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目的:测定芎冰喷雾剂经鼻腔给药后主要成分磷酸川芎嗪(TMPP)在大鼠脑内的药代动力学参数。方法:大鼠鼻腔或静脉注射给予芎冰喷雾剂后,利用微透析技术进行脑内药动学研究,高效液相色谱法测定透析液样品中TMPP的浓度,用Das2.0药动学软件计算主要药动学参数。结果:鼻腔给药和静注给药后TMPP在脑内的吸收均符合一室模型,芎冰喷雾剂鼻腔给药与静注给药TMPP都迅速进入脑内达到峰浓度,鼻腔给药TMPP在脑内的停留时间更长。结论:微透析法能较好的反映芎冰喷雾剂鼻腔给药后TMPP的药动学特征,鼻腔给药是治疗缺血性脑血管机能不全急性期的一种速效途径。
OBJECTIVE: To determine the pharmacokinetic parameters of ligustrazine phosphate (TMPP) in rat brain after intranasal administration of ligusticum chuanxiong. Methods: Rats were injected nasal or intravenous injection of Xiong Bing aerosol. The rats were anesthetized by microdialysis technique and the concentrations of TMPP in dialysate samples were determined by high performance liquid chromatography. The concentration of TMPP was calculated by Das2.0 pharmacokinetic software The main pharmacokinetic parameters. Results: Nasal administration and intravenous administration of TMPP in the brain are consistent with a one-compartment model of absorption, the Xiongbing spray nasal and intravenous administration of TMPP rapidly into the brain to reach peak concentration, nasal administration of TMPP in Stay longer in the brain. Conclusion: The microdialysis method can better reflect the pharmacokinetic characteristics of TMPP after nasal administration of Xiongbing spray. Nasal administration is a quick way to treat acute ischemic cerebrovascular insufficiency.