Brazier M, Fardelonne P, Bellony R, Sebert J L, Desmet G, Hary L, Richard M O
Laboratoire de Chimie des Explorations Fonctionnelles et Endocriniennes, CHU Amiens.
Therapie. 1990 May-Jun;45(3):235-41.
We studied, in twelve healthy volunteers, the pharmacokinetics of inorganic fluoride and calcium variations in serum and urine, parathormone variations in serum after administration of two oral preparations containing 100 mg of disodium monofluorophosphate (13.2 mg F as element) with different calcium salts (500 mg Ca as element). Fluoride was estimated in serum and urine with an ion specific electrode. The fluoride bioavailability from two preparations is identical with an areas under the curve corresponding to 61.05 and 62.53 mumols.l-1 h (after deduction of physiological fluoride concentrations) and urinary fluoride excretion after 72 hours corresponding to 266.6 and 246.1 mumols. The plasma peak appearance is rapid (one hour) and similar. The significant increase of urinary Ca-Creat ratio (70 to 100%) is identical four hours after drug administration. In the same way, a significant and early decrease of intact PTH in serum, measured with chemiluminometric method, was observed from two drugs. From these observations we may conclude that the two preparations are biologically equivalent.
我们对12名健康志愿者进行了研究，观察了服用两种分别含有100毫克单氟磷酸二钠（以元素计含13.2毫克氟）并搭配不同钙盐（以元素计含500毫克钙）的口服制剂后，血清和尿液中无机氟的药代动力学、血清和尿液中钙的变化以及血清中甲状旁腺激素的变化。采用离子特异性电极测定血清和尿液中的氟。两种制剂的氟生物利用度相同，曲线下面积分别对应61.05和62.53微摩尔·升⁻¹·小时（扣除生理氟浓度后），72小时后的尿氟排泄量分别对应266.6和246.1微摩尔。血浆峰值出现迅速（1小时）且相似。给药4小时后，尿钙 - 肌酐比值显著增加（70%至100%）且相同。同样，采用化学发光法测定，两种药物均可使血清中完整甲状旁腺激素显著且早期降低。从这些观察结果我们可以得出结论，这两种制剂在生物学上是等效的。
