本文選題：尼群地平 + β-環(huán)糊精　； 參考：《中國(guó)新藥雜志》2015年06期

【摘要】：目的:采用飽和水溶液法制備尼群地平-β-環(huán)糊精包合物,并以包合物為原料制成片劑,提高片劑的體外溶出度。方法:以包封率、收率、載藥量為指標(biāo),采用加權(quán)評(píng)分法,通過(guò)正交設(shè)計(jì)優(yōu)選最佳包合工藝。以粉末直接壓片法制備尼群地平包合物片劑,測(cè)定其在4種不同介質(zhì)(含0.15%聚山梨酯-80的水溶液、p H1.2鹽酸溶液、p H 4.0醋酸鹽緩沖液、p H 6.8磷酸鹽緩沖液)中的溶出度。結(jié)果:采用"反加法",最佳包合工藝為包合溫度70℃,尼群地平與β-環(huán)糊精摩爾比為1∶2,醇水比為2∶5,包合時(shí)間2 h。包合物包封率可達(dá)79%,收率為84%,載藥量為14%。所制備片劑的體外溶出度顯著提高,45 min時(shí)溶出度70%。結(jié)論:采用最佳包合工藝制備的包合物可顯著改善尼群地平的溶出性能,所制備的包合物片劑能達(dá)到日本橙皮書(shū)的要求。
[Abstract]:Aim: to prepare nitrendipine-尾-cyclodextrin inclusion compound by saturated aqueous solution, and to improve the dissolution rate of the tablet in vitro by using the inclusion compound as raw material. Methods: with the encapsulation efficiency, yield and drug loading as the index, the optimal inclusion process was selected by orthogonal design. Nitrendipine inclusion compound tablets were prepared by direct powder pressing method and their dissolution in four different media (pH1.2 hydrochloric acid solution, pH 4.0 acetate buffer solution, pH 6.8 phosphate buffer solution) was determined. Results: the optimum inclusion temperature was 70 鈩，

本文編號(hào)：1981165