ABSTRACT
OBJECTIVE: To investigate the pharmacokinetics of 10 mg adefovir dipivoxil tablet formulations in 12 Chinese healthy subjects after a single dose and multiple doses. METHODS: A single dose and multiple doses of the formulations of adefovir dipivoxil tablets were given to each of 12 healthy male subjects. The concentrations of adefovir in plasma were determined by LC-MS/MS. The pharmacokinetic parameters were calculated by DAS2.0 programme. RESULTS: The obtained pharmacokinetic parameters of adefovir following adefovir dipivoxil tablets in a single dose and multiple doses group were as follows: ρmax were (24 ± 9), (24 ± 8) μg · L-1; AUC0-24 h were (210 ± 54), (213 ± 73) μg · h · L-1; AUC0-∞ were(236 ± 64), (250 ± 90) μg · h · L-1; t1/2 were (7.4 ± 1.2), (8.5 ± 2.1)h; tmax were (1.3 ± 0.7), (1.5 ± 0.6) h, respectively. Other main parameters in multiple doses group were ρavss (8.90 ± 3.06) μg · L-1 and DF (2.52 ± 0.66). CONCLUSION: There was no significant difference in pharmacokinetic parameters between single dose and multi-dose group. There is no accumulation following multiple doses of adefovir dipivoxil. Adefovir dipivoxil tablets were safe and well tolerated in Chinese subjects. Copyright 2012 by the Chinese Pharmaceutical Association.