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目的:通过比较通窍散瘀(TQSY)方经不同途径给药后血药及脑药动力学,评价通窍散瘀方治疗脑中风的最佳给药途径。方法:通窍散瘀方经不同途径给予小鼠后于不同时间点取血和全脑,以甲醇沉淀血浆蛋白质,反相高效液相色谱测定葛根素在小鼠血浆和脑组织中的浓度,用Kinetica程序软件计算药代动力学参数和生物利用度,并计算脑靶向系数(Re)和药物脑靶向指数(DTI)。结果:鼻腔给药后脑药Re为132.25%,DTI为2.70,要显著高于注射组。灌胃组DTI为0.50。结论:TQSY方鼻腔给药后脑靶向性要高于注射组和灌胃给药组,显示出了鼻腔给药“引药入脑”的优势。
OBJECTIVE: To evaluate the optimal route of administration of Tongqiao Sanyufang for the treatment of stroke by comparing the blood and brain pharmacokinetics of TQSY after administration by different routes. Methods: Tongqiao Sanyu Recipe was administered to mice by different routes and then blood and whole brain were taken at different time points. Plasma protein was precipitated by methanol and the concentration of puerarin in plasma and brain of mice was determined by RP-HPLC. Kinetica program software calculates pharmacokinetic parameters and bioavailability and calculates brain targeting (Re) and drug brain targeting indices (DTI). Results: After intranasal administration, brain Re was 132.25% and DTI was 2.70, which was significantly higher than that of the injection group. The intragastric group had a DTI of 0.50. CONCLUSION: The brain targeting of TQSY prescriptions after nasal administration is higher than that of injection group and gavage administration group, which shows the advantage of nasal administration “introduction into brain ”.