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目的研究岩白菜素透膜吸收机制及促吸收方法,为优化安全、稳定、有效的渗透泵制剂奠定基础。方法 围绕难溶性药物渗透泵制剂设计各相关因素,测定各转运样品在Caco-2细胞单层模型中的表观渗透系数Papp值及转运速率。结果 岩白菜素Papp值随浓度的增加变化不大,流出率ER值均小于1.5。分别与3种挥发油及3种皂苷合用后,岩白菜素Papp值及转运速率均显著增加;2种制剂增溶技术及渗透泵制剂常用的两种亲水性高分子辅料对岩白菜素Papp值没有明显影响。结论 岩白菜素未表现出主动转运特性;本实验揭示了岩白菜素渗透泵制剂设计的可能方向。
Objective To study the absorption mechanism and absorption promoting method of heliotrope of pericardium, which lays the foundation for optimizing the safe, stable and effective osmotic pump preparation. Methods The relevant factors were designed around the drug-insoluble osmotic pump formulation, and the Papp value and translocation rate of each transporter sample in the monolayer model of Caco-2 cells were determined. Results Bergenin Papp value did not change much with the increase of concentration, and the efflux rate ER values were less than 1.5. Papp value and translocation rate of bergenin were significantly increased when combined with three volatile oils and three saponins, respectively. Papp value of hematan for two formulations of solubilizing technology and two hydrophilic polymeric adjuvants commonly used in osmotic pump formulations No significant effect. Conclusions Bergenin did not exhibit active transport properties; this experiment revealed possible directions for the design of the bergenin osmotic pump formulation.