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Assessment of Intestinal Absorption of vitexin-2''-o-rhamnoside in Hawthorn Leaves Flavonoids in Rat Using in Situ and in Vitro Absorption Models

Assessment of Intestinal Absorption of vitexin-2''-o-rhamnoside in Hawthorn Leaves Flavonoids in Rat Using in Situ and in Vitro Absorption Models

Ying-ai Xu, Guorong Fan, Shen Gao, Zhanying Hong

Drug Dev Ind Pharm. 2008 Feb;34(2):164-70.

PMID: 18302035

Abstract:

The purpose of this study was to investigate the absorption mechanism of vitexin-2''-O-rhamnoside, the index component in hawthorn leaves flavonoids (HLF) in the rat intestine, using two different absorption models, the in situ single-pass intestinal perfusion and the in vitro everted gut sac model. The effective permeability coefficients (P(eff)) in the in situ single-pass intestinal perfusion experiments and the apparent permeability coefficients (P(app)) in the in vitro everted gut sac experiments were calculated. Furthermore, the influences of the P-glycoprotein inhibitors, verapamil and digoxin, on the intestinal absorption of vitexin-2''-O- rhamnoside in HLF were studied using the above-mentioned two models. Results showed that there were no significant differences in the absorption of vitexin-2''-O-rhamnoside in HLF in four segments of the rat intestine, duodenum, jejunum, ileum, and colon, and at different concentrations of HLF ranging from 0.05 mg/ml to 0.5 mg/ml (P > 0.05). The P(eff) values for vitexin-2''-O-rhamnoside in the rat jejunal perfusion at the concentration of 0.05, 0.1, 0.25, and 0.5 mg/ml were (2.48 +/- 0.33) x 10(-5); (2.23 +/- 0.67) x 10(-5); (2.18 +/- 0.48) x 10(-5); and (2.25 +/- 0.17) x 10(-5) cm/s, respectively. But there was significant difference between absence and presence of verapamil or digoxin (P < 0.05). P(eff) and P(app) values of vitexin-2''-O-rhamnoside in HLF were increased in the presence of verapamil or digoxin. In conclusion, vitexin-2''-O-rhamnoside can be classified into high permeability class drug according to the biopharmaceutical classification system. Passive diffusion dominates the absorptive transport behavior of vitexin-2''-O-rhamnoside in HLF. The absorption and secretion are mediated by the efflux transport system, P-gp. The absorption of vitexin-2''-O-rhamnoside in HLF can be enhanced administered together with P-gp inhibitors.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP64820991	Vitexin 2-O-rhamnoside		64820-99-1	Price

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