氟化钠缓释片人体药动学与体内外相关性研究

Pharmacokinetics of sodium fluoride sustained-release tablet and the correlation between the absorption in vivo and the releasing rate in vitro

目的 :研究氟化钠缓释片在人体内药动学和体内外的相关性。方法 :采用氟离子选择电极 ,测定10名自愿者单剂量口服25mg氟化钠缓释片后的血清氟离子浓度 ,计算药动学参数 ;按照Wagner-Nelson法计算的药物吸收分数与体外释放度进行相关性研究。结果 :体内过程符合一室开放模型 ,AUC0→r为1216 03ng·h -1·ml -1,Ka为0 72h ,Tlag 为0 55h ,Ke为0 19h ,t12,Ke为3.75h ;药物体外释放与体内吸收具良好相关性。结论 :该研究可为氟化钠缓释片的内在质量评价和制剂开发提供一定科学依据。

Objective:To study the pharmacokinetics and the correlation between the absorption in vivo and the releasing rate in vitro of sodium fluoride between the absorption in vivo and the releasing rate in vitro of sodium fluoride sustained-release table(SFSRT).Methods:The F concentrations in serum were determined by fluoride ion selective elevtrode method following a single oral dose of SFSRT given to 10 volunteers.The correlation between the absorption in vivo and the releasing rate in vitro was studied with Wangner-Nelson method.Results:The concentration-time curve of SFSRT was conformed to an one compartment open model with a first order absorption.The AUC0→r,Ka,Tlag,Ke and T1/2,ke were 1216.03 ng.h.ml-1,0.72h,0.55h,0.19h-1 and 3.75h,respectively.The absorption in vivo and the releasing rate in vitro of SFSRT were of good correlation.Conclusion:This study will provide a scientific basis for the quality evaluation and dosage forms reformation of SFSRT.