Arginine Complexes with Simvastatin: Apparent Solubility, In Vitro Dissolution and Solid State Characterization

Author(s): Meor Mohd Redzuan Meor Mohd Affandi , Minaketan Tripathy* , Abu Bakar Abdul Majeed .

Journal Name: Current Drug Delivery

Volume 15 , Issue 1 , 2018

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Graphical Abstract:


Background: Categorized as a Biopharmaceutics Classification System (BCS) Class II drugs, statin exhibit low aqueous solubility and bioavailability thus presenting an obstacle and great challenge to formulation researchers. This paper describes a de novo approach to enhance the aqueous solubility of one of the most commonly prescribed statins i.e., simvastatin (SMV) by forming a complex (SMV-ARG) with cosolute arginine (ARG).

Methods: The complex has been characterized for its apparent solubility and in vitro dissolution. The solid state characterization has been carried out using Fourier Transform Infra-Red (FTIR) Spectroscopy, Elemental Analysis, X-Ray Powder Diffraction (XRD), Differential Scanning Calorimetry (DSC) analysis, Thermal Gravimetric Analysis (TGA) and Scanning Electron Microscopy (SEM).

Results: Simvastatin-Arginine (SMV-ARG) complex exhibited massive solubility enhancement by 12,000 fold and significant improvement in both acidic and alkaline dissolution media. A conversion of coherent crystalline to non-coherent pattern, and certain extent of amorphization in SMV-ARG complex, fully justifies the enhanced solubility, and hence the dissolution profile.

Conclusion: The present study provides a significant evidence that ARG molecules are capable to form a complex with small molecules and increase their aqueous solubility which prove to be beneficial in drug formulation and development.

Keywords: Solubility, dissolution, solid state, X-Ray powder defractometric, arginine complexes, simvastatin.

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Article Details

Year: 2018
Page: [77 - 86]
Pages: 10
DOI: 10.2174/1567201814666170320144259

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