Madan Jyotsana R, Pawar Akshaya R, Patil Rajesh B, Awasthi Rajendra, Dua Kamal
Department of Pharmaceutics, Smt. Kashibai Navale College of Pharmacy, Savitribai Phule Pune University, India.
Amity Institute of Pharmacy, Amity University, Noida, India.
Polim Med. 2018 Jan-Jun;48(1):17-24. doi: 10.17219/pim/99801.
Solid dispersions are among the techniques successfully employed to enhance the dissolution of poorly water-soluble drugs. Microwave (MW)-assisted evaporative crystallization has been used to prepare solid dispersions of drugs and polymers.
The aim of the study was to investigate the solubility of apremilast (APM) in water by exploring the effect of MW-assisted solid dispersion technology.
In the present study, solid dispersions of APM, a poorly water-soluble drug, were prepared. The solid dispersions were prepared using the conventional method (CM) and the MW-based solvent evaporation technique. Microwave energy was used to enhance the solubility and dissolution rate of APM. The physical mixture and solid dispersions were characterized using Fourier-transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Apremilast tablets containing MW-assisted solid dispersions were prepared by the direct compression technique and compared with the marketed formulation (Aprezo tablets).
The results obtained confirmed the conversion of crystalline APM to an amorphous form. The XRPD pattern of the MW-assisted formulation at a 2:1 ratio suggests the amorphous structure of APM within the formulation. Based on solubility studies results, Syloid® 244FP was selected as the best carrier. The dissolution study results suggested that the APM tablet prepared using MW-assisted solid dispersions at a 2:1 carrier/drug ratio improved the APM dissolution rate compared to the marketed formulation.
Based on the results, it can be concluded that the MW-assisted solid dispersion technique may be an effective approach to enhancing the dissolution profile of other poorly water-soluble drugs.
固体分散体是成功用于提高难溶性药物溶出度的技术之一。微波（MW）辅助蒸发结晶已被用于制备药物与聚合物的固体分散体。
本研究旨在通过探索MW辅助固体分散技术的效果来研究阿普米拉斯（APM）在水中的溶解度。
在本研究中，制备了难溶性药物APM的固体分散体。采用常规方法（CM）和基于MW的溶剂蒸发技术制备固体分散体。利用微波能量提高APM的溶解度和溶出速率。使用傅里叶变换红外光谱（FTIR）、X射线粉末衍射（XRPD）、差示扫描量热法（DSC）和扫描电子显微镜（SEM）对物理混合物和固体分散体进行表征。采用直接压片技术制备了含有MW辅助固体分散体的阿普米拉斯片剂，并与市售制剂（Aprezo片剂）进行比较。
所得结果证实了结晶态APM转变为无定形形式。MW辅助制剂在2:1比例下的XRPD图谱表明制剂中APM为无定形结构。基于溶解度研究结果，选择Syloid® 244FP作为最佳载体。溶出度研究结果表明，与市售制剂相比，以2:1载体/药物比例使用MW辅助固体分散体制备的APM片剂提高了APM的溶出速率。
基于这些结果，可以得出结论，MW辅助固体分散技术可能是提高其他难溶性药物溶出度的有效方法。
