Transport characteristics and absorption promoting methods of bergenin across Caco-2 cell monolayer model / 中国药学杂志

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.