TY - JOUR
T1 - Comparative pharmacokinetic evaluation of sustained-release theophylline formulations in dogs and humans
AU - Hussein, Ziad
AU - Bialer, Meir
AU - Friedman, Michael
AU - Raz, Itamar
PY - 1987/6
Y1 - 1987/6
N2 - Several new sustained-release formulations of theophylline were developed and their sustained-release performance was evaluated in a comparative pharmacokinetic analysis. These new formulations, Theo-Dur, Theotrim and aminophylline were administered to 5 dogs and 6 healthy volunteers. Plasma levels of theophylline were determined by an HPLC assay. The absorption profiles of the various formulations were analyzed pharmacokinetically, using the Wagner-Nelson procedure. Two new formulations, Theotrim and Theo-Dur demonstrated very good sustained-release performance in humans and dogs. One formulation (T-2-A) showed incomplete absorption in both species, and its bioavailability relative to aminophylline was about 65% in humans and 78% in dogs. These results were also confirmed by the Wagner-Nelson Procedure. In this study the dog was found to be a good animal model as far as the rate and extent of absorption of the various tested theophylline formulations were concerned; the dog may be useful in primary screening of new formulations from this series.
AB - Several new sustained-release formulations of theophylline were developed and their sustained-release performance was evaluated in a comparative pharmacokinetic analysis. These new formulations, Theo-Dur, Theotrim and aminophylline were administered to 5 dogs and 6 healthy volunteers. Plasma levels of theophylline were determined by an HPLC assay. The absorption profiles of the various formulations were analyzed pharmacokinetically, using the Wagner-Nelson procedure. Two new formulations, Theotrim and Theo-Dur demonstrated very good sustained-release performance in humans and dogs. One formulation (T-2-A) showed incomplete absorption in both species, and its bioavailability relative to aminophylline was about 65% in humans and 78% in dogs. These results were also confirmed by the Wagner-Nelson Procedure. In this study the dog was found to be a good animal model as far as the rate and extent of absorption of the various tested theophylline formulations were concerned; the dog may be useful in primary screening of new formulations from this series.
KW - Animal model
KW - Pharmacokinetics
KW - Sustained-release dosage form
KW - Theophylline
UR - http://www.scopus.com/inward/record.url?scp=0023194471&partnerID=8YFLogxK
U2 - 10.1016/0378-5173(87)90013-5
DO - 10.1016/0378-5173(87)90013-5
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AN - SCOPUS:0023194471
SN - 0378-5173
VL - 37
SP - 97
EP - 102
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -