Brazier M, Fardelonne P, Bellony R, Sebert J L, Desmet G
Laboratoire de Pharmacie Galenique et Biopharmacie U.E.R. de Pharmacie, Amiens, France.
Eur J Drug Metab Pharmacokinet. 1991;Spec No 3:161-5.
Fluoride pharmacokinetics were studied in twelve healthy subjects after oral administration of one tablet of osteofluor-containing 25 mg of sodium fluoride alone or associated with different calcium salts (500 mg Ca element) given as microcrystalline hydroxyapatite compound or powdered tri-calcium phosphate. Fluoride was measured in plasma and urine with a specific electrode and fluoride bioavailability from the three drugs was compared. Calcium absorption after oral load was assessed by measuring variations from the fasting state of plasma calcium and parathyroid hormone and of the urinary calcium to creatinine ratio. The bioavailability of fluoride is significantly decreased by the association to sodium fluoride of hydroxyapatite but not of tri-calcium phosphate. Calcium absorption seems greater after administration of hydroxyapatite compound. The decrease of the fluoride bioavailability is probably dependent on the capacity of calcium absorption from the calcium salts. The association of calcium to fluoride is absolutely required for treatment of osteoporosis. The microcrystalline hydroxyapatite compound seems preferable in view of its greater calcium absorption and of its limited decrease in fluoride bioavailability.
在12名健康受试者口服一片含25毫克氟化钠的骨氟片后,单独或与不同钙盐(500毫克钙元素)联合给药,钙盐以微晶羟基磷灰石化合物或磷酸三钙粉末形式提供,研究了氟化物的药代动力学。用特定电极测量血浆和尿液中的氟化物,并比较三种药物的氟化物生物利用度。通过测量空腹状态下血浆钙、甲状旁腺激素以及尿钙与肌酐比值的变化,评估口服负荷后钙的吸收情况。与羟基磷灰石联合使用时,氟化物的生物利用度显著降低,但与磷酸三钙联合使用时则不然。服用羟基磷灰石化合物后,钙的吸收似乎更大。氟化物生物利用度的降低可能取决于钙盐中钙的吸收能力。钙与氟化物联合使用是治疗骨质疏松症的绝对必要条件。鉴于其更大的钙吸收能力和有限的氟化物生物利用度降低,微晶羟基磷灰石化合物似乎更可取。