羧甲基壳聚糖阴道温敏性原位凝胶的研制及体外质量考察  

Preparation and in vitro Quality Evaluation of Carboxymethyl Chitosan Temperature-sensitive In-situ Gel for Vaginal Use

作　　者：宋玲[1] 胡拥军[1] Song Ling;Hu Yongjun(Department of Pharmacy,Maternal and Child Health Care Hospital,Wuhan 430070,China)

机构地区：[1]湖北省妇幼保健院药剂科,武汉430070

出　　处：《中国药师》2021年第7期361-364,共4页China Pharmacist

摘　　要：目的:优化羧甲基壳聚糖(CCS)阴道温敏性原位凝胶的处方,并对其体外性质进行考察。方法:拟定CCS质量分数为1.0%,以pH 4.2乳酸-乳酸钠为缓冲体系,在单因素试验的基础上,以胶凝温度(T_(gel))为评价指标,以正交试验优化泊洛沙姆407(P407)、泊洛沙姆188(P188)、甘油及聚卡波菲(PCP)的用量。对最佳处方制备的CCS温敏性原位凝胶的pH、胶凝时间、黏度及体外释药特性进行考察。结果:优化的最佳处方为18%P407,5%P188,5%甘油及0.4%PCP。最佳处方制备的CCS温敏性原位凝胶平均T_(gel)为29.5℃,pH为4.12,胶凝时间为22.6 s,在8个温度单位内完成黏度的增加,体外释药符合一级动力学过程,且主要由基质溶蚀控制。结论:CCS温敏性原位凝胶体外性质符合阴道给药制剂的要求,并可迅速发生相转变,可望在阴道局部发挥缓释长效作用。Objective:To optimize the formula of carboxymethyl chitosan(CCS)thermal sensitive in-situ gel for vaginal use,and to study its quality in vitro.Methods:The mass fraction of CCS was 1.0%,and pH 4.2 lactic acid-sodium lactate solution was used as the buffer system.Based on the results of single factor experiment,and gelation temperature(T_(gel))as the evaluation index,orthogonal test was used to optimize the amounts of poloxmer 407(P407),poloxmer 188(P188),glycerin and polycarbophil(PCP).The pH value,gelation time,viscosity and release property in vitro of the optimized in-situ gel were explored.Results:The optimized formula was as follows:18%P407,5%P188,5%glycerin and 0.4%PCP.The T_(gel) of the in-situ gel was 29.5℃,the pH value was 4.12,the gelation time was 22.6 s,the viscosity was increased to the top within 8 time unit,and the in vitro release fit first-order kinetic property under the control of matrix erosion.Conclusion:The in vitro properties of CCS thermal sensitive in-situ gel meet the requirements of vaginal use with quick phase transition,which can be used for vagina with sustained and prolonged effects.

关 键 词：羧甲基壳聚糖 温敏性原位凝胶 阴道 制备 质量评价 

分 类 号：R944.T5[医药卫生—药剂学]