Polarimetric Research of Pharmaceutical Substances in Aqueous Solutions With Different Water Isotopologues Ratio

Сыроешкин, А. В.; Pleteneva, T. V.; Uspenskaya, E. V.; Levitskaya, O. V.; Tribot-Laspiere, M. A.; Zlatsky, I. A.; Ходорович, Н. А.; Nikifirova, M. V.; Zaytseva, S. A.

doi:10.22159/ijap.2018v10i5.28151

Cited by 10 publications

(15 citation statements)

References 27 publications

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“…But any complication of the system due to the addition of excipients to the aqueous solution leads to a decrease in lifetime leads of the biological object. At the same time, there is also a noticeable increase in the specific optical rotation, which reflects a change in the chiral properties of the API solution [1,2]. ; (pH=6,30, n=3, P=0,95).…”

Section: Aa and Dhaamentioning

confidence: 99%

“…Since the middle of the last century, the stability of ascorbic acid (AA), which has antioxidant properties in mammals and in foodstuffs, has been actively studied [1][2][3][4][5][6][7][8][9]. AA degradation can occur spontaneously, even in an anaerobic environment, and under the influence of a number of factors [1,2,5]. An increase in temperature and in alkalinity of its solution, exposure to radiation, the presence of d-elements ions and compounds with a more positive redox potential are the main causes of AА degradation.…”

Section: Introductionmentioning

confidence: 99%

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The the Effect of Thermal Sterilization and Excipients on the Stability of Ascorbic Acid in Aqueous Solutions

Сыроешкин¹,

Pleteneva²,

Uspenskaya³

et al. 2019

Int J App Pharm

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Objective: To investigate the thermal stability of aqueous solutions of L-ascorbic acid (AA) and its reactions with excipients for the improvement of the injection forms technology. Methods: Solutions of L-ascorbic acid were prepared using deuterium depleted water (DDW-«light» water, D/H=4 ppm) and natural deionized high-ohmic water (BD, D/H=140 ppm). The optical rotation was observed using an automatic polarimeter Atago POL-1/2. Electrospray tandem mass spectra were recorded by Sciex X500R QTOF. Electronic spectra were recorded by UV-spectrometer Cary 60 (Agilent). Unicellular biosensor (Spirotox-test) was used for investigation of excipients influence on the AA biological activity. The statistical analysis was carried out using the OriginPro®9 packages. Results: The results demonstrate the thermal instability of AA. The optical activity of injection forms of AA differs from model solutions with the same concentration and pH value but without heat treatment. Monitoring of solutions by the LC-ESI-MS/MS method made it possible to characterize the nature of some thermal decomposition products. Thermodynamic calculations and evaluation of biological activity (Spirotox-test) indicate that AA interacts with sulfite-ion by redox mechanisms. Excipients in AA aqueous solutions decrease, but DDW increases the biological object lifetime. Conclusion: The use of the set of physicochemical and biological methods to study the effect of heat treatment of L-ascorbic acid solutions in the presence of sulfur (IV) compounds as excipients made it possible to identify decomposition products of the active pharmaceutical ingredient. The results indicate the need to exclude sterilization of the AA injection form by the thermal method and replace it with an alternative one, for example, with gamma radiation treatment.

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Section: Aa and Dhaamentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

The the Effect of Thermal Sterilization and Excipients on the Stability of Ascorbic Acid in Aqueous Solutions

Сыроешкин¹,

Pleteneva²,

Uspenskaya³

et al. 2019

Int J App Pharm

Self Cite

View full text Add to dashboard Cite

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“…Due to the polarity of DMF molecules, it was of interest to study the initiation of optical activity in solvent associates under the influence of chiral substances, as was found for giant heterogeneous water clusters [9][10][11][12]. It turned out that in the region of low concentrations (≤0.1%), the specific optical activity of L-ascorbic acid solutions in DMF drops sharply ( fig.…”

Section: Resultsmentioning

confidence: 99%

Ascorbiс Acid Degradation in N, N-Dimethylformamide Solutions

et al. 2020

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Objective: Investigate the mechanisms of L-ascorbic acid transforтmation and formation of coloured enamines in N, N-dimethyl-formamide solutions. Methods: An automatic polarimeter Atago POL-1/2 was used for polarimetric investigation. Electronic spectra were recorded by UV-spectrometer Cary 60 (Agilent). The statistical analysis was carried out using the OriginPro 9.1 packages. Results: The Biot’s law violation was found in below 0.1% solutions of L-ascorbic acid (AA) in N, N-dimethylformamide (DMF). During the day, the specific rotation of 1% AA solution varied from+37 to-1.0. Gradually, the solution acquired the red colour, and its intensity depended on the AA concentration. Spectrophotometrically, it was shown that after 15 min AA was absent in the n·10-3% solutions. The decomposition followed the first-order kinetics (k1=1.83·10-2с-1). At the same time, new absorption bands appeared at 273, 390, 533 nm. Model solutions containing dimethylamine (DMA) had a similar spectrum, and the intensity of the absorption bands increased in proportion to the concentration of DMA. Conclusion: The results show that the first step in the decomposition of ascorbic acid AA in DMF follows first-order kinetics. Numerous decomposition products are optically active compounds and reverse the sign of the optical rotation of the solution. The water resulting from the decomposition of AA is involved in the hydrolysis of the solvent. The hydrolysis product, the secondary amine DMA, interacts with the carbonyl groups of the AA decomposition products to form coloured enamines. Magnesium (II) accelerates the formation of coloured products.

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“…Accordingly, the biological activity of solutions of the dispersed lactose monohydrate samples exceeds that of the native samples, which may be associated with the mechanochemical activation [19]. The highest biological activity corresponds to the solutions of the dried lactose monohydrate samples.…”

Section: Study Of Biological Activity Of Native Dispersed and Dried mentioning

confidence: 99%

Mechanochemical Activation of Pharmaceutical Substances as a Factor for Modification of Their Physical, Chemical and Biological Properties

et al. 2019

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Objective: Study the influence of the mechanical preparation methods (grinding, fluidization) of solid pharmaceutical substances (PS) and herbal raw material on their physicochemical properties and biological activities. Methods: Test substances and solvents-Lactose monohydrate (DFE Pharma, Germany). Sodium chloride, bendazol hydrochloride (all Sigma-Aldrich, USA) and herbal raw material (Callisia fragrans). The dispersity and native structure of pharmaceutical substances were analyzed by several methods: optical microscopy–Altami BIO 2 microscope (Russia); low angle laser light scattering (LALLS) method (Malvern Instruments, UK); Spirotox method–Quasichemical kinetic of cell transition of cellular biosensor Spirostomum ambiguum; Fourier-transform infrared spectroscopy–the analysis in the middle IR region was carried out using an IR Cary 630 Fourier spectrometer (Agilent Technologies, USA). The analysis of dried leaves of C. fragrans before and after mechanical activation was performed using Shimadzu EDX-7000 X-ray fluorescence spectrophotometer without mineralization (Shimadzu, Japan). Results: It was established that the mechanical change, such as dispersion and drying, alters the biological activity of PS and herbal raw materials. The observed increase in the influence of the dispersed substance on the biosensor S. ambiguum is quantitatively estimated from the values of the activation energy (obsEa), which turns to be valued 1,5 (P≤0,05) times more than for the native form substance. In the study of the dependence of the availability of chemical elements K, Ca, Zn on the degree of dispersion of herbal raw materials was established a quantitative 4-fold (P≤0,05) increase in the concentration of elements in mechano-activated raw materials. Conclusion: By the example of the biological model of Spirotox (single-celled biosensor S. ambiguum) and herbal raw materials obtained from C. fragrans, the increase of biological activity of PS at the dispersion of initial preparations was proved.

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Polarimetric Research of Pharmaceutical Substances in Aqueous Solutions With Different Water Isotopologues Ratio

Cited by 10 publications

References 27 publications

The the Effect of Thermal Sterilization and Excipients on the Stability of Ascorbic Acid in Aqueous Solutions

The the Effect of Thermal Sterilization and Excipients on the Stability of Ascorbic Acid in Aqueous Solutions

Ascorbiс Acid Degradation in N, N-Dimethylformamide Solutions

Mechanochemical Activation of Pharmaceutical Substances as a Factor for Modification of Their Physical, Chemical and Biological Properties

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