Oleanolic acid is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) has been developed to enhance the solubility and oral bioavailability of oleanolic acid. The formulation design was optimized by solubility assay, compatibility tests, and pseudoternary phase diagrams. The morphology, droplet size distribution, zeta potential, viscosity, electrical conductivity, and refractive index of a SMEDDS loaded with oleanolic acid were studied in detail. Compared with oleanolic acid solution, the in vitro release of oleanolic acid from SMEDDS showed that the drug could be released in a sustained manner. A highly selective and sensitive high-performance liquid chromatographymass spectrometry method was developed for determination of oleanolic acid in rat plasma. This method was used for a pharmacokinetic study of an oleanolic acid-loaded SMEDDS compared with the conventional tablet in rats. Promisingly, a 5.07-fold increase in oral bioavailability of oleanolic acid was achieved for the SMEDDS compared with the marketed product in tablet form. Our studies illustrate the potential use of a SMEDDS for delivery of oleanolic acid via the oral route.

译文

齐墩果酸是一种水溶性差的药物,口服生物利用度低。已开发出一种自微乳化药物递送系统 (SMEDDS),以增强齐墩果酸的溶解度和口服生物利用度。通过溶解度测定,相容性测试和假三元相图优化了配方设计。详细研究了装有齐墩果酸的SMEDDS的形态,液滴尺寸分布,ζ 电位,粘度,电导率和折射率。与齐墩果酸溶液相比,齐墩果酸从SMEDDS的体外释放表明该药物可以持续释放。建立了一种高选择性,灵敏的高效液相色谱质谱测定大鼠血浆中齐墩果酸的方法。与传统片剂相比,该方法用于齐墩果酸负载的SMEDDS的药代动力学研究。令人鼓舞的是,与片剂形式的市售产品相比,SMEDDS的齐墩果酸的口服生物利用度提高了5.07倍。我们的研究说明了SMEDDS通过口服途径递送齐墩果酸的潜在用途。

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