布洛芬缓释滴丸的处方工艺优化及体外释药行为评价
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篇名: 布洛芬缓释滴丸的处方工艺优化及体外释药行为评价
TITLE:
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 technology of Ibuprofen sustained-release dropping pill and evaluate its in vitro drug-release characteristics. METHODS: Using stearic acid as sustained-release matrix, polyethylene glycol 6 000 as immediate-release matrix, melting method was used to prepare the Ibuprofen sustained-release dropping pill. Using the comprehensive scores of roundness, weight difference, drug loading rate, in vitro drug-release time as indexes, drug-matrix mass ratio, liquid temperature, condensation temperature, dropping distance as factors, orthogonal test was adopted to optimize the formulation technology, and verification test was conducted. In media of deionized water, hydrochloric acid solution (pH 1.2), phosphate buffer (pH 4.5, 6.8), the in vitro drug-release were compared between self-made sustained-release dropping pill and commercially available Ibuprofen sustained-release capsule, which were fitted for former drug-release behavior. RESULTS: The optimal formulation technology was as follows as mass ratio of ibuprofen-polyethylene glycol 6000-stearic acid of 4.0 ∶ 15.3 ∶ 0.7, liquid temperature of 83 ℃, condensation temperature of 8 ℃, and dropping distance of 11 cm. The weight difference of prepared 3 batches of Ibuprofen sustained-release dropping pill was 2.067% (RSD=1.19%), roundness was 96.73% (RSD=0.28%), drug loading rate was 96.31% (RSD=0.19%), cumulative release rate in 12 h was 93.05% (RSD=0.81%). The f2 values of self-made sustained-release dropping pill and commercially available Ibuprofen sustained-release capsule were greater than 50, the former one fitted more into Higucci equation (r=0.988 1-0.997 2). CONCLUSIONS: The formulation technology of Ibuprofen sustained-release dropping pill is successfully optimized, and in vitro drug-release behavior of prepared sustained-release dropping pill is similar to commercially available Ibuprofen sustained-release capsule.
期刊: 2017年第28卷第28期
作者: 孟戎茜,邵圣娟,朱雪莲
AUTHORS: MENG Rongqian,SHAO Shengjuan,ZHU Xuelian
关键字: 布洛芬缓释滴丸;制备工艺;正交试验;体外释药
KEYWORDS: Ibuprofen sustained-release dropping pill; Preparation technology; Orthogonal test; in vitro drug-release
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