Physicochemical properties of the original pharmaceutical substance TST-9 based on the 3,7-diazabicyclo[3.3.1]nonane derivative with the chemical name IUPAC 6-[4methoxy-3-(1H-pyrazol-1-ylmethyl) benzyl]-1,11-dimethyl-3,6,9-triazatricyclo[7.3.1.1]tetradecane-4,8,12-trion, were studied. TST-9 is used as an active substance for the development of the composition and technology for the preparation of an innovative oral drug. The pharmaceutical substance TST-9 is an amorphous white powder, odorless, soluble in chloroform, acetonitrile, methylene chloride, acetone, dimethyl sulfoxide, dimethylformamide and alcohol, sparingly soluble in diethyl ether, dioxane and is very slightly soluble in water, hexane, and heptane. The melting point ranged from 94°C to 96°C without visible decomposition of the substance. The microbiological purity corresponds to category 2.2. Residual organic solvents in the form of chloroform did not exceed 0.006%. The amount of impurities was not more than 0.15%. The loss in mass upon drying was not more than 0.5%. The “identity” was confirmed using nuclear magnetic resonance spectroscopy and HPLC with UV detection. The data obtained in the study will contribute to the further development of the dosage form, the choice of the route of administration and the dosage regimen, as well as the selection of analytical methods for analyzing the quality of the finished dosage form and the effective, high-precision determination of the content of the active substance and its likely decay products.
Download PDF:
Keywords: TST-9, pharmaceutical substance, physicochemical properties, 3,7-diazabicyclononane derivative, pharmaceutical development
Citation:
Brkich G.E., Pyatigorskaya N.V., Beregovykh V.V., Zyryanov O.A., Demina N.B., Bakrushina E.O. (2020) The development of the physicochemical characteristics of the new original nootropic substance TST-9. Biomeditsinskaya Khimiya, 66(3), 257-264.
Brkich G.E. et al. The development of the physicochemical characteristics of the new original nootropic substance TST-9 // Biomeditsinskaya Khimiya. - 2020. - V. 66. -N 3. - P. 257-264.
Brkich G.E. et al., "The development of the physicochemical characteristics of the new original nootropic substance TST-9." Biomeditsinskaya Khimiya 66.3 (2020): 257-264.
Brkich, G. E., Pyatigorskaya, N. V., Beregovykh, V. V., Zyryanov, O. A., Demina, N. B., Bakrushina, E. O. (2020). The development of the physicochemical characteristics of the new original nootropic substance TST-9. Biomeditsinskaya Khimiya, 66(3), 257-264.
References
Hohlov A.L., Pyatigorskaya N.V. (2019) Promyshlennaya farmaciya. Put' sozdaniya produkta, Moscow, 394 p. Scholar google search
Ged Sh.K. (2008) Pharmaceutical Manufacturing Handbook: Regulations and Quality. A John Wiley & Sons, Inc. Scholar google search
ICH Harmonised Tripartite Guidelineich Q8 “Pharmaceutical development”. URL: http://gmp-compliance.org/guidemgr/files/3-1-16.pdf. Data base 23.03.2020. Scholar google search
Am Ende D.J. (2014) Production of drugs. Chemical technology from R&D to production. Cambridge Press. Scholar google search
ICH Q6A Guidelines “Specifications: Analytical Procedures and Acceptance Criteria for New Drugs and Drugs — Chemicals”. URL: http://gmp-compliance.org/guidemgr/files/3-1-16.pdf. Data base 23.03.2020. Scholar google search
Beregovyh V.V. (2018) Rukovodstva ICH dlya farmacevticheskoj otrasli. Mezhdisciplinarnye rukovodstva – COP “Professiya”, Sankt-Peterburg, 416 p. Scholar google search
State Pharmacopoeia of the Russian Federation, XIV edition, 2018. Scholar google search
