In Vitro Intestinal Absorption and Metabolism of Magnoflorine and its Potential Interaction in Coptidis Rhizoma Decoction in Rat.

BACKGROUND AND OBJECTIVES

In our previous studies, it was found that there existed pharmacokinetic interactions between magnoflorine and the rest of the ingredients in Coptidis Rhizoma. In this study, the pharmacokinetic interaction mechanism of magnoflorine with the rest of the components in Coptidis Rhizoma was researched based on the intestinal absorption and metabolism characteristics.

METHODS

The absorption characteristics of magnoflorine in each rat intestinal segments were evaluated by non-everted intestinal sac model. To identify the metabolites of magnoflorine, the acceptor solutions of each intestinal segment at 120 min were analyzed by HPLC-LTQ-Orbitrap MS.

RESULTS

The accumulative absorption (Q), the absorption rate (J) and the apparent permeability coefficient (P ) of magnoflorine were increased in duodenum, jejunum, ileum and colon of the Coptidis Rhizoma group as compared to the magnoflorine group, but there was no statistical difference between the two groups (P > 0.05). Four phase I metabolites of magnoflorine were identified in intestinal acceptor solutions of pure compound, while eight metabolites were detected in that of Coptidis Rhizoma decoction including six phase I metabolites and two phase II metabolic products.

CONCLUSIONS

It was shown that the rest of the ingredients in Coptidis Rhizoma accelerated the absorption of magnoflorine weakly and promoted the metabolism of magnoflorine in the gut. The effects of other processes in the pharmacokinetics should be further evaluated.