中国当代医药
中國噹代醫藥
중국당대의약
China Modern Medicine
2015年
27期
10-13
,共4页
醋酸艾塞那肽%缓释微球%体外释放
醋痠艾塞那肽%緩釋微毬%體外釋放
작산애새나태%완석미구%체외석방
Exenatide Acetate%Sustained-release Microspheres%Release in v itro
目的：制备注射用醋酸艾塞那肽缓释微球，以达到缓释作用，从而减少用药次数。方法以聚乳酸-羟基乙酸为载体，羧甲基纤维素钠水溶液为分散介质，乙酸乙酯为有机溶剂，甘露醇为保护剂，通过复乳-液中干燥法和冷冻干燥法制备注射用醋酸艾塞那肽缓释微球。以微球收率、粒径、包封率为指标，采用正交试验法来优化微球的处方和制备工艺。采用透析法考察含药微球的体外释药特性，计算微球累积释药百分率，绘制体外释药曲线。结果通过正交设计筛选出制备注射用醋酸艾塞那肽缓释微球的处方和制备工艺，载药量为21.3%，包封率为94.6%，Zeta电位为（-29.3±1.51）mV，含药缓释微球的体外释药过程符合Higuchi方程。结论制备的注射用醋酸艾塞那肽缓释微球具有30 d的缓释效果。
目的：製備註射用醋痠艾塞那肽緩釋微毬，以達到緩釋作用，從而減少用藥次數。方法以聚乳痠-羥基乙痠為載體，羧甲基纖維素鈉水溶液為分散介質，乙痠乙酯為有機溶劑，甘露醇為保護劑，通過複乳-液中榦燥法和冷凍榦燥法製備註射用醋痠艾塞那肽緩釋微毬。以微毬收率、粒徑、包封率為指標，採用正交試驗法來優化微毬的處方和製備工藝。採用透析法攷察含藥微毬的體外釋藥特性，計算微毬纍積釋藥百分率，繪製體外釋藥麯線。結果通過正交設計篩選齣製備註射用醋痠艾塞那肽緩釋微毬的處方和製備工藝，載藥量為21.3%，包封率為94.6%，Zeta電位為（-29.3±1.51）mV，含藥緩釋微毬的體外釋藥過程符閤Higuchi方程。結論製備的註射用醋痠艾塞那肽緩釋微毬具有30 d的緩釋效果。
목적：제비주사용작산애새나태완석미구，이체도완석작용，종이감소용약차수。방법이취유산-간기을산위재체，최갑기섬유소납수용액위분산개질，을산을지위유궤용제，감로순위보호제，통과복유-액중간조법화냉동간조법제비주사용작산애새나태완석미구。이미구수솔、립경、포봉솔위지표，채용정교시험법래우화미구적처방화제비공예。채용투석법고찰함약미구적체외석약특성，계산미구루적석약백분솔，회제체외석약곡선。결과통과정교설계사선출제비주사용작산애새나태완석미구적처방화제비공예，재약량위21.3%，포봉솔위94.6%，Zeta전위위（-29.3±1.51）mV，함약완석미구적체외석약과정부합Higuchi방정。결론제비적주사용작산애새나태완석미구구유30 d적완석효과。
Objective To prepare Exenatide Acetate Sustained-release Microspheres to realize the sustained-release effect and reduce the frequency of drug use. Methods Exenatide Acetate Sustained-release Microspheres were pre-pared by the method of double-elusion drying in liquid with PLGA as the carrier,ethyl acetate as the organic solvent, CMC-Na water solution as the dispersion medium and mannitol as the diluents and the method of freezing drying.The prescription and preparation process were optimized by orthogonal test with particle size,yield and encapsulation as the investigating index.The property of releasing drug in vitro was investigated by the method of dialysis.The cumulative drug-releasing percentage of Sustained-release Microspheres was calculated and the drug-releasing curve was drawn. Results The prescription and preparation process were screened according to the orthogonal test with a drug loading capacity of 21.3%,an encapsulation efficiency of 94.6% and a Zeta potential of (-29.3±1.51) mV.The releasing profile in vitro was in accordance with Higuchi equation. Conclusion The Exenatide Acetate Sustained-release Microspheres for injection have releasing effect of 30 days.
