Marzo A, Ripamonti M, Benatti P, Marzo P, Wool C, Cerutti R, Reiner V
Real s.r.l., Laboratory of Pharmacokinetics and Drug Metabolism, Como, Italy.
Arzneimittelforschung. 1997 Apr;47(4):381-4.
The S-naproxen betainate sodium salt monohydrate (naproxen-betaNa, CAS 104124-26-7, Aprenin) was synthesized to improve bioavailability and tolerability of naproxen. 24 albino rats were treated with naproxen-betaNa (84 mg/kg) and 24 with S-naproxen (naproxen) (50 mg/kg) by the oral route, the doses being equimolar. The animals were sacrificed and naproxen was assayed in timed plasma samples drawn off over a 24-h period and in tissues excised 1 h after administration. Peak concentrations of naproxen proved to be higher with naproxen-betaNa than with naproxen as such. The area under the curve of naproxen concentrations observed with the two administrations overlapped as did concentrations of the drug in the lungs, myocardium and liver. Naproxen concentrations in the gastric wall after naproxen-betaNa proved to be lower than after administration of naproxen as such, which allowed the authors to assume that naproxen-betaNa has a better gastric tolerability.
合成了S - 萘普生甜菜碱钠盐一水合物（萘普生 - βNa，CAS 104124 - 26 - 7，Aprenin）以提高萘普生的生物利用度和耐受性。通过口服途径，给24只白化大鼠服用萘普生 - βNa（84毫克/千克），给另外24只大鼠服用S - 萘普生（萘普生）（50毫克/千克），剂量为等摩尔。处死动物后，在24小时内定时采集的血浆样本以及给药1小时后切除的组织中测定萘普生。结果表明，萘普生 - βNa的萘普生峰值浓度高于萘普生本身。两种给药方式下观察到的萘普生浓度曲线下面积以及药物在肺、心肌和肝脏中的浓度相互重叠。萘普生 - βNa给药后胃壁中的萘普生浓度低于萘普生本身给药后，这使作者认为萘普生 - βNa具有更好的胃耐受性。
