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为了提高难溶性药物尼莫地平的溶出度,并在此基础上研制出其速释制剂,本研究选用PVP(k30)为载体制备了尼莫地平的固体分散体及机械混合物,比较了二者体外药物溶出度及药物的结晶形态,并考查了共沉淀物的稳定性。进而进行了尼莫地平速释片剂处方的筛选,并按最优处方制备了胶囊剂。比较了自制速释胶囊剂与市售片剂的释药情况。体外实验结果表明,固体分散体对尼莫地平溶出度的提高大大优于机械混合物,5分钟的释药量,前者为89%,而后者仅为45%。X-射线衍射实验表明,尼莫地平在以PVP为载体的固体分散体中是以非晶体形式存在,并且在室温并密封于玻璃瓶中放置一年后仍无结晶出现。本研究制备的片剂和胶囊剂都具有速释性质,而以胶囊剂为优,说明压片压力可能影响溶出。速释胶囊的释药速率大大高于市售普通片剂。
In order to improve the dissolution rate of nimodipine, a poorly soluble drug, and to develop its immediate release preparation, PVP (k30) was used as a carrier to prepare the solid dispersion and mechanical mixture of nimodipine. In vitro drug dissolution and drug crystal morphology, and examined the stability of coprecipitate. Further, the formulation of nimodipine immediate release tablets was screened and the capsules were prepared according to the optimal prescription. The release profiles of self-made instant capsules and commercial tablets were compared. In vitro experimental results show that the dissolution rate of solid dispersion for nimodipine is much better than that of mechanical mixture, which is 89% for 5 minutes, while the latter is only 45%. X-ray diffraction experiments showed that nimodipine was present in amorphous form in solid dispersions with PVP as carrier and no crystallisation occurred after one year at room temperature and sealed in glass bottles. The tablets and capsules prepared in this study all have immediate-release properties, while the capsules are the best, indicating that the tabletting pressure may affect the dissolution. The release rate of immediate release capsules is much higher than that of ordinary tablets.