Lefebvre H P, Toutain P L, Serthelon J P, Lassourd V, Gardey L, Braun J P
Département de Physiopathologie, Ecole National Vétérinaire, Toulouse, France.
Am J Vet Res. 1994 Apr;55(4):487-93.
Pharmacokinetic variables of skeletal muscle creatine kinase (CK) activity after IV administration of a muscle extract; CK bioavailability after IM administration of the muscle extract; and effect of IM administration of saline solution, to appreciate the possible release of CK consecutive to muscle puncture, were determined in 6 cows. A general equation for the quantitative estimation of skeletal muscle damage also was derived. Administration of saline solution IM had no effect on plasma CK activity (ANOVA, P > 0.05) in any of the cows. After IV administration of the muscle extract (150 U/kg of body weight), mean volume of the central compartment, plasma half-life, and plasma clearance of CK were 0.027 +/- 0.007 L/kg, 520 +/- 109 minutes, and 6.43 +/- 2.29 ml/kg/h, respectively. After IM administration (150 U/kg), mean bioavailability of CK was 51 +/- 17% and maximal plasma CK activity (500 +/- 97 U/L) was observed at 454 +/- 131 minutes. The rate of CK activity entry into plasma was determined by use of deconvolution analysis. Two peaks were observed; the first appeared before the 30th minute after IM administration, and the second appeared at 3.3 +/- 1.1 hours. Amplitudes were 6.31 +/- 4.45 and 6.57 +/- 3.08 U/kg/h, for the first and the second peaks, respectively. The quantity of CK liberated from control muscle was 0.69 +/- 0.12 U/kg/h, corresponding to a normal daily catabolism of 5.8 +/- 1.0 mg of muscle/kg.(ABSTRACT TRUNCATED AT 250 WORDS)
对6头奶牛静脉注射肌肉提取物后骨骼肌肌酸激酶（CK）活性的药代动力学变量；肌肉注射该肌肉提取物后CK的生物利用度；以及肌肉注射生理盐水的效果（以评估肌肉穿刺后CK可能的释放情况）进行了测定。还推导了骨骼肌损伤定量评估的通用方程。肌肉注射生理盐水对任何一头奶牛的血浆CK活性均无影响（方差分析，P>0.05）。静脉注射肌肉提取物（150 U/kg体重）后，CK的中央室平均容积、血浆半衰期和血浆清除率分别为0.027±0.007 L/kg、520±109分钟和6.43±2.29 ml/kg/h。肌肉注射（150 U/kg）后，CK的平均生物利用度为51±17%，在454±131分钟时观察到最大血浆CK活性（500±97 U/L）。通过反卷积分析确定了CK活性进入血浆的速率。观察到两个峰值；第一个峰值出现在肌肉注射后第30分钟之前，第二个峰值出现在3.3±1.1小时。第一个和第二个峰值的幅度分别为6.31±4.45和6.57±3.08 U/kg/h。对照肌肉释放的CK量为0.69±0.12 U/kg/h，相当于正常情况下每千克肌肉每天5.8±1.0 mg的分解代谢量。（摘要截断于250字）
