Pharmaceutical Sciences Department, University of Perugia, via del Liceo 1, 06123 Perugia, Italy.
Pharmaceutical Sciences Department, University of Perugia, via del Liceo 1, 06123 Perugia, Italy.
Int J Pharm. 2020 Nov 15;589:119860. doi: 10.1016/j.ijpharm.2020.119860. Epub 2020 Sep 7.
Carbamazepine (CBZ) is a poorly water soluble drug owing to the Biopharmaceutic Classification System (BCS) class II. It is characterized by a variable bioavailability and by the presence of different polymorphs. In this paper the effects of CaCO on the physicochemical properties of CBZ and its solubility and release were evaluated. CaCO is a naturally non-toxic biomineral and was chosen because it is a safe, cheap and eco-friendly excipient able to dissolve in an acidic environment. Composites with different CBZ loadings were prepared by ball milling and antisolvent method. The composites were characterized by X-ray powder diffraction, differential scanning calorimetry analysis and attenuated total reflectance FT-IR which revealed that both the presence of CaCO and the preparation procedure affect the polymorphic form crystallinity and intermolecular interactions among the drug molecules. Scanning electron microscopy showed that small drug crystals with different crystalline forms were deposited on the surface of the CaCO particles. Solubility and dissolution tests showed an increase in the apparent solubility of CBZ and improved drug release. These results demonstrated that CaCO affected the drug release properties likely due to its pH-sensitive characteristics.
卡马西平（CBZ）由于生物药剂学分类系统（BCS）类别 II，水溶性较差。它的特点是生物利用度可变，存在不同的多晶型。本文研究了 CaCO 对 CBZ 的物理化学性质及其溶解度和释放的影响。CaCO 是一种天然无毒的生物矿物质，因其安全、廉价且环保，能在酸性环境中溶解，而被选为赋形剂。通过球磨和反溶剂法制备了不同 CBZ 负载的复合材料。通过 X 射线粉末衍射、差示扫描量热分析和衰减全反射傅里叶变换红外光谱对复合材料进行了表征，结果表明 CaCO 的存在和制备过程都会影响药物分子的多晶型、结晶度和分子间相互作用。扫描电子显微镜显示，不同结晶形式的小药物晶体沉积在 CaCO 颗粒表面。溶解度和溶出度试验表明，CBZ 的表观溶解度增加，药物释放得到改善。这些结果表明，CaCO 可能由于其 pH 敏感性而影响药物释放特性。
