橘红素自微乳给药系统的制备及体内吸收研究

目的：设计和优化橘红素自微乳给药系统，改善药物的溶解及吸收，提高橘红素的口服生物利用度。方法：通过考察自微乳的粒径与粒径分布、乳化速度、Zeta电位、外观等指标，筛选并优化橘红素自微乳给药系统的处方，利用MDCK模型测定自微乳给药系统的体外吸收转运行为，并评价该给药系统在大鼠体内的药动学特性。结果：MDCK实验证实橘红素自微乳给药系统能够提高橘红素的吸收和转运，在SD大鼠体内的药动学结果表明橘红素的AUC_（0-∞）由（3 491.77±404.06）μg·L^-1·h提高至（9 435.18±1 633.81）μg·L^-1·h（P<0.01），C_max由（1 211.39±382.73）μg·L^-1·h提高至（2 371.73±481.87）μg·L^-1·h（P<0.05）。结论：制备出稳定的橘红素自乳化给药系统，体外溶出速度显著提高，从而有效提高橘红素的生物利用度。

Study of preparation and absorption of tangeretinself-microemulsifying administration systems

OBJECTIVE To design and optimize the tangeretinself-microemulsifying drug delivery system, in order to improve the drug dissolution and absorption as well as the oral bioavailability of tangeretin. METHODS By investigating the particle size and size distribution, emulsification rate, Zeta potential, appearance and other indicators of the microemulsion, the formulation of the tangeretinself-microemulsifying drug delivery system was screened and optimized. MDCK model was used to determinate the absorption and transport behavior of microemulsion drug delivery systemin vitro, and evaluate pharmacokinetic propertiesof the drug delivery system in rats. RESULTS MDCK experiments confirmed that the self-microemulsifying drug delivery system can improve the absorption and transport of tangeretin, pharmacokinetic results showed that the AUC_(0-∞) increased from (3 491.77±404.06)μg·L^-1·h to (9 435.18±1 633.81)μg·L^-1·h (P<0.01), C_max increased from (1 211.39±382.73)μg·L^-1·h to (2 371.73±481.87)μg·L^-1·h(P<0.05) in SD rats. CONCLUSION Preparation of a stable tangeretin self-microemulsifying drug delivery system increased the in vitro dissolution rate significantly, thus improve the bioavailability of tangeretin effectively.