尼莫地平固体分散体的制备及体外研究

 目的：制备尼莫地平速释型固体分散体，增加其溶解度和溶解速度。方法：以聚乙烯吡咯烷酮(PVP)、聚乙二醇6000(PEG 6000)和泊洛沙姆188(Pol 188)为载体溶剂法和溶剂熔融法制备固体分散体，差热分析和X射线粉末衍射分析鉴别药物在载体中的存在状态，并进行体外溶出度研究。结果：尼莫地平在PVP中以无定形存在，在PEG 6000和Pol 188中以微细结晶存在。载体比例越大，药物溶出愈快；比例相同时，Pol 188-尼莫地平固体分散体溶出最快，且载体比例愈小，差异愈显著。结论：Pol 188作为尼莫地平固体分散体的载体，载药量大，增溶效果显著。

Preparation and in vitro evaluation of nimodipine solid dispersions

To improve the dissolution of nimodipine (NM). METHOD: Nimodipine solid dispersions were prepared using solvent-melting and coevaporation methods with poloxamer 188, PEG 6000 and PVP as carriers. Differential thermal analysis and X-ray powder diffractometry were used to determine the status of nimodipine in carriers, and in vitro dissolution characteristics were studied in simulated gastric juice. RESULT: In Poloxamer 188-NM and PEG 6000-NM solid dispersions, nimodipine existed as fine crystalline; while in PVP-NM solid dispersions, NM was amorphous. In vitro dissolution results showed that higher carrier-NM ratio led to faster drug dissolution. Poloxamer 188 was superior to PEG 6000 and PVP in its ability to accelerate the dissolution of NM. CONCLUSION: Poloxamer 188 was potent in improving the solubility and dissolution of NM and had the potentiam for practical use.