Cover Image

Development and characterization of ternary system for solubility enhancement of a second-generation COX-II inhibitor

Santosh Girani*, Shidallingapa Zalki, Mahantesh Kavatekar, Ajay Shahapur, Vitthal K. Vijapure

Abstract


Etoricoxib is a highly selective COX-II inhibitor, used to treat pains of different etiologies. Etoricoxib has low aqueous solubility (201µg/ml) and high permeability and therefore classified as BCS class II drug. By formulating these drugs with cyclodextrins as inclusion complexes have shown to increase the bioavailability. Cyclodextrins when used as complexing agents, enhance the solubility of poor water soluble lipophilic drugs. The objective of the present work is to formulate Etoricoxib cyclodextrin complexes by using ternary systems as Citric acid, Tartaric acid and PVP K-30 in order to enhance solubility and evaluate the enhanced solubility by in-vitro dissolution.

Keywords


NSAIDs; Etoricoxib; cyclodextrins; ternary system; inclusion complex; Kneading method; Solvent evaporation method; Spray drying; Freeze drying; XRD; DSC; FTIR; SEM

Full Text:

PDF

References


Peter B, Kubler P. Etoricoxib for arthritis and pain management. Therapeutics and Clinical Risk Management 2006;2(1)45-57.

Quercia O, Emiliani F, Foschi FG, Stefanini GF. Safety of etoricoxib in patients with reactions to NSAIDs. Journ Investig Allergol ClinImmunol 2008;18(3):163-7.

Yuan Y, Hunt RH. Global Gastrointestinal Safety Profile of Etoricoxib and Lumiracoxib. Curr Pharm Des 2007; 13:2237-47.

Shah M, Karekar P, Sancheti P, Vyas V, Pore Y. Effect of PVP K30 and/or L-Arginine on stability constant of etoricoxib-HPβCD inclusion complex: Preparation and characterization of etoricoxib-HPβCD binary system. Drug DevInd Pharm 2009; 35:118-29.

Martin A, Swarbrick J, Cammarata A. Physical pharmacy: Physical chemical principles in the pharmaceutical sciences. Indian edition: 3rd ed. Varghese Publishing House; 1991. 272.

Solubilisation of poorly soluble drugs: A review [Online]. 2007 Nov 13[Cited 2011 Aug 15]; Available from:URL:www.pharmainfo.net/reviews/solubilization-poorly-soluble-drugs-review

Zaheer A, Naveen M, Santosh MK, Khan I. Solubility enhancement of poorly water soluble drugs: a review. IJPT 2011;3(1):807-23.

Chowdary KPR, Enturi V, Pulya S. Formulation development of etoricoxib tablets by wet granulation and direct compression methods employing starch citrate. RJPBCS 2011;2(3):983-93.




DOI: http://dx.doi.org/10.21746/ijbio.2016.12.0010

Refbacks

  • There are currently no refbacks.




Copyright (c) 2016 International Journal of Bioassays

Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

International Journal of Bioassays is a member of the Publishers International Linking Association, Inc. (PILA), CROSSREF and CROSSMARK (USA). Digital Object Identifier (DOI) will be assigned to all its published content.