Assessment of the effect of base type and surfactant on the release properties and kinetics of paracetamol suppositories

Ilomuanya Margaret. O, Ifudu N

Abstract

In the formulation of different drugs as suppositories, there is the need to determine the optimum formulation factors which depend on the drug candidate itself, suppository base and the presence of an adjuvant or absorption enhancers. 1g paracetamol suppositories each containing 250mg of paracetamol were prepared by the fusion method (BP, 2012) utilizing cocoa butter, PEG 1500, PEG 4000, PEG 1500/4000(3:1) and Suppocire® as suppository bases. A proper combination of the polyethylene glycol bases (PEG) i.e. PEG 1500/4000 in ratio of 75%:25% gave more suitable release profile than the singular use of either water soluble base examined. The base Suppocire S2 blend incorporating 0.5% tween 40 was the best base in terms of release profiles with over 95% of paracetamol being released within 10minutes. The major mechanism of drug release fit the Higuchi release kinetic model. The presence of 2% span 80 and 0.5% tween 40 not only affected drug release but also the physicochemical characteristics of the suppository bases.

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