In Vitro In Vivo Pharmacokinetic Interaction Study of Escitalopram Oxalate when Co Administered with Caffeine/caffeinated Beverages

ABSTRACT

The effect of caffeine and caffeinated beverage (green tea) on the pharmacokinetics of escitalopram oxalate was evaluated by in vitro and in vivo studies.

In the in vitro study, the release of escitalopram oxalate in the presence and absence of caffeine/green tea (Caffeinated beverage) was studied using dissolution procedure. Water was used as the dissolution media. For the in vivo study, rabbits were used to predict the pharmacokinetic data. The escitalopram oxalate concentrations in the dissolution and plasma samples were analyzed by a Reverse phase High performance liquid chromatographic method (RP HPLC method). This method was carried out on a Hibar C18 (250 mm × 4.6 mm id., 5é) using mobile phase containing 25mM potassium dihydrogen ortho phosphate (pH adjusted to 3.0 with ortho phosphoric acid) and acetonitrile with the ratio of 60:40 % v/v with UV detection at 234 nm. The flow rate was maintained at 1.2 ml/min. The developed method was validated according to the ICH guidelines using various validation parameters. The dissolution study was carried out for one hour in the presence of synthetic caffeine and green tea decoction. The presence of synthetic caffeine and green tea decreased the release of escitalopram oxalate by 33.75 and 13.12% respectively. In the in vivo study carried out with new zealand rabbits a difference was observed in the Cmax and AUC(0-t) values when the drug was co administered with caffeine and green tea.

The absorption of escitalopram oxalate was decreased to a maximum of 28% and 18% when co administered with caffeine and green tea respectively.

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