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Absorption characteristic of Paeoniflorin-6＇O-benzene sulfonate in an situ single-pass intestinal perfusion model

中国药理学通报 2015年第B11期31卷 215-215页

Aim Paeoniflorin-6＇O-benzene sulfonate （CP-25） was synthesized to improve oral absorption. This study was performed to investigate absorptive behavior and mechanism of CP-25 in intestine. Methods The effects of drug concentration, intestinal segments, gender as well as ATP binding cassette （ABC） transporter inhibitors on absorption of CP-25 were studied in a situ single-pass intestinal perfusion rat model. Meanwhile, Paeoniflorin （Pae） was tested and served as control group. The concentration of tested drugs was measured by HPLC. Results The results showed intestinal absorption of CP-25 was neither segmental dependent changes nor gender difference. Transepithelial transportation would not change with increasing concentrations of CP-25, which suggest a passive transport was the main pattern of CP-25. Additionally, absorption of CP-25 was much better than that of Pae in small intestine. When compared with Pae, CP-25 gave a 1.82-fold permeability rate. Finally, the results indicated Pae was substrate of P-glycoprotein （P-gp） , but was not the substrate of breast cancer resistance protein and muhi- drug resistance associated protein 2. Among the used ABC inhibitors, the absorption rate of Pae could only be in- creased by？ P-gp inhibitor Verapamil and GF120918, while CP-25 had no remarkable alteration. Conclusion CP-25 has better absorptive features than that of Pae, which may be attributed to its lipophicity enhancement and be unaffected by P-gp efflux.

关键词： Paeoniflorin Paeoniflorin-60-benzene sulfonate single-pass intestinal peffusion P-glycoprotein

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