复方氨酚曲马多片中对乙酰氨基酚的人体药代动力学研究

目的 研究氨酚曲马多片在中国健康人体内的药代动力学特性。方法 10名健康志愿者(男女各半)单剂量口服2片氨酚曲马多片（每片曲马多/对乙酰氨基酚为37.5 mg/325 mg）。对乙酰氨基酚血药及尿药浓度采用高效液相色谱-紫外（HPLC-UV）检测法测定。结果 受试者单次口服给药后，以HPLC-UV法测血浆及尿液中对乙酰氨基酚浓度。采用DAS软件计算对乙酰氨基酚的药代参数。C_max为(10.95±7.85)mg·L^-1，T_max为(0.83±0.29)h，t_1/2为(2.09±0.34)h，AUC_0～24为(26.93±11.64)mg·h·L^-1，AUC_0-∞为(27.74±11.57)mg·h·L^-1，尿液中24 h以原形排泄百分比(2.90±1.32)%；受试者各项检查未见异常，无不良反应发生。结论 对血浆药代动力学参数及尿中药物排泄量进行性别单因素方差分析，结果未显示性别差异。该药在试验剂量下具有良好的安全性。

Study on the pharmacokinetics of paracetamol in compound tramadol and paracetamol tablet in Chinese healthy volunteers

Objective To study on the pharmacokinetics of compound tramadol and paracetamol tablet in Chinese healthy volunteers. Methods 5 male and 5 female healthy volunteers received single dose of compound tramadol and paracetamol tablet（37.5 mg/325 mg）. The plasma and urine concentrations were detected by high performance liquid chromatography-ultraviolet(HPLC-UV) detection assay method. Results The main pharmacokinetic parameters of the preparation were: Cmax=(10.95±7.85)mg·L^-1；T_max=(0.83±0.29)h ；t_1/2=(2.09±0.34)h；AUC_0-24=(26.93±11.64)mg·h·L^-1；AUC0-∞=(27.74±11.57)mg·h·L^-1. The percentages of urinary excretive amount of the parent compound in 24 h were estimated to be (2.90±1.32)%. All the lab examination before and after drug administration was normal，no adverse events were found. Conclusion The preparation is safe for people in dose of 75 mg/650 mg. The pharmacokinetic parameters and urinary excretive amount show remarkable differences among individuals but no differences between male and female volunteers.