Warneke G, Setnikar I
Zentrum Innere Medizin, Medizinische Klinik und Poliklinik, Georg August Universität, Göttingen, Fed. Rep. of Germany.
Arzneimittelforschung. 1993 May;43(5):584-90.
A two-way cross-over study was conducted on 12 Caucasian male healthy volunteers aged between 25 and 38 years in order to determine the bioavailability and pharmacokinetics of fluoride after single oral administration in fasting conditions of two products (tablets and powder for oral use) of L-glutamine monofluorophosphate (G-MFP, CAS 116420-36-1). The two products contained the equivalent of 10 mg F and the equivalent of 300 mg CA as calcium gluconate and calcium citrate. The two products were found bioequivalent with regard to the release of fluoride, both on the basis of the AUC and Cmax of fluoride in plasma and of the urinary excretion of fluoride during the 48 h following the administration. The pharmacokinetics of fluoride in plasma is characterized by a short lag time (< 6 min), a rapid absorption, a peak which is reached 0.5-1.0 h after administration, followed by a biphasic elimination. The first phase with a k alpha of 1.8 h-1 is followed by a slower phase with a K beta of 0.14 h-1. Probably the terminal elimination rate is slower, about 0.05 h-1. The urinary excretion of fluoride during the 48 h after administration accounted for 40-50% of the administered dose of fluoride. The results are consistent with those found in previous studies after administration in fasting conditions of sodium fluoride or sodium monofluorophosphate alone or in combination with calcium salts.
对12名年龄在25至38岁之间的白种男性健康志愿者进行了一项双向交叉研究，以确定在空腹条件下单次口服两种L - 谷氨酰胺单氟磷酸酯产品（片剂和口服粉剂）（G - MFP，CAS 116420 - 36 - 1）后氟化物的生物利用度和药代动力学。这两种产品含有相当于10 mg氟和相当于300 mg钙（以葡萄糖酸钙和柠檬酸钙形式存在）。基于血浆中氟化物的AUC和Cmax以及给药后48小时内氟化物的尿排泄量，发现这两种产品在氟化物释放方面具有生物等效性。血浆中氟化物的药代动力学特征为滞后时间短（<6分钟）、吸收迅速、给药后0.5 - 1.0小时达到峰值，随后是双相消除。第一相的kα为1.8 h-1，随后是较慢的相，Kβ为0.14 h-1。可能终末消除速率较慢，约为0.05 h-1。给药后48小时内氟化物的尿排泄量占所给氟化物剂量的40 - 50%。这些结果与之前在空腹条件下单独给予氟化钠或单氟磷酸钠或与钙盐联合给药后的研究结果一致。
