盐酸齐拉西酮自微乳的制备及其体内外活性

发布时间：2018-03-31 02:36

本文选题：盐酸齐拉西酮　切入点：自微乳　出处：《沈阳药科大学学报》2015年08期

【摘要】：目的制备盐酸齐拉西酮自微乳,提高其体外溶出度及其空腹口服生物利用度。方法选择对盐酸齐拉西酮溶解能力较强的油相,乳化剂和助乳化剂,观察微乳的形成并绘制伪三元相图比较微乳区域大小,通过乳化时间的测定,粒径和Zeta电位测定来确定最佳处方,测定盐酸齐拉西酮自微乳的体外溶出度以及其在Beagle犬体内药物动力学研究。结果以油酸乙酯(油相)-吐温80(乳化剂)-聚乙二醇200(助乳化剂)(质量比为30∶47∶23)时制得的自微乳经水稀释后可形成稳定的微乳,平均粒径为58.4nm,Zeta电位为-31mV。自制盐酸齐拉西酮自微乳和市售胶囊相比,其体外溶出度显著提高,达到93%。Beagle犬体内实验表明,自制盐酸齐拉西酮自微乳的吸收不受食物影响。结论盐酸齐拉西酮自微乳制备简单,微乳粒径小,可显著提高盐酸齐拉西酮的体外溶出度,及其空腹口服生物利用度。
[Abstract]:Objective to prepare ziprasidone hydrochloride self-microemulsion and to improve its dissolution in vitro and its oral bioavailability.Methods the oil phase, emulsifier and co-emulsifier with strong solubility to ziprasidone hydrochloride were selected. The formation of microemulsion was observed and the pseudo-ternary phase diagram was drawn to compare the size of microemulsion. The emulsifying time was determined.Particle size and Zeta potential were used to determine the optimum formulation, dissolution of ziprasidone hydrochloride self-microemulsion in vitro and pharmacokinetics of ziprasidone hydrochloride in Beagle dogs were studied.Results the stable microemulsion was obtained by water dilution with ethyl oleate (oil phase / tween 80) (emulsifier / polyethylene glycol 200 (mass ratio 30: 47: 23)). The average particle size of the self-microemulsion was -31mV with an average particle size of 58.4 nm 路m ~ (-1) 路L ~ (-1) 路min ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1).The dissolution of self-made ziprasidone hydrochloride microemulsion was significantly higher than that of commercial capsule in vitro. The results showed that the absorption of self-made ziprasidone hydrochloride microemulsion was not affected by food.Conclusion the preparation of ziprasidone hydrochloride self-microemulsion is simple and the particle size of microemulsion is small. The dissolution of ziprasidone hydrochloride in vitro and the bioavailability of ziprasidone hydrochloride on an empty stomach can be improved significantly.
【作者单位】：南京工业大学生物与制药工程学院;南京军区南京总医院制剂科;南京工业大学药学院;
【分类号】：R943

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