Domperidone

ABSTRACTDomperidone (DOM), an antidopaminergic medication, is primarily used as an antiemetic to treat nausea and vomiting caused by a variety of etiologies. It is very insoluble in water and has a poor oral bioavailability of 13-17%. The objective of the current work is to increase domperidone aqueous solubility using nano-structured hydroxy-terminated dendrimers. Dendrimers are distinctive carriers for drug solubilization because of their many special characteristics in terms of size, shape, branching length, and surface functioning. Dendrimers have unique properties that make them potential carriers for many active medicinal compounds due to their structural adaptability. The potential of hydroxy-terminated dendrimers UG1.0, UG2.0, and UG3.0 as solubility enhancers for domperidone was investigated. The effect of concentration and generation of synthesized nano-structured dendritic macromolecules on the solubility of domperidone was studied. The formation of the complexes between domperidone drug molecules and dendrimers was characterized by the FT-IR spectra. The experimental results showed that the solubility of the domperidone was approximately proportional to dendrimer concentration and generation. The water solubility of domperidone has been increased as generation of the hydroxy-terminated dendrimer. Cytotoxicity assay using A-549 lung cancer cell lines and hemolysis results revealed that synthesized dendritic macromolecules are more biocompatible than commercially available polyamidoamine dendrimers (PAMAM). Keywords: Antiemetic, Cytotoxicity, Dendrimer, Domperidone, Hemolysis, Phase solubility.

ABSTRACTA new precise, accurate, robust and stability indicating high-performance liquid chromatographic method has been developed and validated for the simultaneous estimation of domperidone (DOM) and esomeprazole (ESO) in their pharmaceutical formulation. The proposed method carried out on Waters Symmetry C18 column (250 mm x 4.6 mm, 5.0 µm particle size) using an isocratic elution technique at a column temperature of 30 ?C. The mobile phase was a mixture of 0.01M sodium acetate buffer: methanol (45:55 v/v) and it was adjusted to pH 4.5 using glacial acetic acid with a flow rate of 1 mL/min and an injection volume of 20 µL. The retention times were 3.7 and 5.0 min with UV detection at 290 nm for DOM and ESO, respectively. The proposed method was linear over the concentration ranges of 0.04-60.0 and 0.08-120.0 µg/mL for DOM and ESO, respectively. Limit of detection and limit of quantitation values were 0.48 and 1.44 µg/mL for DOM and 0.47 and 1.43 µg/mL for ESO, respectively. The method also exhibited good levels of recovery from 100.23% to 101.59% for DOM and from 99.74% to 101.57% for ESO. From the validation study, it was found that the method was specific, rapid, accurate and reproducible. The high percentage of recovery and low relative standard deviation confirm the suitability of the method for routine pharmaceutical analysis of both drugs separately or in their combined dosage form. Keywords: HPLC; Esomeprazole; Domperidone; Validation; Formulation.