Abstract
Purpose: In the present study the incompatibility of FLM (fluvoxamine) with lactose in solid state mixtures was investigated. The compatibility was evaluated using different physicochemical methods such as differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR) spectroscopy and mass spectrometry. Methods: Non-Isothermally stressed physical mixtures were used to calculate the solid–state kinetic parameters. Different thermal models such as Friedman, Flynn–Wall–Ozawa (FWO) and Kissinger–Akahira–Sunose (KAS) were used for the characterization of the drug-excipient interaction. Results: Overall, the incompatibility of FLM with lactose as a reducing carbohydrate was successfully evaluated and the activation energy of this interaction was calculated. Conclusion: In this research the lactose and FLM Maillard interaction was proved using physicochemical techniques including DSC and FTIR. It was shown that DSC- based kinetic analysis provides fast and versatile kinetic comparison of Arrhenius activation energies for different pharmaceutical samples.
Highlights
Fluvoxamine (FLM) (2-{[(E)-{5-Methoxy-1-[4(trifluoromethyl) phenyl] pentylidene}amino] oxy} ethanamine) maleate is an antidepressant drug belonging to selective serotonin reuptake inhibitor which is used in obsessive or compulsive disorders treatment.[1]
differential scanning calorimetry (DSC) (Differential Scanning Calorimetry) DSC is widely used in drug-excipient compatibility studies and provides valuable information such as drug purity,drug stability, polymorphic forms and their stabilities.[12,13]
We have previously studied the compatibility of acyclovir, baclofen, gabapentin and doxepin with lactose and dextrose in physical mixtures and commercial tablets using mass spectrometry[21,22,23,24,25]
Summary
Fluvoxamine (FLM) (2-{[(E)-{5-Methoxy-1-[4(trifluoromethyl) phenyl] pentylidene}amino] oxy} ethanamine) maleate is an antidepressant drug belonging to selective serotonin reuptake inhibitor which is used in obsessive or compulsive disorders treatment.[1]. Have been used to evaluate the drug- excipient interactions.[3,4] Since 1970, thermal methods have been used to evaluate the incompatibility of formulation component in pharmaceutical industries.[4,5,6]. It is used to form a diluent powder for dry-powder inhalations.[7,8] Lactose is a reducing disaccharide and can react with amine containing drugs such as FLM during Maillard reaction.[9,10] The possibility of this chemical reaction lead to conduct this study to provide analytical documentation about the progress of the reaction in solid state pharmaceutical dosage forms and to study the kinetic of the reaction using non-isothermal DSC techniques. In this study different analytical methods (DSC, FTIR and Mass spectrometry) were applied to study the FLM- lactose incompatibility reaction and the activation energy of the proposed interaction was calculated using different kinetic models
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