Ling T L, Yee J P, Cohen A, Hsiao C, Gonzalez M A, Garg D C, Weidler D J
Syntex Research, Department of Drug Metabolism, Palo Alto, CA 94304.
J Clin Pharmacol. 1987 Apr;27(4):325-9. doi: 10.1002/j.1552-4604.1987.tb03024.x.
The bioequivalence and absorption kinetics of naproxen in a new controlled-release tablet (750 mg or 1,000 mg naproxen) administered once daily were determined relative to an equivalent dose of the conventional naproxen tablet (375 mg or 500 mg naproxen) administered q12h. Naproxen was well absorbed from the controlled-release tablet (about 90%) compared with the conventional tablet. Absorption was dependent on drug release from the tablet matrix. The mean absorption time of naproxen averaged 8.4 hours for the 750-mg controlled-release tablet and 9.2 hours for the 1,000-mg controlled-release tablet. Once-daily administration of the controlled-release tablet resulted in equivalent trough concentrations of naproxen, and steady-state plasma concentrations were maintained within narrower limits than with twice-daily naproxen.
测定了一种新型缓释片(含萘普生750毫克或1000毫克)每日服用一次时萘普生的生物等效性和吸收动力学,并与等量的常规萘普生片(含萘普生375毫克或500毫克)每12小时服用一次进行比较。与常规片剂相比,萘普生从缓释片中的吸收良好(约90%)。吸收取决于药物从片剂基质中的释放。750毫克缓释片的萘普生平均吸收时间为8.4小时,1000毫克缓释片为9.2小时。每日一次服用缓释片可使萘普生的谷浓度相当,且稳态血浆浓度维持在比每日两次服用萘普生更窄的范围内。