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本文将水不溶性药物葛根素制备成自乳化制剂。测定了葛根素在不同油相及表面活性剂的溶解度,结果表明葛根素在油酸、Tween 80中的溶解度较好,1,2-丙二醇不但能增加药物的溶解度,而且能够提高自乳化能力。以油酸为油相,Tween 80为表面活性剂,1,2-丙二醇为助表面活性剂,配制一系列混合物,通过绘制三元相图得到自乳化区,考察不同自乳化处方的自乳化性质,采用激光粒度散射仪测定乳化后粒子大小,在体外评价基础上选择较好的3个处方进行比格犬体内药动学研究,比较不同处方自乳化制剂在比格犬体内的生物利用度包括药代动力学参数Cmax,Tmax,AUC0-t。结果表明处方2和处方3的AUC0-t值[(5.201±0.511)ng.mL-1.h,(5.174±0.498)ng.mL-1.h]和Cmax值[(1.524±0.125)ng.mL-1,(1.513±0.157)ng.mL-1]显著高于处方4[(3.013±0.623)ng.mL-1.h,(0.939±0.089)ng.mL-1],通过体内研究结果获得较优处方为油酸(17.5%)、Tween 80(34.5%)、1,2-丙二醇(34.5%)。自乳化释药系统提供了水不溶性药物口服给药的新途径。
In this paper, the water insoluble drug puerarin is prepared into a self-emulsifying formulation. The solubility of puerarin in different oil phases and surfactants was measured. The results showed that puerarin had good solubility in oleic acid and Tween 80. 1,2-propanediol not only increased drug solubility, but also improved self-emulsifying capacity. Using oleic acid as the oil phase, Tween 80 as the surfactant and 1,2-propanediol as the cosurfactant, a series of mixtures were prepared. The self-emulsification zone was obtained by plotting the ternary phase diagram to investigate the self-emulsification properties of different self-emulsifying formulations. The particle size after emulsification was measured with a laser particle size scatterometer. Three in vivo pharmacokinetic studies of beagle dogs were selected on the basis of in vitro evaluation. The bioavailability of different formulations of self-emulsified preparations in beagle dogs was compared. Pharmacokinetic parameters Cmax, Tmax, AUC0-t. The results showed that the AUC0-t value of prescription 2 and prescription 3 [(5.201±0.511) ng.mL-1.h, (5.174±0.498) ng.mL-1.h] and Cmax value [(1.524±0.125) ng. mL-1, (1.513±0.157) ng.mL-1] was significantly higher than the prescription 4 [(3.013±0.623) ng.mL-1.h, (0.939±0.089) ng.mL-1], and the in vivo study results The best prescriptions were oleic acid (17.5%), Tween 80 (34.5%), and 1,2-propanediol (34.5%). The self-emulsifying drug delivery system provides a new route for the oral administration of water-insoluble drugs.