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赤芍总苷是从传统中药赤芍中提取纯化得到的有效部位,它具有许多的生物学活性。然而,由于其生物利用度很低,目前上市的赤芍总苷制剂很少。本研究将溶解性差的赤芍总苷制备成自微乳化给药系统以提高其生物利用度。通过构建三元相图,得到最优的处方组成:赤芍总苷18.70%、油酸乙酯16.27%、聚氧乙烯氢化蓖麻油43.34%和乙二醇单乙基醚21.73%。同时评价了赤芍总苷的理化性质,包括形态学特征、粒径、zeta电位、乳化时间及溶出度。结果显示,赤芍总苷自微乳化制剂稳定性良好,在4种不同的溶出介质中(0.1 mol.L-1 HCl、pH 6.8磷酸盐缓冲液、pH 7.4磷酸盐缓冲液和水)的溶出速率较快。通过赤芍总苷自微乳化制剂与赤芍总苷混悬液在大鼠体内药代动力学实验结果比较,显示其相对生物利用度为152%,表明自微乳化给药系统可以提高赤芍总苷的生物利用度。
Radix paeoniae Rubra is extracted from the traditional Chinese medicine Paeoniae Alba extract the effective site, which has many biological activity. However, due to its low bioavailability, there are currently only a few formulations of total glycosides glycosides available. In this study, the poorly soluble total glycosides of Radix Paeoniae Alba prepared into a self-microemulsifying drug delivery system to improve its bioavailability. Through the construction of ternary phase diagram, the optimal formulation was obtained: total glucosides of paeoniae albicans 18.70%, ethyl oleate 16.27%, polyoxyethylene hydrogenated castor oil 43.34% and ethylene glycol monoethyl ether 21.73%. The physical and chemical properties of total glucosides of paeony were evaluated, including morphological characteristics, particle size, zeta potential, emulsifying time and dissolution. The results showed that the TPG self-microemulsifying formulation had good stability and dissolution in 4 different dissolution media (0.1 mol·L -1 HCl, pH 6.8 phosphate buffer, pH 7.4 phosphate buffer and water) Faster. The comparison of the pharmacokinetics of erythromycin total glycoside self-microemulsion and erythorboside suspension in rats showed that the relative bioavailability was 152%, indicating that self-microemulsifying drug delivery system can improve the radix paeoniae rubra Bioavailability of glycosides.