Sun C, Grant D J
Department of Pharmaceutics, University of Minnesota, Minneapolis 55455-0343, USA.
Pharm Res. 2001 Mar;18(3):281-6. doi: 10.1023/a:1011090510875.
To examine the effects of salt form, i.e., different anions with a common cation (L-lysinium), on compaction properties and to identify the factors that determine the tensile strength of tablets.
L-Lysine salts with the following anions were compressed at various pressures: acetate, monochloride, dichloride, L-aspartate, L-glutamate (dihydrate), and L-lysine (zwitterionic monohydrate). The yield strength of each salt was evaluated from the "out-of-die" Heckel plot.
At low compaction pressures, the tensile strength of the compacts increases linearly with increasing compaction pressure. Simultaneously. the compact tensile strength decreases exponentially with increasing yield strength of the salt. However, at high compaction pressures, the compact tensile strength is determined by the interparticulate bonding strength and not by the yield strength. The compact tensile strength, extrapolated to zero porosity, increases linearly with increasing melting temperature of the salts.
The counterion affects the tableting properties of L-lysine salts. The tensile strength is controlled by both the yield strength and the interparticulate interaction strength with the former predominant at low compaction pressures and the latter predominant at high compaction pressures. The melting temperature of each L-lysine salt is a good indicator of the tensile strength of its compacts at zero porosity.
研究盐的形式，即具有共同阳离子（L - 赖氨酸）的不同阴离子，对压实性能的影响，并确定决定片剂抗张强度的因素。
将含有以下阴离子的L - 赖氨酸盐在不同压力下进行压制：乙酸盐、一氯化物、二氯化物、L - 天冬氨酸盐、L - 谷氨酸盐（二水合物）和L - 赖氨酸（两性离子一水合物）。根据“模外”赫克尔图评估每种盐的屈服强度。
在低压实压力下，压实体的抗张强度随压实压力的增加呈线性增加。同时，压实体的抗张强度随盐的屈服强度增加呈指数下降。然而，在高压实压力下，压实体的抗张强度由颗粒间结合强度决定，而非屈服强度。外推至零孔隙率时，压实体的抗张强度随盐的熔点升高呈线性增加。
抗衡离子影响L - 赖氨酸盐的压片性能。抗张强度受屈服强度和颗粒间相互作用强度的控制，在低压实压力下前者占主导，在高压实压力下后者占主导。每种L - 赖氨酸盐的熔点是其在零孔隙率下压实体抗张强度的良好指标。
