复方血栓通软胶囊药代动力学研究

目的:建立家兔灌胃给予复方血栓通软胶囊后,房水、血液、眼组织中其化学成分之一人参皂苷Rg1含量的RPHPLC测定法,并测定灌胃给药后不同时间家兔眼内人参皂苷Rg1质量浓度变化,研究其药代动力学特点.方法:取合格一级新西兰家兔,按每只10 mg·kg-1剂量灌胃给予复方血栓通软胶囊,采用RP-HPLC测定给药后不同时间点房水、血液和眼组织中人参皂苷Rg1的药物浓度.结果:建立的RP-HPLC可用于兔房水、血液及眼组织中人参皂苷Rg1的含量测定.房水中人参皂苷Rg1在质量浓度7.6～152 mg·L-1线性关系良好,r=0.999 6；血液中人参皂苷Rg1在质量浓度10.35～103.5 mg·L-1线性关系良好,r=0.999 8.回收率方法符合要求.结论:复方血栓通软胶囊经灌胃给药后,其中的人参皂苷Rg1能够通过血-眼屏障进入眼部,达到一定浓度,此研究结果为复方血栓通软胶囊全身用药治疗眼部疾病提供了理论与临床应用依据.

Pharmacokinetics study of compound Xueshuantong soft capsules

Objective: To establish a RP-HPLC method for determination of the content of ginsenoside Rg₁ in the rabbits aqueous humor, blood and ocular tissues, which were given intragastric administration with the co-xueshuantong soft capsules. The drug concentration in rabbits at different times after oral administration has been determined and the pharmacokinetics characteristics has been researched. Method: The compound xueshuantong soft capsules were administrated to the healthy New Zealand rabbits by gavage(10 mg·kg^-1 per rabbit). The concentration of Ginseng Rg₁ in aqueous humor, blood and ocular tissues at different time was determined by RP-HPLC. Result: RP-HPLC can be established for the determination of ginsenoside Rg₁ in the rabbits aqueous humor, blood, ocular tissue. The calibration of curves was linear within the range of 7.60-152.0 mg·L^-1(r=0.999 6) for ginsenoside Rg₁ in aqueous humor and the calibration of curves were linear within the range of 10.35-103.50 mg·L^-1(r=0.999 8) for ginsenoside Rg₁ in blood. Determination of the recovery rate to meet the requirements. Conclusion: The ginsenosides Rg₁ could transmit the blood-ocular barrier into the eyes and reach a certain concentration. The research provides a theoretical and experimental basis for the systemic administration of compound Xueshuantong to treat eye diseases.