Arginine Complexes with Simvastatin: Apparent Solubility, In Vitro Dissolution and Solid State Characterization.
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.
['Affandi|Meor Mohd Redzuan Meor Mohd|MMRMM|', 'Tripathy|Minaketan|M|', 'Majeed|Abu Bakar Abdul|ABA|']
D001120:Arginine D002152:Calorimetry, Differential Scanning D006863:Hydrogen-Ion Concentration D008855:Microscopy, Electron, Scanning D033362:Powder Diffraction D019821:Simvastatin D012995:Solubility D013696:Temperature D014867:Water
arginine complexes simvastatin Solubility dissolution solid state X-Ray powder defractometric