Čierna Martina, Mučaji Pavel, Špaglová Miroslava, Čuchorová Mária, Macho Oliver
Department of Galenic Pharmacy, Faculty of Pharmacy, Comenius University Bratislava, 832 32 Bratislava, Slovakia.
Department of Pharmacognosy and Botany, Faculty of Pharmacy, Comenius University Bratislava, 832 32 Bratislava, Slovakia.
Polymers (Basel). 2022 Jul 11;14(14):2822. doi: 10.3390/polym14142822.
This study aimed to prepare and evaluate pellets containing acyclovir as a model drug. Pellets were prepared by the extrusion-spheronization process. Aqueous solutions of natural marine polymers (sodium alginate, chitosan) were compared to semi-synthetic hydroxypropyl methylcellulose (HPMC) in the role of binders. The study focused on the characterization of the pellet properties that are crucial for the formulation of the final dosage form, such as in multi-unit pellet system (MUPS) tablets or hard gelatin capsules filled with the pellets. Finally, the mentioned dosage forms were tested for drug dissolution. The morphology of pellets observed by scanning electron microscopy correlated with the shape evaluation performed by dynamic image analysis. Sodium alginate pellets exhibited the lowest value of sphericity (0.93), and many elongated rods and dumbbells were observed in this batch. Chitosan pellets had the highest value of sphericity (0.97) and were also less rough on the surface. The pellets maintained a constant surface geometry during the dissolution studies; they only reduced in size. The most significant reduction in size and weight was assessed after 2 h of dissolution testing. This fact was in line with the drug release from pellets in capsules or MUPS tablets, which was massive during the first hour, in both cases. The dissolution profiles of all of the batches were comparable.
本研究旨在制备并评价以阿昔洛韦为模型药物的微丸。微丸通过挤出滚圆法制备。将天然海洋聚合物（海藻酸钠、壳聚糖）的水溶液与半合成羟丙基甲基纤维素（HPMC）作为黏合剂的作用进行了比较。该研究聚焦于对最终剂型（如多单元微丸系统（MUPS）片剂或填充微丸的硬明胶胶囊）的制剂至关重要的微丸性质的表征。最后，对上述剂型进行了药物溶出度测试。通过扫描电子显微镜观察到的微丸形态与通过动态图像分析进行的形状评估相关。海藻酸钠微丸的球形度值最低（0.93），且在该批次中观察到许多细长棒状和哑铃状微丸。壳聚糖微丸的球形度值最高（0.97），且表面也较光滑。在溶出度研究过程中，微丸保持恒定的表面几何形状；它们只是尺寸减小。在溶出度测试2小时后评估出尺寸和重量的最大减小。这一事实与胶囊或MUPS片剂中微丸的药物释放情况一致，在这两种情况下，药物在第一小时内大量释放。所有批次的溶出曲线具有可比性。
