[Bioavailability of theophylline in a new oral sustained-release preparation (author's transl)].
On the basis of biopharmaceutic-pharmacokinetic and galenic aspects a new sustained-release preparation of theophylline according to the "divided-dose" principle was developed. The technological procedure used allows a reproducible manufacture of a stable product with narrow limits of pharmaceutical quality. The bioavailability of the sustained-release pellets in a dose corresponding to 350 mg active principle is examined in comparison to an aqueous solution or retard-tablet formulation on the marked (containing 260 mg drug/dose), respectively, after single or multiple dose administration to 7 healthy volunteers. The relative bioavailability of the new formulation is about 100%. During chronic application the controlled drug delivery from the sustained-release pellets warrants only slight fluctuations of plasma levels by avoiding peak concentrations. Formulations with a dosage of 200, 350 or 500 mg, respectively, allow adaptation of continuous plasma levels in the therapeutic range between 5--20 micrograms/ml according to the therapeutic necessities of a patient.
D000328:Adult; D001682:Biological Availability; D003692:Delayed-Action Preparations; D004355:Drug Stability; D006801:Humans; D007700:Kinetics; D008297:Male; D008954:Models, Biological; D013806:Theophylline / Q000008:administration & dosage* / Q000378:metabolism; D013997:Time Factors
D003692:Delayed-Action Preparations; D013806:Theophylline
Bioverfügbarkeit von Theophyllin in einer neuen oralen Retardzubereitung.