Kamba Masaharu, Seta Yasuo, Takeda Nao, Hamaura Takeshi, Kusai Akira, Nakane Hisanori, Nishimura Kenji
Pharmacokinetics and Drug Delivery Research Laboratories, Sankyo Co., Ltd., 2-58, 1-chome, Hiromachi, Shinagawa-ku, Tokyo 140, Japan.
Int J Pharm. 2003 Jan 2;250(1):99-109. doi: 10.1016/s0378-5173(02)00535-5.
The purpose of this study was to investigate the effect of the agitation force and mechanical destructive force on the drug dissolution of a tablet in the paddle rotation dissolution test and in the disintegration test. The agitation in the paddle method and the mechanical destructive force in the disintegration test were considered to be conclusive factors for drug dissolution. The dissolution rate of planar-constant-release tablets increased with increasing paddle rotation speed and increased with increasing distance from the center of the vessel bottom. Separately, the fluid resistance (agitation force) in the vessel was measured using a modified paddle method apparatus equipped with a fluid resistance sensor. The fluid resistance was 0.03 x 10(-3) N/(64 mm(2)) when the paddle rotation speed was 50 rpm at a position 4 mm away from the center. A considerable position-dependent change in agitation force intensity was seen with the fluid resistance sensor. The impulsive force (mechanical destructive force) in the disintegration test apparatus was measured using a modified basket-rack assembly with a strain gauge transducer. The fluid resistance was measured using the basket-rack assembly with a different sensor probe and amplifier. The impulsive force applied by the auxiliary disk was 0.31 N and the fluid resistance at the bottom of the basket-rack assembly was 1.66 x 10(-3) N/(64 mm(2)).
本研究的目的是在桨板旋转溶出试验和崩解试验中，研究搅拌力和机械破坏力对片剂药物溶出的影响。桨板法中的搅拌和崩解试验中的机械破坏力被认为是药物溶出的决定性因素。平面恒释片剂的溶出速率随桨板转速的增加而增加，且随距容器底部中心距离的增加而增加。另外，使用配备有流体阻力传感器的改良桨板法装置测量容器中的流体阻力（搅拌力）。当桨板转速为50 rpm且在距中心4 mm处时，流体阻力为0.03×10(-3) N/(64 mm(2))。使用流体阻力传感器可观察到搅拌力强度存在明显的位置依赖性变化。在崩解试验装置中，使用带有应变片传感器的改良篮架组件测量冲击力（机械破坏力）。使用带有不同传感器探头和放大器的篮架组件测量流体阻力。辅助圆盘施加的冲击力为0.31 N，篮架组件底部的流体阻力为1.66×10(-3) N/(64 mm(2))。
