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目的 通过健康受试者的双交叉试验比较萘普生缓释胶囊与普通片的药物动力学和生物利用度。方法１０位健康受试者一次服用这两种制剂５００ｍｇ，在稳态试验中８位受试者接受两种制剂５天，缓释胶囊５００ｍｇ每天一次，普通片每天两次，每次２５０ｍｇ。血药浓度用ＨＰＬＣ方法测定。结果 一次服药试验证明该缓释胶囊血药浓度上升缓慢，浓度变化平稳，Ｇｍａｘ为８５．９μｇ／ｍｌ，Ｔｐｅａｋ为６．０ｈ，而普通片的Ｃｍａｘ为１４０．４μｇ／ｍｌ，Ｔｐｅａｋ为３．２ｈ，两种制剂的生物利用度相当，缓释胶囊与普通片生物等效。通过８位健康受试者交叉连续服用萘普生缓释胶囊与普通片的稳态药代动力学研究表明，到第３天给药后已达到稳态，由第５天给药后的血药浓度测定数据计算其主要的稳态药代动力学参数，缓释胶囊的峰浓度（Ｃｍａｘ）、峰谷比和波动度（ＤＦ）明显低于普通片，这些参数分别为７３，１μｇ／ｍｌ、１．４８和３７．７ｏ；而普通片的上述参数分别为 １００．８μｇ／ｍｌ、２．５１和７８．２％。结论 奈普生缓释胶囊具有缓释作用，能较好维持血药治疗浓度。
OBJECTIVE To compare the pharmacokinetics and bioavailability of naproxen sustained-release capsules with conventional tablets in healthy subjects through a double-crossover trial. Methods Ten healthy subjects took both formulations 500 mg at a time and in a steady state test eight subjects received two formulations for 5 days, sustained release capsules 500 mg once daily, and common tablets 250 mg twice daily. Plasma concentration was determined by HPLC method. The results of a medication test showed that the sustained-release capsules blood concentration rose slowly, the concentration changes smoothly, Gmax 85.9μg / ml, Tpeak 6.0h, while the common tablets Cmax 140.4μg / ml, Tpeak 3.2h , Two formulations of bioavailability quite, sustained-release capsules and bio-equivalent bio-tablets. Steady-state pharmacokinetic studies of croscarmellose naproxen sustained-release capsules and conventional tablets across 8 consecutive healthy subjects demonstrated that steady state has been reached after dosing on day 3 and that blood from day 5 after dosing The main steady-state pharmacokinetic parameters were calculated by drug concentration determination data. The peak concentration (Cmax), peak-to-valley ratio and volatility (DF) of sustained-release capsules were significantly lower than those of ordinary tablets. The parameters were 73,1μg / ml , 1.48 and 37.7o, respectively; while the above parameters of common tablets were 100.8μg / ml, 2.51 and 78.2% respectively. Conclusion Naproxen sustained release capsules with sustained release, can better maintain blood drug concentration.