Polymorphic properties and dissolution profile of efavirenz due to solvents recrystallization

Abstract

Polymorphism occurs in pharmaceutical compounds affect to the physicochemical quality and goal of therapy. Thus, quality evaluation of different crystal forms should be assessed especially the solubility and dissolution behaviors among polymorphic forms, which correlate to bioavailability and therapy efficacy. To achieved the different of a polymorph various solvent were used such as acetonitrile, methanol, ethyl acetate, acetone, water, n-hexane, and nheptane. All of the crystal modification resulted were characterized by a polarization light microscopy (PLM), FourierTransform Infrared (FTIR) differential scanning calorimetry (DSC) and powdered X-ray diffraction (PXRD). Besides that, nature of solubility in water (24 and 48 hours test times) and particulate dissolution profile (an hour test) were carried out. There were various polymorphs success resulted and have significant differences in morphology, definite spectral fingerprints, crystal structure and thermal behavior. From the solubility of the samples found the top three highest soluble forms i.e. Form 6, 2 and 3, respectively. But there are showed became in order reverse performance after 60 minutes dissolution (Form 3, 2 and 6, respectively). The polymorphic forms of EFV were successful to obtained by the solvents treatment. Therefore, the physicochemical properties of polymorphic forms from active pharmaceutical ingredients (APIs) should be carefully considered in dosage forms pre-formulation approaches.