Abstract
Objective: This study aimed to enhance the solubility of simvastatin using noncovalent derivatives (NCDs) with oxalic acid (OA), fumaric acid (AF), and nicotinamide (NK) as conformers.
 Methods: NCDs were prepared using by a solvent drop grinding (SDG). The NCDs formed were evaluated for saturated solubility test, NCDs with the highest saturation solubility were then characterized by Fourier transform infrared spectrophotometry (FT-IR), differential scanning calorimeter (DSC), powder x-ray diffractometry (PXRD) and the particulate dissolution using type II of USP test.
 Results: SV-OA NCDs showed the highest solubility; thus NCDS of SV-OA were characterized by X-ray diffraction showing a new peak at 2ϴ = 28.96 °C and differential scanning calorimeter showed a change of endothermic peak from 134.3 °C to 69 °C. Infrared spectroscopy indicated that there were no functional group changes from simvastatin, while the dissolution rate increased from 68.22% to 76.08%.
 Conclusion: SV-OA NCDs show an increased profile of solubility and dissolution compared to pure simvastatin.
Highlights
Biological availability is a rate value and the quantity of the drug that reaches the blood circulation
Based on the results of the Scandinavian Simvastatin Survival Study (4S) and The Heart Protect Study (HPS), simvastatin can reduce the incidence of ischemic stroke, myocardial infarction, and death in cardiovascular patients with atherosclerosis and hypercholesterolemia [3]
The equivalent to 20 mg simvastatin was dissolved with 10 ml aquades in an Erlenmeyer, placed in a mechanical agitator for 48 h at room temperature (25 °C) and the saturated solubility was measured by UV spectrophotometry in the wavelength range of 247–257 nm [6]
Summary
Biological availability is a rate value and the quantity of the drug that reaches the blood circulation. Solubility is an important factor in predicting the bioavailability of drugs in blood circulation. Drugs that have poor solubility in water show low bioavailability, so the dissolution rate is the rate-limiting step in the absorption process of drugs in the body. The solubility of a drug is related to its physicochemical properties [1, 2]. Simvastatin is a drug that inhibits the action of the HMG-CoA reductase enzyme, thereby helping to reduce cholesterol levels in the blood. Based on the results of the Scandinavian Simvastatin Survival Study (4S) and The Heart Protect Study (HPS), simvastatin can reduce the incidence of ischemic stroke, myocardial infarction, and death in cardiovascular patients with atherosclerosis and hypercholesterolemia [3]
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