西沙必利HPMC固体分散体的制备及对药物体外释放的促进作用

Preparation of HPMC-cisapride solid dispersion and the improvement effect on in vitro release

目的以羟丙基甲基纤维素(HPMC)为载体、西沙必利为模型药物制备固体分散体,以此来提高药物在水中的溶解度和体外释放速度。方法利用溶剂挥发法,分别用乙醇和0.1 mol·L-1HCl将药物和载体溶解,使药物均匀分散在载体中,再减压除去溶剂得到固体分散体。结果当载体与药物的比例为4:1时,X射线衍射实验表明药物的晶体峰已经消失。与西沙必利的原药相比,固体分散体中药物在水、人工胃液和人工肠液中的溶解度分别提高了339.43%、232.62%和217.95%。体外药物释放结果表明,当以水和人工胃液为介质时,用固体分散体制备的缓释片的药物释放速度要快于用原料药制备的缓释片。结论羟丙基甲基纤维素(HPMC E 5-LV)作为载体材料可以和西沙必利形成固体分散体,并提高了药物的溶解度和体外释药速度。

Objective To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose(HPMC) as carrier for the purpose to accelerate the in vitro drug release by means of improving the solubility of model drug.Methods Alcohol and 0.1 mol·L-1HCl were used separately to dissolve cisapride and HPMC so as to make the model drug dispersed homogeneously in the carrier.The HPMC-cisapride solid dispersion was then obtained by drying under reduced pressure,called solvent-evaporation technique.Results An increased drug solubility was noted by 339.43%,232.62%and 217.95% for the HPMC-cisapride solid dispersion in water,simulated gastric fluid and simulated intestinal fluid compared with pure drug.A was the faster with the tablets in vitro drug release from the tablet prepared by the HPMC-cisapride solid dispersion of the pure drug as a control.Conclusion Solid dispersion of cisapride can be prepared with HPMC E 5 LV as a carrier with drug solubility increased and in vitro drug release enhanced.