Pak C Y, Sakhaee K, Parcel C, Poindexter J, Adams B, Bahar A, Beckley R
Center for Mineral Metabolism and Clinical Research, Southwestern Medical School, University of Texas Southwestern Medical Center, Dallas 75235-8885.
J Bone Miner Res. 1990 Aug;5(8):857-62. doi: 10.1002/jbmr.5650050809.
Clinical pharmacology of slow-release sodium fluoride given with calcium citrate was examined in acute and long-term studies. Following a single oral administration of 50 mg slow-release sodium fluoride, a peak serum fluoride concentration (Cmax) of 184 ng/ml was reached in 2 h; thereafter, serum fluoride concentration declined with a T1/2 of 5.9 h. The concurrent administration of calcium citrate (400 mg calcium) gave an equivalent Tmax (time required to attain Cmax) and T1/2, but a lower Cmax of 135 ng/ml. The coadministration of a meal with fluoride also reduced Cmax but increased Tmax. The area under the serum concentration curve of slow-release sodium fluoride was reduced 17-27% by a meal or calcium citrate. Thus, calcium citrate reduced fluoride absorption and peak fluoride concentration in serum of slow-release sodium fluoride but did not affect the time required to reach peak concentration or the rate of subsequent decline. The effect of a meal was similar, except for a longer period required to reach peak serum concentration. During long-term administration of 25 mg slow-release sodium fluoride coadministered with 400 mg calcium as calcium citrate on a twice daily schedule, the trough level of serum fluoride could be kept between 95 and 190 ng/ml, believed to be the therapeutic window.
在急性和长期研究中对与枸橼酸钙合用的缓释氟化钠的临床药理学进行了研究。单次口服50 mg缓释氟化钠后，2小时内血清氟浓度峰值（Cmax）达到184 ng/ml；此后，血清氟浓度以5.9小时的半衰期下降。同时给予枸橼酸钙（400 mg钙）时，达峰时间（达到Cmax所需时间）和半衰期相当，但Cmax较低，为135 ng/ml。氟化物与食物同服也会降低Cmax，但会延长达峰时间。食物或枸橼酸钙使缓释氟化钠的血清浓度曲线下面积减少17 - 27%。因此，枸橼酸钙减少了缓释氟化钠的氟吸收和血清氟峰值浓度，但不影响达到峰值浓度所需的时间或随后下降的速率。食物的影响类似，只是达到血清峰值浓度所需时间更长。在长期每日两次给予25 mg缓释氟化钠与400 mg钙（以枸橼酸钙形式）合用的过程中，血清氟的谷浓度可维持在95至190 ng/ml之间，这被认为是治疗窗。
