A fixed dose combination of desloratadine, a long-acting tricyclic antihistamine with selective peripheral histamine\nH1 receptor antagonistic activity, and betamethasone, a glucocorticoid, can potentially provide synergistic effect\nin the treatment of severe allergic conditions and improve clinical outcomes. Co-administration of an anti-allergy\nmedication and a corticosteroid is extensively used in clinical practice, either as single drug tablets or as a fixed\ndose combination tablet. The current study was conducted to compare the pharmacokinetics of fixed combination\ntablets of desloratadine and betamethasone in 40 healthy human volunteers after a single oral dose in a randomized\ntwo-period, two-treatment, and two-sequence cross-over study. The study protocol was prepared in accordance to\nthe requirements set in the EMA guidance for conducting bioequivalence studies. Reference (Frenaler Cort 5 mg\ndesloratadine/0.6 mg betamethasone film coated tablet, Roemmers S.A.I.C.F., Argentina) and test (Oradus Ã?² 5 mg\ndesloratadine/0.6 mg betamethasone film coated tablet, Pharmaline, Lebanon) drugs were administered to fasted\nvolunteers and blood samples were collected up to 72 h and assayed for desloratadine, hydroxydesloratadine metabolite\nand betamethasone using a validated LC-MS/MS method. The pharmacokinetic parameters AUC0-t, Cmax,\nTmax, T1/2, Ke, in addition to (for betamethasone only) AUC0-âË?ž, MRTinf, and residual area (%) were determined\nfrom plasma concentration-time profile by non-compartmental analysis method using thermos Scientific Kinetica\n(version 5.1). The analysis of variance did not show any significant difference between the two formulations and 90%\nconfidence intervals fell within the acceptable range for bioequivalence (80-125%). The resulting data demonstrated\nthat when administered as fixed dose combination, the pharmacokinetics of desloratadine and betamethasone were\nbioequivalent and were well-tolerated.
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