solid dispersions,which were exposed to 75% relative humidity for 3 months at 40 ℃,were compared.Results The study showed that adefovir dipivoxil in solid dispersion could be dispersed in carrier material with amorphous stabilities.Conclusions The dissolution of adefovir dipivoxil is increased by solid dispersion method.