European Journal of Biomedical and Pharmaceutical Sciences

PRECLINICAL STUDIES TO DEVELOP A NOVEL SOFT GELATIN CAPSULE FOR PARACETAMOL WITH FASTER ONSET TIME OF ACTION

Jyothirmayee Devineni*, Sai Gautham Naidu and Thirumala Rao Pathini

ABSTRACT

Objectives: The present research study was carried out to develop a novel soft gelatin capsule of paracetamol (PRT), an antipyretic and analgesic agent in which the pain relief onset time is improved to less than 4 minutes. The role of liquid fill formulation of PRT (PRT-LF) in a soft gelatin capsule SGC (commercial oblong empty SGC of size 20) in increasing the in vitro and preclinical in-vivo bioavailability of PRT in Sprague Dawley rats was studied. Experimental: PRT-LF were formulated and optimized using permeation enhancer/permeability glyco- protein (p-gp) inhibitor polyethylene glycol (PEG-400). The optimized PRT-LF formulation was then incorporated into the empty commercial SGC and tested for the increased drug percent released at 2 minutes, 4 minutes (DP2 and DP4) by the assistance of PEG-400. In vitro permeation studies were carried out using Franz diffusion cells for a period of 24 h. Results and Discussion: The optimized PRT-LF SGC had good physicochemical properties. The formulations were stable up to 6 months without undergoing any degradation.From the Franz diffusion cell apparatus permeation studies it was evident that the delivery of PRT into the dialysis membrane by liquid fill formulations for soft gels was significantly higher than that from marketed formulation paracip-650, with apparent permeability coefficient of 0.815±0.006 cm/h for F3 formulation. Conclusion: when compared to existing oral onset action time of 37 minutes and intravenous pain relief onset time of 8 minutes, F3 PRT-LF SGC could be used to show the faster onset of action evident from in-vivo studies in rats.

Keywords: Paracetamol, soft gelatine capsules, Bioavailability.