吲达帕胺肠溶微球的制备及影响因素考察-中国现代应用药学.PDF

·药 剂· 吲达帕胺肠溶微球的制备及影响因素考察 郭海丽1,2 1,3 1* 1 1 1 ，阎志飞 ，丁红 ，张文静 ，赵志娟 ，杜艳 (1. 山西医科大学药学院药剂学教研室，太原 030001 ；2.太原市 妇幼保健院，太原 030001 ；3. 山西大医院，太原 030001) 摘要：目的 制备吲达帕胺肠溶微球及影响因素考察。方法 以羟丙甲纤维素酞酸酯(HPMCP)为肠溶载体材料，采用乳 化溶剂扩散法制备吲达帕胺肠溶微球，对影响微球的成型性、收率、载药量、包封率及其释药性能等因素进行了考察。 结果 微球形态圆整，架桥剂和乳化剂是其成型主要影响因素；载药量 14.85%，包封率76.30% ，药物在模拟肠液中累计 释放度符合要求，载体材料用量控制药物释放速度。结论 本方法适宜制备吲达帕胺肠溶微球，工艺简单，体外肠溶释 放性良好。 关键词：吲达帕胺；羟丙甲纤维素酞酸酯；肠溶微球；乳化溶剂扩散法 中图分类号：R943 文献标志码：B 文章编号：1007-7693(2012)11-0993-05 Preparation of the Enteric Microspheres of Indapamide and Investigation of the Influencing Factors GUO Haili1,2 1,3 1* 1 1 1 , YAN Zhifei , DING Hong , ZHANG Wenjing , ZHAO Zhijuan , DU Yan (1.Department of Pharmaceutics, Shanxi Medical University, Taiyuan 030001, China; 2.Taiyuan Hospital Health Center for Women and Children, Taiyuan 030001, China; 3.Shanxi Dayi Hospital, Taiyuan 030001, China) ABSTRACT: OBJECTIVE To prepare the enteric microspheres of indapamide and investigate the influencing factors. METHODS Enteric microsphere of indapamide was prepared by emulsion solvent diffusion method using hydroxypropyl methylcellulose phthalate(HPMCP) as an enteric polymer. The formulation of the microspheres, recovery, drug loading, encapsulation efficiency and the releasing characteristic of microspheres in vitro were investigated. RESULTS The microspheres were spherical and smooth in appearance, bridging agent and emulsifying agent were the main factors affecting the formation of microspheres. The drug loading and encapsulation were 14.85% and 76.30%, respectively. The cumulative release of drug in simulated intestinal fluid met the requirements and the amount of carrier material controlled the drug release rate. CONCLUSION This method i