The phase diagram of the binary medicinal condensed system «Ketoprofen - Phenylbutazone»; anti-inflammatory activity of the binary eutectic system


Cite item

Full Text

Open Access Open Access
Restricted Access Access granted
Restricted Access Subscription or Fee Access

Abstract

The data of phase equilibria of the condensed system «Ketoprofen - Phenylbutazone » are represented according to the results of measurements by the method of the differential scanning calorimetry (DSC) in the heating mode. It is established that the eutectic system reters to the eutectic systems with restricted (partial) mutual solubility in the solid state. Congruent equilibrium for this system is implemented at a ratio of 60:40% mol. (55,3:44,7% of mass.) of Ketoprofen and Phenylbutazone respectively. Melting point of the eutectic structure is 68 °C. Data shows the phase diagram of a system melting state. Preclinical tests of antiinflammatory activity were carried out on model of acute exudative inflammation (carrageenan edema of rats paw) on white outbred rats in comparative option with the use of: substances of Phenylbutazone, substance of Ketoprofen, mix of Phenylbutazone and Ketoprofen in the ratio 1:1 mol. and the eutectic system «Ketoprofen - Phenylbutazone». The results of experiments showed that the anti-exudative and antiinflammatory activity of the eutectic structure is twice higher than activities of individual components and their mix 1:1 mol. in comparable doses.

Full Text

Restricted Access

About the authors

A. N Seryakova

Samara State Medical University

Email: seryakova_annet@mail.ru
Assistant, Department of Chemistry of Pharmaceutical Faculty

M. L Tkachenko

Samara State Medical University

Email: tka-mikhail@yandex.ru
Ph.D. (Chem.), Associate Professor, Department of chemistry of Pharmaceutical Faculty

Y. V Moschenskyi

Samara State Technical University

Email: yvmos@yandex.ru
Dr.Sc. (Chem.), Professor, Head of Department of Radio Engineering Devices

References

  1. Zalac S., Zahirul M., Khan I., Gabelica V., Tudja M., Mestrovic E., Romih M. Paracetamol-propyphenazone inter action and formulation difficulties associated with eutectic formation in combination solid dosage forms. Chem. Pharm. Bull. 1999; 47:302-307.
  2. Hwang M. Bi, S.-J., Morris K.R. Mechanism of eutectic formation upon compaction and its effects on tablet properties. Thermochim. Acta. 2003; 404:213-226.
  3. Chiarella R.A., Davey R.J., Peterson M.L. Making co-crystals - the utility of ternary phase diagrams. Cryst. Growth Des. 2007; 7:1223-1226.
  4. Ткаченко М.Л., Жнякина Л.Е., Мощенский Ю.В., Лосева М.А., Леванюк И.А. Термические исследования и некоторые технологические свойства тройной лекарственной системы «кофеин-парацетамол-мочевина» // Фармация. 2008. № 2. С. 29-32.
  5. Bonain A. Note au sujet de l’anesthesique local employe en otorhinolaryngologie sous la domination liquide de Bonain. Ann Malad Oreille Larynx. 1907; 33:216-217.
  6. Fiala Sarah, Jonesa Stuart A., Brown Marc B. A fundamental investigation into the effects of eutectic formation on transmembrane transport. International Journal of Pharmaceutics. 2010; 393:68-73.
  7. Matsuoka M., Ozawa R. Determination of solid-liquid phase equilibria of binary organic systems by differential scanning calorimetry. J. Cryst. Growth 1989; 96:96-604.
  8. Мощенский Ю.В. Дифференциальный сканирующий калориметр ДСК-500 // Приборы и техника эксперимента. 2003. № 6. С. 143-144.
  9. Аносов В.Я., Озерова М.И., Фиалков Ю.Я. Основы физико-химического анализа. М.: Наука. 1976. С. 125-127.
  10. Руководством по экспериментальному (доклиническому) изучению новых фармакологических веществ» / Под ред. чл.-корр. РАМН проф. Р.У. Хабриева. М.: Медицина. 2005.

Supplementary files

Supplementary Files
Action
1. JATS XML

Copyright (c) 2019 Russkiy Vrach Publishing House

This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies