Busignies V, Leclerc B, Porion P, Evesque P, Couarraze G, Tchoreloff P
Centre d'études Pharmaceutiques de l'Université Paris XI, France.
Eur J Pharm Biopharm. 2006 Aug;64(1):66-74. doi: 10.1016/j.ejpb.2006.03.004. Epub 2006 May 11.
The compressibility of three pharmaceutical excipients (microcrystalline cellulose, lactose and anhydrous calcium phosphate) and their binary mixtures was studied. The aim of this work was to observe the impact of the mass composition of the mixture on the compressibility. The single-compound materials and their mixtures were compacted using instrumented presses. It allowed obtaining compression cycles (i.e., force-displacement curves) which were associated with energy measurements (specific compaction energy, Esp cp and specific expansion energy, Esp exp). It was observed that for the mixtures studied, the change of Esp cp with the mass composition could be fitted using a linear relationship (it was not the case with Esp exp). A linear relationship between the porosity of mixture's compacts and the mass composition was also obtained. Heckel's plots were then obtained for the three excipients and the mixtures. The mean yield pressure was calculated with the "in-die-method" and the "out-of-die method". A proportional relationship was not valid for the mean yield pressures. But, a predictive approach was proposed in order to obtain indirectly the mean yield pressure of a binary mixture if the data of the single materials were known. It used the linear mixing rule observed with the porosity. The validity was verified and compared with the experimental values. This comparison showed that it was possible to predict the mean yield pressure of binary mixtures from the accessible data of the single excipients.
研究了三种药用辅料（微晶纤维素、乳糖和无水磷酸钙）及其二元混合物的可压缩性。这项工作的目的是观察混合物的质量组成对可压缩性的影响。使用仪器化压力机对单一化合物材料及其混合物进行压实。由此获得了与能量测量（比压实能，Esp cp和比膨胀能，Esp exp）相关的压缩循环（即力-位移曲线）。观察到，对于所研究的混合物，Esp cp随质量组成的变化可以用线性关系拟合（Esp exp情况并非如此）。还获得了混合物压块的孔隙率与质量组成之间的线性关系。然后得到了三种辅料及其混合物的Heckel图。用“模内法”和“模外法”计算平均屈服压力。平均屈服压力不成比例关系。但是，如果已知单一材料的数据，提出了一种预测方法以间接获得二元混合物的平均屈服压力。它使用了孔隙率观察到的线性混合规则。验证了其有效性并与实验值进行了比较。该比较表明，可以从单一辅料的可获取数据预测二元混合物的平均屈服压力。
