Surface Solid Dispersion: A Novel Method for improving in-vitro dissolution and in-vivo pharmacokinetics of Meclizine hydrochloride

Bhaskar Daravath

doi:10.5958/0974-360X.2021.00121.9

Research Journal of Pharmacy and Technology

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0974-360X (Online)
0974-3618 (Print)

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Surface Solid Dispersion: A Novel Method for improving in-vitro dissolution and in-vivo pharmacokinetics of Meclizine hydrochloride

Author(s): Bhaskar Daravath

Email(s): bdaravat@gitam.edu

DOI: 10.5958/0974-360X.2021.00121.9

Address: Bhaskar Daravath*
Department of Pharmaceutics, GITAM School of Pharmacy, GITAM Deemed to be University, Hyderabad, Telangana, India-502329.
*Corresponding Author

Published In: Volume - 14, Issue - 2, Year - 2021

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ABSTRACT:
The current work is aimed to evaluate the role of Gelucire on the solubility; in-vitro dissolution rate and oral bioavailability of a poorly water soluble drug meclizine hydrochloride (MZ). Polyethylene glycol 8000, Gelucire 50/13 and Gelucire 44/14 solid dispersions with surface adsorbents (SSDs) and physical mixtures were prepared using MZ as a model drug. Interaction between carrier and drug, solid state characterization of drug in formulations as well as in physical mixtures was studied using FTIR, DSC and XRD. The effect of Gelucire on solubility and dissolution of MZ was studied through in-vitro dissolution studies. The results indicated that no interactions between Gelucire and drug. Solid state characterization showed reduction in crystallinity that further supports increment in solubility and dissolution. The presence of Gelucire 44/14 in the formulation showed significant enhancement in solubility (152 folds) and dissolution rate (7.23 folds). In vivo bioavailability studies indicated significant (p<0.05) increase in AUC (5497.76±67.83ng-h/ml) with higher Cmax (791.10±40.04 ng/ml) and faster onset of action of MZ from the formulation containing Gelucire 44/14. In vivo pharmacokinetic studies showed optimised formulation was 209 % relatively bioavailable compared with MZ pure drug. The results suggest that Gelucire can be useful in delivering poorly soluble drug such as meclizine hydrochloride with improved solubility, dissolution and bioavailability.

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Cite this article:
Bhaskar Daravath. Surface Solid Dispersion: A Novel Method for improving in-vitro dissolution and in-vivo pharmacokinetics of Meclizine hydrochloride. Research J. Pharm. and Tech. 2021; 14(2):685-693. doi: 10.5958/0974-360X.2021.00121.9

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