Drugs properties in solid state and biological media

About the group:

Bioavailability of physiologically active compounds is determined by a whole number of processes, among them solubility, distribution in the biological fluids and membrane permeability are the most important. The solubility is estimated to be an important characteristic of drug substances as it influences optimal therapeutic doses and possible side effects. From the fundamental point of view the solubility of the compounds is determined by the crystal lattice energy and solvation processes. The investigation of the main processes which occur during the dissolution, distribution and membrane permeability allows to carry out a direct synthesis of drug compounds.

Experiments:

  1. Investigation of the solubility in the solutions modeling the biological media.
  2. Studying the crystal state of the substances based on the thermophysic and sublimation parameters.
  3. Investigation of the distribution and membrane permeability coefficients of drug compounds.
Senior researcher
Phd in chemistry
Researcher
Phd in chemistry
  1. M.V. Ol’khovich, A.V. Sharapova, S.V. Blokhina, G.L. Perlovich, A.N. Proshin Vapor Pressures and Sublimation Thermodynamic Parameters for Novel Drug-Like Spiro-Derivatives. J. Chem. Eng. Data. 2012. V.57. 3452-3457.
  2.  S.V. Blokhina, M.V. Ol’khovich, A.V. Sharapova, A. N. Proshin, G. L. Perlovich Thermodynamics of Solubility Processes of Novel Drug-like Spiro-Derivatives in Model Biological Solutions J. Chem. Eng. Data 2012, 57, 1996−2003.
  3. Perlovich G.L., Blokhina S.V., Volkova T.V.,Manin N.G., Tkachev V.V Polymorphism and Solvatomorphism of Bicalutamide: Thermophysical Study and Solubility J. Thermal Analysis and Calorimetry . 2012. 111. 655–662
  4. Blokhina S.V., Ol’khovich M.V., Sharapova A.V., Proshin A.N., Perlovich G.L. Partition Coefficients and Thermodynamics of Transfer of Novel Drug-like Spiro-derivatives in Model Biological Solutions. J. Chem. Thermodynamics. 61. 2013.  11–17.
  5. Ol’khovich M.V., Blokhina S.V., Sharapova A.V., Perlovich G.L., Proshin A.N. Thermodynamics of sublimation and solvation for bicyclo-derivatives of 1,3-thiazine. Thermochimica Acta. 2013.  569, 61– 65.
  6. Perlovich G.L., Blokhina S.V., Ol’khovich M.V., Sharapova A.V., Proshin A.N. Solubility, Solvation and Distribution of Novel Spiro-Derivatives of 1,3-Thiazine in Aqueous and Organic Solutions. J. Solution Chem. 2013. V.42. 2057-2069.
  7. Perlovich G.L., Proshin A.N., Ol’khovich M.V., Sharapova A.V., Lermontov A.S. Novel Spiro-Derivatives of 1,3-Thiazine Molecular Crystals: Structural and Thermodynamic Aspects. Crystal Growth & Design. 2013. 13(2). 804-815.
  8. Blokhina S.V., Ol’khovich M.V., Sharapova A.V., Perlovich G.L., Proshin A.N. Vapor pressures and sublimation enthalpies of novel bicyclic heterocycle derivatives. J. Chem. Thermodynamics , 2014. V. 69. 107-111.
  9. Blokhina S.V., Ol’khovich M.V., Sharapova A.V., Volkova T.V., Proshin A.N., Bachurin S.O., Perlovich G.L. Synthesis, Biological Activity, Distribution and Membrane Permeability of Novel Spirothiazines as Potent Neuroprotectors.  Eur. J. Med. Chem. 2014.V.77. 8–17
  10. Blokhina S.V., Ol’khovich M.V., Sharapova A.V., Volkova T.V., Proshin A.N., Perlovich G.L. Effect of the structure, solid state and lipophilicity on the solubility of novel bicyclic derivatives J. Chem. Therm. 2014.V. 78. 152–158.
  11. .Blokhina S.V., Ol’khovich M.V., Sharapova A.V., Volkova T.V., Proshin A.N., Perlovich G.L. Solubility and Solution Thermodynamics of Novel Bicyclic Derivatives of 1,3-Selenazine in Biological Relevant Solvents J. Chem. Eng. Data. 2014.V.59. 2298-2304
  12.  M.V. Ol’khovich, A.V. Sharapova S. N. Lavrenov, S.V. Blokhina, G.L. Perlovich Inclusion complexes of hydroxypropyl-β-cyclodextrin with novel cytotoxic compounds: Solubility and thermodynamic properties Fluid Phase Equilibria. 2014. V. 384. 68–72
  13.  S.V. Blokhina, T. V. Volkova, M.V. Ol’khovich, A. V. Sharapova,  A. N. Proshin, G. L. Perlovich. New bicyclic 1,3-selenazine derivatives: distribution in model biological media and membrane permeability. J. Chem. Eng. Data. 2015. 60. 1146−1152.
  14.  S.V. Blokhina,M.V. Ol’khovich, A.V. Sharapova, T.V. Volkova, G.L. Perlovich Solution thermodynamics of pyrazinamide, isoniazid, and p-aminobenzoic acid in buffers and octanol J. Chem. Therm. 2015. DOI 10.1016/j.jct.2015.08.022
  15.  T.V. Volkova, S.V. Blokhina, A.V. Sharapova, M.V. Ol’khovich, G.L. Perlovich Vapor pressure and sublimation thermodynamics of aminobenzoic acid, nicotinic acid and related amido-derivatives J. of Thermal Analysis and Calorimetry. 2015. DOI: 10.1007/s10973-015-4969-2
  16.  S.V. Blokhina, A.V. Sharapova, M.V. Ol’khovich,  T.V. Volkova, G.L. Perlovich Vapor pressure and Thermodynamic Sublimation of Antitubercular Drugs: Pyrazinamide and Hydrazides Isonicotinic Acid. J. of Thermal Analysis and Calorimetry 2015 DOI 10.1007/s10973-015-4410-x