Johnson B F, O'Grady J, Bye C
Br J Clin Pharmacol. 1978 May;5(5):465-7. doi: 10.1111/j.1365-2125.1978.tb01657.x.
1 The influence of particle size on absorption of digoxin was studied in ten healthy volunteers who received 0.5 mg digoxin as two standard Lanoxin tablets, or tablets containing micronized digoxin or large particle size digoxin. Tablets were given 30 min after 15 mg propantheline, 10 mg metoclopramine or a placebo tablet, and following an overnight fast. 2 The overall mean cumulative 4 day urinary excretion of digoxin was significantly lower (P less than 0.01) after large particle size digoxin than after standard or micronized digoxin. Mean cumulative urinary excretion following large particle size digoxin was reduced when administered after metoclopramide and increased after propantheline, the difference between these two treatments being significant (P less than 0.05). There was a significantly lower (P less than 0.05) overall mean cumulative excretion following standard by comparison with micronized digoxin. However, by comparison with placebo, neither metoclopramide nor propantheline significantly altered mean cumulative excretion after standard or micronized digoxin. Propantheline and metoclopramide affect absorption of digoxin from formulations of large particle size and slow dissolution rate only.
在10名健康志愿者中研究了粒径对地高辛吸收的影响,这些志愿者分别服用0.5毫克地高辛,形式为两片标准的地高辛片、含微粉化地高辛的片剂或大粒径地高辛片剂。片剂在服用15毫克丙胺太林、10毫克甲氧氯普胺或安慰剂片剂30分钟后,且经过一夜禁食后给予。
大粒径地高辛服用后,地高辛4天的总体平均累积尿排泄量显著低于(P<0.01)标准或微粉化地高辛服用后的情况。大粒径地高辛在甲氧氯普胺后服用时,平均累积尿排泄量降低,在丙胺太林后服用时增加,这两种治疗之间的差异具有显著性(P<0.05)。与微粉化地高辛相比,标准地高辛的总体平均累积排泄量显著更低(P<0.05)。然而,与安慰剂相比,甲氧氯普胺和丙胺太林均未显著改变标准或微粉化地高辛后的平均累积排泄量。丙胺太林和甲氧氯普胺仅影响大粒径且溶出速率慢的制剂中地高辛的吸收。