Solid-State Characterization and Dissolution Properties of Reserpine – Hydroxypropyl-β-Cyclodextrin Inclusion Complex

Author(s)

Patel, N.A., Patel, R.P.

Author's Affiliation

Abstract

The objectives of this research were to prepare and characterize inclusion complex of Reserpine with hydroxypropyl-b-cyclodextrin and to study the effect of complex on the dissolution rate of Reserpine, a water insoluble drug.  Phase-solubility profile indicated that the solubility of Reserpine was significantly increased in the presence of hydroxypropyl-b-cyclodextrin and was classified as A_L-type, indicating the 1:1 stoichiometric inclusion complexes. Gibbs free energy (DG_tr°) values were all negative at different concentration of hydroxypropyl-b-cyclodextrin, indicating the spontaneous nature of Reserpine solubilization, and they decreased with increase in the b-cyclodextrin concentration, demonstrating that the reaction conditions became more favorable as the concentration of hydroxypropyl-b-cyclodextrin increased. The equimolar inclusion complex of Reserpine and hydroxypropyl-b-cyclodextrin was prepared by various methods such as kneading, coevaporation and physical mixing. The molecular behaviors of drug in all samples were characterized by Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) patterns, SEM. The results of these studies indicated that complex prepared kneading and co-evaporation methods exhibited the amorphousness as well as the successful inclusion of the Reserpine molecule into the cyclodextrin cavity. The complexation resulted in a marked improvement in the solubility of Reserpine. These complexes exhibited substantially higher and faster rates of dissolution compared to that of Reserpine and physical mixture. Physical mixture also showed significant improvement in the dissolution rate compared to pure Reserpine. Mean dissolution time (MDT) of Reserpine decreased significantly after preparation of complexes and physical mixture. Similarity factor (f₂) indicated significant difference between the release profiles of Reserpine from complexes and physical mixture and from pure Reserpine.

Keywords

Reserpine, Hydroxypropyl-b-Cyclodextrin, Inclusion complexation, In Vitro dissolution Studies

Cite This Article

Patel, N.A., Patel, R.P. (2015). Solid-State Characterization and Dissolution Properties of Reserpine – Hydroxypropyl-β-Cyclodextrin Inclusion Complex, International Journal for Pharmaceutical Research Scholars (IJPRS), 4(1), 316-327.