Intranasal pharmacokinetics and mucociliary toxicity of ketamine hydrochloride nasal spray

OBJECTIVE To study the pharmacokinetics of ketamine hydrochloride(KET·HCl)through nasal mucosa and its mucociliary toxicity.METHODS The blood drug concentrations were measured after the intranasal administration of ketamine to calculate the pharmacokinetic parameters;batrachian maxilla was adopted to evaluate the effect of KET·HCl on the ciliary movement.RESULTS Intranasal administration of KET·HCl,the peak time and concentration,MRT,AUC and absolute bioavailability were 2.83min,69.07μg·mL-1,44.59min,567.43μg·min·mL-1 and 42.29%,respectively;the lasting time of ciliary movement after administration of ketamine hydrochloride nasal spray and control nasal spray were 510±63min and 562±51min,respectively.CONCLUSION The transmucosal pharmacokinetics of KET·HCl can be described by the one-compartment model and follows the first-order kinetics;the mucociliary toxicity of this ketamine hydrochloride nasal spray is low.