盐酸米诺环素的人体药动学研究

Pharmacokinetics of minocycline hydrochloride in healthy volunteers

目的:研究注射用盐酸米诺环素在中国健康人体内的药动学特性。方法:12名健康志愿者采用随机自身交叉试验设计,单剂量静脉滴注给药(50,100,200 mg)。每次用药间隔1周。药物浓度采用高效液相色谱法(HPLC)测定。结果:血浆中原型药物的Cm ax和AUC随剂量的增大而增加,用药剂量为50,100,200 mg时,三个剂量组的Cmax分别为(1.41±0.21),(2.55±0.55),(6.13±1.29)μg.mL-1;AUC0-tn分别为(25.43±5.50),(44.08±6.72),(87.53±17.88)μg.mL-1.h;t1/2分别为(24.69±3.87),(25.52±3.06),(23.78±1.83)h。尿中原形药物的排出,随着给药剂量的增加而增加,男性与女性相比较,其排泄率未显示性别差异。结论:本方法专属性强,灵敏度高。因尿中药物浓度较高,用于泌尿系统感染时可获得较佳疗效。

Objective： To evaluate pharmacokinetics of minocycline injection in healthy volunteers. Methods： Twelve healthy volunteers were randomized into three groups. A single dose of 50,100, 200 mg were injected every period,respectively,in a self-control cross over test. The concentration was determined by HPLC. There was one-week washout between every period. Results： The value of Cmax and AUC showed dose-dependent increase. Cmax were （ 1.41 ± 0.21 ）, （2.55 ± 0.55 ）, （6. 13 ± 1.29 ） μg·mL^-1; AUC0-tn were （25.43± 5.50）, （44.08 ±6.72）, （87.53 ± 17.88）μg·mL^-1·h; t1/2 were （24. 69 ± 3.87）, （25.52 ± 3.06）, （23.78 ± 1.83 ） h, respectively. The excretion of drug in urine showed dose-dependent increase. No gender difference in the excretory rate was found. Conclusion： This specific, sensitive HPLC method offers an alternative to analysis and evaluated the pharmaeokineties of minoeyelin. High distribution of minoeyeline in urine make it suitable for the treatment of urinary system infection.