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Decomposition of beclomethasone propionate esters in human plasma
Author(s) -
Foe Kuncoro,
Brown Kenneth F.,
Seale John P.
Publication year - 1998
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199801)19:1<1::aid-bdd67>3.0.co;2-3
Subject(s) - chemistry , kinetics , chromatography , high performance liquid chromatography , decomposition , incubation , propionate , nuclear chemistry , human serum albumin , organic chemistry , biochemistry , physics , quantum mechanics
The kinetics of decomposition of beclomethasone dipropionate (BDP), the 17‐monopropionate ester (17‐BMP), and beclomethasone (BOH) were characterized in whole human plasma (HP), pH 7.1, and in solutions of 1% human serum albumin (HSA), pH 7.4, and 0.067 M phosphate buffer, pH 7.4 (μ = 0.17). A reversed‐phase, high‐performance liquid chromatography (HPLC) assay enabled simultaneous separation and quantification of beclomethasone propionate esters and six degradation products including three unidentified products, D1–D3, not previously reported. Following incubation of BDP, products were formed in the following sequence, D1, 17‐BMP, beclomethasone‐21‐monopropionate (21‐BMP), D3, BOH, and D2. Following incubation of 17‐BMP, the same sequence of degradation products was formed with the exception of D1. Following incubation of BOH, only D2 was formed. The decomposition reactions of BDP, 17‐BMP, and BOH in HP exhibit pseudo‐first‐order kinetics. However the degradation reactions of BDP in solutions of 1% HSA and phosphate buffer were found to follow pseudo‐zero‐order kinetics. At an initial concentration of 40 μg mL −1 , the half‐lives for BDP, 17‐BMP, and BOH in HP were 10.9±0.4, 3.0±0.2 and 24.8±0.2 h, respectively. © 1998 John Wiley & Sons, Ltd.