Physicochemical evaluation and non-isothermal kinetic study of the drug–excipient interaction between doxepin and lactose

Ghaderi, Faranak; Nemati, Mahboob; Siahi-Shadbad, Mohammad Reza; Valizadeh, Hadi; Monajjemzadeh, Farnaz

doi:10.1016/j.powtec.2015.09.007

Cited by 20 publications

(9 citation statements)

References 24 publications

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“…All the maillard reaction tracking was done qualitatively and the reason for this was because of the identity of the maillard product reported as an unstable intermediate agent resulting from condensation of ACV with DEX and, thus, cannot be synthesized as a pure material to be used for accurate qualitative calculations. Similar researches have reported the maillard reaction in a similar way (5,41) as well as we have done previously (9,13,28,29,31,42).…”

Section: Real Time Infusion Evaluationsupporting

confidence: 89%

“…Thus, physicochemical evaluations have been performed on solid materials in a concentrated condition to force the chemical reaction to take place. DSC DSC has been widely used in monitoring the presence of incompatibility in pharmaceutical preparations (22)(23)(24)(25)(26)(27)(28)(29)(30)(31). Compatibility data should be interpreted carefully as lots of deviations from principal laws can be explained.…”

Section: Resultsmentioning

confidence: 99%

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Investigation of Possible Maillard Reaction Between Acyclovir and Dextrose upon Dilution Prior to Parenteral Administration

et al. 2016

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Abstract. In this study the stability of parenteral acyclovir (ACV) when diluted in dextrose (DEX) as large volume intravenous fluid preparation (LVIF) was evaluated and the possible Maillard reaction adducts were monitored in the recommended infusion time. Different physicochemical methods were used to evaluate the Maillard reaction of dextrose with ACV to track the reaction in real infusion condition. Other large volume intravenous fluids were checked regarding the diluted drug stability profile. Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and mass data proved the reaction of glucose with dextrose. A Maillard-specific high performance liquid chromatography (HPLC) method was used to track the reaction in real infusion condition in vitro. The nucleophilic reaction occurred in diluted parenteral preparations of acyclovir in 5% dextrose solutions. The best diluent solution was also selected as sodium chloride and introduced based on drug stability and also its adsorption onto different infusion sets (PVC or non PVC) to provide an acceptable administration protocol in clinical practices. Although, the Maillard reaction was proved and successfully tracked in diluted solutions, and the level of drug loss when diluted in dextrose was reported to be between 0.27 up to 1.03% of the initial content. There was no drug adsorption to common infusion sets. The best diluent for parenteral acyclovir is sodium chloride large volume intravenous fluid.

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Section: Real Time Infusion Evaluationsupporting

confidence: 89%

Section: Resultsmentioning

confidence: 99%

Investigation of Possible Maillard Reaction Between Acyclovir and Dextrose upon Dilution Prior to Parenteral Administration

et al. 2016

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“…Condensation products of lactose and different drug substances such as hydrochlorothiazide, fluoxetine and metoclopramide have detected in several investigations. 9 , 19 , 20 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 - 25 Based on the mass results in this study the condensation product of FLM with lactose was successfully detected.…”

Section: Resultsmentioning

confidence: 91%

Thermal Stability and Kinetic Study of Fluvoxamine Stability in Binary Samples with Lactose

et al. 2017

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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.

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“…Selected DSC thermograms of (A) FLM, lactose and FLM- lactose 1:1 W/W binary mixture 10 (B) SER, lactose and SER- lactose 1:1 W/W binary mixture 11 (C) DOX, lactose and DOX- lactose 1:1 W/W binary mixture 12 (β=10) [Presented with permission].…”

Section: Resultsmentioning

confidence: 99%

“…Multiple scan method using isoconversional calculation procedures have been recently used by many researchers in assessment of pharmaceutical product stability and also kinetic study. 8,11,12 While increasing heating rate DSC thermograms were shifted to higher temperature and this issue was used to calculation of kinetic parameters. 14,15 DSC thermograms of FLM-lactose, SER-lactose and DOX-lactose 1:1 binary mixtures at different heating rates are presented in Figure 3.…”

Section: Resultsmentioning

confidence: 99%

Evaluation the Effect of Amine Type on the Non-isothermally Derived Activation Energy for the Interaction of 3 Antidepressant Drugs with Lactose

et al. 2019

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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.

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Physicochemical evaluation and non-isothermal kinetic study of the drug–excipient interaction between doxepin and lactose

Cited by 20 publications

References 24 publications

Investigation of Possible Maillard Reaction Between Acyclovir and Dextrose upon Dilution Prior to Parenteral Administration

Investigation of Possible Maillard Reaction Between Acyclovir and Dextrose upon Dilution Prior to Parenteral Administration

Thermal Stability and Kinetic Study of Fluvoxamine Stability in Binary Samples with Lactose

Evaluation the Effect of Amine Type on the Non-isothermally Derived Activation Energy for the Interaction of 3 Antidepressant Drugs with Lactose

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