Joneja S K, Harcum W W, Skinner G W, Barnum P E, Guo J H
Hercules Incorporated, Wilmington, DE 19808-1599, USA.
Drug Dev Ind Pharm. 1999 Oct;25(10):1129-35. doi: 10.1081/ddc-100102279.
For solid dosage forms, a better understanding of the fundamental properties of the binders helps in developing better formulations and products. The objective of this study was to determine the effects of binder toughness and plastic flow on tablet hardness, friability, and capping. The characteristic of binder toughness was determined, and the correlation between the ejection force of the tablet and the toughness of the binder was established. Evaluation was conducted using acetaminophen tablets with different kinds of binders (i.e., hydroxypropylcellulose, methylcellulose [MC], povidone [PVP], starch, etc.). A rotary tablet press was used for tableting at three different speeds. The properties of binders and acetaminophen tablets were determined using a diametral compression test. The toughness was measured as the curve of the area under the load versus deflection. The microbehavior of these binders was also studied. The acetaminophen tablets with the binders were subjected to predetermined loads and then examined under a scanning electron microscope. The tablets that contained hydroxypropylcellulose as a binder showed the highest toughness and had the lowest ejection force. The ejection force of tablets decreased with increasing concentrations of hydroxypropylcellulose in the dosage forms. The tablets that contained other binders failed by capping and random cracking in the middle. These results show that hydroxypropylcellulose, a thermoplastic polymer, provides the best physical characteristics for the tablets. This effect could help in improving tablet manufacturing conditions (e.g., compression force and speed).
对于固体制剂,更好地了解粘合剂的基本特性有助于开发更好的制剂和产品。本研究的目的是确定粘合剂韧性和塑性流动对片剂硬度、脆碎度和裂片的影响。测定了粘合剂韧性的特征,并建立了片剂顶出力与粘合剂韧性之间的相关性。使用含有不同种类粘合剂(即羟丙基纤维素、甲基纤维素[MC]、聚维酮[PVP]、淀粉等)的对乙酰氨基酚片进行评估。使用旋转式压片机以三种不同速度进行压片。使用径向压缩试验测定粘合剂和对乙酰氨基酚片的性能。韧性通过载荷与挠度曲线下的面积来测量。还研究了这些粘合剂的微观行为。对含有粘合剂的对乙酰氨基酚片施加预定载荷,然后在扫描电子显微镜下检查。含有羟丙基纤维素作为粘合剂的片剂显示出最高的韧性,并且顶出力最低。剂型中羟丙基纤维素浓度增加时,片剂的顶出力降低。含有其他粘合剂的片剂因裂片和中间随机开裂而失败。这些结果表明,热塑性聚合物羟丙基纤维素为片剂提供了最佳的物理特性。这种效果有助于改善片剂制造条件(例如,压力和速度)。