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。
Abstract
Objective To study the transdermal absorption mechanism and Methods of absorption promotion of bergenin so as to optimize its safe, stable and effective osmotic pump preparation. Methods Caco-2 cell monolayer model was used to measure the apparent permeability coefficients(Papp) and transport rate of all samples considering the major relevant factors of osmotic pump preparation design of insoluble drugs. Results Pappvaried little while concentration of bergenin increased.The efflux rate(ER) was smaller than 1.5. Angelica dahurica extract, agnuside, Artemisia argyi oil, platycodin, oleanolic acid and ursolic acid had significant effects on the Papp and transport rate of bergenin. The inclusion compound and solid dispersion techniques could enhance the absorption of bergenin. The two common hydrophilic polymer excipients of osmotic pump preparation could not improve the membrane absorption rate and permeability of bergenin. Conclusion The absorption of bergenin across Caco-2 cell monolayer model may be passive transport. The study reveals possible directions for design of bergenin osmotic pump preparation.
关键词
Caco-2细胞 /
岩白菜素 /
渗透泵 /
促吸收 /
表观渗透系数
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Key words
Caco-2 cell /
bergenin /
osmotic pump /
absorption enhancement /
apparent permeability coefficient
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中图分类号:
R944
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参考文献
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脚注
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基金
成都医学院2009年科研基金课题(CYZ09-011)
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