穿心莲内酯自微乳化释药系统的处方优化与评价

Optimization and evaluation of prescription for andrographolide self-microemulsifying drug delivery system

目的研究穿心莲内酯自微乳化释药系统(AP-SMEDDS)的处方工艺。方法通过溶解度试验、相容性试验、三元相图的绘制及星点设计-效应面法的优化,以粒径、Zeta电位和自微乳化时间为指标,筛选各组分的最佳组合和处方配比。并对优化的AP-SMEDDS的理化性质和体外溶出度进行测定。结果穿心莲内酯的自微乳处方是:Maisine35-1∶吐温20∶Transcutol P=14.3∶39.7∶46.0(质量比)。AP-SMEDDS的平均粒径为19.96 nm,自微乳化时间<20 s,Zeta电位-9.76 m V,1 h累积溶出度为94.6%,为市售滴丸的2.14倍。结论所制备的穿心莲内酯自微乳可显著提高穿心莲内酯的体外溶出度,有望提高穿心莲内酯的口服生物利用度。

Objective To develop the formulation of andrographolide self-microemulsifying system（ APSMEDDS）. Methods The optimum formulations of AP-SMEDDS were screened by solubility,compatibility,ternary phase diagram and Box-Behnken design-response surface methodology,with the particle size,Zeta electric potential and self-microemulsifying time as parameters. The physic-chemical property and dissolution characters of AP-SMEDDS were also determined. Results The optimum AP-SMEDDS was maisine35-1 ∶ Tween20 ∶ Tronssutol P = 14.3 ∶39.7 ∶46.0. The mean particle diameter was 19. 96 nm,the Zeta potential was- 9. 76 m V,and the self-microemulsifying time was less than 20 s. The accumulative dissolution of AP-SMEDDS was 94.6%,which was about 2.14 times as much as that of the marketed pills.Conclusion AP-SMEDDS can increase the accumulative dissolution of andrographolide significantly,which is advantageous to improve oral bioavailability of andrographolide.