牛皮下注射卡洛芬注射液的药动学试验研究

Pharmacokinetic Study of Carprofen Injection Given by Subedermal Injection

为研究卡洛芬注射液在牛体内的药动学特征,将8头健康牛随机分为两组,每组4头,给药剂量为1.4 mg/kg BW,给药后按设计的采血点采集血样,采用超高液相色谱-串联质谱法(UPLC-MS/MS)测定血浆中卡洛芬的药物浓度,用WinNonlin8.1软件计算药动学参数。结果显示:牛单次皮下注射受试制剂卡洛芬注射液在牛体内主要药动学参数如下:平均最高血药浓度(Cmax)为(17473.30±2398.73)ng·mL^(-1),平均药时曲线下面积(AUClast)为(1052647.93±143055.37)h·ng·mL^(-1),平均达峰时间(Tmax)为8.00±2.62 h,平均消除半衰期(T_(1/2))为55.69±3.25 h;牛单次皮下注射参比制剂卡洛芬注射液的主要药动学参数如下:平均最高血药浓度(Cmax)为(15695.98±4865.73)ng·mL^(-1),平均药时曲线下面积(AUClast)为(1002858.15±297235.31)h·ng·mL^(-1),平均达峰时间(Tmax)为8.50±2.98 h,平均消除半衰期(T_(1/2))为(55.03±2.64)h。结果表明,牛皮下注射受试制剂卡洛芬注射液,吸收迅速,消除较慢,生物利用度是参比制剂的104.96%。

In order to study the pharmacokinetic characteristics of carprofen injection in cattle,eight healthy cattle were randomly divided into two groups,4 in each group with a dose of 1.4 mg/kg BW.Blood samples of carprofen were determined by ultra-high liquid chromatography-tandem mass spectrometry(UPLC-MS/MS),and the pharmacokinetic parameters were calculated by WinNonlin8.1 software.The results showed that the main pharmacokinetic parameters of carprofen injection in cattle were as follows:the highest mean plasma concentration(Cmax)was(17473.30±2398.73)ng·mL^(-1),the mean area under the curve(AUClast)is(1052647.93±143055.37)h·ng·mL^(-1),The mean peak reaching time(Tmax)was 8.00±2.62 h,The mean elimination half-life(t_(1/2))was 55.69±3.25 h;The main pharmacokinetic parameters of the reference formulation,are as follows:the highest mean plasma concentration(Cmax)was(15695.98±4865.73)ng·mL^(-1),The mean area under the drug curve(AUClast)is(1002858.15±297235.31)h·ng·mL^(-1),The mean time to peak reach(Tmax)is 8.50±2.98 h,The mean elimination half-life(T_(1/2))was(55.03±2.64)h.The results showed that carprofen injection was absorbed rapidly and eliminated more rapidly,and the bioavailability was 104.96%of the reference preparation.