Development of a new controlled-release formulation of chlorpheniramine maleate using in vitro/in vivo correlations.
Development of a controlled-released formulation of chlorpheniramine maleate is described, using in vitro/in vivo correlates, according to a process that has been termed "biorelevant dissolution". The process begins with simulations using several possible input rates combined with known disposition parameters of chlorpheniramine maleate. Based on desired plasma concentrations, an input rate is selected for further development which consists of a combination of clinical bioequivalence studies and further in vitro testing and simulations. The method is designed to reduce the requirements for trial and error clinical bioequivalence testing of a new controlled-release formulation.
Williams
R L
RL
Drug Studies Unit, School of Pharmacy, University of California, San Francisco 94143.
Upton
R A
RA
Ball
L
L
Braun
R L
RL
Lin
E T
ET
Liang-Gee
W
W
Leeson
L J
LJ
D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D002744:Chlorpheniramine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003198:Computer Simulation; D003692:Delayed-Action Preparations; D006801:Humans; D007441:Intubation, Gastrointestinal; D008297:Male; D008954:Models, Biological; D012995:Solubility
D003692:Delayed-Action Preparations; D002744:Chlorpheniramine