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目的研究磷酸川芎嗪的鼻黏膜吸收特性及体内药动学。方法采用大鼠在体鼻腔重循环法研究磷酸川芎嗪的体外吸收规律,计算吸收速率常数;采用固相萃取-高效液相色谱法测定大鼠血浆中药物浓度,计算药动学参数和生物利用度。结果一定范围内不同浓度药物的鼻黏膜吸收速率常数k无显著性差异;磷酸川芎嗪在大鼠体内的过程属于二室模型,溶液鼻腔给药的生物利用度为86.33%,凝胶剂鼻腔给药的生物利用度为77.25%。结论药物吸收呈一级动力学特征;磷酸川芎嗪鼻腔给药吸收迅速,生物利用度高。
Objective To study the nasal mucosal absorption and pharmacokinetics of ligustrazine phosphate. Methods Rat nasal cavity reperfusion method was used to study the in vitro absorption of ligustrazine phosphate and the absorption rate constants were calculated. The concentration of drug in rat plasma was determined by solid-phase extraction and high performance liquid chromatography, and the pharmacokinetic parameters and bioavailability were calculated degree. Results There was no significant difference in nasal mucosa absorption rate constant k between different concentrations of drugs within a certain range. Ligustrazine phosphate in rats was a two-compartment model with a bioavailability of 86.33% The bioavailability of the drug was 77.25%. Conclusion The drug absorption is characterized by first order kinetics. Ligustrazine phosphate nasal administration absorbs quickly and has high bioavailability.