布洛芬缓释滴丸的处方工艺优化及体外释药行为评价

发布时间：2019-06-07 14:53

【摘要】：目的:优化布洛芬缓释滴丸的处方工艺并评价其体外释药特征。方法:以硬脂酸为缓释基质、聚乙二醇6000为速释基质,采用熔融法制备布洛芬缓释滴丸。以圆整度、丸重差异、载药率、体外释药时间的综合评分为指标,以药物与基质质量比、药液温度、冷凝温度、滴距为因素,通过正交试验优化处方工艺并验证。在去离子水、盐酸溶液(pH 1.2)、磷酸盐缓冲液(pH 4.5、6.8)4种介质中,比较自制缓释滴丸与市售布洛芬缓释胶囊的体外释药行为,并对前者的释药行为进行拟合。结果:最优处方工艺为布洛芬-聚乙二醇6000-硬脂酸的质量比为4.0∶15.3∶0.7,药液温度为83℃,冷凝温度为8℃,滴距为11 cm;所制3批布洛芬缓释滴丸的丸重差异为2.067%、圆整度为96.73%、载药率为96.31%、12 h的累积释放度为93.05%,RSD分别为1.19%、0.28%、0.19%、0.81%。自制缓释滴丸与市售布洛芬缓释胶囊体外释药行为的相似因子f2均大于50,前者释药更符合Higuchi方程(r为0.988 1~0.997 2)。结论:成功优化布洛芬缓释滴丸的处方工艺,所制缓释滴丸的体外释药行为与市售布洛芬缓释胶囊相似。
[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，

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