Abstract
Purpose: The individual and interaction effects of formulation variables on the release of suppositories were investigated using a 23 factorial experimental design. The variables studied were nature of base (B), type of drug (D), and presence of surfactant (S). Method: Suppositories were formulated with theobroma oil and Witepsol H15 as bases at ‘low' and ‘high' levels respectively. Chloroquine and aminophylline, both water-soluble drugs, were incorporated as active constituents at ‘low' and ‘high' levels respectively while Tween 80 was incorporated as surfactant in some of the formulations. Disintegration time and time taken for 50% of the drug to dissolve were used as assessment parameters. Results: The inclusion of surfactant in the suppository formulation proved to be the most significant variable in the formulation. The ranking for the individual coefficient values for the formulations was S>>B>D for disintegration time DT and S>>>D>B for the dissolution parameter t50. While the ranking for the interaction effects was B-D>B-S>S-D on DT and on t50 S-D>B-S>B-D. Conclusion: The results suggest that in formulating water-soluble drugs such as chloroquine and aminophylline as suppositories in a hydrophobic base, the presence of a surfactant is the most influential variable. Keywords: Suppositories, chloroquine, aminophylline, surfactant, interacting variables. > Tropical Journal of Pharmaceutical Research Vol. 3 (1) 2004: pp. 285-290
Highlights
The processes of release and absorption of drugs from suppositories are complex
The representative plot of the dissolution profiles of the chloroquine and aminophylline suppositories are given in Figure 1 and 2
The incorporation of Tween 80 at a concentration of 0.5%w/v resulted in a significant increase (p
Summary
The processes of release and absorption of drugs from suppositories are complex. Release and subsequent absorption depend to a great extent on the viscosity of the suppository mass and on the mechanism of release from fatty bases. It has been found reasonable[1] to use a fat-like base for watersoluble drugs. Chloroquine is slightly acidic in solution, while aminophylline is slightly alkaline. Both are freely water-soluble and the aim of the work is to obtain the best formulation for the drugs that would serve as a template for the suppository formulation of such watersoluble drugs
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