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地高辛从一种新型微囊化制剂中的吸收情况。

Absorption of digoxin from a new microencapsulated formulation.

作者信息

Bergdahl B, Bogentoft C, Jonsson U E, Magnusson J O

出版信息

Eur J Clin Pharmacol. 1980 Jun;17(6):443-7. doi: 10.1007/BF00570162.

Abstract

The absorption of digoxin from two capsule preparations containing a large number of small, enteric-coated granules of the glycoside (0.38 mg) was compared with that of the same amount from ultrarapidly dissolving commercial tablets. Eight volunteers were studied during steady state conditions. Digoxin concentrations in plasma and urine were measured by radioimmunoassay. Peak plasma concentrations of digoxin were significantly (p < 0.01) delayed after taking the capsules (2.6 +/- 1 h and 2.6 +/- 0.9 h, mean +/- SD) as compared to the tablets (1.3 +/- 0.7 h). The peak concentrations produced by the capsules were 3.1 +/- 1.0 and 2.6 +/- 1.1 nmol/l; only the latter was significantly (p less than 0.05) lower than after the tablets (3.4 +/- 1.0 nmol/l). Areas under the plasma concentration-time curves during a 24 h dosage interval were similar for the three preparations, and so was the 24 h urinary excretion of digoxin, which averaged 60-63% of the daily dose. Thus, this particular enteric coating of digoxin delayed absorption without reducing the amount absorbed.

摘要

将含有大量小的肠溶包衣苷类颗粒(0.38毫克)的两种胶囊制剂中地高辛的吸收情况,与相同剂量的超快速溶解商业片剂中地高辛的吸收情况进行了比较。在稳态条件下对8名志愿者进行了研究。通过放射免疫分析法测定血浆和尿液中的地高辛浓度。与片剂(1.3±0.7小时)相比,服用胶囊后地高辛的血浆峰值浓度显著延迟(p<0.01)(2.6±1小时和2.6±0.9小时,平均值±标准差)。胶囊产生的峰值浓度分别为3.1±1.0和2.6±1.1纳摩尔/升;只有后者显著低于服用片剂后(3.4±1.0纳摩尔/升)(p<0.05)。三种制剂在24小时给药间隔期间的血浆浓度-时间曲线下面积相似,地高辛的24小时尿排泄量也相似,平均为日剂量的60-63%。因此,地高辛的这种特殊肠溶包衣延迟了吸收,但没有减少吸收量。

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