The effect of food on the absorption of controlled-release theophylline in mini-swine.
The effect of differing fat contents of food on the bioavailability of theophylline following a 400-mg single dose of Theo-24 was studied in mini-swine. The pharmacokinetics of theophylline, following the intravenous administration of aminophylline equivalent to 5 mg/kg as a single dose, were also studied in the same animals. The terminal plasma half-life of theophylline following an i.v. dose was found to be approximately 24 hr. The volume of distribution, Vdext, and clearance following the i.v. dose were approximately 0.7 liter/kg and 0.023 liter/hr/kg, respectively. The terminal half-life of theophylline following the administration of theophylline capsules under fasting conditions was 21 hr. The average bioavailability under fasting conditions was approximately 80% compared to the i.v. dose. Food appeared to have decreased the rate of absorption but no significant effect on the extent of absorption.
Shiu
G K
GK
Biopharmaceutics Research Branch, Food and Drug Administration, Washington, D.C. 20204.
Sager
A O
AO
Velagapudi
R B
RB
Prasad
V K
VK
Skelly
J P
JP
D000628:Aminophylline / Q000008:administration & dosage / Q000493:pharmacokinetics; D000818:Animals; D001682:Biological Availability; D003692:Delayed-Action Preparations; D004347:Drug Interactions; D005215:Fasting; D005502:Food; D007275:Injections, Intravenous; D013552:Swine; D013556:Swine, Miniature; D013806:Theophylline / Q000008:administration & dosage / Q000493:pharmacokinetics*
D003692:Delayed-Action Preparations; D000628:Aminophylline; D013806:Theophylline