Maremanda Vishnu Datta, Maertin Dirk, Bitar Malak, Pandey Abhijeet
Formulation Research and Development, Global Drug Development/Technical Research and Development, Novartis Healthcare Pvt. Ltd., Genome Valley, Hyderabad, 500101, India.
Material Science, Global Drug Development/Technical Research and Development, 4056, Novartis, Basel, Switzerland.
AAPS PharmSciTech. 2024 Feb 29;25(3):50. doi: 10.1208/s12249-024-02773-2.
The advancement in the formulation and characterization techniques have paved the path for development of new as well as modification of existing dosage forms. The present work explores the role of micro-computed tomography (micro-CT) as advanced characterization technique for multi-layered-coated pellets to ascertain the quality of coated pellets. The work further explored in-house e-tongue technique for understanding palatability of formulation in early stages of development thus by reducing clinical taste evaluation time. The developed multi-layered-coated pellets were characterized using microscopy (optical and electron microscopy). The obtained results demonstrated formation of spherical-shaped pellets with uniform coating. The uniform coating was further confirmed by results obtained from scanning electron microscopy (SEM) and cross-sectional SEM analysis, which showed visible difference in pellet surface before and after multi-layered coating. The micro-CT results confirmed the visible demarcation of layers (drug and polymer, i.e., hydroxypropyl methylcellulose (HPMC) and eudragit (EPO)) along with uniform thickness of various layering. The dissolution study of developed pellets suggested the role of layering EPO on drug release from pellets. The e-tongue analysis proved to be an excellent tool for early prediction of taste masking of drug via multi-layered pellets and can serve as potential platform for taste masking with high specificity. The overall results suggest the suitability of developed multi-layered platform as efficient dosage form (sprinkle) in pediatric/geriatric product development.
制剂和表征技术的进步为新剂型的开发以及现有剂型的改进铺平了道路。本研究探讨了微计算机断层扫描（micro-CT）作为多层包衣微丸先进表征技术在确定包衣微丸质量方面的作用。该研究还进一步探索了内部电子舌技术，以在开发早期阶段了解制剂的适口性，从而缩短临床口味评估时间。使用显微镜（光学显微镜和电子显微镜）对所制备的多层包衣微丸进行表征。所得结果表明形成了具有均匀包衣的球形微丸。扫描电子显微镜（SEM）和横截面SEM分析结果进一步证实了包衣的均匀性，其显示了多层包衣前后微丸表面的明显差异。微CT结果证实了各层（药物和聚合物，即羟丙基甲基纤维素（HPMC）和丙烯酸树脂（EPO））之间有明显的界限以及各层的厚度均匀。所制备微丸的溶出度研究表明EPO层对微丸中药物释放的作用。电子舌分析被证明是通过多层微丸早期预测药物掩味效果的优秀工具，并且可以作为具有高特异性的掩味潜在平台。总体结果表明所开发的多层平台作为儿科/老年产品开发中的有效剂型（散剂）是合适的。
