和厚朴酚自乳化释药系统的制备与药动学评价  

Preparation and pharmacokinetic evaluation of honokiol self-emulsifying drug delivery systems

作　　者：王萌 WANG Meng(Xianyang Vocational and Technical College,Xianyang 712000,China)

机构地区：[1]咸阳职业技术学院,咸阳712000

出　　处：《西北药学杂志》2023年第5期84-91,共8页Northwest Pharmaceutical Journal

摘　　要：目的开发和厚朴酚自乳化释药系统(honokiol-self-emulsifying drug delivery systems,HK-SEDDSs),以改善药物的口服生物利用度。方法以丙二醇单辛酸酯(capryol 90)为油相、辛酸癸酸聚乙二醇甘油酯(labrasol)为表面活性剂、二乙二醇单乙基醚(transcutol P)为助表面活性剂,用伪三元相图法结合Box-Behnken实验设计优化HK-SEDDSs的处方;考察HK-SEDDSs的热力学稳定性,并用透射电镜对HK-SEDDSs形成的微乳进行表征;评价HK-SEDDSs的体外溶出以及大鼠口服生物利用度。结果优化得到HK-SEDDSs的处方:capryol 90、labrasol与transcutol P的质量比为10∶60∶30。用优化后的处方制备的HK-SEDDSs热力学稳定性良好,在透射电镜下微乳呈类球形。HK-SEDDSs中的药物在30 min内可完全溶出,远快于原料药的溶出速率。与HK混悬剂相比,HK-SEDDSs显著提高了大鼠的口服生物利用度。结论将HK制备成SEDDSs,有助于药物的快速溶出,显著提高了HK的口服生物利用度。Objective To develop honokiol self-emulsifying drug delivery systems(HK-SEDDSs)to improve the oral bioavailability of honokiol.Methods Capryol 90 was used as the oil phase,labrasol was used as the surfactant,and transcutol P was used as the cosurfactant.The formulation of HK-SEDDSs was optimized by pseudo-ternary phase diagram method combined with Box-Behnken experimental design.The thermodynamic stability of HK-SEDDSs was investigated,and the microemulsion formed by HK-SEDDSs was characterized by transmission electron microscopy.The in vitro dissolution and oral bioavailability of HK-SEDDSs in rats were evaluated.Results The optimized formulation of HK-SEDDSs was as follows:The mass ratio of capryol 90∶labrasol∶transcutol P was 10∶60∶30.HK-SEDDSs had a good thermodynamic stability.And the microemulsion formed by HK-SEDDSs was spherical under transmission electron microscope.The drug in HK-SEDDSs could be completely dissolved within 30 minutes,which was much higher than the dissolution rate of honokiol.Compared with honokiol suspension,HK-SEDDSs could significantly improve the oral bioavailability in rats.Conclusion HK was prepared into SEDDSs,which was helpful for the rapid dissolution and significantly improved the oral bioavailability of HK.

关 键 词：和厚朴酚 自乳化释药系统 Box-Behnken实验设计 口服生物利用度 

分 类 号：R94[医药卫生—药剂学]