[Pharmacokinetics of fudosteine in healthy volunteers].
OBJECTIVE
To study the pharmacokinetics of fudosteine in healthy volunteers after the single and multiple dose administration.


METHODS
Thirty-six volunteers were divided into three groups randomly, each group included six men and six women. In the single dose design, the volunteers received either a single dose of 600 mg, 400 mg or 200 mg fudosteine. After a one-week wash out period, the volunteers of 400 mg group participated in the multiple dose design in which each volunteer received 400 mg fudosteine three times a day for five consecutive days. The plasma concentrations were determined by pre-column derivatization HPLC-FL method and the pharmacokinetic parameters of fudosteine were calculated.


RESULTS
The obtained pharmacokinetic parameters of fudosteine in single dose of 600 mg, 400 mg and 200 mg groups were as follows: T1/2 were (2.8 +/- 0.5), (2.7 +/- 0.5) and (3.2 +/- 0.6) h, respectively. T(max) were (0.51 +/- 0.22), (0.59 +/- 0.21) and (0.48 +/- 0.18) h, respectively. C(max) were (16 +/- 4), (11 +/- 3) and (6.1 +/- 1.5) microg x mL(-1), respectively. The AUC(0-10 h) and C(max) correlated linearly with doses, respectively (r > 0.99). The T(max), C(max) and AUC values of fudosteine in healthy male volunteers were smaller than those in female volunteers, and the T1/2 value was longer than that in female volunteers. The obtained multi-dose pharmacokinetic parameters of fudosteine were as follows: C(ss) was (4.1 +/- 0.8) microg x mL(-1); DF was 3.0 +/- 0.7; T1/2 was (2.5 +/- 0.4) h; T(max) was (0.6 +/- 0.3) h; C(max) was (13.2 +/- 1.3) microg x mL(-1).


CONCLUSIONS
The values of pharmacokinetic parameters in healthy volunteers were linear in the range from 200 mg to 600 mg. Statistic analysis results showed that the differences of AUC and C(max) between men and women were not resulted from sexual differences, but from the weight differences. There was no significant difference in pharmacokinetic parameters between single dose and multi-dose.
Ding
Li
L
Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China. dinglidl@hotmail.com
Yang
Jin
J
Li
Rong-Shan
RS
Zhou
Mei
M
Shen
Jian-Ping
JP
Zhang
Yin-Di
YD
D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D001835:Body Weight; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D003553:Cystine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male; D012737:Sex Factors
D003553:Cystine; C113797:fudosteine