Tho T, Kleinebudde P, Sande S A
Department of Pharmaceutics, School of Pharmacy, University of Oslo, Norway.
AAPS PharmSciTech. 2001 Dec 1;2(4):26. doi: 10.1208/pt020426.
This study investigated the possibility of producing pectin-based pellets by extrusion/spheronization. The study also identified factors influencing the process and the characteristics of the resulting product. Three types of pectin with different degrees of amid and methoxyl substitution were studied in combination with different granulation liquids (water, calcium chloride, citric acid, and ethanol) and/or microcrystalline cellulose. Pellets were prepared in a power-consumption-controlled, twin-screw extruder; then they were spheronized and dried. The products were characterized by image analysis, sieving analysis, and disintegration and dissolution tests. The results were evaluated by multivariate analysis. Different additives, either in the granulation liquid or in the powder mixture, influenced the ability of the extruded mass to form pellets (the processability) with this technique. However, the various pectin types responded to modifications to a different extent. Short, nearly spherical pellets are obtained with granulation liquids, such as ethanol, that reduce the swelling ability of pectin. Pellets produced with ethanol are, however, mechanically weak and tend to disintegrate. Pectin molecules with a high degree of free carboxylic acid groups seem to be more sensitive to changes in the granulation liquid. Addition of microcrystalline cellulose as an extrusion aid generally resulted in improvements in shape and size. It was demonstrated that the processability of pectin as well as the characteristics of the products can be influenced in different ways during the process (eg, adding substances to the granulation liquid or to the powder mixture).
本研究探讨了通过挤出/滚圆法制备果胶基微丸的可能性。该研究还确定了影响该过程的因素以及所得产品的特性。研究了三种不同酰胺化和甲氧基取代度的果胶，并将其与不同的制粒液体（水、氯化钙、柠檬酸和乙醇）和/或微晶纤维素结合使用。微丸在功率控制的双螺杆挤出机中制备；然后进行滚圆和干燥。通过图像分析、筛分分析以及崩解和溶出试验对产品进行表征。结果通过多变量分析进行评估。制粒液体或粉末混合物中的不同添加剂会影响挤出物料用该技术形成微丸的能力（加工性能）。然而，不同类型的果胶对改性的反应程度不同。使用能降低果胶溶胀能力的制粒液体（如乙醇）可获得短的、近乎球形的微丸。然而，用乙醇制备的微丸机械强度较弱，容易崩解。具有高度游离羧酸基团的果胶分子似乎对制粒液体的变化更敏感。添加微晶纤维素作为挤出助剂通常会改善微丸的形状和尺寸。结果表明，在该过程中（例如，向制粒液体或粉末混合物中添加物质），果胶的加工性能以及产品的特性可以受到不同方式的影响。
