Abstract
Purpose: Evaluation of drug-excipients compatibility is an important stage during preformulation studies. In the present research, differential scanning calorimetry (DSC) at different heating rates (2.5, 10, 15°C/min) was applied for the kinetic evaluation of fluvoxamine (FLM), sertraline (SER) and doxepin (DOX) binary mixtures with lactose. Methods: Solid state kinetic parameters of the mixtures were calculated using two different thermal methods including ASTM E698 and Starink and the effect of amine type (pKa value) was investigated based on the calculated activation energies. Results: Based on obtained results mean activation energy calculated for FLM, SER and DOX with lactose using ASTM E698 and Starink methods are equal to 335.23, 132.02 and 270.99 kJ/ mol respectively. Conclusion: Results showed that the probability of drug-lactose interaction is higher in the SERlactose mixture in comparison with other two antidepressant drugs which is consistent with their pKa values.
Highlights
Preformulation studies supporting development of safe and high quality dosage forms
The results indicate that in pharmaceutical molecules there are more other determining factor which should be considered along with the pKa values and differential scanning calorimetry (DSC) kinetic evaluation provides an easy way to calculate kinetic parameters in solid state mixtures
Thermokinetic and thermodynamic parameters corresponding to drug – excipient interaction in some antidepressant drugs containing amine group were calculated using DSC curves obtained by multiple scan method at various heating rates
Summary
Preformulation studies supporting development of safe and high quality dosage forms. Physical and chemical properties of drug agents are considered in select of formulation ingredients. Compatibility of dosage form components and kinetic study are main objectives of preformulation studies in order to develop the stable, safe, efficient and high quality dosage forms. Drug-excipient interaction is one of the most common incompatibility reported. Excipients are added to formulations to facilitate manufacture, absorption, stability and administration. Lactose is a reducing disaccharide and one of the most widely used filler in oral formulations
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