Matsumoto T, Kaneniwa N, Higuchi S, Otsuka M
School of Pharmaceutical Sciences, Showa University, Tokyo, Japan.
J Pharm Pharmacol. 1991 Feb;43(2):74-8. doi: 10.1111/j.2042-7158.1991.tb06635.x.
The effects of temperature on the polymorphic transformation of chlorpropamide during compression and on the physical properties of the tablet have been investigated. A heater and liquid nitrogen pool were mounted on the die of a single punch eccentric tableting machine, and the die temperature was controlled by a thermocontroller. A tableting machine with two load cells (upper and lower punches) and a non-contact displacement transducer were used to measure compression stress, distance and energy. The X-ray diffraction profiles of the deagglomerated compressed sample powder were measured to calculate the polymorphic content. The amount of form C transformed from form A at 45 degrees C was about twice that at 0 degree C with the same compression energy. The amount of form A transformed from form C by compression at 45 degrees C was almost the same as that at 0 degree C. This suggests that the mechanochemical effect of form A depended on the compression temperature, but that of form C was independent of temperature. The crushing strength of tablets of form A was about twice that of form C, even at the same porosity. The plots of log (crushing strength of tablet) against porosity of form A tablets compressed at 0 and 45 degrees C were linear with the same slope; the slope for form C tablets compressed at 45 degrees C was less than that at 0 degree C.
研究了温度对氯磺丙脲在压片过程中多晶型转变以及片剂物理性质的影响。在单冲压片机的模具上安装了加热器和液氮池，通过温度控制器控制模具温度。使用一台带有两个测力传感器（上冲头和下冲头）和一个非接触式位移传感器的压片机来测量压缩应力、距离和能量。测量解聚后压缩样品粉末的X射线衍射图谱以计算多晶型含量。在相同压缩能量下，45℃时从A晶型转变为C晶型的量约为0℃时的两倍。45℃时通过压缩从C晶型转变为A晶型的量与0℃时几乎相同。这表明A晶型的机械化学效应取决于压缩温度，而C晶型的机械化学效应与温度无关。即使在相同孔隙率下，A晶型片剂的抗压强度约为C晶型片剂的两倍。在0℃和45℃下压缩的A晶型片剂，其log（片剂抗压强度）与孔隙率的关系图呈线性，斜率相同；45℃下压缩的C晶型片剂的斜率小于0℃时的斜率。
