【摘要】：目的:優(yōu)化布洛芬緩釋滴丸的處方工藝并評價其體外釋藥特征。方法:以硬脂酸為緩釋基質(zhì)、聚乙二醇6000為速釋基質(zhì),采用熔融法制備布洛芬緩釋滴丸。以圓整度、丸重差異、載藥率、體外釋藥時間的綜合評分為指標,以藥物與基質(zhì)質(zhì)量比、藥液溫度、冷凝溫度、滴距為因素,通過正交試驗優(yōu)化處方工藝并驗證。在去離子水、鹽酸溶液(pH 1.2)、磷酸鹽緩沖液(pH 4.5、6.8)4種介質(zhì)中,比較自制緩釋滴丸與市售布洛芬緩釋膠囊的體外釋藥行為,并對前者的釋藥行為進行擬合。結(jié)果:最優(yōu)處方工藝為布洛芬-聚乙二醇6000-硬脂酸的質(zhì)量比為4.0∶15.3∶0.7,藥液溫度為83℃,冷凝溫度為8℃,滴距為11 cm;所制3批布洛芬緩釋滴丸的丸重差異為2.067%、圓整度為96.73%、載藥率為96.31%、12 h的累積釋放度為93.05%,RSD分別為1.19%、0.28%、0.19%、0.81%。自制緩釋滴丸與市售布洛芬緩釋膠囊體外釋藥行為的相似因子f2均大于50,前者釋藥更符合Higuchi方程(r為0.988 1~0.997 2)。結(jié)論:成功優(yōu)化布洛芬緩釋滴丸的處方工藝,所制緩釋滴丸的體外釋藥行為與市售布洛芬緩釋膠囊相似。
[Abstract]:Objective: to optimize the formulation process of ibuprofen sustained-release dropping pills and evaluate its release characteristics in vitro. Methods: ibuprofen sustained release pills were prepared by melting method with stearic acid as slow release matrix and polyethylene glycol 6000 as quick release matrix. Taking the comprehensive score of roundness, pill weight difference, drug loading rate and drug release time in vitro as indexes, taking the mass ratio of drug to matrix, liquid temperature, condensation temperature and drop distance as factors, the prescription process was optimized and verified by orthogonal test. In four media, deionized water, hydrochloric acid solution (pH 1.2) and phosphate buffer solution (pH 4.5, 6.8), the in vitro release behavior of self-made sustained-release dropping pills and ibuprofen sustained-release capsules was compared, and the drug release behavior of the former was fitted. Results: the optimum formulation process was as follows: the mass ratio of ibuprofen to polyethylene glycol 6000 stearic acid was 4.0 鈮，

本文編號：2494882