Ins paper describes the development and validation of a liquid chromatography mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propafenone hy...Ins paper describes the development and validation of a liquid chromatography mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propafenone hydrochloride sustained-release capsule (SR-test), as an instant-release tablet (IR-reference) and as the market leader sustained-release capsule (Rythmod SR-reference) in male beagle dogs (n= 8). In Study A comparing SR-test with IR-reference in a crossover design T-max and t(1/2) of propafenone for SR-test were significantly higher than those for IR-reference while C-max and AUC were lower demonstrating the sustained release properties of the new formulation. In Study B comparing SR-test with SR-reference the observed C and A TIC of propafenone for SR test (124.5 +/- 140.0 ng/mL and 612.0 +/- 699.2 ng.h/mL, respectively) were higher than for SR-reference (78.52 +/- 72.92 ng/mL and 423.6 +/- 431.6 ng.h/mL, respectively) although the differences were not significant. Overall, the new formulation has as good if not better sustained release characteristics to the market leader formulation. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier By All rights reserved.展开更多
文摘Ins paper describes the development and validation of a liquid chromatography mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propafenone hydrochloride sustained-release capsule (SR-test), as an instant-release tablet (IR-reference) and as the market leader sustained-release capsule (Rythmod SR-reference) in male beagle dogs (n= 8). In Study A comparing SR-test with IR-reference in a crossover design T-max and t(1/2) of propafenone for SR-test were significantly higher than those for IR-reference while C-max and AUC were lower demonstrating the sustained release properties of the new formulation. In Study B comparing SR-test with SR-reference the observed C and A TIC of propafenone for SR test (124.5 +/- 140.0 ng/mL and 612.0 +/- 699.2 ng.h/mL, respectively) were higher than for SR-reference (78.52 +/- 72.92 ng/mL and 423.6 +/- 431.6 ng.h/mL, respectively) although the differences were not significant. Overall, the new formulation has as good if not better sustained release characteristics to the market leader formulation. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier By All rights reserved.
