尼莫地平固体分散物的研究

尼莫地平临床上主要用于防治缺血性脑血管疾病．该药为难溶性药物，生物利用度低，本文采用了固体分散技术制备了尼莫地平两种固体分散物，其体外溶出速率１０分钟以内达８０％以上，较市售片有显著提高．两种固体分散物中，固体分散物Ⅰ为本实验室研制，固体分散物Ⅱ参照国内、外文献用ＰＶＰ为载体制备．两种固体分散物均能明显提高尼莫地平的体外溶出速率，但固体分散物Ⅱ易于老化，经相对湿度ＲＨ７５％４０℃贮藏３个月溶出速率明显下降，同样条件下，固体分散物Ⅰ则无明显变化．二种固体分散物Ｘ－射线衍射图谱表明尼莫地平以非晶体状态存在，而在ＲＨ７５％４０℃条件下放置３个月后，固体分散物ⅡＸ－射线衍射图谱出现了尼莫地平结晶峰．

Study on the Preparation and Dissolution of the Solid Dispersions of Nimodipine

Two kinds of solid dispersion of nimodipine were prepared.Solid dispersion Ⅰ was studied in our department.Solid dispersion Ⅱ(nimodipine pvp)was prepared according to directions of a report.The dissolution rates of the two solid dispersions were obviously greater than that of the pure drug,but solid dispersion Ⅱ was very ready to age.When the two solid dispersions were exposed to an atmosphere of 75% relative humidity for 3 months at 40℃,dissolution rate of solid dispersion Ⅱ reduced obviously while that of solid dispersion Ⅰ didnot change.X ray powder diffraction analysis showed that the drug of two solid dispersions existed in amorphous form,but solid dispersion Ⅱ gave crystal peak when exposed to RH 75% at 40℃ for 3 months.