Arnold P, Wermeille M, Chapuy M C, Biollaz J, Grandjean E M, Schelling J L, Meunier P J
Division of Clinical Pharmacology, CHUV Lausanne, Switzerland.
Bone. 1989;10(6):401-7. doi: 10.1016/8756-3282(89)90070-7.
The relative bioavailability of enteric-coated sodium fluoride (NaF) tablets (10 mg F-) has been assessed following administration with a standard calcium-rich breakfast or calcium-poor lunch, and 2 h before or simultaneously with antacid administration (2.4 g aluminum-magnesium hydroxide), versus intake on an empty stomach. Twelve volunteers were studied 3 times according to an open, three-way crossover design over a 24 h period at weekly intervals. Meals were found to decrease the peak serum concentration of NaF from 122 micrograms/L during fasting (after baseline subtraction) to 71 and 88 micrograms/L with breakfast and lunch respectively, and to slow its absorption rate with Tmax increasing from 3.3 to 7.3 and 11.2 hours, without altering its bioavailability. Antacid impaired the bioavailability of NaF by 80% when administered simultaneously, with AUC decreasing from 987 to 155 micrograms.h/L, but had no significant effect when taken 2 h before NaF. In conclusion, the enteric-coated NaF tablets used in this study can be administered with food or after a 2-hour delay following antacid administration, but should not be taken simultaneously with antacid.
在与标准的高钙早餐或低钙午餐同时服用后,以及在服用抗酸剂(2.4克氢氧化铝镁)前2小时或同时服用后,对肠溶氟化钠(NaF)片(10毫克F-)的相对生物利用度进行了评估,并与空腹服用的情况进行了对比。12名志愿者按照开放的三向交叉设计,在24小时内每周进行3次研究。结果发现,进餐会使NaF的血清峰值浓度从空腹时(减去基线后)的122微克/升分别降至早餐和午餐后的71微克/升和88微克/升,并减缓其吸收速度,Tmax从3.3小时增加到7.3小时和11.2小时,但不改变其生物利用度。同时服用抗酸剂时,抗酸剂会使NaF的生物利用度降低80%,AUC从987微克·小时/升降至155微克·小时/升,但在NaF前2小时服用时无显著影响。总之,本研究中使用的肠溶NaF片可以与食物一起服用,或在服用抗酸剂2小时后服用,但不应与抗酸剂同时服用。