米诺环素注射剂的药动学

目的:研究健康志愿者静脉滴注米诺环素后的药动学特征,为临床合理用药提供参考依据。方法:8名健康志愿者分别静脉滴注米诺环素单剂量(200mg)、多剂量(100mg,bid×5d),于规定时间点取血,以高效液相色谱法测定血药浓度,计算单剂量和多剂量给药后的药动学参数。结果:单剂量给药后的主要药动学参数分别为cmax=(5.4±s0.9)mg·L-1;tmax=2h;t1/2=(26±3)h;MRT=(36±5)h;AUC0~72=(94±24)mg·h·L-1;AUC0~∞=(109±29)mg·h·L-1。多剂量给药达稳态后的药动学参数分别为cmssax=(8.4±1.5)mg·L-1;cmssin=(1.0±0.4)mg·L-1;csavs=(2.1±0.6)mg·L-1;AUCss=(149±42)mg·h·L-1;DF=3.7±0.6。结论:受试制剂米诺环素注射剂在人体内的药动学特征与文献报道基本一致。

Pharmacokinetics of minocycline injection in healthy volunteers

AIM:To study the pharmacokinetics characteristics of minocyline and provide the evidence for proper clinical application METHODS: Eight healthy male volunteers participated in this trail and were giv en minocyline by means of intravenous infusion in a single (200 mg) and multiple (100 mg,bid× 5 d ) doses.A HPLC method was applied to determine the serum dr ug c o ncentrations and calculate the pharmacokinetic parameters. RESULTS: The pharmacokinetic parameters obtained from the single-dose study w ere as follows:c_ max =(5.4±s 0.9) mg·L -1 ;t_ max = 2 h ; t_ 1/2 :(26±3) h;MRT=(36±5) h;AUC_ 0-72 = (94±24) mg· h ·L  -1 ;AUC_ 0-∞ =(109±29) mg· h· L -1 .The steady-state pha rmac okinetic parameters after giving multiple doses were:c ss _ max =(8.4 ±1.5) mg·L -1 ;c ss _ min =(1.0±0.4) mg·L -1 ; c ss _ av =(2.1± 0.6) mg·L -1 ;AUC SS =(149± 42) mg ·h·L -1 ;DF= 3.7±0.6 . CONCLUSION: The main pharmacokinetic parameters of minocyline are consistent with those hav e been reported previously.