Enhancement of dissolution rate of racecadotril by liquisolid compact technology

Abstract The current investigation was used to improve the rate of dissolution of an anti-diarrheal drug i.e., racecadotril (RT) at low pH conditions (i.e., in the stomach) by reducing the water secretion and electrolyte in to the intestine by liquisolid tablets. Different formulations (liquisolid) were prepared using Avicel PH 102 as a carrier. Aerosil 200 as a coating material and sodium starch glycolate used as a disintegrant. Polyethylene glycol 200 was used as a non-volatile vehicle to dissolve the drug. FTIR, DSC, XRD and dissolution studies were conducted to characterise liquisolid tablets. Characterisation studies indicated that no interactions between carrier and drug. Solid state characterization had shown a reduction in crystallinity that further supports increment in solubility and dissolution. The optimised formulation showed a significant increase in dissolution i.e., 99.54±0.62% in 30 min compared to directly compressible tablets (38.47±0.26%). The % dissolution efficiency of racecadotril liquisolid tablets 76.86% compared to marketed tablet (27.56%) and conventional direct compression tablet (17.11%). Significant reduction in mean dissolution time of racecadotril from liquisolid tablets (6.84 min) compared to direct compression tablet (44.57 min), indicating faster release of drug and faster onset of action. Formulation of liquisolid tablets could enhance solubility, dissolution and bioavailability of racecadotril

Solubility and dissolution enhancement of flurbiprofen by solid dispersion using hydrophilic carriers

ABSTRACT The intent of the current work is to study the effect of polyethylene glycol 8000 and polyethylene glycol 10000 as hydrophilic carriers on dissolution behaviour of flurbiprofen. In the present study, solvent evaporation method was used to prepare flurbiprofen solid dispersions and evaluated for physico-chemical properties, drug-carrier compatibility studies and dissolution behaviour of drug. Solubility studies showed more solubility in higher pH values and formulations SD4 and SD8 were selected to prepare the fast dissolving tablets. FTIR and DSC study showed no interaction and drug was dispersed molecularly in hydrophilic carrier. XRD studies revealed that there was change in the crystallinity of the drug. The results of In vitro studies showed SD8 formulation confer significant improvement (p<0.05) in drug release, Q20 was 99.08±1.35% compared to conventional and marketed tablets (47.31±0.74% and 56.86±1.91%). The mean dissolution time (MDT) was reduced to 8.79 min compared to conventional and marketed tablets (25.76 and 22.22 min.) indicating faster drug release. The DE (% dissolution efficiency) was increased by 2.5 folds (61.63%) compared to conventional tablets (23.71%). From the results, it is evident that polyethylene glycol solid dispersions in less carrier ratio may enhance the solubility and there by improve the dissolution rate of flurbiprofen.

Formulation and in vitro evaluation of flurbiprofen-polyethylene glycol 20000 solid dispersions.

Solid dispersion is one of the most widely used methods to enhance the solubility and dissolution rate of poor water soluble drugs. In the present study, flurbiprofen solid dispersions were prepared using solvent evaporation method by incorporating polyethylene glycol 20000 and evaluated for solubility studies, drug-carrier compatibility studies and in vitro dissolution studies. From the solubility studies, formulations F4 were selected to prepare in the form of tablets and compared with control tablets (conventional tablets using pure drug). From the results of in vitro dissolution study, tablets containing polyethylene glycol 20000 showed almost complete drug release within the 15 min. The percent drug release in 15 min (Q15) and initial dissolution rate for formulation F4 was 99.26±1.12%, 6.62%/min. These were very much higher compared to control tablets (34.95±1.29%, 2.33%/min). The relative dissolution rate was found to be 2.84 and dissolution efficiency was found to be 57.48 and it is increased by 3.5 fold with F4 formulation compared to control tablets (17.91). From the above results, it is concluded that the formulation of solid dispersions using polyethylene glycol 20000 is a suitable approach to improve the solubility and dissolution rate of flurbiprofen.