Jonat S, Hasenzahl S, Gray A, Schmidt P C
Department of Pharmaceutical Technology, University of Tübingen, Tübingen, Germany.
Drug Dev Ind Pharm. 2005 Aug;31(7):687-96. doi: 10.1080/03639040500216451.
The effect of noncompacted and compacted hydrophilic as well as hydrophobic colloidal silicon dioxide (CSD) on tableting properties of three different pharmaceutical excipients used for direct compression, namely, Avicel PH 101, Starch 1500, and Tablettose 80, was investigated. Binary powder mixtures containing 0.5% CSD and 99.5% excipient were compressed on an instrumented single-punch tablet press, and the radial tensile strength/compaction load profiles were examined. The Ryshkewitch-Duckworth relationship shows that the influence of CSD on tablet strength was dependent on the hydrophobic and hydrophilic nature of the CSD and on the compaction characteristics of the excipients. Tablets from each excipient with and without CSDs were subjected to different levels of relative humidity at 20 degrees C for 7 days. The sorption isotherms and the radial tensile strengths of the tablets after the storage period showed that neither hydrophilic nor hydrophobic CSD influenced the tablet properties of Avicel PH 101, Starch 1500, and Tablettose 80. Moreover, ternary powder mixtures containing magnesium stearate as a third component were compressed in order to study the influence of CSD on the deleterious effect of magnesium stearate on the interparticle bonding. The radial tensile strength/compaction load profiles and the residual and ejection forces of tablets made from ternary mixtures showed that CSD eliminated the negative effect of magnesium stearate on interparticle bonding while maintaining the lubrication action, in a manner that was affected by its hydrophobicity/hydrophilicity and by the particle deformation properties of the excipient upon compression.
研究了未压实和压实的亲水性以及疏水性胶体二氧化硅（CSD）对三种用于直接压片的不同药用辅料（即微晶纤维素PH 101、淀粉1500和乳糖80）压片性能的影响。将含有0.5% CSD和99.5%辅料的二元粉末混合物在单冲压片机上进行压制，并检查径向拉伸强度/压实载荷曲线。Ryshkewitch-Duckworth关系表明，CSD对片剂强度的影响取决于CSD的疏水和亲水性质以及辅料的压实特性。将添加和未添加CSD的每种辅料制成的片剂在20℃下置于不同水平的相对湿度环境中7天。储存期后的吸附等温线和片剂的径向拉伸强度表明，亲水性和疏水性CSD均未影响微晶纤维素PH 101、淀粉1500和乳糖80的片剂性能。此外，为了研究CSD对硬脂酸镁对颗粒间结合的有害影响，还压制了含有硬脂酸镁作为第三成分的三元粉末混合物。由三元混合物制成的片剂的径向拉伸强度/压实载荷曲线以及残余力和顶出力表明，CSD消除了硬脂酸镁对颗粒间结合的负面影响，同时保持了润滑作用，其方式受其疏水性/亲水性以及辅料在压缩时的颗粒变形特性影响。
