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目的:研究通窍散瘀方经不同给药途径给药后葛根素在大鼠体内的药代动力学。方法:通窍散瘀方经注射给药(iv)、鼻腔给药(in)、灌胃给药(ig)后于不同时间点取血,以甲醇沉淀血浆蛋白质,反相高效液相色谱测定葛根素在大鼠血浆中的浓度,用Kinetica程序软件计算药代动力学参数和生物利用度。结果:通窍散瘀方静脉注射后,葛根素血中AUC0～120 min为(787.99±70.44)mg.min.L-1,鼻腔给药后AUC0～120 min为(376.56±93.93)mg.min.L-1,而灌胃给药后AUC0～120 min为(491.18±110.64)mg.min.L-1。鼻腔给药葛根素绝对生物利用度F为47.78%,灌胃给药葛根素绝对生物利用度F为6.23%。结论:通窍散瘀方经鼻腔给药的生物利用度显著高于灌胃,该结果可以为通窍散瘀方的剂型研究和给药途径选择提供实验依据。
OBJECTIVE: To study the pharmacokinetics of puerarin in rats after administration of Tongqiao Sanyu prescription by different routes of administration. Methods: Tongqiao Sanyu recipe was injected intraperitoneally (iv), intranasally (ig), intragastrically (ig) and then blood was taken at different time points. Plasma protein was precipitated with methanol and determined by reverse phase high performance liquid chromatography Plasma concentrations in rat plasma, pharmacokinetic parameters and bioavailability were calculated using the Kinetica program software. Results: After intravenous injection of Tongqiao Sanyu Recipe, the AUC0 ~ 120 min of puerarin was (787.99 ± 70.44) mg.min.L-1, and the AUC of 0 ~ 120 min after nasal administration was (376.56 ± 93.93) mg.min. L-1, while the intragastric administration of AUC 0 ~ 120 min was (491.18 ± 110.64) mg.min.L-1. Nasal administration of puerarin absolute bioavailability F was 47.78%, intragastric administration of puerarin absolute bioavailability F was 6.23%. Conclusion: The bioavailability of Tongqiao Sanyu Decoction administered intranasally is significantly higher than that given by intragastric administration. This result can provide experimental evidence for the formulation and administration of Tongqiao Sanyu recipe.