Developing A High-performance Liquid Chromatography Method for Simultaneous Determination of Loratadine and its Metabolite Desloratadine in Human Plasma.

BACKGROUND Allergic diseases are considered among the major burdons of public health with increased prevalence globally. Histamine H1-receptor antagonists are the foremost commonly used drugs in the treatment of allergic disorders. Our target drug is one of this class, loratadine and its biometabolite desloratadine which is also a non sedating H1 receptor antagonist with anti-histaminic action of 2.5 to 4 times greater than loratadine. To develop and validate a novel isocratic reversed-phase high performance liquid chromatography (RP-HPLC) method for rapid and simultaneous separation and determination of loratadine and its metabolite, desloratadine in human plasma. METHODS The drug extraction method from plasma was based on protein precipitation technique. The separation was carried out on a Thermo Scientific BDS Hypersil C18 column (5µm, 250 x 4.60 mm) using a mobile phase of MeOH : 0.025M KH2PO4 adjusted to pH 3.50 using orthophosphoric acid (85 : 15, v/v) at ambient temperature. The flow rate was maintained at 1 mL/min and maximum absorption was measured using PDA detector at 248 nm. RESULTS The retention times of loratadine and desloratadine in plasma samples were recorded to be 4.10 and 5.08 minutes respectively, indicating a short analysis time. Limits of detection were found to be 1.80 and 1.97 ng/mL for loratadine and desloratadine, respectively, showing a high degree of method sensitivity. The method was then validated according to FDA guidelines for the determination of the two analytes in human plasma. CONCLUSION The results obtained indicate that the proposed method is rapid, sensitive in the nanogram range, accurate, selective, robust and reproducible compared to other reported methods.