Tuberc Respir Dis.  1986 Jun;33(2):88-94. 10.4046/trd.1986.33.2.88.

Pharmacokinetics of Oral Pyrazinamide in Normal Subjects

• KMID: 2528702
• DOI: http://doi.org/10.4046/trd.1986.33.2.88

Abstract

The pharmacokinetics of single oral dose(l gm) of pyrazinamide was studied in 13-normal subjects. Three of them received the dose as the commercial tablet and again as the solution preparation with at least 7 days interval. Serum and urine samples were collected at frequent intervals for up to 12 and 24hr, respectively. Peak serum concentrations ranged from 22.05 to 39.92 μg/ml. The mean serum half-life of pyrazinamide was 8. 21±1. 38 hr. Unchanged drug excreted in urine up to 24 hr averaged 28.3 ± 5.9% of the dose administered. The rnean value for the volurne of distribution(Vl_daea/F) and total clearance(Cl_t/F) using a non-method was 0.52 ± 0.09 L/kg and 46.02 ± 9.46 rnl/hr/kg, respectively. Renal clearance ranged from 10.49 to 26.68 ml/hr/ kg, indicating dominant tubular reabsorption. Excretion ratio of pyrazinamide in two subjects with relatively constant urine flow during experiment was gradually increased parallel to the reduction of serum concentration, meaning existence of active tubular secretion. The mean in vivo dissolution time of pyrazinamide tablet was 0.62 ± 0.88 hr and its relative bioavailability to a aqueous solution was 1.03 ± 0.07.