Evaluation of thermal stability and parameters of dissolution of nifedipine crystals
Nifedipine is a calcium channel blocker as well as a powerful vasodilator used to treat ischemic heart disease and hypertension. Its photosensitivity and very low solubility in water have been widely acknowledged as important properties deserving improvements. The main thrust of this study is to cha...
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Veröffentlicht in: | Journal of thermal analysis and calorimetry 2013-03, Vol.111 (3), p.2117-2123 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Nifedipine is a calcium channel blocker as well as a powerful vasodilator used to treat ischemic heart disease and hypertension. Its photosensitivity and very low solubility in water have been widely acknowledged as important properties deserving improvements. The main thrust of this study is to characterize the nature and the solid-state of nifedipine crystals obtained using different solvents as well as assess the stability by thermal methods (TG and DSC) and crystals structure by means of spectroscopic techniques (MID FTIR and XRD) and assess the dissolution parameters for such crystals. The calculated kinetic parameters activation energy (
E
a
= 123.3 kJ mol
−1
± 0.1), the factor frequency (
A
= 25.93 ± 0.9 min
−1
), and the reaction order (
n
= 0.2) of the main stage of thermal decomposition of nifedipine raw material were performed according to the Ozawa model. The data showed a zero-order kinetic behavior for all crystals despite the different values of
E
a
and
A
. The dissolution profiles were obtained for such crystals in three dissolution media with different pH values. After 1 h of dissolution, the higher amount of nifedipine dissolved was observed for crystals obtained in isopropyl alcohol (52.5 %, pH 4.5), followed by those in chloroform (48.1 %, pH 1.2) and subsequently in acetone (32.5 %, pH 6.8). Results showed different thermal stabilities and significant variations in the solubility of the crystals. |
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ISSN: | 1388-6150 1588-2926 1572-8943 |
DOI: | 10.1007/s10973-012-2605-y |