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高乌甲素脂质体凝胶的制备及体外释药特性研究
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篇名: 高乌甲素脂质体凝胶的制备及体外释药特性研究
TITLE:
摘要: 目的:优化高乌甲素脂质体的处方与工艺,制备高乌甲素脂质体凝胶并考察其体外释药特性。方法:采用薄膜分散法制备高乌甲素脂质体,以包封率为评价指标,卵磷脂-胆固醇质量比、药脂质量比、水化温度为考察因素设计L9(34)正交试验,优化高乌甲素脂质体的处方工艺并验证。以最优处方工艺制备高乌甲素脂质体,观察其形态并测其粒径分布和Zeta电位;以1.0%卡波姆940为凝胶基质,制备高乌甲素脂质体凝胶并采用透析袋扩散法考察其体外释药特性,并与高乌甲素凝胶比较。结果:高乌甲素脂质体最优处方工艺为卵磷脂-胆固醇质量比8 ∶ 1,药脂质量比1 ∶ 10,水化温度55 ℃。最优处方所制乌甲素脂质体外观呈球状,结构完整,平均粒径为(379.6±0.71) nm(RSD=0.18%,n=3);多分散系数为(0.171±0.003)(RSD=1.58%,n=3);Zeta电位为(-23.1±0.02) mV(RSD=0.85%,n=3);包封率为(63.84±0.36)%(RSD=0.57%,n=3)。所制高乌甲素脂质体凝胶呈黏稠状乳白色半固体;体外释放试验结果显示,高乌甲素凝胶与高乌甲素脂质体凝胶分别在9、15 h左右药物释放达到平衡,其累积释放率分别为70.2%、63.9%,两者释药均符合Higuchi方程。结论:采用优化后的高乌甲素脂质体的处方及工艺所制高乌甲素脂质体凝胶质量较好,可有效延缓药物的释放。
ABSTRACT: OBJECTIVE: To optimize the formulation and technology of Lappaconitine liposome, to prepare Lappaconitine liposome gel and investigate the characteristics of its drug release in vitro. METHODS: Thin film dispersion method was used to prepare Lappaconitine liposome. L9(34) orthogonal test was designed to optimize the formulation technology of Lappaconitine liposome using encapsulation rate as evaluation index, the mass ratio of lecithin to cholesterol, the mass ratio of drug to lipid and hydration temperature as factors. Validation test was also conducted. Lappaconitine liposome was prepared by optimal technology. The morphology, particle size distribution and Zeta potential were observed. Using 1.0% carbomer 940 as gel matrix, Lappaconitine liposome gel was prepared and dialysis bag release test was used to investigate the characteristics of its drug release in vitro, and compared with Lappaconitine gel. RESULTS: The optimal formulation technology of Lappaconitine liposome was that mass ratio of lecithin to cholesterol was 8 ∶ 1; mass ratio of drug to lipid was 1 ∶ 10; hydration temperature was 55 ℃. The optimal formulation of lappaconitine liposome with a spherical appearance and complete structure, the average particle size was (379.6±0.71) nm (RSD=0.18%, n=3); PDI was (0.171±0.003) (RSD=1.58%,n=3); Zeta potential was (-23.1±0.02) mV (RSD=0.85%,n=3); encapsulation rate was (63.84±0.36)% (RSD=0.57%,n=3). Prepared liposome gel was sticky milky white semisolid. In vitro release experiments showed that the drug release of Lappaconitine gel and Lappaconitine liposome gel reached balance at 9 h and 15 h, and the accumulative release rate were 70.2% and 63.9%, both drugs release were in line with Higuchi equation. CONCLUSIONS: Use the optimized formulation and technology of Lappaconitine liposome to prepared Lappaconitine liposome gel with good quality and can effectively delay the release.
期刊: 2018年第29卷第15期
编辑: 肖卫红,徐宏峰,张耕,成薇婷
AUTHORS: XIAO Weihong,XU Hongfeng,ZHANG Geng,CHENG Weiting
关键字: 高乌甲素脂质体凝胶;薄膜分散法;正交试验;处方工艺;制备;体外释药
KEYWORDS: Lappaconitine liposome gel; Fhin film dispersion method; Orthogonal test; Formulation and technology; Prepare; Drug release in vitro
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