Pharmacokinetic principles in the design of immediate-release components in sustained-release formulations with zero-order release characteristics.
The potential advantages and disadvantages of incorporating an immediate-release (IR) component in sustained-release formulations with zero-order release characteristics (SR) are discussed. The dose of the IR component for SR doses other than the first one (DIS) should be less than that for the first SR dose (DI). Multiple dosing of an SR formulation with an IR component of dose DI may lead to unnecessary accumulation and fluctuation of plasma drug concentrations. An innovative and practical method for estimating the DI and DIS doses of this IR component is also presented.
Cheung
W K
WK
Clinical Pharmacokinetics & Disposition, CIBA-GEIGY Corporation, Ardsley, NY 10502.
Silber
B M
BM
Yacobi
A
A
D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations; D008954:Models, Biological; D010599:Pharmacokinetics
D003692:Delayed-Action Preparations