1,4-Dihydropyridines (DHPs) are a classification of compounds used as calcium channel blockers in the treatment of various conditions. These compounds readily undergo photodegradation. The degradants produced have no pharmaceutical activity and render the drugs ineffective. DHPs also exhibit polymorphism. Nifedipine and Nimodipine are two such drugs. This study aimed to monitor the photodegradation of these two drugs and to establish the effect of particle size, polymorphism and β-Cyclodextrin (β-CD) on the rate of photodegradation. Different polymorphs (namely the amorphous and stable crystalline polymorphs) of the two drugs were prepared for use in the study. Mixtures of each drug with β-CD were also prepared for photostability studies. The mixtures were prepared in a 1:1 molar ratio. The rate of photodegradation was studied with a 500 W metal halide lamp in accordance to ICH guidelines. The study employed samples on a small scale where degradation was analysed with High Performance Liquid Chromatography, and also samples on a larger scale where degradation was monitored with Powder X-ray Diffraction. The two sets of results of observing the degradation process by two analytical techniques where compared in terms of their quantification methods. The extent of photodegradation was suitably modelled and fitted using the Avrami-Erofeyev kinetic equation. Smaller particle size showed increased photodegradation for Nimodipine; the effect was insignificant for Nifedipine however. For both drugs it was found that the amorphous polymorph underwent faster photodegradation. The study showed that β-CD caused an increase in photodegradation for both drugs under these experimental conditions.
| Identifer | oai:union.ndltd.org:netd.ac.za/oai:union.ndltd.org:nmmu/vital:10378 |
| Date | January 2011 |
| Creators | Francis, Farzaana |
| Publisher | Nelson Mandela Metropolitan University, Faculty of Science |
| Source Sets | South African National ETD Portal |
| Language | English |
| Detected Language | English |
| Type | Thesis, Masters, MSc |
| Format | vi, 98 leaves, pdf |
| Rights | Nelson Mandela Metropolitan University |
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