Бібліотека Вінницького національного медичного університету ім. М.І.Пирогова

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The reactivity of propyl esters of N-[(2-oxoindolin-3-ylidene)-2-oxiacetyl]amino acids [Текст] / O. M. Svechnikova [et al.] // Вісн. фармації. - 2017. - № 2. - С. 3-6

MeSH-головна:
СТРУКТУРА-АКТИВНОСТЬ, ВЗАИМОСВЯЗЬ -- STRUCTURE-ACTIVITY RELATIONSHIP
ПРОПАНОЛЫ -- PROPANOLS (химия)
ИНДОЛЫ -- INDOLES (химия)
АМИНОКИСЛОТЫ -- AMINO ACIDS (химия)
Анотація: The study of the reactivity of substances allows optimizing the conditions of their synthesis and creating mathematical models of the “structure-biological activity” relationship that enable to carry out the targeted search of compounds with a specified high level of the biological action. Aim. To study the reactivity of propyl esters of N-[(2-oxoindolin-3-ylidene)-2-oxiacetyl]amino acids. Materials and methods. The reactivity of propyl esters of N-[(2-oxoindolin-3-ylidene)-2-oxiacetyl]amino acids was studied in reversible conditions on the model of acid-base equilibria by the method of potentiometric titration. Results and discussion. The ionization constants of 9 propyl esters of N-[(2-oxoindolin-3-ylidene)-2-oxiacetyl]amino acids indicate that these compounds are weak acids. Elongation of the methylene fragments in the amino acid groups of molecules decreases their acidity. In contrast to the length of the methylene fragments their branching and the presence of the substituents do not affect acidity of the esters studied. In the framework of the principle of linearity of free energies the effect of the length of the methylene chain in the amino acid fragment of the molecules of propyl esters of N-[(2-oxoindolin-3-ylidene)-2-oxiacetyl]amino acids was quantitatively assessed by Hammett equation. Conclusions. It has been found that propyl esters of N-[(2-oxoindolin-3-ylidene)-2-oxiacetyl]amino acids have the functions of weak monobasic acids. Elongation of the polymethylene chain weakens ionization. The low sensitivity of the reaction center to elongation of the methylene chain has been identified
Дод.точки доступу:
Svechnikova, O. M.
Kolisnyk, S. V.
Vinnyk, O. F.
Kolisnyk, O. V.

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Determination of related impurities in glimepiride tablets by the HPLC method [Текст] / N. O. Savina [et al.] // Вісн. фармації. - 2017. - № 2. - С. 7-12

MeSH-головна:
ГИПОГЛИКЕМИЧЕСКИЕ СРЕДСТВА -- HYPOGLYCEMIC AGENTS (анализ, стандарты)
ТАБЛЕТКИ -- TABLETS (анализ)
ХРОМАТОГРАФИЯ ЖИДКОСТНАЯ -- CHROMATOGRAPHY, LIQUID (методы)
Анотація: Glimepiride is one of the modern and effective drugs that counteract diabetes mellitus type 2. Like other drugs glimepiride must comply with quality standards set by relevant government departments. Aim. To determine the content of related impurities in glimepiride tablets in order to assess the drug quality. Materials and methods. The study was performed by the reversed-phase HPLC with a spectrophotometric detector in the isocratic mode, in the UV-region of the spectrum. To determine impurities the method of comparison with the solution having the known concentration of impurities and the active substance was used. Results and discussion. It has been shown that the drug contains ≤ 0.18 % of identified and unidentified impurities. Conclusions. The purity of the drug complies with the requirements of normative documents
Дод.точки доступу:
Savina, N. O.
Ocherethyana, N. M.
Britsun, V. M.
Ostanina, N. V.

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Tomarovska, L. Yu.
Development of the methods for atomoxetine identification suitable for the chemical and toxicological analysis [Текст] / L. Yu. Tomarovska, S. V. Baiurka, S. A. Karpushyna // Вісн. фармації. - 2017. - № 2. - С. 13-20

Рубрики: Атомоксетин

MeSH-головна:
АНТИДЕПРЕССАНТЫ -- ANTIDEPRESSIVE AGENTS (анализ, выделение и очистка, отравления)
ТОКСИКОЛОГИЯ -- TOXICOLOGY (методы)
Анотація: The cases of acute and lethal poisonings by atomoxetine, an antidepressant, have been registered. Therefore, development of the available and reliable methods for its chemical and toxicological analysis is the topical issue. Aim. To develop the conditions for atomoxetine detection in the presence of a number of its pharmacological and structural analogs when performing the general TLC-screening and identification of the antidepressant by UV spectrophotometry. Materials and methods. Chromatographic mobility of antidepressants in thin sorbent layers was studied in 11 mobile phases, including those recommended by TIAFT, using five types of chromatographic plates. A number of chromogenic reagents was used for visualization. The UV-spectrum of atomoxetine was studied in 0.1 Mol • L-1 solution of hydrochloric acid. Results and discussion. Chromatographic systems with the low correlation of Rf values for atomoxetine that make them suitable for the general TLC-screening have been found. The UV spectrum of atomoxetine in the acid solution had light absorption maxima at wavelengths of 270 (ε = 1300; A11 = 45) and 277 nm. Conclusions. A combined use of three mobile phases: methanol – 25 % ammonia solution (100 : 1.5), cyclohexane – toluene – diethylamine (75 : 15 : 10), and toluene – acetone – 25 % ammonia solution (45 : 45 : 7.5 : 2.5) provides a reliable atomoxetine detection in the presence of a number of its pharmacological and structural analogs when performing the general TLC-screening. The presence of specific light absorption in the UV region of the spectrum for atomoxetine makes the UV spectrophotometry method suitable for identification of the antidepressant in toxicological studies metry method suitable for identification of the antidepressant in toxicological studies
Дод.точки доступу:
Baiurka, S. V.
Karpushyna, S. A.

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Comparison of chromatographic methods of analysis in a thin layer of the sorbent for identification of famotidine in tablets [Текст] / A. V. Myhal [et al.] // Вісн. фармації. - 2017. - № 2. - С. 21-24

MeSH-головна:
ФАМОТИДИН -- FAMOTIDINE (анализ)
ТАБЛЕТКИ -- TABLETS (анализ)
ХРОМАТОГРАФИЯ ТОНКОСЛОЙНАЯ -- CHROMATOGRAPHY, THIN LAYER (использование, методы)
Анотація: Today three national manufacturers produce famotidine tablets, but the SPhU does not contain any monograph for this dosage form. Aim. To verify TLC and study the possibility of using the HPTLC method for identification of famotidine in tablets. Materials and methods. The objects of the study were three batches of famotidine tablets. TLC and HPTLC were used as the methods of the study. Results and discussion. The possibility of using TLC and HPTLC methods for identification of famotidine tablets was confirmed in the study. The main spots of the test solutions corresponded to the size and the Rf value of the main spots of the standard solution. The Rf value for all solutions was 0.5. Conclusions. Thus, TLC as well as HPTLC can be recommended for inclusion to the SPhU; however, HPTLC is more economically advantageous
Дод.точки доступу:
Myhal, A. V.
Marksa, M.
Golovchenko, O. S.
Georgiyants, V. A.
Ivanauskas, L.

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The synthesis of the substituted 4-alkyl/arylsulfonyl-5-amino-3-alkylthiopyrazoles as promising pharmaceutical agents with the antifungal action [Текст] / P. V. Tkachenko [et al.] // Вісн. фармації. - 2017. - № 2. - С. 25-30

MeSH-головна:
ПИРАЗОЛЫ -- PYRAZOLES (химический синтез)
ПРОТИВОГРИБКОВЫЕ СРЕДСТВА -- ANTIFUNGAL AGENTS (химический синтез)
СТРУКТУРА-АКТИВНОСТЬ, ВЗАИМОСВЯЗЬ -- STRUCTURE-ACTIVITY RELATIONSHIP
БИБЛИОТЕКИ МАЛЫХ МОЛЕКУЛ -- SMALL MOLECULE LIBRARIES
Анотація: One of the promising directions for development of antifungal agents is the synthesis of new chemical compounds that can be used as active pharmaceutical ingredients to produce highly effective drugs for the treatment of fungal infestations. Aim. To create the combinatorial library of 4-alkyl/arylsulfonyl-5-amino-3-alkylthiopyrazoles derivatives for the total antimicrobial screening to search for new substances with the antifungal activity, and study their spectral properties. Materials and methods. The methods of organic synthesis, instrumental methods of organic compound analysis were used. Results and discussion. The design of the library of small molecules based on the core structure of 5-aminopirazole has been developed. The useful and effective synthetic scheme for preparing N1-subsituted 4-alkyl/arylsulfonyl-5-amino-3-alkylthiopyrazoles and their acylation products has been proposed and approved. This approach consists of cyclization of substituted alkyl/arylsulfoacetonitriles under the action of hydrazine hydrate with further alkylation and acylation of 5-aminopyrazoles obtained. The total yield of the target products is 50-85 %. The structure of all compounds synthesized has been confirmed using elemental analysis, 1H NMR- and chromato-mass spectrometric methods. Conclusions. The design and the synthetic scheme for obtaining 4-alkyl/arylsulfonyl-5-amino-3-alkiltiopirazoles and products of their chemical modification have been proposed. The compounds synthesized are of certain interest as potential pharmaceutical agents and can be used to develop new antifungal agents
Дод.точки доступу:
Tkachenko, P. V.
Tkachenko, O. V.
Netosova, K. Yu.
Borisov, O. V.
Zhuravel, I. O.

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Slipchenko, G. D.
Development of the methods for spectrophotometric determination of the flavonoid concentration in solution to study bioavailability of the amount of bioactive substances in capsules containing the powder of Scutellaria baikalensis roots and rhizomes [Текст] / G. D. Slipchenko, V. O. Hrudko, O. A. Ruban // Вісн. фармації. - 2017. - № 2. - С. 31-36

MeSH-головна:
ФЛАВОНОИДЫ -- FLAVONOIDS (анализ)
(химия)
КАПСУЛЫ -- CAPSULES
СПЕКТРОФОТОМЕТРИЯ -- SPECTROPHOTOMETRY (использование, методы)
Анотація: Recently, the test “Dissolution”, which allows evaluating bioavailability of active ingredients, has become one of the most important tools in the quality control of new and generic drugs development (“biowaiver” procedure). However, for some drugs the use of classical pharmacopoeia buffer solutions in vitro does not always completely adequately reflect their behavior in vivo. As a solution of this problem the group of biorelevant media, which allow simulating dissolution and adsorption of drugs in the gastrointestinal tract of a patient, has been developed
To develop the methods of spectrophotometric determination of the flavonoid concentration in0.1 M hydrochloric acid solution and biorelevant media FaSSIF and FeSSIF with pH 6.5 and 6.8 calculated with reference to baicalin for further study of bioavailability of hard gelatine capsules containing a finely divided powder of Scutellaria baicalensis roots and rhizomes. Materials and methods. For the studies on bioavailability determination of pharmacologically active substances of a finely divided powder of Scutellaria baicalensis roots and rhizomes the method of absorption spectrophotometry in the ultraviolet and visible regions of the spectrum calculated with reference to baicalin was chosen. Results and discussion. Adsorption spectra of baicalin solutions in 0.1 M hydrochloric acid solution and biorelevant media FaSSIF (pH 6.5) and FeSSIF (pH 6.8) in the range from 230 to 370 nm consist of two absorption bands. The band with the maximum at 276 nm is more intense, while the band in the near ultraviolet region is less intensive, but broader. The use of this maximum for quantification will allow increasing the specificity of the analysis. The analysis of adsorption spectra of the solutions obtained during extraction of the powder from Scutellaria baicalensis roots and rhizomes with 0.1 M hydrochloric acid solution and biorelevant media FaSSIF and FeSSIF with pH 6.5 and pH 6.8 has shown that their structure is virtually the same as the spectral structure of baicalin solutions. In order to test the possible impact of the dissolution media on the total optical density at the analytical wavelength the adsorption spectra of the biorelevant media FaSSIF and FeSSIF with pH 6.5 or 6.8 have been studied. The analysis of the data obtained has shown that the media are really nontransparent in ultraviolet light and have quite intensive absorption in the range of 230-290 nm. The absorbance testing of baicalin solutions in 0.1 M hydrochloric acid solution and biorelevant media FaSSIF and FeSSIF with pH 6.5 and pH 6.8 has shown that the dependence is linear and obeys the Beer-Lambert law in the range of the concentration from 0.4 to 3.6-4.0 · 10-3 %. Conclusions. To develop the method for determining the concentration of solutions of pharmacologically active substances while studying bioavailability of capsules containing a finely divided powder of Scutellaria baicalensis roots and rhizomes the adsorption spectra of baicalin in0.1 M hydrochloric acid solution and biorelevant media FaSSIF and FeSSIF with pH of 6.5 and 6 8 have been studied
Дод.точки доступу:
Hrudko, V. O.
Ruban, O. A.

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The study of the chemical composition and the immunomodulatory activity of polysaccharide complexes from Veronica teucrium L. [Текст] / A. P. Osmachko [et al.] // Вісн. фармації. - 2017. - № 2. - С. 37-42

MeSH-головна:
ВЕРОНИКА -- VERONICA (химия)
АДЪЮВАНТЫ ИММУНОЛОГИЧЕСКИЕ -- ADJUVANTS, IMMUNOLOGIC (анализ)
ПОЛИСАХАРИДЫ -- POLYSACCHARIDES (анализ)
Анотація: To determine and study the qualitative composition and the quantitative content of polysaccharide complexes (PsC of V. teucrium flowers, leaves and rhizomes, as well as their effect on the transformation and functional activity of macrophages and their hematogenic precursors. Materials and methods. The PsC of V. teucrium flowers, leaves and rhizomes were obtained by multiple extraction of the plant raw material with water when heating and with the subsequent concentration of combined extracts and their precipitation. Monosaccharides of PsC hydrolyzates were studied by the methods of paper chromatography and spectrophotometry. The immunomodulatory activity of PsC of V. teucrium flowers, leaves and rhizomes was studied in vitro in the reaction of macrophage transformation of mononuclear cells of the peripheral blood. Results and discussion. The yield of the complexes is as follows: in flowers – 8.40 %, in leaves – 5.30 %, in rhizomes – 1.95 %. The qualitative composition and the quantitative content of monosaccharides in the complexes have been determined, and the hydrolysis kinetics of the components has been studied. The results of the in vitro study of the effect of PsC of V. teucrium flowers, leaves and rhizomes on transformation and the functional activity of immune competent cells of the peripheral blood are presented. Conclusions. The yield of polysaccharide complexes of V. teucrium is as follows: in flowers – 8.40 %, in leaves – 5.30 %, in rhizomes – 1.95 %. Monosaccharides of PsC in flowers are presented by galactose, glucose, fructose, arabinose and xylose; in leaves – by glucose and arabinose, there is galactose, fructose, xylose in a minor amount; in rhizomes there is mainly glucose. It has been found that the optimal time for hydrolysis for PsC in flowers and leaves is 60 min; in rhizomes – 150 min. It has been determined that the PsC studied in the dose of 50 μg/ml maximally stimulate the functional activity of immune competent cells; the PsC of V. teucrium flowers in the dose range from 5 to 100 μg/ml possesses the more expressed immunomodulatory activity
Дод.точки доступу:
Osmachko, A. P.
Kovaleva, A. M.
Ilyina, T. V.
Kashpur, N. V.
Koshovyi, O. M.
Komisarenko, A. M.

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Zujkina, S. S.
The pharmacotechnological studies of the phytospecies composition for the complex therapy of mastopathy [Текст] / S. S. Zujkina, L. I. Vishnevska // Вісн. фармації. - 2017. - № 2. - С. 43-47

MeSH-головна:
МАСТОПАТИЯ ФИБРОЗНО-КИСТОЗНАЯ -- FIBROCYSTIC BREAST DISEASE (лекарственная терапия)
РАСТИТЕЛЬНЫЕ ПРЕПАРАТЫ -- PLANT PREPARATIONS
ТЕХНОЛОГИЯ ФАРМАЦЕВТИЧЕСКАЯ -- TECHNOLOGY, PHARMACEUTICAL (методы)

Анотація: Today mastopathy is the most common benign breast disease. It is diagnosed in almost one in four women aged 30 years. In women over 40 different breast pathologies are found in 60 % of cases. Mastopathy that has not been diagnosed in proper time and corrected pharmacologically can be the cause of breast cancer. The urgency of the problem is caused by widespread mastopathy and currently ineffective treatment of this disease. Aim. To study the pharmacotechnological parameters of the medicinal plant raw material (MPRM) in order to create a phytospecies for use in the treatment of mastopathy. Materials and methods. Using the technological research methods according to the State Pharmacopoeia of Ukraine and the method described by P. Vetrov the main technological characteristics of the raw material such as the content of extractive substances, specific density, bulk volume, and bulk density, pore volume, porosity, and free volume of the layer for MPRM under research and the phytospecies developed were studied. The technological parameters of different types of the plant raw material are determined by the following methods given above. The raw material was previously crushed to the particle size of 0.3-0.6 cm by the combined method. The data obtained were processed by the methods of economic and statistical analysis of the treatment results using computer programs. Results and discussion. The main technological parameters of the raw material are moisture, the content of extractive substances, specific density, bulk volume, and bulk density of the raw material, pore volume, porosity and free volume of the layer of the raw material. The results obtained when studying the main technological parameters of MPRM in the composition of the drug developed allow us to determine the optimal ratio between the raw material and the extractant, choose the type and size of packing of the phytospecies. Based on the analysis of the chemical composition and pharmacological properties of active substances of MPRM and the results of the technological studies the composition of the phytospecies for the complex treatment of mastopathy has been developed. The data obtained will serve as a basis for choosing the parameters of extraction and type of packing of a drug. Conclusions. The main pharmacotechnological parameters of the samples of MPRM (parsley leaves, corn silk, cranberry fruits, hop cones, common horsetail herb, rose hips, nettle leaves, stevia herb) and the phytospecies have been determined. The phytospecies developed can be used as a medicated product in the treatment of mastopathy due to the presence of the hormone-regulating, oncoprotective, choleretic, diuretic and immunomodulatory action
Дод.точки доступу:
Vishnevska, L. I.

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Garkusha, M. I.
Analysis of the Ukrainian employer current requirements to the pharmaceutical personnel [Текст] / M. I. Garkusha, R. V. Sahaidak-Nikitiuk, G. A. Gretska // Вісн. фармації. - 2017. - № 2. - С. 48-53

MeSH-головна:
ФАРМАЦЕВТЫ -- PHARMACISTS (организация и управление, психология)
ПРОФЕССИОНАЛЬНАЯ КОМПЕТЕНТНОСТЬ -- PROFESSIONAL COMPETENCE
ФАРМАЦИЯ -- PHARMACY (кадры, организация и управление)
Анотація: The introduction of modern approaches to the management of pharmacy institutions and Good Pharmacy Practice (GPP) requires the special knowledge, skills, and “client orientation” among pharmacy professionals. Aim. To determine the socio-psychological characteristics that a pharmacy professional should have. Materials and methods. To determine the requirements set by employers to pharmacists over 900 topical vacancies for October 2016 provided by pharmacy institutions in Ukraine have been analyzed. The analysis was carried out according to the data of the leading job sites, such as work.ua, rabota.ua, trud.ua, job.i.ua, hh.ua, job.ukr.net. Results and discussion. Based on the analysis of vacancies presented by pharmacy institutions, the requirements of employers to pharmacists have been determined. It has been found that employers still focus on the professionalism of a specialist. The requirements to knowledge and skills that a modern pharmacist should possess have been analyzed. The certain rules that a pharmacy specialist must adhere in his/her professional activities have been determined. The socio-psychological characteristics of pharmacy professionals have been studied. Conclusions. The requirements set by employers to pharmacists in modern conditions have been studied, and the ideal pharmacist portrait has been formed
Дод.точки доступу:
Sahaidak-Nikitiuk, R. V.
Gretska, G. A.

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10.

Tovchiga, O. V.
The effects of goutweed (Aegopodium podagraria L.) preparations on glycemia in intact rats and against the background of metformin [Текст] / O. V. Tovchiga // Вісн. фармації. - 2017. - № 2. - С. 54-62

MeSH-головна:
РАСТЕНИЙ ЭКСТРАКТЫ -- PLANT EXTRACTS (фармакология)
ГИПОГЛИКЕМИЧЕСКИЕ СРЕДСТВА -- HYPOGLYCEMIC AGENTS (фармакология)
Кл.слова (ненормовані):
СНЫТЬ
Анотація: The preparations obtained from goutweed (Aegopodium podagraria L.) are characterized by favorable metabolic effects, including the antidiabetic activity. Aim. To determine the dose dependence of the effect of the extract and the tincture of goutweed on the glucose metabolism in intact rats, to evaluate the metabolic effects and the possibility of the combined use of the goutweed preparations with metformin. Materials and methods. The experiments were conducted on intact rats. The influence of the extract and the tincture of goutweed (per se and combined with metformin) on the basal glycemia and the results of the glucose tolerance test were determined. The metabolic effects which are possibly interrelated (the changes in uric acid and electrolyte exchange) were also studied. Results and discussion. The goutweed tincture exhibits the hypoglycemic action in intact rats after administration of single doses of 0.5; 1.0; 5.0 ml/kg, while the goutweed extract (100; 250; 500 mg/kg and 1.0 g/kg) does not demonstrate this action. The correlation analysis results indicate that certain interrelationship may exist between the effect of the extract on the electrolyte homeostasis and glucose metabolism (though these changes are moderate in intact animals), as well as between the effect of goutweed preparations on uric acid and the glucose exchange. The goutweed tincture in the doses of 0.5 and 1.0 ml/kg does not block the effects of metformin, and does not enhance its effect with the excessive decrease of the blood glucose concentration. The absence of a significant decrease of glycemia after combined administration of the tincture and low doses of metformin may reflect synergoantagonism (however, these phenomena were seen in intact animals, and the dose dependence of the metformin action did not change). In the glucose tolerance test the tincture in the dose of 1.0 ml/kg (but not 0.5 ml/kg) combined with metformin allows reducing its effective dose from 400 mg/kg to 200 mg/kg. Conclusions. Goutweed tincture, in contrast to the extract, shows a dose-dependent hypoglycemic effect and is promising for combined use with metformin
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11.

Tryschuk, N. M.
The effect of benzilic acid derivatives on the pain threshold using the “hot plate” test [Текст] / N. M. Tryschuk, I. V. Kireyev, Kolisnyk S. V., K. M. Sytnik // Вісн. фармації. - 2017. - № 2. - С. 63-66

Рубрики: Бензиловая кислота

MeSH-головна:
АНАЛГЕЗИРУЮЩИЕ СРЕДСТВА -- ANALGESICS (фармакология)
БОЛЕВОЙ ПОРОГ -- PAIN THRESHOLD (действие лекарственных препаратов)
Анотація: The search for new highly effective analgesics is a topical issue of modern pharmacology since drugs currently used in clinical practice do not meet the requirements of efficiency and safety. Aim. To study of the effect of new derivatives of benzilic acid on the pain threshold using the “hot plate” test. Materials and methods. The objects of the study were new derivatives of benzilic acid. Determination of the pain threshold was carried out by the “hot plate” test. The substances studied were introduced orally as aqueous solutions in the dose of 12 mg/kg. The latent periods of the first licking of the paw sole and the first jump were recorded during the study. Results. Six- and seven-membered thienolactames did not show the analgesic activity, and acid benzilic amides yielded far exceeded their activity. Hence, formation of cyclic products led to a decrease of the activity. Introduction of the chlorine atom into molecules also led to the decrease of activity. At the same time, the structural modification of the amide group in thienopyrroles was effective. In the experiment the most active substance was KMS-49 containing the dimethylacetyl group. Another active compound was a derivative of KMS-284 belonging to other chemical group of compounds under study – benzilic acid amides. Conclusions. The most active compounds under research appeared to be KMS-49 and KMS-284 after their introduction the latent period of the first licking of the paw sole increased by 2.2 and 1.6 times, respectively; and the latent period of the first jump – by 2.8 and 2.5 times, respectively, compared to the control group at the significance level p ≤ 0.05
Дод.точки доступу:
Kireyev, I. V.
Kolisnyk S. V.
Sytnik BK. M.

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(Асоціація ЕБНІТ)