聚乙二醇
生物利用度
化学
药代动力学
赋形剂
熊果酸
体内
药理学
色谱法
核化学
有机化学
医学
生物技术
生物
作者
Tingting Zhao,Chenming Gu,Jianbo Qi,Jingwen Liu,Yajun Wang,Xiaojing Chen,Fujiang Guo,Yiming Li
摘要
Abstract Objectives The objective of this research was to enhance the bioavailability of ursolic acid (UA) by preparing multielement amorphous solid dispersion (ASD) systems comprising excipients. Methods The ASDs were prepared via the solvent evaporation method, characterized by a range of techniques, and investigated with respect to permeability of human colorectal adenocarcinoma cell line (Caco-2) cells monolayers and pharmacokinetics, with comparisons made to the physical mixture and the pure drug. Key findings The (UA-choline)-Polyethylcaprolactam—polyvinyl acetate—polyethylene glycol grafted copolymer (Soluplus)-Vitamin E polyethylene glycol succinate (TPGS) ASD demonstrated superior dissolution properties compared to the corresponding binary solid dispersions and ternary solid dispersions (P< .05). The permeability studies of Caco-2 cell monolayers revealed that the ASD exhibited moderate permeability, with an efflux rate that was significantly lower than that of the UA raw material (P< .05). Pharmacokinetic studies in rats demonstrated that the oral bioavailability of the ASD was 19.0 times higher than that of UA (P< .01). Conclusions The research indicated that the multielement ASD could be employed as an efficacious drug delivery system for UA. Furthermore, the Soluplus/TPGS/choline combination represents a promising candidate for the fabrication of ASDs that can load weakly acidic and poorly soluble drugs.
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