The study of the physico-chemical properties of the substance efavirenz

S. A Zolotov; Золотов С. А; E. S Ponomarev; Пономарев Е. С; I. A Dain; Даин И. А; N. B Demina; Демина Н. Б; A. S Zolotova; Золотова А. С; V. M Retivov; Ретивов В. М; G. A Buzanov; Бузанов Г. А

doi:10.29296/25877313-2022-02-04

The study of the physico-chemical properties of the substance efavirenz

Authors: Zolotov S.A¹, Ponomarev E.S¹, Dain I.A¹, Demina N.B², Zolotova A.S¹, Retivov V.M³, Buzanov G.A⁴
Affiliations:
1. AMEDART LLC
2. I.M. Sechenov First Moscow State Medical University of the Ministry of Healthcare of the Russian Federation (Sechenov University)
3. National Research Center "Kurchatov Institute"
4. Institute of General and Inorganic Chemistry n.a. N.S. Kurnakov of RAS (IONC RAS)
Issue: Vol 25, No 2 (2022)
Pages: 24-29
Section: Articles
URL: https://journals.eco-vector.com/1560-9596/article/view/112932
DOI: https://doi.org/10.29296/25877313-2022-02-04
ID: 112932

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Abstract

The aim of the work was to study the physicochemical properties of the domestic active pharmaceutical substance efavirenz produced by AMEDART LLC of the Russian Federation. Modern methods are used: differential scanning calorimetry, X-ray powder diffraction, spectral emission microscopy, high performance liquid chromatography, etc. The melting point, lipophilicity coefficient, wave numbers, shape and size of crystal particles, solubility in the biological pH range and in some organic solvents were determined. It has been established that the studied API has a minimum endothermic peak in the region of 140°C, the obtained lipophilicity coefficient is 4.67, it is practically insoluble in aqueous media in the biological pH range, but it is well soluble in most polar organic solvents, such as: methanol, ethyl alcohol, acetone and tetrahydrofuran, has a crystalline structure in the form of sticks from 3 to 18 microns and irregularly shaped particles from 1 to 7 microns in size, as well as wave numbers - angles of 6.1, 6.4, 10.4, 11.0, 12.3, 13.3, 14.2, 16.9, 20.1, 21.3, 24.9. DSC, IR spectrometry and X-ray powder diffraction data showed that the substance is a polymorph form I.

Keywords

efavirenz, solubility, lipophilicity, polymorphism

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References

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