Preparation, Characterization, and In Vitro Evaluation of Aceclofenac PVP-Solid Dispersions

Abstract

The objective of the present investigation was to study the effect of polyvinylpyrrolidone (PVP) on in vitro dissolution of aceclofenac from solid dispersions. Aceclofenac binary solid dispersions (SD) with different drug loadings were prepared using the melting or fusion method. In vitro dissolution of pure drug, physical mixtures, and solid dispersions were carried out. Solid dispersion of aceclofenac with PVP showed considerable increase in the dissolution rate in comparison with physical mixture and pure drug in 0.1 N HCl, pH 1.2 and phosphate buffer, pH 7.4. Solid dispersions in 1:2 ratio showed maximum dissolution rate in comparison to other ratios. The amorphous nature of the drug in solid dispersion was confirmed by scanning electron microscopy and a decrease in enthalpy of drug melting in solid dispersion compared to the pure drug. FTIR spectroscopy and differential scanning calorimetry studies indicated no interaction between aceclofenac and PVP in solid dispersions in solid state. Dissolution enhancement was attributed to decreased crystallinity of the drug and to the wetting, eutectic formation, and solubilizing effect of the carrier from the solid dispersions of aceclofenac. In conclusion, dissolution of aceclofenac can be enhanced by the use of hydrophilic carriers like PVP.

Keywords:

• Aceclofenac
• dissolution
• PVP

Acknowledgments

The authors are very thankful to Ipca Laboratories, Mumbai, India, for their generous gift sample of aceclofenac. The authors thanks U. P. Technical University, Lucknow, India, for valuable support.

Notes

AF: aceclofenac; PVP: polyvinyl pyrrolidone; SD: solid dispersion. Values in parenthesis indicates the standard deviation (n = 3) and values given in the parenthesis marked with *indicates theoretical values of drug content.

AF: aceclofenac; PVP: polyvinyl pyrrolidone; SD: solid dispersion. Values in parenthesis indicates the standard deviation (n = 3).

AF: aceclofenac; PVP: polyvinyl pyrrolidone; SD: solid dispersion. Values in parenthesis indicates the standard deviation (n = 3).

AF: aceclofenac; PVP: polyvinyl pyrrolidone; SD: solid dispersion; U: urea.