Osei-Yeboah Frederick, Chang Shao-Yu, Sun Changquan Calvin
Pharmaceutical Materials Science and Engineering Laboratory Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., Minneapolis, Minnesota, 55455, USA.
Pharm Res. 2016 May;33(5):1126-32. doi: 10.1007/s11095-016-1858-8. Epub 2016 Jan 14.
Although the bonding area (BA) and bonding strength (BS) interplay is used to explain complex tableting behaviors, it has never been experimentally proven. The purpose of this study is to unambiguously establish the distinct contributions of each by decoupling the contributions from BA and BS.
To modulate BA, a Soluplus® powder was compressed into tablets at different temperatures and then broken following equilibration at 25°C. To modulate BS, tablets were equilibrated at different temperatures. To simultaneously modulate BA and BS, both powder compression and tablet breaking test were carried out at different temperatures.
Lower tablet tensile strength is observed when the powder is compressed at a lower temperature but broken at 25°C. This is consistent with the increased resistance to polymer deformation at lower temperatures. When equilibrated at different temperatures, the tensile strength of tablets prepared under identical conditions increases with decreasing storage temperature, indicating that BS is higher at a lower temperature. When powder compression and tablet breaking are carried out at the same temperature, the profile with a maximum tensile strength at 4°C is observed due to the BA-BS interplay.
By systematically varying temperature during tablet compression and breaking, we have experimentally demonstrated the phenomenon of BA-BS interplay in tableting.
尽管结合面积(BA)与结合强度(BS)的相互作用被用于解释复杂的压片行为,但从未得到实验验证。本研究的目的是通过分离BA和BS的贡献,明确确定两者各自的独特作用。
为调节BA,将尤特奇®粉末在不同温度下压制成片,然后在25°C平衡后破碎。为调节BS,将片剂在不同温度下平衡。为同时调节BA和BS,在不同温度下进行粉末压片和片剂破碎试验。
当粉末在较低温度下压片但在25°C破碎时,观察到片剂的拉伸强度较低。这与较低温度下聚合物变形阻力增加一致。当在不同温度下平衡时,在相同条件下制备的片剂的拉伸强度随储存温度降低而增加,表明较低温度下BS较高。当在相同温度下进行粉末压片和片剂破碎时,由于BA-BS相互作用,观察到在4°C时拉伸强度最大的曲线。
通过在压片和破碎过程中系统地改变温度,我们通过实验证明了压片中BA-BS相互作用的现象。