美沙拉嗪羟丙基β-环糊精包合物温敏型液体栓的制备及性质考察  

Preparation and in vitro Properties of Thermosensitive Liquid Suppositories of Mesalazine HP-β-CD Complex

作　　者：宋兴龙[1,2] 何文[1] 张玲莉[1] 李卫华[3] 

机构地区：[1]武汉大学人民医院药学部,武汉430060 [2]武汉大学药学院 [3]枝江市人民医院药剂科

出　　处：《中国药师》2016年第4期639-642,共4页China Pharmacist

摘　　要：目的:研制美沙拉嗪羟丙基β-环糊精(HP-β-CD)包合物温敏型液体栓,并对其体外性质进行考察。方法:以泊洛沙姆407和泊洛沙姆188为温敏材料,负载美沙拉嗪HP-β-CD包合物,制备美沙拉嗪HP-β-CD包合物温敏型液体栓;比较美沙拉嗪HP-β-CD包合物温敏型液体栓和美沙拉嗪液体栓的黏度、胶凝强度、生物黏附性、体外凝胶溶蚀及药物释放等。结果:与MSZ液体栓相比,美沙拉嗪HP-β-CD包合物的加入不影响液体栓的胶凝温度,能使液体栓的黏度、胶凝强度及生物粘附性显著增加。凝胶溶蚀不受包合物的影响,而药物释放率得到显著提高,且药物释放与凝胶溶蚀呈现良好的线性关系。结论:美沙拉嗪HP-β-CD包合物温敏型液体栓具有较理想的胶凝温度,以及良好的粘性、胶凝强度及生物粘附性,且体外释药速度较MSZ液体栓快。Objective： To prepare thermosensitive liquid suppositories of mesalazine（MSZ） HP-β-CD complex and study the in vitro properties. Methods： Poloxamer 407 （P407） and poloxamer 188 （P188） were used as the thermosensitive polymers to load MSZ HP-β-CD complex to prepare the thermosensitive liquid suppositories. The viscosity, gel strength, bioadhesion,in vitro gel erosion and drug release of MSZ HP-β-CD complex were compared with those of MSZ liquid suppositories. Results： Compared with that of MSZ liquid suppositories, the gel terhperature of MSZ HP-β-CD complex liquid suppositories was stable, while the viscosity, gel strength and bioadhesion of MSZ HP-β-CD complex liquid suppositories were increased significantly. The in vitro gel erosion was not affected by MSZ HP-β-CD complex, while the drug release was notably enhanced. The drug release and gel erosion showed a good linear relation- ship. Conclusion： MSZ HP-β-CD complex liquid suppositories show good gel temperature, viscosity, gel erosion and bioadhesion, and the in vitro release rate is faster than that of MSZ liquid suppositories.

关 键 词：美沙拉嗪 羟丙基β-环糊精 包合物 温敏型液体栓 制备 体外性质 

分 类 号：R944.9[医药卫生—药剂学]