摘要
目的将鸢尾苷元(TG)制备成自微乳口服释药系统(SMEDDS),并对其体外溶出行为进行考察。方法以D-optimal设计原理为基础使用Design Expert软件对制剂处方进行优化,对制备出的制剂进行质量评价及体外溶出度研究。结果最终制备得到的TG-SMEDDS用水稀释10倍后得到粒径为(14.95±0.31)nm的O/W型微乳。粒径分布较均匀,Zeta电位为(-12.53±0.80)mV,载药量为20 mg/g,平均测定量为标示量的(99.03±0.70)%。TG-SMEDDS在pH 1.2盐酸溶液及pH6.8磷酸盐缓冲液中10 min累积溶出率均接近100%。结论 D-optimal设计可成功应用于TG-SMEDDS的处方优化,制备出的TG-SMEDDS相比TG原料药溶出度有显著改善,可以预期相较于TG原料药,TG-SMEDDS将更有利于胃肠道吸收,该研究结果可为TG剂型设计以及临床研究提供数据支持及参考。
Objective To prepare self micro-emulsifying drug delivery system(SMEDDS) of tectorigenin(TG),and investigate its dissolution.Methods The formulation was optimized using Design Expert based on D-optimal design.The microemulsion's physicochemical and in vitro dissolution were evaluated after self-microemulsification.Results The particle size and Zeta potential of the final formulation were(14.95 ± 0.31) run and(-12.53 ± 0.80) mV after it was diluted by 10 times with pure water.The microemulsion appeared to be spheres with homogeneous size,which canbe observed through a transmission electron microscope.The drug loading capacity was 20 mg/g,and the average content was(99.03 ± 0.70)%.The results of in vitro dissolution study showed that the accumulative dissolution could be close to 100%after 10 min in both hydrochloric acid solution(pH 1.2) and PBS(pH 6.8).Conclusion D-optimal design could be used to optimize the formulations of TG-SMEDDS successfully.The TG-SMEDDS exhibits a larger accumulation dissolution than TG.This formulation would be easier absorbed through gastrointestinal tract compared to TG.The results of this study are expected to offer data support and reference for the TG's formulation design and clinical application.
引文
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