Research Scholar, Faculty of Pharmacy, Dharmsinh Desai University, Nadiad, Gujarat, India.
Assistant Professor, Department of Pharmacology, Laxminarayan Dev College of Pharmacy, Bharuch, Gujarat, India.
Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2024 Jun 12;40:e20240002. doi: 10.62958/j.cjap.2024.002.
Raloxifene hydrochloride (RLX) is used extensively in the treatment of osteoporosis, only 2% of RLX's bioavailability remains after a significant first pass metabolism. Besides coming from BCS class II, RLX is not very soluble in water. Thus, the goal of the current study was to improve RLX solubility by creating an inclusion complex using β cyclodextrin (β-CD) as a carrier and solid dispersion with Poloxamer 407.
Inclusion complex and solid dispersion were made using a variety of techniques, including kneading, co-precipitation, and physical mixing and solid dispersion using different drug to carrier ratios (1:1, 1:2 and 1:3).
Inclusion complex made using the co-precipitation method had shown 9-fold improvements in water solubility when compared with plain RLX. In order to assess the optimized complex's compatibility, thermal analysis, and crystallinity, X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy were used. The XRD and DSC study's results indicated that RLX changed from a crystalline to an amorphous state. IC-6 exhibits effective water solubility based on the outcome. However, upon comparison of the two techniques, the β-CD complexation method shown an impressive rise in drug solubility when compared to solid dispersion.
盐酸雷洛昔芬（RLX）广泛用于治疗骨质疏松症，其生物利用度在经过显著的首过代谢后仅保留 2%。除了属于 BCS 分类 II 类药物外，RLX 在水中的溶解度也不是很高。因此，目前的研究目标是通过使用β-环糊精（β-CD）作为载体形成包合物，并与泊洛沙姆 407 形成固体分散体来提高 RLX 的溶解度。
使用多种技术包括捏合、共沉淀和物理混合以及不同药物与载体比例（1:1、1:2 和 1:3）的固体分散体来制备包合物和固体分散体。
与普通 RLX 相比，通过共沉淀法制备的包合物的水溶性提高了 9 倍。为了评估优化复合物的相容性，使用热分析、X 射线衍射、差示扫描量热法和傅里叶变换红外光谱进行了评估。XRD 和 DSC 研究结果表明，RLX 从结晶态转变为无定形态。IC-6 的结果表明具有有效的水溶性。然而，通过比较这两种技术，β-CD 包合方法显示出药物溶解度的显著提高，而固体分散体则不然。
