Abstract
POLYMORPHISM OF SIMVASTATIN: AN EFFORT TO REPAIR SOLUBILITY AND DISSOLUTION RATE
Iyan Sopyan*, Thachaiyini Pallanisamy and Yoga Windhu Wardhana
ABSTRACT
Objective: Simvastatin (SV) is most commonly used as a hypercholesterolemia drug, although it is poorly soluble in water and poorly absorbed by the gastrointestinal tract and has a bioavailability approaching 5%. This study tried to improve the solubility and dissolution rate of simvastatin through the evaporation solvent method. Methods: The evaporation solvent method has used the variation of solvent purification (recrystallization) of simvastatin compound. A difference of solvent would be formedsimvastatin a different crystal habit after being recrystallized. This study used a variation of equimolar mixed solvent methanol: ethanol (B), methanol: chloroform (C), and ethanol: chloroform (D). A Crystals that obtained from the purification are characterized by a solubility test, powder x-ray diffraction, and Fourier transforms infrared spectroscopy. Results: Powder X-ray diffraction results showed a significant difference compared to the diffractogram standard simvastatin, while the results of Fourier infrared spectroscopy transform showed no significant difference. Solubility test results obtained by an increase in solubility compared with the standard initial simvastatin (A). The dissolution test results showed an increase in dissolution rate at pH 1.2, 4.5, and 6.8 significantly compared to the standard simvastatin. Conclusion: Crystal modification using recrystallized by a mixture of solvents represented the modification results showed an increase in the solubility and dissolution test.
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