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目的考察健康受试者单次和连续肌肉注射精氨酸酮洛芬后的药代动力学特点,并观察安全性。方法采用3剂量组,开放、随机、平行的单中心设计,30名健康受试者分别接受单次肌肉注射50、100、200 mg的注射用精氨酸酮洛芬,10名健康受试者连续4 d,每天3次接受50 mg的注射用精氨酸酮洛芬后,用HPLC法测定血药浓度。结果单次肌肉注射注射用精氨酸酮洛芬50、100、200 mg后的主要药代动力学参数为AUC0-24分别为(11.796±1.713)mg·h·L-1、(21.507±4.805)mg·h·L-1和(51.802±13.537)mg·h·L-1,t1/2分别为(1.996±0.299)h、(3.630±1.117)h和(3.147±0.919)h,tmax分别为(0.525±0.171)h、(0.533±0.125)h和(0.750±0.167)h,ρmax分别为(6.151±1.378)mg·L-1、(9.961±2.549)mg·L-1和(20.284±4.865)mg·L-1。连续注射注射用精氨酸酮洛芬50 mg后的主要药代动力学参数为AUCss为(9.572±1.958)mg·h·L-1;AUC0-24为(9.984±2.067)mg·h·L-1,t1/2为(2.597±0.924)h,tmax为(0.417±0.088)h,ρmax为(4.994±1.252)mg·L-1,蓄积因子R为(1.143±0.132)。结论单次注射50、100、200 mg注射用精氨酸酮洛芬后,酮洛芬在体内符合线性动力学特征。多次注射50 mg注射用精氨酸酮洛芬后,酮洛芬在人体内几乎无蓄积。
Objective To investigate the pharmacokinetic characteristics of single and continuous intramuscular injection of ketoprofen in healthy subjects and to observe the safety. Methods A three-dose, open, randomized, parallel, single-center design was used. 30 healthy subjects received a single intramuscular injection of 50, 100, and 200 mg of ketamine arginine for ketamine, 10 healthy subjects After 4 consecutive days, 50 mg of ketamine arginine for injection were taken 3 times a day, and the plasma concentration was determined by HPLC. Results The main pharmacokinetic parameters of 50, 100 and 200 mg arginine ketoprofen injection after intramuscular injection were AUC0-24 (11.796 ± 1.713) mg · h · L-1, (21.507 ± 4.805 (1.996 ± 0.299) h, (3.630 ± 1.117) h and (3.147 ± 0.919) h, respectively, and tmax respectively were (5180 ± 13.537) mg · h · L-1 and Were (0.525 ± 0.171) h, (0.533 ± 0.125) h and (0.750 ± 0.167) h, respectively. The values of ρmax were (6.151 ± 1.378) mg · L -1 and (9.961 ± 2.549) mg · L -1 and (20.284 ± 4.865) mg · L-1. The main pharmacokinetic parameters of continuous injection of ketoprofen arginine 50 mg were AUCss (9.572 ± 1.958) mg · h · L-1 and AUC0-24 (9.984 ± 2.067) mg · h · L (2.597 ± 0.924) h, tmax was (0.417 ± 0.088) h, ρmax was (4.994 ± 1.252) mg · L-1, and accumulation factor R was (1.143 ± 0.132). Conclusions After a single injection of 50, 100, 200 mg of arginine ketoprofen for injection, ketoprofen in the body meets the linear kinetic characteristics. After multiple injections of 50 mg ketamine arginine for injection, ketoprofen has almost no accumulation in the human body.