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目的:研究土荆芥油自微乳化给药系统(MTH-SMEDDS)的体外释药特性。方法:测定土荆芥油在不同分散介质中的表观油水分配系数,及自微乳化制剂中土荆芥油的相分布,考察释放度实验方法、释放介质、不同制剂组成比例对于药物释放特性的影响,并对释放曲线进行了方程拟合。结果:MTH在pH6.8的缓冲液中油水分配系数最大,且主要分布在乳剂的界面层。同一处方在人工胃液(含1%聚山梨酯80)中,以总体液平衡反相透析法测得释放量较大,且能够模拟体内条件。处方D(土荆芥油为40%,辛酸三酰甘油为10%,聚山梨酯80为50%,苯甲酸为2%)的释药量最大,释放曲线符合H ixson-crowell方程。结论:SMEDDS可以显著提高Ⅱ型药物MTH的释药速度与程度。
Objective: To study the in vitro drug release characteristics of the self-microemulsifying drug delivery system (MTH-SMEDDS). METHODS: The apparent oil/water partition coefficients of D. Nepeta oil in different dispersion media and the phase distribution of D. Nepeta oil in self-microemulsifying formulations were determined. The release rate test method, release medium, and composition ratios of different formulations were used to determine drug release characteristics. The effect of the equation was fitted to the release curve. RESULTS: MTH had the largest oil-water partition coefficient in pH 6.8 buffer and was mainly distributed in the interface layer of the emulsion. The same prescription in the artificial gastric fluid (containing 1% polysorbate 80), the total liquid equilibrium dialysis method measured greater release, and can simulate the in vivo conditions. Prescription D (40% for D. argentinus oil, 10% for caprylic acid triacylglycerol, 50% for polysorbate 80, and 2% for benzoic acid) had the highest drug release, and the release curve was consistent with the Hixson-crowell equation. Conclusion: SMEDDS can significantly increase the release rate and extent of type II drug MTH.