CAJ | 학술논문

目的以羟丙基甲基纤维素(HPMC-E5 LV)为载体材料制备HPMC-西沙必利固体分散体,通过提高模型药物的溶解度来改善药物的体外释放.方法分别用乙醇和人工胃液将药物和载体材料溶解,使药物均匀分散在载体中, 减压干燥除去溶剂得到HPMC-西沙必利固体分散物; 用X射线粉末衍射法分别测定了纯载体材料、纯西沙必利、载体材料和西沙必利物理混合物以及载体材料和西沙必利固体分散体4:1的晶体衍射峰, 以确定是否有晶体存在; 分别考察纯西沙必利和HPMC-西沙必利固体分散体在水、人工胃液和人工肠液中的溶解度; 分别以纯西沙必利和载体材料和西沙必利固体分散体制备了西沙必利缓释片并考察了其在水和人工胃液中的药物释放.结果当载体与药物的比例达到4:1时,X 射线衍射实验表明药物的晶体峰已经消失, 形成无定型固体分散体; 与西沙必利原料药相比, 固体分散体中药物在人工胃液、水和人工肠液中的溶解度分别提高了239.4%、132.6% 和117.9%; 体外药物释放结果表明, 当以水和人工胃液为介质时,药物从固体分散体制备的缓释片中的释放速度要快于用纯原料药制备的缓释片中的释放速度, 体外释药规律可以用 Higuchi's 动力学方程描述.结论以HPMC为载体材料与西沙必利制成固体分散体, 可以通过改善药物的溶解度来加快缓释制剂中药物的溶出速度.
목적이간병기갑기섬유소(HPMC-E5 LV)위재체재료제비HPMC-서사필리고체분산체,통과제고모형약물적용해도래개선약물적체외석방.방법분별용을순화인공위액장약물화재체재료용해,사약물균균분산재재체중, 감압간조제거용제득도HPMC-서사필리고체분산물; 용X사선분말연사법분별측정료순재체재료、순서사필리、재체재료화서사필리물리혼합물이급재체재료화서사필리고체분산체4:1적정체연사봉, 이학정시부유정체존재; 분별고찰순서사필리화HPMC-서사필리고체분산체재수、인공위액화인공장액중적용해도; 분별이순서사필리화재체재료화서사필리고체분산체제비료서사필리완석편병고찰료기재수화인공위액중적약물석방.결과당재체여약물적비례체도4:1시,X 사선연사실험표명약물적정체봉이경소실, 형성무정형고체분산체; 여서사필리원료약상비, 고체분산체중약물재인공위액、수화인공장액중적용해도분별제고료239.4%、132.6% 화117.9%; 체외약물석방결과표명, 당이수화인공위액위개질시,약물종고체분산체제비적완석편중적석방속도요쾌우용순원료약제비적완석편중적석방속도, 체외석약규률가이용 Higuchi's 동역학방정묘술.결론이HPMC위재체재료여서사필리제성고체분산체, 가이통과개선약물적용해도래가쾌완석제제중약물적용출속도.
Aim To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose (HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means of improving the solubility of the model drug. Methods Alcohol and simulated gastric fluid (SGF) were used to dissolve cisapride and HPMC in order to make the model drug dispersed homogeneously in the carrier. The HPMC-cisapride solid dispersion was then obtained by conventional solvent evaporation method. Powder X-ray diffraction (XRD) was used to measure the diffraction peaks of pure carrier, pure cisapride, physical mixture of HPMC with cisapride existence. The solubility of pure drug and HPMC-cisapride solid dispersion was measured with water, SGF and simulated intestinal fluid (SIF). The in vitro drug releases of the sustained release tablet prepared with pure cisapride or HPMC-cisapride solid dispersion were investigated with water and SGF as media, respectively. Results No diffraction peaks were found by that the drug existed in an amorphous form at that drug-carrier ratio. Compared with the pure drug, the solubilities of HPMC-cisapride solid dispersion are increased by 239.4% in SGF, 132.6% in water, and 117.9% in SIF. According to the in vitro drug release, the sustained release tablet prepared with HPMC-cisapride solid dispersion had a faster drug release than did that prepared with pure drug. The in vitro drug release profiles were found to comply with Higuchi's rule. Conclusion The in vitro drug release of the sustained release tablet made by HPMC-cisapride solid dispersion is improved owing to the increased drug solubility.