单剂量美他多辛注射液在健康人体的药代动力学

Pharmacokinetics of metadoxine injection in healthy volunteers

目的研究美他多辛注射液在健康人体的药代动力学。方法10名健康受试者随机分为3组，先后静滴美他多辛600，900，1200mg，点滴时间为3h；2次实验间隔1周，用高效液相色谱法测定血药浓度。结果主要药代动力学参数：Cmax分别为（4．4±0．79），（8．35±1．64）和（11．61±2．33）mg·L^-1；t1／2分别为（0．78±0．09），（0．83±0．10）和（0．81±0．12）h；AUC0-tn分别为（12．02±2．074），（22．89±4．79）和（35．02±7．07）mg·h·L^-1；AUC0-∞分别为（13．14±2．06），（23．52±4．6）和（35．46±7．48）mg·h·L^-1。约有10％～30％的美他多辛以原形物经。肾脏排泄。对3组t1/2分别做t检验，结果显示无显著性差异（P〉0．05）。结论不同给药剂量，其分布及消除过程基本一致。

Objective To study the pharmacokinetics of single dose of metadoxine injection in healthy volunteers. Methods In a randomized three period cross - over study, Ten male subjects were administrated intravenously 600,900 and 1200 mg of metadoxine within 3 h infusion. The concentrations of metadoxine in serum and in urine were obtained by HPLC. Results The main pharmacokinetic parameters were as follows： Cmax were （4.4±0.79）, （8.35±1.64） and （11.61±2.33）mg· L^-1; t1/2 were （0.78±0.09） ,（0.83±0.10） and （0.81±0.12） h; AUC0-tn were （ 12.02±2. 074 ）, （ 22.89±4.79 ） and （ 35.02±7.07 ） mg·h· L^-1; AUC0-∞ were （13.14±2.06）, （23.52±4.6） and （ 35.46±7.48 ） mg·h·L^-1, respectively. Urinary recovery rates were （17.28±13.43）%, （16.73±12.97）% and （ 12.07 ±5.32）%, respectively. There were no singnifigant difference among 3 dose groups in t 1/2 （ P 〉 0. 05 ）. Conclusion The pharrnacokinetics of metadoxine in different dose is not significantly.