香叶木苷凝胶剂的制备及体外释药特性研究
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篇名: | 香叶木苷凝胶剂的制备及体外释药特性研究 |
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摘要: | 目的:筛选香叶木苷凝胶剂的最优处方,并考察其体外释药特性。方法:以卡波姆940为基质制备香叶木苷凝胶剂;以累积释放率为考察指标,卡波姆940、乙醇、丙三酮用量以及pH值为考察因素设计L9(34)正交试验,优化香叶木苷凝胶剂的处方并验证。以香叶木苷软膏剂为参照,采用透析袋扩散法考察按最优工艺所制香叶木苷凝胶剂的体外释药特性。结果:香叶木苷凝胶剂最优处方为卡波姆940 1.5 g、乙醇15 mL、丙三醇8 g、pH 6。按最优处方所制凝胶剂呈黏稠状棕黄色半固体,涂展性良好;释药2 h时的平均累积释放率为(12.67±0.12)%。体外释药试验结果显示,香叶木苷凝胶剂在12 h内释放较快,然后逐渐放缓,12、24 h时的累积释放率分别为(71.93±0.42)%、(80.47±0.54)%,其释药符合Higuchi方程;香叶木苷软膏剂释放较慢,12、24 h时的累积释放率分别为(41.74±0.18)%、(62.63±0.59)%,其释药符合一级方程。结论:成功优化了香叶木苷凝胶剂的处方;所得香叶木苷凝胶剂释药性良好。 |
ABSTRACT: | OBJECTIVE: To optimize the formulation of Diosmin gel and to investigate its in vitro release property. METHODS: Diosmin gel were prepared by using Carbomer 940 as matrix. Using accumulative release rate as index, with the amount of Carbomer 940, ethanol, acetone and pH as factors, L9(34) orthogonal test was conducted. The formulation of Diosmin gel was optimized and validated. Using Diosmin ointment as reference, dialysis bag diffusion method was used to investigate in vitro release property of Diosmin gel prepared by optimal formulation. RESULTS: The optimal formulation of Diosmin gel included Carbomer 940 1.5 g, ethanol 15 mL, glycerol 8 g, pH 6. The gel prepared with optimal formulation was sticky brown-yellow semi solid, and had good coating and spreading properties. The average accumulative release rate (2 h) was (12.67±0.12)%. Results of drug release test showed that Diosmin gel released rapidly within 12 h, then gradually slowed down. The accumulative release rates were (71.93±0.42)% (12 h) and (80.47±0.54)% (24 h), drug release of which were in line with Higuchi equation. Diosmin ointment was released slowly. The accumulative release rates were (41.74±0.18)% (12 h) and (62.63±0.59)% (24 h). Drug release of it were in line with first-order equation. CONCLUSIONS: The formulation of Diosmin gel is optimized successfully. Prepared Diosmin gel has good drug release property. |
期刊: | 2019年第30卷第20期 |
作者: | 崔明宇,刘媛媛,胡启萌,关枫,马英丽 |
AUTHORS: | CUI Mingyu,LIU Yuanyuan,HU Qimeng,GUAN Feng,MA Yingli |
关键字: | 香叶木苷;凝胶剂;工艺优化;体外释药;累积释放率 |
KEYWORDS: | Diosmin; Gel; Formulation optimization; in vitro release; Accumulative release rate |
阅读数: | 315 次 |
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