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目的:制备黄芩素自微乳化制剂(SMEDDS),考察其大鼠体内生物利用度。方法:采用伪三元相图法筛选自微乳的油相、表面活性剂及助表面活性剂;采用HPLC法测定大鼠血浆中药物浓度,与原料比较,对黄芩素自微乳进行大鼠体内生物利用度评价。结果:通过使用混合油相、混合表面活性剂及助表面活性剂,可获得较为理想的黄芩素自微乳。大鼠体内血药浓度-时间曲线结果表明,黄芩素自微乳的AUC是原料的3.77倍,且药时曲线的形状发生一定的改变。结论:自微乳系统可显著增加黄芩素的溶解度,有利于提高口服生物利用度,且自微乳可能改变其胃肠道吸收行为。
Objective: To prepare baicalein self-microemulsifying preparation (SMEDDS) and investigate its bioavailability in rats. Methods: The oil phase, surfactant and cosurfactant of self-microemulsion were screened by pseudo-ternary phase diagram. The plasma concentration of drug was determined by HPLC. Compared with the raw material, In vivo bioavailability assessment. Results: The ideal baicalein self-microemulsion was obtained by using mixed oil phase, mixed surfactants and cosurfactants. The concentration-time curve of rat plasma showed that the AUC of baicalein self-microemulsion was 3.77 times of that of the original material, and the shape of drug curve was changed. Conclusion: Self-microemulsion system can significantly increase the solubility of baicalein, which is beneficial to improve the oral bioavailability, and self-microemulsion may change its gastrointestinal absorption.