摘要
目的：酮洛芬缓释片与常释片单次给药的生物利用度和多次给药的峰谷浓度波动大小。方法：采用以萘普生（ｎａｐｒｏｘｅｎ）为内标的ＨＰＬＣ测定方法，测定健康男性受试者按交叉试验单剂量和多剂量服用酮洛芬缓释片和常释片后的血中酮洛芬浓度。结果：单剂量服用酮洛芬缓释片和常释片后，常释片的Ｃｍａｘ显著高于缓释片（Ｐ＜００１），缓释片给药后的Ｔｍａｘ延迟，ｔ１／２ｋｅ显著延长，相对生物利用度为９７１３％。缓释片在稳态时的Ｃｍｉｎ为０４０１μｇ·ｍＬ－１，而常释片为０１９０μｇ·ｍＬ－１（Ｐ＜００１）。在稳态时缓释片的峰谷浓度波动度（ＤＦ）、峰谷比（ＰＴＲ）都显著小于常释片，说明缓释片的峰谷浓度波动程度优于常释片。结论：经统计学检验表明这两种制剂具有生物等效性，该缓释片具有峰谷浓度差异小，波动幅度小的特点，显示出缓释特征。
AIM: To compare the pharmacokinetics and bioavailability of ketoprofen sustained release tablets (ST) with those of regular tablets (Reference tablet, RT) in 10 healthy volunteers after single and repeated oral administrations in randomized crossover design. METHODS: A sensitive and rapid HPLC method was used to determine the serum ketoprofen concentration. RESULTS: The results from single oral dose in 8 healthy volunteers indicated that the C max of RT was significantly higher than that of ST. The T max and t 1/2ke of ST were significantly longer than those of RT ( P <0 01). The relative bioavailability of ST was found to be 97 13%. As there was no difference in the AUC between the two preparations, it can be concluded that the new sustained release tablet was bioequivalent to RT. The C min of ST and RT at steady state were 0 401 μg·mL -1 and 0 190 μg·mL -1 , respectively, with a significant difference ( P <0 01) between them. The ketoprofen concentration peak trough ratio (PTR) and the degree of fluctuation (DF) of ST were significantly smaller than those of RT. CONCLUSION: The new sustained release tablet showed less fluctuation of peak and trough serum drug concentrations than those of the regular tablet at steady state and exhibited good sustained release property.
出处
《药学学报》
CAS
CSCD
北大核心
1999年第7期547-551,共5页
Acta Pharmaceutica Sinica
