Pharmacokinetics of oral cyclosporine A microemulsion, Noeral®, in Vietnamese healthy volunteers
- Author:
Phan Thi Danh
- Publication Type:Journal Article
- Keywords:
cyclosporine A
- MeSH:
Pharmacokinetics;
Cyclosporine
- From:Journal Ho Chi Minh Medical
2005;9(3):181-188
- CountryViet Nam
- Language:Vietnamese
-
Abstract:
The study was carried out on 30 healthy volunteers (16 males, 14 females), aged 21-40. Cyclosporine A (CsA), Neoral®, dosage of 2 mg/kg body weight (rounded nearest to 25 mg), was given at hours as 0 (starting time), 12, and 24. The blood samples were collected at hours 0, 2, 4, 6, 8, 12 (before the 2nd dose), 24 (before the 3rd dose) and 36. The CsA concentrations were measured with fluorescence polarization immunoassay (FPIA) with the TDx analyser, Abbott. Results: Pharmacokinetics of CsA, oral micro-emulsion, in Vietnamese volunteers have the characteristics: Cmax = 763 ± 241 ng/ml, Cmin = 358 ± 104 mg/ml/mg/kg, tmax = 2.3 ± 1.1 h, AUC 0-4 = 1756 ± 561 ng.h/ml, AUC0-4 /dose/kg = 827 ± 250 ng.h/ml/mg/kg, AUCinf = 3725 ± 983 ng.h/ml,
AUCinf/dose/kg = 1756 ± 433 ng.h/ml/mg/kg, t1/2 = 4.1 ± 1.2, Cl/F = 30.5 ± 6.9 L/h. The inter-individual variation in pharmacokinetics is presented with the coefficient of variations (CVs) of Cmax, AUC 0-4, AUCinf as 31.6%, 31.9% and 26.4%, respectively. The concentration of C2 has an important linear relationship with AUC0-4 (r = 9.987, p <0.0005), inversely there is no linear relation between C12 (the trough C0: before 2nd dose of CsA) (r = -0.189, p= 0.32). Cmax/dose/kg, AUC0-4/dose/kg and AUCinf/dose/kg in female volunteers were lower than those in male volunteers (p<0.005)
