Becker R
Fortschr Med. 1979 Jan 4;97(1):39-42.
The bioavailability of Ossin, a drug for the treatment of osteoporosis, containing 40 mg of NaF, was investigated. Because of the enteric coating of the tablet, intestinal absorption occurs when the tablet leaves the stomach. The sustained release of the F--in the intestine results in a slow F-- -absorption. Maximal F-- -serum concentrations are reached more than 4 hours after absorption has begun. In contrast to non-sustained release NaF tablets the slow absorption of Ossin leads to lower, and less variable F-- -serum concentrations. Following administration of 1 tablet Ossii b.i.d., the steady state concentrations were between 130 and 220 ng/ml. The absorption was at least 86%. As calculated by the renal F-- -elimination, the therapeutically important F-- -retention in bone amounted to more than 50%. The enteric coating of the Ossin tablets, the low and relatively steady F-- -serum concentrations and the high F-- -retention in bone, are expected to contribute to an improvement in tolerance and therapeutic efficacy in the treatment of osteoporosis.
对一种用于治疗骨质疏松症的药物奥辛（Ossin）的生物利用度进行了研究，该药物含40毫克氟化钠（NaF）。由于该片剂有肠溶包衣，当片剂离开胃部时会在肠道发生吸收。肠道中氟离子（F⁻）的持续释放导致F⁻吸收缓慢。吸收开始后4个多小时才能达到血清F⁻的最高浓度。与非缓释NaF片剂相比，奥辛吸收缓慢导致血清F⁻浓度更低且变化更小。每日服用2次，每次1片奥辛后，稳态浓度在130至220纳克/毫升之间。吸收率至少为86%。根据肾脏对F⁻的排泄计算，骨骼中具有治疗意义的F⁻潴留量超过50%。预计奥辛片剂的肠溶包衣、较低且相对稳定的血清F⁻浓度以及骨骼中较高的F⁻潴留量，将有助于提高骨质疏松症治疗中的耐受性和治疗效果。
