Comparative assessment of the osmotic and anti-inflammatory activity of soft dosage forms of pyrimidine drugs on hydrophilic bases in an experiment

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Abstract

BACKGROUND: Despite the constant search for new medications for local prevention of surgical infection, the problem of purulent-inflammatory complications from postoperative soft tissue wounds remains relevant to this day.

AIM: To experimentally study the osmotic activity and anti-inflammatory properties of the developed xymedone-containing ointment composition levoxycol in comparison with the well-known ointment dioxomethyltetrahydropyrimidine + chloramphenicol (levomekol).

MATERIAL AND METHODS: The anti-inflammatory properties of the ointments were studied in vivo on 60 outbred male Wistar rats, which were divided into three groups, 20 animals each. The first group served as control. In the second group of animals, levomekol ointment was used, in the third group — levoxycol. An assessment of the osmotic activity of the experimental ointment composition levoxycol in comparison with a known drug was carried out in an in vitro experiment. To evaluate the anti-inflammatory activity of ointments, a model of carrageenan-induced edema of rat paws was used. To analyze differences in the frequency of the studied outcomes in groups of animals, the Mann–Whitney U test was used.

RESULTS: Osmotic activity showed that wipes soaked in ointment forms absorbed the following amount of contrast (Me [Q1; Q3]): levomekol — 28.2 (26.4; 31.3) ml; levoxycol — 41.8 (39.5; 43.4) ml (p=0.001). The anti-inflammatory activity of the ointment forms manifested itself in the form of suppression of swelling of the rats' paws at 3 and 5 hours after the injection of carrageenan. When using the ointment form of levomekol, the volume of displaced liquid with the introduction of carrageenan, starting from 3 hours, was 1.8±0.19 ml. When using the ointment form of levoxicol, the amount of displaced liquid when carrageenan was administered, starting from 3 hours, was 1.57±0.16 ml (p=0.013).

CONCLUSION: In vitro experiments have shown that the ointment form of levoxicol has a longer osmotic activity; experimental data in vivo indicated that the use of the developed ointment form of levoxicol, in contrast to the ointment form of levomekol, has a positive effect on the course of inflammatory processes in soft tissues in the first 2–3 hours by reducing the volume of displaced fluid.

About the authors

Alexander G. Izmailov

Kazan State Medical University

Author for correspondence.
Email: izmailov_alex@mail.ru
ORCID iD: 0000-0001-9559-550X
SPIN-code: 1004-4454

MD, Dr. Sci. (Med.), Assoc. Prof., Depart. of General Surgery

Russian Federation, Kazan

Sergey V. Dobrokvashin

Kazan State Medical University

Email: gsurgery1@yandex.ru
ORCID iD: 0000-0002-9817-9816
SPIN-code: 3882-1906

MD, Dr. Sci. (Med.), Prof., Head of Depart., Depart. of General Surgery

Russian Federation, Kazan

Sergey G. Izmailov

City Clinical Hospital No. 7 of Nizhny Novgorod named after E.L. Berezov

Email: izi28082009@yandex.ru
ORCID iD: 0000-0001-7998-9277
SPIN-code: 3984-2070

MD, Dr. Sci. (Med.), Prof., Professor-Consultant

Russian Federation, Nizhny Novgorod

Egor E. Lukoyanychev

City Clinical Hospital No. 7 of Nizhny Novgorod named after E.L. Berezov

Email: egor-lukoyanychev@yandex.ru
ORCID iD: 0000-0001-6392-2692
SPIN-code: 7896-4581

MD, Cand. Sci. (Med.), Assoc. Prof., Consultant

Russian Federation, Nizhny Novgorod

Andrey Yu. Zharinov

City Clinical Hospital No. 7 of Nizhny Novgorod named after E.L. Berezov

Email: zharinov78@yandex.ru
ORCID iD: 0000-0001-9894-8673
SPIN-code: 9904-6140

MD, Cand. Sci. (Med.), Consultant

Russian Federation, Nizhny Novgorod

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Supplementary files

Supplementary Files
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2. Fig. 1. а. General view of laboratory materials used in the experiment to assess the osmotic activity of ointment compositions. Gauze strips are fixed to the tripod at an equal height. Explanations in the text. b. Experiment to evaluate the osmotic activity of ointment compositions. The edge of the gauze strip is immersed in a contrast agent of 0.3% K2Сr2О7; 1 — dry cloth; 2 — hypertonic NaCl solution; 3 — levosmekol ointment; 4 — levoxycol ointment. Explanations in the text

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3. Fig. 2. General view of the experiment to evaluate the osmotic activity of ointment compositions, a diagram of the saturation degree of gauze napkins with contrast 12 hours from the start of the expe­riment. Impregnation of strips with ointments with contrast conti­nues, but the rate of staining of strips with levomekol ointment has noticeably decreased. Explanations in the text

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4. Fig. 3. General view of the experiment to evaluate the osmotic activity of ointment compositions, a diagram of the saturation degree of gauze napkins with contrast 24 hours from the start of the expe­riment. End of the experiment. Explanations in the text

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5. Fig. 4. Volume of displaced fluid at different stages of inflammation (%)

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6. Fig. 5. Changes in the number of leukocytes in the blood of rats under the influence of inflammation and the studied ointment forms

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