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Pharmacokinetics, tissue distribution and relative bioavailability of geniposide-solid lipid nanoparticles following oral administration

机译:口服后side子苷-固体脂质纳米粒的药代动力学,组织分布和相对生物利用度

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摘要

Geniposide has various pharmacological effects; however, low oral bioavailability limits its clinical utility. This study explores the pharmacokinetics, tissue distribution and relative bioavailability of geniposide-solid lipid nanoparticles (SLNs) following oral administration. The geniposide solution and geniposide-SLNs were orally administered to the rats, respectively. The C-max value of geniposide in the geniposide-SLNs was significantly higher than that obtained with geniposide solution. Compared with the geniposide solution, the t(1/2) and MRT were prolonged; the CL and V1/F were increased with geniposide-SLNs. The AUC(0-infinity)values of geniposide-SLNs were 50 times greater than geniposide solution. The ratios of AUC(0-8 h) in the liver, spleen, heart, kidney, brain and lung of the geniposide-SLNs to geniposide solution were 25.93, 4.28, 27.91, 10.15, 5.16 and 16.22, respectively. Prepared geniposide-SLNs are very helpful for increasing the bioavailability of geniposide. These data suggest that SLNs are a promising delivery system to enhance the oral bioavailability of geniposide.
机译:子苷具有多种药理作用。但是,口服生物利用度低限制了其临床应用。这项研究探讨了口服后子苷固体脂质纳米颗粒(SLNs)的药代动力学,组织分布和相对生物利用度。将子苷溶液和子苷-SLN分别口服给予大鼠。子苷-SLNs中子苷的C-max值显着高于子苷溶液获得的C-max值。与子苷溶液相比,t(1/2)和MRT延长; gen子苷-SLNs增加CL和V1 / F。子苷-SLNs的AUC(0-无穷大)值是子苷溶液的50倍。子苷-SLNs在肝,脾,心,肾,脑和肺中的AUC(0-8 h)与子苷溶液的比例分别为25.93、4.28、27.91、10.15、5.16和16.22。制备的gen子苷-SLNs对于提高子苷的生物利用度非常有帮助。这些数据表明SLN是增强to子苷口服生物利用度的有前途的递送系统。

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