Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh, Egypt.
Faculty of Pharmacy, Tanta University, Tanta, Egypt.
Pharm Dev Technol. 2021 Jul;26(6):693-700. doi: 10.1080/10837450.2021.1922441. Epub 2021 May 6.
Apigenin is a natural flavonoid which is claimed to have many pharmacological activities ranging from simple anti-inflammatory to anticancer action. However, poor dissolution slowed the advancement of this drug through the development pipelines. The objective of this work was to probe ethanol-aided kneading of apigenin with arginine as a new strategy for enhanced dissolution rate. The work was extended to develop rapidly disintegrating tablets of apigenin. Apigenin was mixed with increasing molar ratios of arginine before ethanol-aided kneading. The resulting products were examined using Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction in addition to probing the dissolution characteristics of apigenin. The analytical techniques highlighted the existence of new crystalline species with a possibility of salt formation. The recorded alterations in the crystalline properties were associated with a significant enhancement in the dissolution rate of apigenin. The presence of arginine did not have any negative effect of the cytotoxic power of apigenin. Optimum formulation was successfully prepared as rapidly disintegrating tablets which showed fast liberation of apigenin. The study introduced arginine as a potential excipient for enhanced dissolution of apigenin after ethanol-assisted kneading.
芹菜素是一种天然类黄酮，据称具有许多药理学活性，从简单的抗炎作用到抗癌作用。然而，较差的溶解性减缓了该药物在开发管道中的进展。本工作的目的是探讨乙醇辅助揉捏与精氨酸结合作为提高溶解速率的新策略。工作扩展到开发迅速崩解的芹菜素片剂。在乙醇辅助揉捏之前，将芹菜素与精氨酸的摩尔比逐渐增加混合。使用傅里叶变换红外光谱、差示扫描量热法和 X 射线衍射对所得产物进行了检查，此外还研究了芹菜素的溶解特性。分析技术强调了存在具有盐形成可能性的新晶型。记录的晶体性质的变化与芹菜素溶解速率的显著提高有关。精氨酸的存在对芹菜素的细胞毒性没有任何负面影响。成功地制备了作为迅速崩解片剂的最佳配方，其显示出芹菜素的快速释放。该研究引入了精氨酸作为乙醇辅助捏合后提高芹菜素溶解度的潜在赋形剂。
