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首页> 外文期刊>Journal of pharmaceutical sciences. >Enhanced bioavailability of a new thiazolidine derivative FPFS-410, an antidiabetic and lipid-lowering drug, after oral administration of its hydroxypropyl-beta-cyclodextrin complex to bile duct-cannulated rats.
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Enhanced bioavailability of a new thiazolidine derivative FPFS-410, an antidiabetic and lipid-lowering drug, after oral administration of its hydroxypropyl-beta-cyclodextrin complex to bile duct-cannulated rats.

机译：在将其羟丙基-β-环糊精复合物口服给予胆管插管大鼠后，新的噻唑烷衍生物FPFS-410是一种抗糖尿病和降脂药物，具有更高的生物利用度。

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The effect of bile acids on bioavailability of FPFS-410 (2-(N-Cyanoimino)-5-{(E)-4-styrylbenzylidene}-4-oxothiazolidine) after oral administration of the drug and its 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) complex was investigated. The complexation with HP-beta-CyD increased the oral bioavailability of FPFS-410 in normal rats in a HP-beta-CyD concentration-dependent manner, compared with that of drug alone. In bile duct-cannulated rats, bile acid concentrations in pylic serum and biliary were decreased to 18% and 14% of sham-operated rats, respectively. After oral administration of the HP-beta-CyD complex, the plasma levels of FPFS-410 were lower in bile duct-cannulated rats than in sham-operated rats up to 1 h, however, this order reversed from 2 to 12 h. The plasma levels of M1, a dominant metabolite of FPFS-410 in rats, significantly decreased until 2 h after administration of the complex in bile duct-cannulated rats, compared with in sham-operated rats. Bioconversion of FPFS-410 to M1 and CYP3A2 expression in the liver was markedly lowered by bile duct-cannulation. Bile duct-cannulation did not, however, affect the serum levels of estradiol. These results suggest that bile acids have a pivotal role for bioavailability of FPFS-410 after oral administration of the FPFS-410 complex with HP-beta-CyD through CYP3A2 activity in liver of rats.
机译：口服给药后胆汁酸对FPFS-410（2-（N-氰基氨基）-5-{（E）-4-苯乙烯基亚苄基} -4-氧噻唑烷）生物利用度的影响研究了环糊精（HP-β-CyD）复合物。与HP-β-CyD的复合物与单独药物相比，以HP-β-CyD浓度依赖性的方式增加了正常大鼠中FPFS-410的口服生物利用度。在胆管插管的大鼠中，幽门手术的大鼠的胆汁中胆汁酸的浓度分别降低至18％和14％。口服给予HP-β-CyD复合物后，直到1 h时，胆管插管大鼠的FPFS-410血浆水平均低于假手术大鼠，但此顺序从2到12 h相反。与假手术大鼠相比，胆管插管大鼠中，复合物给药后2小时，血浆中M1（FPFS-410的主要代谢产物）的血浆水平显着降低。胆管插管显着降低了肝脏中FPFS-410到M1和CYP3A2表达的生物转化。但是，胆管插管并不会影响雌二醇的血清水平。这些结果表明，胆汁酸在大鼠肝脏中通过CYP3A2活性口服给予FPFS-410与HP-β-CyD的复合物后，对FPFS-410的生物利用度具有关键作用。

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