Pharmacokinetics of isosorbide-5-mononitrate sustained-release capsules in healthy volunteers
- VernacularTitle:5-单硝基异山梨醇酯缓释胶囊的人体药代动力学研究
- Author:
Guorong FAN
;
Jinhong HU
;
Mei LIN
;
- Publication Type:Journal Article
- Keywords:
isosorbide 5 mononitrate;
delayed action preparations;
pharmacokinetics;
biological availability
- From:
Academic Journal of Second Military Medical University
1985;0(05):-
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To study the pharmacokinetics and relative bioavailability of isosorbide 5 mononitrate(5 ISMN)sustained release capsules in 12 male healthy volunteers. Methods: A capillary gas chromatography method with electron captured detector was established for the determination of 5 ISMN in plasma, after administrating a daily dose of 40 mg 5 ISMN domestic and imported sustained release capsules in a randomized crossover design.The fluctuation of 5 ISMN valley concentrations observed and the steady state pharmacokinetics was characterized in a multiple dose schedule of 40 mg 5 ISMN sustained release capsules.Results:The steady state of 5 ISMN plasma concentrations reached at the fourth oral administration.The steady state pharmacokinetic parameters after multiple oral dose of 40 mg 5 ISMN domestic and imported sustained release capsules were as follows: t max were (4.8?0.6) and (4.8?0.9) h, c max were (802.46?94.45) and (807.09?109.16) ?g/L, c min were (127.83?23.76) and (121.85?22.00) ?g/L, AUC ss were (8 114.7?1 393.4) and (8 174.8?1 219.7) ?g?h/L, c av were (338.12?58.06) and (340.62?50.82) ?g/L,the degree of fluctuation (DF) were (2.04?0.39) and (2.03?0.33), respectively. Conclusion:The relative bioavailability of multiple oral dose of 40 mg domestic 5 ISMN sustained release capsules is (99.07?5.45)%, there are no significant differences in the main steady state pharmacokinetic parameters between domestic and imported sustained release capsules, and so the 2 capsules are bioequivalent.
