磷酸川芎嗪脂质微球在大鼠鼻黏膜吸收的特性

目的研究磷酸川芎嗪（tetramethylpyrazine phosphate,TMPP）脂质微球在大鼠鼻黏膜吸收的特性。方法采用大鼠鼻腔循环灌流法,考察循环液流速、TMPP溶液浓度、TMPP脂质微球浓度对鼻黏膜吸收的影响,并对TMPP脂质微球和TMPP溶液的鼻吸收水平进行比较。结果在流速为2.0ml/min时,TMPP脂质微球鼻黏膜吸收速率常数有最大值;在浓度为0.25～1.0mg/ml范围内,TMPP溶剂的鼻黏膜吸收速率常数随浓度变化趋势不明显;而TMPP脂质微球的鼻黏膜吸收速率常数随浓度的增大而减小,与同浓度TMPP溶液比较,TMPP脂质微球吸收更快,鼻黏膜随时间延长吸收量更高。结论将TMPP制备成脂质微球能促进药物在鼻黏膜的吸收。

Absorption Characteristics of Tetramethylpyrazine Phosphate Lipid Microspheres in Rat Nasal Mucosa

Objective To study the absorption characteristics of tetramethylpyrazine phosphate(TMPP) lipid microspheres in rat nasal mucosa.Methods Nasal circulatory perfusion method in rats was used to study the effects of circulatory rate,concentrations of TMPP solution and TMPP lipid microspheres on nasal mucosa absorption.Nasal mucosa absorption rate constants of TMPP lipid microspheres and TMPP solutions at the same concentration were also compared.Results When the circulatory rate was 2.0ml/min,the absorption rate constant of TMPP lipid microspheres had a maximum value.The changes of absorption rate constant of TMPP solutions were not obvious when TMPP concentration ranged from 0.25to 1.0 mg/ml;and the absorption rate constants of TMPP lipid microspheres were decreasing with the increasing of TMPP concentrations.The absorbing amount of TMPP for TMPP lipid microspheres was higher than that for TMPP solutions at the same concentration.Conclusion The prepared TMPP lipid microspheres can promote the absorption of TMPP in nasal mucosa.