丹参注射液对格列喹酮在糖尿病大鼠体内药物代谢动力学参数和肠吸收特性的影响

目的考察丹参注射液对格列喹酮在糖尿病大鼠体内药物代谢动力学参数的影响,为两药的临床合用提供依据。方法链脲佐菌素腹腔注射建立糖尿病大鼠模型,考察丹参注射液对格列喹酮药物代谢动力学参数的影响;建立原位在体肠循环模型,研究丹参注射液对格列喹酮肠吸收特性的影响。结果糖尿病大鼠的药物代谢动力学研究结果表明,两药合用能够显著缩短格列喹酮的达峰时间,增加最大药物浓度、药时曲线下面积,并且可以显著减少清除率。肠吸收特性实验结果显示,丹参注射液可以显著增加格列喹酮在糖尿病大鼠体内吸收速率和表观渗透系数。结论丹参注射液和格列喹酮合用可以显著提高糖尿病大鼠格列喹酮的血药浓度和生物利用度,其原因可能与丹参注射液促进格列喹酮的小肠吸收相关。

Effect of Danshen Injection on Pharmacokinetic Parameters and Intestinal Absorption Characteristics of Gliquidone in Diabetic Rats

Objective To investigate the effect of Danshen injection on the pharmacokinetic parameters of gliquidone in diabetic rats, and to provide a basis for rational drug use in clinical practice. Methods A rat model of diabetes was established by intraperitoneal injection of streptozotocin to evaluate the effect of Danshen injection on the pharmacokinetic parameters of gliquidone in vitro, and an in situ intestinal perfusion model was established to analyze the effect of Danshen injection on the intestinal absorption characteristics of gliquidone. Results The pharmacokinetic parameters of the diabetic rats showed that Danshen injection significantly shortened the time to peak of gliquidone, increased the maximum drug concentration and the area under the drug-time curve, and significantly reduced clearance rate. The results of the intestinal absorption experiment showed that Danshen injection significantly increased the absorption rate and apparent permeability coefficient of gliquidone in diabetic rats. Conclusion Danshen injection combined with gliquidone can significantly increase the plasma concentration and bioavailability of gliquidone, which may be associated with the fact that Danshen injection can promote the small intestinal absorption of gliquidone.