Cyclodextrin Inclusion Complex of Racecadotril: Effect of Drug-β- Cyclodextrin Ratio and the Method of Complexation

ISSN: 1875-6220 (Online)
ISSN: 1570-1638 (Print)

Volume 14, 4 Issues, 2017

Download PDF Flyer

Current Drug Discovery Technologies

This journal supports open access

Aims & ScopeAbstracted/Indexed in

Submit Abstracts Online Submit Manuscripts Online

Vladimir P. Torchilin
Department of Pharmaceutical Science Center
for Pharmaceutical Biotechnology and Nanomedicine
Northeastern University
Boston, MA 02115

View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Cyclodextrin Inclusion Complex of Racecadotril: Effect of Drug-β- Cyclodextrin Ratio and the Method of Complexation

Current Drug Discovery Technologies, 11(2): 154-161.

Author(s): Mona Semalty, Mitali Panchpuri, Devendra Singh and Ajay Semalty.

Affiliation: Department of Pharmaceutical Sciences, H. N. B. Garhwal University, Srinagar (Garhwal) 246 174, Uttarakhand, India.


Racecadotril is an antisecretory and antidiarrheal agent against watery diarrhoea in children. Racecadotril is a class II drug (as per Biopharmaceutical Classification System) with poor aqueous solubility and dissolution rate limited absorption. β-cyclodextrin complexation of solubility or dissolution rate limited drugs provides an amphiphilic complex with improved solubility and dissolution profile. Thus Racecadotril – β-cyclodextrin complex were prepared to improve its solubility and dissolution by imparting an environment of improved hydrophilicity.

Racecadotril was complexed with β-cyclodextrin (in 1:1 and 1:2 molar ratios) by two different methods (solvent evaporation and kneading method). These inclusion complexes were evaluated for solubility, drug content, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD) and in vitro dissolution study.

The highest drug content (30.83%) was found in complex made by kneading method (RK1:1) in 1:1 molar ratio. Complex prepared by solvent evaporation method (RSE1:1, RSE1:2) were found to be showing irregular disc shaped non-porous surface, while the complexes prepared by kneading method (RK1:1, RK1:2) showed rough, fluffy, non-porous and irregular surface in SEM. Solubility of the drug improved up to 2 to 3 folds in the complexes. The complex RK1:1 showed the greatest improvement in solubility (from 28.98 to76.56 µg/ml). The dissolution of the complexes was also found to be improved. Complex prepared by solvent evaporation method in 1:1 molar ratio (RSE1:1) showed a marked improvement in percent drug release (100.33%) than that of pure drug (52.58%) at the end of 1 hour in dissolution study. FTIR, DSC and XRPD data confirmed the formation of inclusion complex. It was concluded that water solubility of all the complexes were increased when the drug was complexed with β-CD in 1:1 molar ratio. The complex made in 1:1 molar ratio (irrespective of the method) showed better solubility and the dissolution profile as compared to the complex made in 1:2 molar ratio. It was concluded that the complex prepared by the solvent evaporation method showed better solubility and the dissolution due to better amorphization of the drug.


BCD complex, in vitro dissolution, Racecadotril, solubility.

Purchase Online Order Reprints Order Eprints Rights and Permissions

Article Details

Volume: 11
Issue Number: 2
First Page: 154
Last Page: 161
Page Count: 8
DOI: 10.2174/15701638113106660043
Price: $58

Related Journals

Webmaster Contact: Copyright © 2016 Bentham Science