期刊
ARCHIVES OF PHARMACAL RESEARCH
卷 34, 期 7, 页码 1161-1170出版社
PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-011-0714-y
关键词
P-glycoprotein; Colchicine; Rhodamine123; Borneol; Intestinal absorption; Bioavailability
资金
- National Natural Science Foundation of China [30973644]
- National Basic Research Program of China (973 Program) [2007CB936004]
- Key Project of National innovative Drug RD [2009ZX09502-009]
- Key Project of national comprehensive technology platforms for innovative drug RD [2009ZX09301-007]
As the most prevalent route of delivery, oral administration has the challenge of potentially low bioavailability in part because P-glycoprotein (P-gp) in the intestinal tract affects absorption. Therefore, absorption enhancers or P-gp inhibitors are strategies to solve this problem. The aim of the present study was to investigate the effects of borneol on transportation of colchicine and rhodamine123, two P-gp substrates, in rats. In vitro transportation was assessed with a diffusion chamber system with isolated rat intestines. Different concentrations of borneol (10, 40 and 80 mu g/mL) were prepared in solutions with two P-gp substrates compared with blank solutions. The in vivo effects on colchicine were assessed by a pharmacokinetic study. Borneol enhanced the absorptive transport of two P-gp substrates, which was relevant to the concentration. A pharmacokinetic study showed that in the presence of borneol, a significant increase in C-max and AUC(0 -> 8) of colchicine occurred when compared to colchicine alone. The study showed that borneol affected two P-gp substrates in the intestine, possibly by inhibiting the effects of P-gp and enhancing intestinal absorption of drugs. Therefore, borneol could be developed as a P-gp inhibitor and absorptive enhancer.
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