DIFFERENCES IN STEADY-STATE PLASMA-LEVELS BETWEEN AMINOPHYLLINE AND THEOPHYLLINE SUSTAINED-RELEASE MICROPELLETS AFTER REPEATED CIRCADIAN DOSING

  • 1 January 1984
    • journal article
    • research article
    • Vol. 22  (11) , 621-625
Abstract
In a randomized double-blind, cross-over study, theophylline plasma levels were compared over 24 h after repeated administration of aminophylline and theophylline sustained-release formulations to 12 healthy volunteers. Although both preparations were capsules containing micropellets, and although they were administered in an identical circadian dosing scheme (1 capsule at 0800 h, 2 capsules at 2200 h), marked differences in theophylline plasma levels were found. Whereas the aminophylline micropellets (Euphyllin CR 350) resulted in the clinically desired concentration/time profile with highest theophylline plasma levels between 0200 and 0600 h, theophylline micropellets failed to do so. Apart from differences in the in-vitro release at low pH-values, this may be due to differences in solubility between aminophylline and theophylline, which become clinically relevant in the supine position at night.

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