St. John Fisher College, Wegmans School of Pharmacy, 3690 East Avenue, Rochester, NY 14618, USA.
Drug Dev Ind Pharm. 2013 Jul;39(7):1113-25. doi: 10.3109/03639045.2012.714786. Epub 2012 Sep 20.
Ammonio methacrylate copolymers Eudragit(®) RS PO and Eudragit® RL PO have found widespread use as key components in various types of extended release solid dosage forms. The deformation behavior of neat polymers and binary mixes was evaluated using Heckel Analysis, strain rate sensitivity, work of compaction and elastic recovery index. Additionally, the compact forming ability of neat materials and binary mixes were evaluated by analyzing their tabletability, compressibility and compactibility profiles. The Heckel analysis of both polymers exhibited a speed-sensitive deformation behavior typical to plastic materials. The yield values of the binary mixes of the polymers with microcrystalline cellulose revealed a linear relationship with the weight fractions of individual components. The yield values of binary mixes of both the polymers with dibasic calcium phosphate exhibited slight negative deviations from linearity. Both polymers exhibited axial relaxation after ejection typical of viscoelastic materials, as measured by the elastic recovery index values. The work of compaction and the elastic recovery index values of the binary mixtures were found to be linearly related to the weight fractions of the individual components thus, confirming ideal mixing behavior based on the composition. Addition of microcrystalline cellulose to both polymers significantly improved their tabletability and compactibility. The tensile strengths of the compacts prepared with neat materials and binary mixes with microcrystalline cellulose, dibasic calcium phosphate and lactose were the function of their solid fraction and independent of the tableting speeds tested; thus, validating compactibility as a reliable parameter in predicting acceptable tablet properties.
氨甲基丙烯酸酯共聚物 Eudragit(®) RS PO 和 Eudragit® RL PO 已广泛用作各种类型的延长释放固体制剂的关键成分。使用 Heckel 分析、应变速率敏感性、压缩功和弹性回复指数评估了纯聚合物和二元混合物的变形行为。此外,通过分析其可压性、可压缩性和压缩性曲线来评估纯材料和二元混合物的压缩成型能力。两种聚合物的 Heckel 分析均表现出典型的塑料材料的速度敏感变形行为。聚合物与微晶纤维素的二元混合物的屈服值与各组分的重量分数呈线性关系。聚合物与磷酸氢钙的二元混合物的屈服值与线性略有负偏差。两种聚合物在推出后均表现出轴向松弛,这是粘弹性材料的典型特征,通过弹性回复指数值来测量。发现压缩功和二元混合物的弹性回复指数值与各组分的重量分数呈线性关系,因此基于组成证实了理想的混合行为。向两种聚合物中添加微晶纤维素可显著提高其可压性和可压缩性。使用纯材料和与微晶纤维素、磷酸氢钙和乳糖的二元混合物制备的压块的拉伸强度是其固体分数的函数,并且与测试的压片速度无关;因此,将可压缩性作为预测可接受片剂性能的可靠参数进行了验证。