|
KMID : 0043320070300070876
|
|
Archives of Pharmacal Research
2007 Volume.30 No. 7 p.876 ~ p.883
|
|
|
Degradation Kinetics of Water-Insoluble Lauroyl-Indapamide in Aqueous Solutions: Prediction of the Stabilities of the Drug in Liposomes
|
|
Suo Xu Bin
Deng Ying Jie
Zhang Han
Wang Yu Qiang
|
|
|
Abstract
|
|
|
|
The aim of this study was to explore the degradation kinetics of water-insoluble lauroyl-indapamide in solutions and predict the stabilities of lauroyl-indapamide encapsulated in liposomes. Buffer-acetone (9:1) was used as the reaction solution and the reaction temperature was maintained at 60oC. The correlation of the apparent degradation constants (kobs) of lauroyl-indapamide in liposomes and in buffer-acetone solutions at different pH has been explored. The degradation of lauroyl-indapamide in solutions was found to follow pseudo-first-order kinetics and was significantly dependent on the pH values. Lauroyl-indapamide was the most stable at pH 6.8, increasing or decreasing the pH of the solutions would decrease its stabilities. Buffer concentration had some effects on the stabilities of lauroyl-indapamide. The degradation active energies Ea were 68.19 kJ·mol-1, 131.75 kJ·mol-1 and 107.72 kJ·mol-1 at pH3.6, 6.8 and 12 respectively in acetone-free buffer solutions (0.05M) calculated according to the Arrhenius equation with the extrapolation method. The apparent degradation constants (kobs) of lauroylindapamide in liposome and in buffer-acetone (9:1) solutions showed a good correlation at different pH levels, which indicates that the stabilities of the drug that dissolved in acetone-buffer mixture solutions can be used to predict the stabilities of the drug in liposomes as well.
|
|
|
KEYWORD
|
|
|
Lauroyl-indapamide, Water-insoluble, Degradation kinetics, Aqueous solutions, Liposomes
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|