Skin pharmacokinetics of inositol nicotinate in heparin sodium inositol nicotinate cream
Objective To establish an HPLC method to determine the concentration of inositol nicotinate(IN)in rat skin,and study the pharmacokinetic characteristics of IN after transdermal administration of heparin sodium inositol nicotinate cream in rats.Methods HPLC method was used to establish a simple and rapid analytical method for the determination of IN concentration in the skin of rats at different time points after administration.The established method was used to study the pharmacokinetics of IN after transdermal administration of heparin sodium inositol nicotinate cream in rats,and the pharmacokinetic parameters were fitted with DAS software.Results The linearity of the analytical method was good in the concentration range of 0.25-20 μg/ml,the quantitative limit was 0.25 μg/ml,and the average recovery rate was 96.18%.The pharmacokinetic parameters of IN after transdermal administration of heparin sodium inositol nicotinate cream in rats were as follows:t1/2 was(4.555±2.054)h,Tmax was(6±0)h,Cmax was(16.929±2.153)mg/L,AUC0-t was(150.665±16.568)mg·h/L,AUC0-∞ was(161.074±23.917)mg·h/L,MRT(0-t)was(9.044±0.618)h,MRT(0-∞)was(10.444±1.91)h,CLz/F was(0.19±0.03)L/(h·kg),and Vz/F was(1.19±0.437)L/(h·kg).Conclusion IN could quickly penetrate the skin and accumulate in the skin for a long time,which was beneficial to the pharmacological action of drugs on the lesion site for a long time.The method is simple,rapid,specific and reproducible,which could be successfully applied to the pharmacokinetic study of IN after transdermal administration in rats.
万方数据
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