Wardhana Yoga Windhu, Soewandhi Sundani N, Wikarsa Saleh, Suendo Veinardi
Department of Pharmaceutics, School of Pharmacy, Institute Technology of Bandung, Bandugn, Indonesia / Department of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, University of Padjadjaran, Bandung, Indonesia.
Department of Pharmaceutics, School of Pharmacy, Institute Technology of Bandung, Bandugn, Indonesia.
Pak J Pharm Sci. 2019 May;32(3):981-986.
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 n-heptane. All of the crystal modification resulted were characterized by a polarization light microscopy (PLM), Fourier-Transform 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.
药物化合物中存在的多晶型现象会影响其物理化学性质和治疗目标。因此，应评估不同晶型的质量，特别是多晶型之间的溶解度和溶解行为，这些与生物利用度和治疗效果相关。为了获得不同的多晶型，使用了各种溶剂，如乙腈、甲醇、乙酸乙酯、丙酮、水、正己烷和正庚烷。所有得到的晶体改性产物都通过偏光显微镜（PLM）、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和粉末X射线衍射（PXRD）进行了表征。此外，还进行了在水中的溶解度（24小时和48小时测试时间）和颗粒溶解曲线（1小时测试）。成功得到了多种多晶型，它们在形态、明确的光谱指纹、晶体结构和热行为方面存在显著差异。从样品的溶解度来看，溶解度最高的前三种晶型分别是晶型6、2和3。但在60分钟溶解后，它们的表现顺序相反（分别为晶型3、2和6）。通过溶剂处理成功获得了依非韦伦的多晶型。因此，在剂型预配方方法中应仔细考虑活性药物成分（API）多晶型的物理化学性质。
