This pharmacokinetic study evaluated diphenhydramine in the plasma of healthy volunteers after a single 25 mg oral dose of dimenhydrinate (diphenhydramine theophyllinate), corresponding to 12.7 mg diphenhydramine, in a chewing gum formulation. Seven volunteers (4 men, 3 women; age: 26.3 ± 1.2 years; body weight: 63.1 ± 4.1 kg; height: 172.4 ± 4.6 cm) chewed the gum for 1 h. Blood samples (10 ml) were collected at different time intervals up to 24 h. Blood plasma was subsequently processed and analyzed for diphenhydramine content using a GLC method and an NPD detector. Analytical data revealed the following kinetic parameters: AUC0-24h: 155.2h x ng x ml-1; AUC0-infinite: 195.3 h x ng x ml-1; Mean resident time: 16 h; t1/2: 10 h; Cmax: 14.5 ng x ml-1; tmax: 2.6 h; and plasma clearance: 9.0 ml x min-1 x kg-1. This study indicates that the pharmaceutical formulation employed provided sustained plasma concentrations of diphenhydramine, presumably sufficient to support its clinical efficacy towards motion sickness owing to the almost complete (> 95%) release by the formulation of the active principle. Moreover, the maximal concentrations of diphenhydramine attained in plasma were much lower than the concentration threshold needed to produce drowsiness.

Valoti, M., Frosini, M., Dragoni, S., Fusi, F., Sgaragli, G.P. (2003). Pharmacokinetic of diphenydramine in young volunteers with a dimenhydrinate 25 mg chewing gum formulation. METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY, 25, 377-381 [10.1358/mf.2003.25.5.769660].

Pharmacokinetic of diphenydramine in young volunteers with a dimenhydrinate 25 mg chewing gum formulation

VALOTI, MASSIMO;FROSINI, MARIA;DRAGONI, STEFANIA;FUSI, FABIO;SGARAGLI, GIAN PIETRO
2003-01-01

Abstract

This pharmacokinetic study evaluated diphenhydramine in the plasma of healthy volunteers after a single 25 mg oral dose of dimenhydrinate (diphenhydramine theophyllinate), corresponding to 12.7 mg diphenhydramine, in a chewing gum formulation. Seven volunteers (4 men, 3 women; age: 26.3 ± 1.2 years; body weight: 63.1 ± 4.1 kg; height: 172.4 ± 4.6 cm) chewed the gum for 1 h. Blood samples (10 ml) were collected at different time intervals up to 24 h. Blood plasma was subsequently processed and analyzed for diphenhydramine content using a GLC method and an NPD detector. Analytical data revealed the following kinetic parameters: AUC0-24h: 155.2h x ng x ml-1; AUC0-infinite: 195.3 h x ng x ml-1; Mean resident time: 16 h; t1/2: 10 h; Cmax: 14.5 ng x ml-1; tmax: 2.6 h; and plasma clearance: 9.0 ml x min-1 x kg-1. This study indicates that the pharmaceutical formulation employed provided sustained plasma concentrations of diphenhydramine, presumably sufficient to support its clinical efficacy towards motion sickness owing to the almost complete (> 95%) release by the formulation of the active principle. Moreover, the maximal concentrations of diphenhydramine attained in plasma were much lower than the concentration threshold needed to produce drowsiness.
2003
Valoti, M., Frosini, M., Dragoni, S., Fusi, F., Sgaragli, G.P. (2003). Pharmacokinetic of diphenydramine in young volunteers with a dimenhydrinate 25 mg chewing gum formulation. METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY, 25, 377-381 [10.1358/mf.2003.25.5.769660].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/24383
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