吲达帕胺肠溶微球的制备及影响因素考察

Preparation of the Enteric Microspheres of Indapamide and Investigation of the Influencing Factors

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。

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 is suitable for preparation of enteric microspheres of indapamide, the technology is simple and the release characters is good in vitro.