尼群地平固体分散体及其片剂的体外溶出度评价

In vitro evaluation of dissolution of nitrendipine solid dispersion and tablets

目的:运用固体分散技术提高尼群地平的体外溶出速率。方法:采用紫外分光光度法测定药物浓度,以体外溶出为指标,对固体分散体的载体、制备方法及比例进行优化。通过粉末直接压片法制备尼群地平固体分散片,根据日本橙皮书的要求对片剂的体外溶出进行考察。结果:采用泊洛沙姆188为载体,药物与载体比例为1∶5,通过熔融法制备的固体分散体体外溶出效果较好,且制成的片剂,在4种介质(含0.15%吐温-80的水溶液、pH1.2盐酸溶液、pH4.0醋酸盐缓冲液、pH6.8磷酸盐缓冲液)中,45 min时最低累积溶出度达80.3%。结论:通过固体分散技术制备的尼群地平片体外溶出能满足日本橙皮书的要求,且工艺简单、易于实施。

OBJECTIVE To improve dissolution rate of nitrendipine by solid dispersion technique.METHODS The nitrendipine concentrations were measured by UV method.The carriers,preparation technology and amounts of carriers were optimized with dissolution as the index.The nitrendipine tablets were prepared by direct powder compression technique,dissolution was determined as per Japan Orange Book.RESULTS Result of solid dispersion dissolution was much preferable via taking poloxamer 188 as the carrier,making the ratio between medicine and carrier 1∶5 and preparing by melting method.The lowest dissolubility of prepared tablets could reach 80.3% at 45 min in four media（0.15% tween-80 water solution,0.15%tween-80 hydrochloric acid solution（pH1.2）,0.15% tween-80 acetate buffer solution（pH4.0）,0.15% phosphate buffer solution（pH6.8）.CONCLUSION The dissolution of nitrendipine tablets prepared by solid dispersion method can meet the requirements in Japan Orange Book.This technique is simple and easy to carry out.