Tanaka I, Tagami H
Nihon Yakurigaku Zasshi. 1985 Mar;85(3):167-71. doi: 10.1254/fpj.85.167.
Effects of TKG01 on gastric ulcers and gastric secretion in rats were investigated in comparison with those of TA903, which is the equimolar clathrate compound of TKG01 anhydride with beta-cyclodextrin. The doses were adjusted on a molecular weight basis to include the same amount of TKG01 anhydride. Water-immersion stress ulcers were dose-dependently (100, 300 mg/kg) inhibited by TA903 given orally, but only significantly inhibited by TKG01 (300 mg/kg). TA903, given orally, even in low doses (30, 100 mg/kg) potently inhibited HCl-ethanol ulcers, whereas TKG01 did not inhibit these ulcers. Both TA903 and TKG01, given orally (100, 300 mg/kg), showed similar inhibition of indomethacin ulcers. TA903, given intraduodenally (100, 300 mg/kg), dose-dependently inhibited gastric secretion (volume, acid output and pepsin output) in pylorus-ligated rats, but TKG01 only inhibited pepsin output (100, 300 mg/kg). These results showed that TA903 had a broader spectrum of anti-ulcer effects than TKG01 and the mechanism of TA903 could involve both its cytoprotective activity and its anti-secretory effect.
将TKG01与TA903（TKG01酸酐与β-环糊精的等摩尔包合物）进行比较，研究了TKG01对大鼠胃溃疡和胃分泌的影响。根据分子量调整剂量，使两者所含TKG01酸酐的量相同。口服给予TA903可剂量依赖性地（100、300mg/kg）抑制水浸应激性溃疡，但TKG01仅在300mg/kg时具有显著抑制作用。口服给予TA903，即使是低剂量（30、100mg/kg）也能有效抑制盐酸-乙醇性溃疡，而TKG01对这些溃疡无抑制作用。口服给予TA903和TKG01（100、300mg/kg）对吲哚美辛性溃疡的抑制作用相似。十二指肠内给予TA903（100、300mg/kg）可剂量依赖性地抑制幽门结扎大鼠的胃分泌（体积、酸分泌量和胃蛋白酶分泌量），但TKG01仅能抑制胃蛋白酶分泌量（100、300mg/kg）。这些结果表明，TA903的抗溃疡作用谱比TKG01更广，其作用机制可能涉及其细胞保护活性和抗分泌作用。
