Correlations between in Vivo and in Vitro Dissolution Rates of (α-Bromoisovaleryl) urea Polymorphs

概要

論文の詳細を見る
Correlations between the in vivo and in vitro dissolution rates of (α-bromoisovaleryl) urea polymorphs were investigated. The calculated dissolution rate constants obtained in the in vitro dissolution experiments were 0.135 and 0.133 (cm/min) for form I and form II, respectively. On the other hand, the crystals were administered intraduodenally into rats and the time course data of the plasma concentration were analyzed by the least-squares method on the basis of the Hixson-Crowell dissolution model for the intestinal dissolution process. The in vivo dissolution rate constants were obtained as 0.0629 and 0.0758 (cm/min) for form I and form II, respectively. These in vivo and in vitro dissolution rate constants are based on the Noyes-Nernst dissolution theory and should be comparable in nature. Nevertheless, the in vivo rate constants were about a half of those in vitro. This result suggests that the stirring efficiency in the intestine is about a half of that of the in vitro dissolution experiment in this study.
公益社団法人日本薬学会の論文
1984-08-25