两种萘普生片在健康人体的药代动力学和相对生物利用度比较

Comparison of pharmacokinetics and relative bioavailability of two types of naproxen in healthy volunteers

目的：测定萘普生片人体相对生物利用度。方法：２０名健康男性志愿者随机自身交叉单剂量口服广州贝氏药业有限公司研制的萘普生片或珠海联邦制药厂有限公司中山分厂生产的萘普生片后，用高效液相色谱法测定血清中萘普生浓度并计算两者的药代动力学参数及相对生物利用度。结果：两种萘普生片的体内药时数据符合药动学二室模型，贝氏和联邦萘普生片消除速率常数 ｔ１／２β 分别为（１７．１０±９．３９）ｈ和（１６．９７±６．７３）ｈ； Ｃｍａｘ分别为 （１３４．４９±２２．１２） μｇ／ｍｌ和（１２９．０８±２６．７４） μｇ／ｍｌ； ｔｐ 分别为 （２．１０±０．６４）ｈ和（１．８８±０．７０）ｈ； ＡＵＣ（０～７２ｈ）分别为（１８１０．５７±４００．６０） ｍｇ·ｈ／Ｌ和（１７６２．５３±３４７．９４）ｍｇ·ｈ／Ｌ。经统计学分析表明，两者无显著性差异（Ｐ ＞０．０５）。结论：贝氏萘普生片对联邦萘普生片的相对生物利用度为 （１０２．７２±１３．７６）％，两种萘普生片具有生物等效性。

Objective: To study pharmacokinetics and relative bioavailability of naproxen tablets in healthy volunteers.Methods: A single oral 500mg dose of Bei Shi naproxen(NAPB) tablets and Lian Bang naproxen(NAPL) tablets were given to 20 healthy volunteers in an open randomized crossover study. Naproxen concentration in serum was determined by HPLC. The pharmacokinetic parameters as well as relative bioavailability were measured.Results:The concentration-time curves of NAPB tablets and NAPL tablets were conformed to a two compartment open model.The t1/2β were (17.10±9.39)h and (16.97±6.73)h, Cmax (134.49±22.12) μg/ml and (129.08±26.74) μg/ml, Tmax(2.10±0.64)h and (1.88±0.70)h , AUC(0～72) (1810.57±400.60) μ g·h/ml and (1762.53±347.94)μ g·h/ml, respectively. There was no significant difference between the two formulations in the AUC(0～72), Cmax, Tmax. Conclusion: The relative bioavailability of NAPB tablets was (102.72±13.76)% compared with NAPL tablets.The result of the statistical analysis showed that the two formations were bioequivalent.