Evaluation of drug disappearance from nasal cavity by the deposit method.

Abstract

In order to evaluate antiallergic intranasal formulations, the rates of drug disappearance from rat nasal cavity were estimated by the deposit and perfusion methods. The deposit method, which estimates changes in the amount of residual drug in the nasal cavity following washout of the deposited drug over time after application, yielded a good correlation between apparent disappearance rate constant and the combination of lipophilicity and molecular weight. Since the deposit method can be used only with delivery of small amounts of drug to the nasal cavity, the physiological characteristics of the nasal membrane readily affect drug disposition in tests performed with it, and adsorptive drugs such as parabens exhibited rapid disappearance. Doses used clinically for intranasal administration are usually small, and in the case of antiallergic formulations, it is important to maintain the drug concentration in the nasal mucous membrane. The deposit method should be useful for evaluating intranasal antiallergic drug formulations.