Search

Modern medicines for the treatment of wounds are developed on the basis of knowledge about their phase healing. The main principle of wound treatment is the creation and maintenance of a moist environment, stable temperature, absorption of excess exudate, minimization of the risk of sensitization, increased intervals between dressings, easy removal of coatings from the surface of the wound. The implementation of this principle is the basis of our research on the creation of a cryogel – a supermacroporous hydrogel that is formed at subzero temperatures by polymerization of monomers or cryogel formation of oligomers without the use of toxic organic solvents and with controlled textural and structural characteristics. A comprehensive study of cryogels has like theoretical as practical interest, because they can serve as a perspectiving new material in pharmacy for obtaining new medicines. The purpose of our research was to substantiate the composition of the cryogel with lidocaine hydrochloride and decamethoxine based on the conducted pharmacotechnological, physicochemical and biopharmaceutical research methods. Model samples (№№ 1–10) with different contents of lidocaine hydrochloride, decamethoxine, and auxiliary substances were selected as research objects. Pharmacotechnological, physicochemical and biopharmaceutical research methods were used. The technological and biopharmaceutical factors of development pharmaceutical composition in the form of a cryogel with lidocaine hydrochloride and decamethoxine were studied. Based on the results of the research, we found that samples (№№ 1–10) are homogeneous without signs of delamination, no changes are observed (aggregation of particles, sediment, odor). Samples №№ 3, 9 and 10 differ in the presence/absence of API. It was shown that APIs do not affect the absorption capacity of the studied samples. Comparative studies confirm our assumption that the presence of PG in the cryogel increases the absorption of liquid by the samples. The prolongation of the action in the composition depends on the presence of PG in the sample of composition. The prolonged effect of pharmaceutical composition was established. For further research, sample № 10 (lidocaine hydrochloride – 0.4; decamethoxine – 0.03; PVA 15% – 20.0; PG – 10.0) was chosen.

Dental diseases are often accompanied by painful sensations, so usually symptomatic treatment of these pathologies includes local anesthetics, as which we have selected anesthetic of local action – lidocaine hydrochloride. The aim of the research is to substantiate the rational concentration of lidocaine hydrochloride in the composition of the dental gel being developed by pharmacological screening of its model samples. The object of the study is dental gel with tincture "Phytodent" (PJSC “CPP “Red Star”, Ukraine), choline salicylate 80% (Basf Pharma, Switzerland) and lidocaine hydrochloride (Societa Italiana Medicinali Scandicci, Italy). The anesthetic was injected into the gel at various concentrations – 1.0%, 1.5% and 2.0%. The study of local anesthetic/analgesic activity of gel test samples was performed by the Randall-Selitto method using an electronic Pressure Analgesiometer (IITC Life Science, USA). The study was conducted on male rats weighing 190–210 g. The animals were divided into three groups: animals of the 1st group were applied with 2.0% lidocaine hydrochloride gel (sample number 1), the second group – with 1.5% concentration (sample number 2), the third group – with 1.0% lidocaine content (sample number 3). The animal was held in the hands of a researcher, its limb was placed in analgesiometer. Determined the force of pressure in grams, which causes the reaction of the paw pull back / squeal in response to a painful stimulus. Analgesic activity was studied on the model of kaolin edema, which was simulated by sub-planar introduction of kaolin solution (10 mg/ml) in the amount of 0.1 ml/100 grams of body weight (administration under the aponeurosis of the posterior paw). In animals, the initial pain sensitivity was evaluated 1 hour after the introduction of the phlogogenic agent, after which the gel was applied to the foot, and in 1 hour 15 minutes, 1 hour 30 minutes and 2 hours after the exudative edema modelling. Calculated the percentage of change to the initial threshold of tactile sensitivity, as well as the percentage of change to the level of algesia (pain response) 1 hour after the introduction of the phlogogenic agent. Statistical processing of the data was performed using Student's t-criterion. According to the results, pronounced pain syndrome was detected in animals of all three groups 1 hour after the introduction of the phlogogenic agent. The use of gel with 1.0% concentration of lidocaine hydrochloride did not show a significant antinociceptive effect and could be considered as a tendency for analgesia. The pronounced local anesthetic effect was observed with the use of gel test specimens with the anesthetic concentrations of 1.5% and 2.0% after 15 and 30 minutes and lasted for at least 2 hours. The drug developed was compared with the dental gel “Kamistad®” (Stada Arzneimittel AG, Germany), which also contains lidocaine hydrochloride in an amount of 2.0%. Taking into account the fact that reliable statistical differences in the severity of analgesic activity between the test samples of gel number 1 and number 2 were not detected, it can be argued that lower lidocaine concentration 1.5% in the composition of the developed dental gel can be used. In addition, the claimed dental gel exceeded the referent drug "Kamistad®" (Stada Arzneimittel AG, Germany) by the expressiveness of antinociceptive effect.

The technique of the qualitative and quantitative determination of active substances – decamethoxine and lidocaine hydrochloride in a new combination drug for preventing and treating inflammatory diseases of the oral cavity was developed.The aim of the work was to develop a methodology to identify and determine the active pharmaceutical ingredient in the composition of the dental gel.The objects were specimens of the developed dental gel containing lidocaine hydrochloride and decamethoxine. The study was conducted using high performance liquid chromatography (HPLC).The conditions for HPLC chromatographic investigations, providing sufficient selectivity and separation efficiency of the gel components were proposed.It was determined that the content of the dental gel component is within acceptable limits, and metrological characteristics of the method allow to recommend it to control the gel quality. 1 gram of the gel contains: decamethoxine – 0.591 mg/g (at a rate of 0.45–0.55 mg/g), lidocaine hydrochloride – 0.396 mg/g (at a rate of 0.36–0.44 mg/g).Approximate retention time of decamethoxine peak is 18.4 min, lidocaine hydrochloride – 13.5 min. Retention time of the peak of decamethoxine and lidocaine hydrochloride investigational solution and reference solution did not exceed 2%.