Simultaneous evaluation of the effect of capsaicin on the activities of CYP1A2, 2C11 and 3 A by cocktail probe drug method / 中国药学杂志

ABSTRACT

OBJECTIVE: To study the effect of capsaicin on the activities of CYP1A2, 2C11 and 3A in rats by cocktail probe drug method. METHODS: Male rats were randomly divided into six groups. Three groups of rats (group A, B and C) were orally given capsaicin 25 mg · kg-1 once daily for 1, 3, 7 d, respectively. The other three groups (group a, b and c) received orally 0.5% carboxymethylcellulose sodium (CMC-Na) once daily for 1, 3, 7 d, respectively, as the blank control groups. Plasma was collected at different time after drug administration. The concentrations of caffeine, tolbutamide and dapsone in plasma were determined by HPLC method. The plasma concentration-time data was analyzed with DAS2.1.1 software to obtain the pharmacokinetic parameters of the cocktail probe drugs. RESULTS: Compared with the blank control group, the AUC0-t AUC0-t and pmax of caffeine in group C significantly decreased, along with significant increase of CL/F. The AUC0-t and pmax of tolbutamide in group C both significantly decreased compared with the blank control group. Meanwhile, the AUC0-t and AUC0-t of dapsone in group C significantly decreased, along with significant increase of CL/F and V/F. CONCLUSION: Capsaicin may significantly induce the activities of CYP1A2, CYP2C11 and CYP3A in rats after consecutive administration for 7 d. Reduced therapeutic efficacy of the drugs metabolized by CYP1A2, CYP2C11 and CYP3A should be anticipated during long-term administration of capsaicin.