二氢青蒿素自乳化药物传递系统油水分配系数的制备与检测。
Oil-water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system.
机构信息
Chongqing Academy of Chinese Materia Medica, No.34 of Nanshan Road, Nanan District, Chongqing, 400065, China.
Chengdu University of TCM, Chegndu, 611137, China.
出版信息
BMC Biotechnol. 2022 May 27;22(1):16. doi: 10.1186/s12896-022-00746-6.
BACKGROUND
The aim of the present study is to increase the solubility of dihydroartemisinin (DHA) using the self-emulsifying drug delivery system (SEDDS).
METHODS
We first conducted solubility test and ternary phase diagram, then, in order to optimize the formulation of the DHA self-emulsifying agent, the design mixture method was selected in the design expert software. Next, optimal prescription validation and preliminary formulation evaluation were conducted. By comparing the oil-water partition coefficient in vitro, the improvement of the in vivo osmotic absorption of DHA via self-emulsification was evaluated.
RESULTS
The optimal prescription ratio of oleic acid polyethylene glycol glyceride, polyoxyethylene hydrogenated castor oil, and diethylene glycol monoethyl ether in the DHA self-emulsifying preparation = 0.511:0.2:0.289 (w/w/w), with a drug-loading capacity of 26.3634 mg/g, solubility of 2.5448 mg/ml, and self-emulsification time of 230 s. The solubility self-emulsification was approximately 20.52 × higher in DHA than in the crude drug. The self-emulsification could improve DHA permeability and promoting in vivo DHA absorption.
CONCLUSION
The DHA SEDDS could significantly improve DHA solubility and in vivo absorption.
背景
本研究旨在通过自乳化药物传递系统（SEDDS）来提高二氢青蒿素（DHA）的溶解度。
方法
我们首先进行了溶解度试验和三元相图，然后，为了优化 DHA 自乳化剂的配方，我们在设计专家软件中选择了设计混合方法。接下来，进行了最佳处方验证和初步配方评估。通过比较体外油水分配系数，评估了通过自乳化提高 DHA 体内渗透吸收的效果。
结果
DHA 自乳化制剂中油酸聚乙二醇甘油酯、聚氧乙烯氢化蓖麻油和二乙二醇单乙基醚的最佳处方比例为 0.511:0.2:0.289（w/w/w），载药量为 26.3634 mg/g，溶解度为 2.5448 mg/ml，自乳化时间为 230 s。DHA 的溶解度自乳化约为原料药的 20.52 倍。自乳化可以提高 DHA 的通透性，促进体内 DHA 的吸收。
结论
DHA SEDDS 可以显著提高 DHA 的溶解度和体内吸收。
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