Pharmacokinetics of crocin-1 after oral administration in rats / 中国药学杂志

ABSTRACT

OBJECTIVE: To elucidate the intestinal absorption and pharmacokinetic characteristics of crocin-1, a major active constituent of the stigmas of saffron (Crocus sativus L) in rats after oral administration. METHODS: Extracted plasma samples were eluted by the mobile phase composed of methanol-2% acetate acid (pH 2) (48 52 for crocin-1 and 74 36 for crocetin) on Agilent Zorbax SB-C18 column monitored at 420 nm. RESULTS: An accurate, precise and selective analysis method was developed to determine crocein in rat plasma with the quantitation limit of 10 ng · mL-1. No crocin-1 was detected in both original and β-glucuronidase treated plasma samples. However, appreciable crocetin, the aglycon form of crocin-1, was observed in the original plasma. The concentration of crocetin did not increase obviously after hydrolization by β-glucuronidase. The average concentration-time data after oral administration of 1 mg · kg-1 crocin-1 showed that crocin-1 was rapidly absorbed as erocein and remained above 50 ng · mL-1 for about 10 h. The first peak appeared at 20 min and the second peak at 6 h. The area under curve (AUC), mean residence time (MRT) during 0 - 24 h and elimination half-life (t1/2k) were calculated as (1.16 ± 0.22) μg · h · mL-1, (5.4 ± 0.7) and (3.0 ± 0.6) h, respectively. CONCLUSION: Crocin-1 is absorbed as its hydrolyzation metabolite and shows relatively good pharmacokinetic characteristics. Crocetin may be thereby related to the pharmacological activities of crocin-1 in vivo. Copyright 2012 by the Chinese Pharmaceutical Association.