A "once a day administration" sustained-release theophylline formulation: disposition and pharmacokinetics.

Abstract:

:The pharmacokinetics of a new sustained-release preparation of theophylline (Dilatrane à Action Prolongée capsules filled with homogenous microgranules) has been after its studied administration to 7 healthy volunteers at 8 p.m. in order to achieve therapeutic levels at night and in the morning. In separate trials the test dose of 500 or 600 mg was administered for 7 days, once daily at 8 p.m. Plasma theophylline levels were measured by capillary gas chromatography with a mass specific detector after pentylation, using internal standards labelled with stable isotopes (15N-1,3 and 13C-2 theophylline). The new sustained-release preparation showed a monophasic regular absorption phase with very low inter-individual variability. After administration, the plasma level stayed within 80% of the peak levels for 8.5 +/- 1.5 h. There was a good correlation between the dose and the steady state plasma level (r = 0.9587; p less than 0.05). This preparation can be chronically administered once daily day at 8 p.m. in order to achieve a therapeutic level during the night and the morning, and to provide sufficient protection during the nycterohemeral period, with a once dose a day schedule.

journal_name

Eur J Clin Pharmacol

authors

Soubeyrand J,Comet F,Gillet A,Georges D,Brazier JL

doi

10.1007/BF00542169

subject

Has Abstract

pub_date

1984-01-01 00:00:00

pages

325-8

issue

3

eissn

0031-6970

issn

1432-1041

journal_volume

27

pub_type

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