THE PHASE DIAGRAM OF THE BINARY MEDICINAL CONDENSED SYSTEM «IBUPROFEN – KETOPROFEN»; ANTIINFLAMMATORY ACTIVITY OF THE EUTECTIC SYSTEM

DOI: https://doi.org/10.29296/25877313-2018-10-06
Issue: 
10
Year: 
2018

A.N. Seryakova Assistant, Department of Chemistry of Pharmaceutical Faculty, Samara State Medical University E-mail: seryakova_annet@mail.ru M.L. Tkachenko Ph.D. (Chem.), Associate Professor, Department of Chemistry of Pharmaceutical Faculty, Samara State Medical University E-mail: tka-mikhail@yandex.ru L.E. Zhnyakina Ph.D. (Pharm.), PHARMACIST-ANALYST, SFHI «Center of Quality Control of Drags of the Samara region» (Samara) E-mail: si5w1245@yandex.ru I.I. Munina Ph.D. (Biol.), Associate Professor, Department of Pharmacology, Samara State Medical University E-mail: munira07@yandex.ru

Non-steroidal anti-inflammatory drugs (NSAIDs) are the most important symptomatic pharmaceuticals of the present. Despite the significant pro-gress achieved in treatment of rheumatic diseases, the variety of nonselective NSAIDs needs expansion including and through the use of the combined pharmaceuticals which could provide fast development of analgetic effect and have satisfactory tolerance. It is possible to consider the eutectic systems of pharmaceutical drugs as combined medicines. The data of phase equilibria of the condensed system «Ketoprofen – Ibufrofen» are represented according to the results of measurements by the method of the differential scanning calorimetry (DSC) in the heating mode. Before measurements the DSK-calorimeter was calibrated according to the high-blank In standard (melting point 156,6 °C) and to the conforming qualification of the Sn standard (melting point 231,9 °C). It is established that the system «Ketoprofen — Ibufrofen» 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 38:62% mol. (43,1:56,9% of mass.) of Ketoprofen and Ibufrofen respectively. Melting point of the eutectic structure is 58 °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 Ibufrofen, substance of Ketoprofen, mix of Ibufrofen and Ketoprofen in the ratio 1:1 mol. and the eutectic system «Ibufrofen — Ketoprofen». The results of experiments showed that the anti-exudative and antiinflammatory activity of the eutectic structure is 60% higher than activities of individual components and their mix 1:1 mol. in comparable doses.

Keywords: 
the differential scanning calorimetry
Ibuprofen
Ketoprofen
the eutectic system
the phase diagram
carraginan
anti-inflammatory activity

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