Pharmacokinetics of pirfenidone after a single dose and multiple-dose administration in Chinese healthy volunteers
- Author:
Xiu-Ling HE
1
Author Information
- Publication Type:Journal Article
- Keywords: HPLC-MS/MS; Pharmacokinetics; Pirfenidone
- From: Chinese Pharmaceutical Journal 2015;50(13):1134-1137
- CountryChina
- Language:Chinese
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Abstract:
OBJECTIVE: To study the pharmacokinetics of pirfenidone in Chinese healthy volunteer after a single dose and multiple-dose administration. METHODS: Twelve Chinese healthy volunteers were randomly divided into low, medium and high dose groups(200, 400, 600 mg). The multiple-dose group was administrated with pirfenidione 400 mg three times daily for 5 d. Intensive blood sampling was performed from 12 volunteers within 12 h after the single dosing and the last dose of the multiple dosing. HPLC-MS/MS was used to determine the plasma concentrations of pirfenidone. The pharmacokinetic parameters were calculated by DAS software. RESULTS: The main pharmacokinetic parameters of pirfenidone after single-dose administration of 200, 400, 600 mg qd as follows: ρ
max were(5.00 ± 1.42), (9.43 ± 2.74) and(14.14 ±3.36)mg · L-1; tmax were(0.57 ±0.33), (0.60 ± 0.30) and(0.60 ± 0.38) h; t½ were(2.16 ±0.77), (2.15 ±0.75) and (2.01 ±0.76)h; AUC0-∞ were(13.87 ±7.79), (29.26 ± 12.02) and (45.85 ± 20.25)mg · h · L-1; AUC0-12 were (13.27 ±7.08), (27.92 ± 10.56) and(43.98 ± 18.14) mg · h · L-1, respectively. The main pharmacokinetic parameters after 400 mg tid for 5 d were as follows: ρmax was(9.46 ±2.77) mg · L-1, ρmin was(1.14 ± 1.11) mg · L-1, tmax was(0.52 ± 0.34) h, t½ was (1.93 ± 0.63) h, AUC0-∞ was (26.74 ± 13.49) mg · h · L-1, AUC0-12 was (25.79 ± 12.34)mg · h · L-1, AUCss was(23.53 ± 10.59)mg · h · L-1. CONCLUSION: The pharmacokinetic parameters of pirfenidone show that ρmax and AUC were linear in the dose range from 200 - 600 mg and the pharmacokinetic parameters were similar as reference.
