Pub Date : 2021-07-20DOI: 10.19163/2307-9266-2021-9-2-114-129
E. A. Jain (Korsakova), D. Demchenko, A. Ozerov, M. Makarova, V. Makarov, V. Balabanyan
The aim of the study is to identify 1-[2-(2-benzoylphenoxy) ethyl]-6-methyluracil using various methods of analysis, as well as to study its action mechanism against wild-type and mutant forms of HIV-1 reverse transcriptase (RT).Materials and methods. To characterize the structure of the test substance, a few kinds of analysis (X-ray diffraction, elemental, thermal) as well as a few kinds of spectroscopy (UV, IR, and NMR) have been used. The study of the action mechanism of the compound as a potential drug was carried out by evaluating the inhibitory activity against HIV-1 RT wild-type and its mutant forms corresponding to drug-resistant viral strains.Results. The studies have been carried out to confirm the structure of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil. The UV spectrum has a pronounced absorption maximum when measuring a solution of the substance in tetrahydrofuran at the concentration of 0.10 mg / ml. In the IR spectrum, there are specific bands in the range of 4000-370 cm–1. These factors make it possible to use UV and IR spectra to identify the test compound in the substance. It has also been established that the number and mutual arrangement of functional groups, the integrated intensity of signals in the 1H-NMR spectrum, as well as the structure of the carbon skeleton, correspond to the structure of 1-[2-(2-benzoylphenoxy) ethyl]-6-methyluracil. The results of studying the action mechanism showed that the test compound is an effective inhibitor of wild-type HIV-1 RT with an inhibition constant of 0.2 µM, as well as an enzyme inhibitor (mutation G190A) with an inhibition constant of 8 µM; enzyme (mutation Y181C) with an inhibition constant of 10 µM, as well as a reverse transcriptase (RT) inhibitor (mutation L100I, K103N, V106A) and a double mutant K103N / Y181C with an inhibition constant of more than 20 µM.Conclusion. As a result of the performed X-ray structural, elemental, 1H-NMR and 13C-NMR analyzes, the structure of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil has been confirmed. The possibility of using UV, IR and NMR spectroscopy, as well as thermal analyzes to confirm the authenticity during the verification of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil, has been shown. The developed methods can be used in the quality control and included in the draft of practice guidelines for the investigated substance. The studies of the action mechanism of the compound of HIV-1 RT reverse transcriptase have shown that this compound belongs to the group of non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV-1.
{"title":"CHARACTERISATION AND STUDY OF 1- [2- (2-BENZOYLPHENOXY) ETHYL] -6-METHYLURACIL MECHANISM OF ACTION","authors":"E. A. Jain (Korsakova), D. Demchenko, A. Ozerov, M. Makarova, V. Makarov, V. Balabanyan","doi":"10.19163/2307-9266-2021-9-2-114-129","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-2-114-129","url":null,"abstract":"The aim of the study is to identify 1-[2-(2-benzoylphenoxy) ethyl]-6-methyluracil using various methods of analysis, as well as to study its action mechanism against wild-type and mutant forms of HIV-1 reverse transcriptase (RT).Materials and methods. To characterize the structure of the test substance, a few kinds of analysis (X-ray diffraction, elemental, thermal) as well as a few kinds of spectroscopy (UV, IR, and NMR) have been used. The study of the action mechanism of the compound as a potential drug was carried out by evaluating the inhibitory activity against HIV-1 RT wild-type and its mutant forms corresponding to drug-resistant viral strains.Results. The studies have been carried out to confirm the structure of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil. The UV spectrum has a pronounced absorption maximum when measuring a solution of the substance in tetrahydrofuran at the concentration of 0.10 mg / ml. In the IR spectrum, there are specific bands in the range of 4000-370 cm–1. These factors make it possible to use UV and IR spectra to identify the test compound in the substance. It has also been established that the number and mutual arrangement of functional groups, the integrated intensity of signals in the 1H-NMR spectrum, as well as the structure of the carbon skeleton, correspond to the structure of 1-[2-(2-benzoylphenoxy) ethyl]-6-methyluracil. The results of studying the action mechanism showed that the test compound is an effective inhibitor of wild-type HIV-1 RT with an inhibition constant of 0.2 µM, as well as an enzyme inhibitor (mutation G190A) with an inhibition constant of 8 µM; enzyme (mutation Y181C) with an inhibition constant of 10 µM, as well as a reverse transcriptase (RT) inhibitor (mutation L100I, K103N, V106A) and a double mutant K103N / Y181C with an inhibition constant of more than 20 µM.Conclusion. As a result of the performed X-ray structural, elemental, 1H-NMR and 13C-NMR analyzes, the structure of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil has been confirmed. The possibility of using UV, IR and NMR spectroscopy, as well as thermal analyzes to confirm the authenticity during the verification of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil, has been shown. The developed methods can be used in the quality control and included in the draft of practice guidelines for the investigated substance. The studies of the action mechanism of the compound of HIV-1 RT reverse transcriptase have shown that this compound belongs to the group of non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV-1.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"47 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85888822","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-07-20DOI: 10.19163/2307-9266-2021-9-2-161-169
E. Oganesyan, S. S. Shatokhin
The quantum-chemical parameters of 52 derivatives related to flavanones, flavanonoles, flavones and flavonoles with a phloroglucinic type of the A ring and containing electron-donating substituents in the B ring were studied.The aim is the analysis of the dynamics of changes in the electron density, bond numbers, free valence indices and unsaturation indices on carbon atoms C-7 → C-8 of the vinyl group of the main conjugation chain in relation to the position and number of substituents in the “B” ring and the type of the pharmacological activity.Materials and methods. The quantum-chemical parameters of the 4 analyzed groups of the compounds, have been calculated by the semi-empirical method PM7 (WinMopac 2016 program) on the workstation with an Intel Xeon E5-1620 3.5 GHz processor, 20 GB of RAM.Results and discussion. When comparing the quantum chemical parameters of the analyzed compounds, it was established that when the C-7 → C-8 multiple bond is formed, the free valency and unsaturation indices increase on both carbon atoms of the vinylene group in flavones and flavonols compared to the corresponding flavanones and flavanonols. This is explained by the fact that the value of the bond numbers Nµ on these atoms, on the contrary, decreases (Fµ = 4.732-Nµ). The transition from flavanone to flavone is accompanied by the formation of a vinyl group C-7 → C-8, and therefore both atoms from the sp3-hybridized state go into the sp2-state. The consequence of this transformation is a change in the electronegativity value and an increase in the unsaturation index of C-7 and C-8 atoms: C sp3 = 2.5; Csp2 = 2.8. At the same time, the transition from flavanone to flavone leads to the formation of a conjugated system with the participation of π-electrons of the aromatic system “B”, C-7, C-8 atoms and the carbonyl group, which is commonly called the “main conjugation chain”. These structural changes, namely, the transition from a less oxidized flavanone to a more oxidized flavone, contribute to a decrease in the electron density on C-7 and C-8 atoms, and an increase in the total unsaturation of the molecules in general. Mulliken charges on C-7 of all groups of compounds are characterized by a positive value. As for the carbon atoms of the B fragment, the following features are revealed here: in the presence of one substituent -OH or -OCH3 on the carbon atom to which the substituent is bounded, the Mulliken charge is positive; if there are two substituents in the B ring -OH or -OCH3, as well as two -OCH3 groups, then the carbon atoms bonded to the indicated substituents also have a positive Mulliken charge; in the case of trihydroxy substituted in the C-2, C-3 and C-4 B ring, all three carbon atoms are characterized by a positive Mulliken charge; if there are methoxy groups in positions C-2, C-3 and C-4, then the positive Mulliken charge is concentrated only on C-2 and C-4 atoms, and on C-3 atom this charge has a negative value.Conclusion. The above data on the
{"title":"USING QUANTUM-CHEMICAL PARAMETERS FOR PREDICTING ANTIRADICAL (HO•) ACTIVITY OF RELATED STRUCTURES CONTAINING A CINNAMOIL FRAGMENT. IV. STRUCTURE-ACTIVITY RELATIONSHIP BETWEEN UNSATURATION INDICES AND FLAVONE DERIVATIVES WITH FLOROGLUCIN RING “A”","authors":"E. Oganesyan, S. S. Shatokhin","doi":"10.19163/2307-9266-2021-9-2-161-169","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-2-161-169","url":null,"abstract":"The quantum-chemical parameters of 52 derivatives related to flavanones, flavanonoles, flavones and flavonoles with a phloroglucinic type of the A ring and containing electron-donating substituents in the B ring were studied.The aim is the analysis of the dynamics of changes in the electron density, bond numbers, free valence indices and unsaturation indices on carbon atoms C-7 → C-8 of the vinyl group of the main conjugation chain in relation to the position and number of substituents in the “B” ring and the type of the pharmacological activity.Materials and methods. The quantum-chemical parameters of the 4 analyzed groups of the compounds, have been calculated by the semi-empirical method PM7 (WinMopac 2016 program) on the workstation with an Intel Xeon E5-1620 3.5 GHz processor, 20 GB of RAM.Results and discussion. When comparing the quantum chemical parameters of the analyzed compounds, it was established that when the C-7 → C-8 multiple bond is formed, the free valency and unsaturation indices increase on both carbon atoms of the vinylene group in flavones and flavonols compared to the corresponding flavanones and flavanonols. This is explained by the fact that the value of the bond numbers Nµ on these atoms, on the contrary, decreases (Fµ = 4.732-Nµ). The transition from flavanone to flavone is accompanied by the formation of a vinyl group C-7 → C-8, and therefore both atoms from the sp3-hybridized state go into the sp2-state. The consequence of this transformation is a change in the electronegativity value and an increase in the unsaturation index of C-7 and C-8 atoms: C sp3 = 2.5; Csp2 = 2.8. At the same time, the transition from flavanone to flavone leads to the formation of a conjugated system with the participation of π-electrons of the aromatic system “B”, C-7, C-8 atoms and the carbonyl group, which is commonly called the “main conjugation chain”. These structural changes, namely, the transition from a less oxidized flavanone to a more oxidized flavone, contribute to a decrease in the electron density on C-7 and C-8 atoms, and an increase in the total unsaturation of the molecules in general. Mulliken charges on C-7 of all groups of compounds are characterized by a positive value. As for the carbon atoms of the B fragment, the following features are revealed here: in the presence of one substituent -OH or -OCH3 on the carbon atom to which the substituent is bounded, the Mulliken charge is positive; if there are two substituents in the B ring -OH or -OCH3, as well as two -OCH3 groups, then the carbon atoms bonded to the indicated substituents also have a positive Mulliken charge; in the case of trihydroxy substituted in the C-2, C-3 and C-4 B ring, all three carbon atoms are characterized by a positive Mulliken charge; if there are methoxy groups in positions C-2, C-3 and C-4, then the positive Mulliken charge is concentrated only on C-2 and C-4 atoms, and on C-3 atom this charge has a negative value.Conclusion. The above data on the","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"124 2-3 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78152996","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-24DOI: 10.19163/2307-9266-2021-9-1-98-100
M. Vasin, I. Esaulenko, V. Kukes, V. Petrov, I. Ushakov, A. Khokhlov
On January 1, 2021, Yuri N.Chernov, Doctor of Sciences (Mediсine), Professor, Honored Doctor of the Russian Federation, Academician of the International Human Academy in Aerospace Systems, Corresponding Member of the Russian Academy of Natural Sciences, passed away. Yuri N.Chernov was Honorary Doctor of the State Research and TestInstitute of Military Medicine ofRF Ministry of Defense,a specialist in the field of clinical pharmacology and aerospace radiobiology, Honorary Professor of Voronezh State Medical University n. a. N.N. Burdenko.
2021年1月1日，尤里·切尔诺夫(医学博士)、教授、俄罗斯联邦荣誉博士、国际航天系统人类科学院院士、俄罗斯自然科学院通讯院士)逝世。Yuri n. chernov是国防部国家军事医学研究和测试研究所的荣誉博士，临床药理学和航空航天放射生物学领域的专家，沃罗涅日国立医科大学名誉教授。
{"title":"OBITUARY FOR YURI N. CHERNOV 5 Nov 1937 – 1 Jan 2021","authors":"M. Vasin, I. Esaulenko, V. Kukes, V. Petrov, I. Ushakov, A. Khokhlov","doi":"10.19163/2307-9266-2021-9-1-98-100","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-1-98-100","url":null,"abstract":"On January 1, 2021, Yuri N.Chernov, Doctor of Sciences (Mediсine), Professor, Honored Doctor of the Russian Federation, Academician of the International Human Academy in Aerospace Systems, Corresponding Member of the Russian Academy of Natural Sciences, passed away. Yuri N.Chernov was Honorary Doctor of the State Research and TestInstitute of Military Medicine ofRF Ministry of Defense,a specialist in the field of clinical pharmacology and aerospace radiobiology, Honorary Professor of Voronezh State Medical University n. a. N.N. Burdenko.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86884983","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-23DOI: 10.19163/2307-9266-2021-9-1-84-97
I. Kodonidi, A. Chiriapkin, D. Tworowski
The first of the most successfully implemented nootropic drugs in medical practice is piracetam, which should be attributed to cyclic derivatives of gamma-aminobutyric acid. The production of new piracetam derivatives with high nootropic activity is a promising direction in the development of new neuroprotective drugs.The aim of the study is to predict GABA-ergic and glutamatergic activities of N-acyl derivatives of 2-(2-oxopyrolidin-1-yl)- acetamide by a molecular docking method through the energy analysis of interaction of modeled structures with GABAA and AMPA receptors with their subsequent targeted synthesis.Materials and methods. The objects of the research are new N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide and a virtual model of the GABAA receptor of the Homo sapiens organism with the identification code 6D6U and a three-dimensional model of the AMPA-receptor of the Rattus norvegicus organism with the identification code 3LSF from the RCSB PDB database. The simulated compounds were designed in the HyperChem 8.0.8 program. This program was also used to optimize geometry using the force field of molecular mechanics MM+. Molecular docking was carried out using the Molegro Virtual Docker 6.0.1 program. The preparation of N-acyl derivatives of 2-(2-oxopyrrolidin-1-yl)-acetamide was carried out by the interaction of 2-(2-oxopyrrolidin-1-yl)-acetamide with an excess of the corresponding anhydride under conditions of acid catalysis.Results. Based on the results of molecular docking, a high affinity of all simulated compounds for the binding site of GABAA and AMPA receptors can be estimated. According to the predict, the maximum GABA-ergic activity should be expected for (N-[2-(2-oxopyrrolidin-1-yl)-acetyl]-butyramide. N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide form a more stable complex with amino acid residues Arg207, Phe200, Thr202, Tyr97, Tyr157, Tyr205 and Phe65 of the GABAA receptor binding site than the GABA molecule. In terms of the minimum interaction energy, the N-acyl derivatives of 2-(2-oxopyrrolidin-1-yl)- acetamide are superior to a number of known ligands such as GABA, piracetam, anipiracetam, picamilon and pramiracetam. The tested compounds have also shown a high affinity for the binding site of the AMPA receptor. The leader compound is also the compound PirBut, as in the case of the GABAА receptor.Conclusion. Molecular modeling of the ligands interaction with the active binding site of gamma-aminobutyric acid of the GABAA receptor by molecular docking showed that all virtual N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide can exceed a number of nootropic drugs by activity. In the course of molecular design, a method for predicting a glutamatergic activity for 2-pyrrolidone derivatives has been developed. It suggests a significant nootropic activity for N-[2-(2-oxopyrrolidin-1-yl)- acetamide amides.
{"title":"MOLECULAR DESIGN OF N-ACYL DERIVATIVES OF 2-(2-OXOPYROLIDIN-1-YL)-ACETAMIDE WITH GABA-ERGIC AND GLUTAMATERGIC ACTIVITIES","authors":"I. Kodonidi, A. Chiriapkin, D. Tworowski","doi":"10.19163/2307-9266-2021-9-1-84-97","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-1-84-97","url":null,"abstract":"The first of the most successfully implemented nootropic drugs in medical practice is piracetam, which should be attributed to cyclic derivatives of gamma-aminobutyric acid. The production of new piracetam derivatives with high nootropic activity is a promising direction in the development of new neuroprotective drugs.The aim of the study is to predict GABA-ergic and glutamatergic activities of N-acyl derivatives of 2-(2-oxopyrolidin-1-yl)- acetamide by a molecular docking method through the energy analysis of interaction of modeled structures with GABAA and AMPA receptors with their subsequent targeted synthesis.Materials and methods. The objects of the research are new N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide and a virtual model of the GABAA receptor of the Homo sapiens organism with the identification code 6D6U and a three-dimensional model of the AMPA-receptor of the Rattus norvegicus organism with the identification code 3LSF from the RCSB PDB database. The simulated compounds were designed in the HyperChem 8.0.8 program. This program was also used to optimize geometry using the force field of molecular mechanics MM+. Molecular docking was carried out using the Molegro Virtual Docker 6.0.1 program. The preparation of N-acyl derivatives of 2-(2-oxopyrrolidin-1-yl)-acetamide was carried out by the interaction of 2-(2-oxopyrrolidin-1-yl)-acetamide with an excess of the corresponding anhydride under conditions of acid catalysis.Results. Based on the results of molecular docking, a high affinity of all simulated compounds for the binding site of GABAA and AMPA receptors can be estimated. According to the predict, the maximum GABA-ergic activity should be expected for (N-[2-(2-oxopyrrolidin-1-yl)-acetyl]-butyramide. N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide form a more stable complex with amino acid residues Arg207, Phe200, Thr202, Tyr97, Tyr157, Tyr205 and Phe65 of the GABAA receptor binding site than the GABA molecule. In terms of the minimum interaction energy, the N-acyl derivatives of 2-(2-oxopyrrolidin-1-yl)- acetamide are superior to a number of known ligands such as GABA, piracetam, anipiracetam, picamilon and pramiracetam. The tested compounds have also shown a high affinity for the binding site of the AMPA receptor. The leader compound is also the compound PirBut, as in the case of the GABAА receptor.Conclusion. Molecular modeling of the ligands interaction with the active binding site of gamma-aminobutyric acid of the GABAA receptor by molecular docking showed that all virtual N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide can exceed a number of nootropic drugs by activity. In the course of molecular design, a method for predicting a glutamatergic activity for 2-pyrrolidone derivatives has been developed. It suggests a significant nootropic activity for N-[2-(2-oxopyrrolidin-1-yl)- acetamide amides.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87346105","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-23DOI: 10.19163/2307-9266-2021-9-1-64-72
O. V. Monogarova, A. A. Chaplenko, K. Oskolok
The aim of this study is to develop a universal, rapid and affordable method for the identification of dydrogesterone, troxeru tin, and ademetionine in drugs by multisensor digital colorimetry using a unique two-dimensional code. The developed approach can be applied to rapid detection of counterfeit drugs at the preliminary stage of the analysis (before using more expensive specialized equipment). Materials and methods. To implement the proposed approach, the substances of dydrogesterone (“Abbott Biologicals B.V.”, Netherlands), troxerutin (JSC “Interfarma”, Prague, Czech Republic) and ademetionine (LLC “Farmamed”, Moscow, Russia), troxerutin capsules 300 mg (LLC “Pranafarm”, Samara, Russia), lyophilisate for an intravenous solution and the intramuscular administration “Heptral” ® (ademetionine) 400 mg (“Abbott Laboratories”, GMBH, Germany), tablets “Duphaston” ® (dydro gesterone) 10 mg (“Abbott Healthcare Products B.V.”, Netherlands), were used. A multisensor colorimetry method has been implemented using the following set of 8 sensors (C 1 –C 8 ): an intact solution – a 96% (v/v) aqueous ethanol solution – C 1 ; 1 mM alcoholic solution of anthraquinone green (CAS#4403-90-1) – C 2 ; a 0.2% aqueous solution of 3-methylbenzothiazoli none hydrazone (CAS#1128-67-2) – C 3 ; a 0.2% methyl orange aqueous solution (CAS#547-58-0) – C 4 ; a 1 mM alcoholic solu tion of sulforhodamine B (CAS#3520-42-1) – C 5 ; a 1 mM alcoholic solution of 1-hydroxypyrene (CAS#5315-79-7) – C 6 ; 1 mM alcoholic solution of allura red AC (CAS#25956-17-6) – C 7 ; a 1 mM aqueous solution of iron (III) chloride – C 8 . Transparent flat-bottomed polypropylene plates with 96 cells, with a cell volume of 350 µl (Thermo Fischer Scientific, USA, cat. No. 430341) were used as a base for the chip. For obtaining raster images, an Epson Perfection 1670 office flatbed scanner (CCD-matrix) with a removable cover was used. The obtained digital images of the cells were processed using the ImageJ software (Wayne Rasband, National Institutes of Health, USA; http://imagej.nih.gov/ij) with a 24-bit RGB color model (8 bits per channel). Results. The adequacy of the developed approach was confirmed by the analysis of the above-listed drugs. It has been shown that the results obtained have no statistically significant differences from the values determined by the spectrophotometric method. Conclusion. The possibility of using multisensor digital colorimetry for pharmaceutical analysis has been shown. The devel oped methods for the identification of the active substances can serve as a good supplement to more expensive traditional methods.
{"title":"MULTISENSORY COLORIMETRIC ANALYSIS OF DRUGS DYDROGESTERONE, TROXERUTIN AND ADEMETIONINE USING BARCODES","authors":"O. V. Monogarova, A. A. Chaplenko, K. Oskolok","doi":"10.19163/2307-9266-2021-9-1-64-72","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-1-64-72","url":null,"abstract":"The aim of this study is to develop a universal, rapid and affordable method for the identification of dydrogesterone, troxeru tin, and ademetionine in drugs by multisensor digital colorimetry using a unique two-dimensional code. The developed approach can be applied to rapid detection of counterfeit drugs at the preliminary stage of the analysis (before using more expensive specialized equipment). Materials and methods. To implement the proposed approach, the substances of dydrogesterone (“Abbott Biologicals B.V.”, Netherlands), troxerutin (JSC “Interfarma”, Prague, Czech Republic) and ademetionine (LLC “Farmamed”, Moscow, Russia), troxerutin capsules 300 mg (LLC “Pranafarm”, Samara, Russia), lyophilisate for an intravenous solution and the intramuscular administration “Heptral” ® (ademetionine) 400 mg (“Abbott Laboratories”, GMBH, Germany), tablets “Duphaston” ® (dydro gesterone) 10 mg (“Abbott Healthcare Products B.V.”, Netherlands), were used. A multisensor colorimetry method has been implemented using the following set of 8 sensors (C 1 –C 8 ): an intact solution – a 96% (v/v) aqueous ethanol solution – C 1 ; 1 mM alcoholic solution of anthraquinone green (CAS#4403-90-1) – C 2 ; a 0.2% aqueous solution of 3-methylbenzothiazoli none hydrazone (CAS#1128-67-2) – C 3 ; a 0.2% methyl orange aqueous solution (CAS#547-58-0) – C 4 ; a 1 mM alcoholic solu tion of sulforhodamine B (CAS#3520-42-1) – C 5 ; a 1 mM alcoholic solution of 1-hydroxypyrene (CAS#5315-79-7) – C 6 ; 1 mM alcoholic solution of allura red AC (CAS#25956-17-6) – C 7 ; a 1 mM aqueous solution of iron (III) chloride – C 8 . Transparent flat-bottomed polypropylene plates with 96 cells, with a cell volume of 350 µl (Thermo Fischer Scientific, USA, cat. No. 430341) were used as a base for the chip. For obtaining raster images, an Epson Perfection 1670 office flatbed scanner (CCD-matrix) with a removable cover was used. The obtained digital images of the cells were processed using the ImageJ software (Wayne Rasband, National Institutes of Health, USA; http://imagej.nih.gov/ij) with a 24-bit RGB color model (8 bits per channel). Results. The adequacy of the developed approach was confirmed by the analysis of the above-listed drugs. It has been shown that the results obtained have no statistically significant differences from the values determined by the spectrophotometric method. Conclusion. The possibility of using multisensor digital colorimetry for pharmaceutical analysis has been shown. The devel oped methods for the identification of the active substances can serve as a good supplement to more expensive traditional methods.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"215 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91479957","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-23DOI: 10.19163/2307-9266-2021-9-1-54-63
E. Y. Zagorulko, A. Karavaeva
The aim of the study was to determine the excipients influence on the characteristics of gels with cetylpyridinium chloride and to select the dental gel formulation gelation agents promising for the development of dental gel compositions. Hereby, the properties of the active pharmaceutical ingredient, characteristics of the specific gelation agents, as well as their influence on stability, biopharmaceutical and application properties of gels, were taken into account. Materials and methods. In this study, polymers with various gelation mechanisms were considered. Their compatibility with cetylpyridinium chloride as well as storing kinetic and colloid kinds of stability, pH of aqueous solutions, spreadability and textural properties, a penetration ability by the agar diffusion method, an osmotic activity and rheological properties of the gels, were examined. For a complex evaluation of gel compositions study results, a desirability function was used.Results. Stable homogenous dental gels with cetylpyridinium chloride can be obtained by using 25% poloxamer 407 and 5.0% high molecular weight chitosan as the basis.The addition of poloxamer 188 to high molecular weight chitosan gels can produce stable systems with improved textural characteristics as well as increase their osmotic activity. Agar and low molecular weight chitosan addition significantly decrease, whereas poloxamer188 and various molecular weight polyethyleneglycol increase the osmotic activity of 25 % poloxamer 407 gels which are also characterized by a high penetration ability.Conclusion. A complex evaluation of biopharmaceutical, physicochemical and application properties of the gels made it possible to establish that combinations of poloxamer 407 with polyvinylpyrrolidone, agar, and low molecular weight chitosan, can be recommended as a base for a dental gel with cetylpyridinium chloride.
{"title":"APPROACHES TO THE SELECTION OF EXCIPIENTS FOR DENTAL GEL WITH CETYLPYRIDINIUM CHLORIDE","authors":"E. Y. Zagorulko, A. Karavaeva","doi":"10.19163/2307-9266-2021-9-1-54-63","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-1-54-63","url":null,"abstract":"The aim of the study was to determine the excipients influence on the characteristics of gels with cetylpyridinium chloride and to select the dental gel formulation gelation agents promising for the development of dental gel compositions. Hereby, the properties of the active pharmaceutical ingredient, characteristics of the specific gelation agents, as well as their influence on stability, biopharmaceutical and application properties of gels, were taken into account. Materials and methods. In this study, polymers with various gelation mechanisms were considered. Their compatibility with cetylpyridinium chloride as well as storing kinetic and colloid kinds of stability, pH of aqueous solutions, spreadability and textural properties, a penetration ability by the agar diffusion method, an osmotic activity and rheological properties of the gels, were examined. For a complex evaluation of gel compositions study results, a desirability function was used.Results. Stable homogenous dental gels with cetylpyridinium chloride can be obtained by using 25% poloxamer 407 and 5.0% high molecular weight chitosan as the basis.The addition of poloxamer 188 to high molecular weight chitosan gels can produce stable systems with improved textural characteristics as well as increase their osmotic activity. Agar and low molecular weight chitosan addition significantly decrease, whereas poloxamer188 and various molecular weight polyethyleneglycol increase the osmotic activity of 25 % poloxamer 407 gels which are also characterized by a high penetration ability.Conclusion. A complex evaluation of biopharmaceutical, physicochemical and application properties of the gels made it possible to establish that combinations of poloxamer 407 with polyvinylpyrrolidone, agar, and low molecular weight chitosan, can be recommended as a base for a dental gel with cetylpyridinium chloride.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81052900","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-23DOI: 10.19163/2307-9266-2021-9-1-17-31
A. L. Budantsev, V. Prikhodko, I. V. Varganova, S. Okovityi
Hypericum perforatum L. (St. John’s wort) is a medicinal plant that has been intensively studied by clinicians, pharmacolo-gists, and chemists. It has resulted in the publication of both original articles and a number of reviews devoted to the general spectrum of the biological activity of its extracts and the separate chemical components of this species. Unlike many other known medicinal plants, the pharmacological study of which is accompanied by the establishment of new (or rediscovered) structures of chemical compounds, the dynamics of the present study of H. perforatum is mostly associated with a detailed study of the mechanisms of its therapeutic effect and less with the search for new components. The aim of this work is to review and analyze the data on the biological activity of extracts and individual compounds of Hypericum perforatum L. (Hypericaceae), or St. John’s wort, published in the scientific literature over the past 10 years. Materials and methods. To collect and analyze the information, such electronic databases as PubMed, Scopus, Web of Sci -ence, Google Scholar, and other available resources have been used. The following keywords and word combinations were used for search in the databases for 2010–2020: “ Hypericum perforatum ”, “St. John’s wort”, “the biological activity of St. John’s wort”, “hypericin”, “hyperforin”. Results. The review provides information on antidepressant, neuroprotective, nootropic, anxiolytic activity, antibacterial, cytotoxic, anti-inflammatory properties, analgesic, hypoglycaemic effects, and other types of activity of H. perforatum ex -tracts, as well as individual compounds (hypericin, hyperforin, amentoflavone, and others) isolated from this species. It is well known that the secondary metabolites of St. John’s wort are naphthodianthrons, flavonoids and other phenolic compounds, several classes of lipophilic substances including phloroglucinol derivatives and terpenoids. Apart from extracts and their fractions, the biological activity of photoreactive naphthodianthrone hypericin and hyperforin (a phloroglucinol derivative) has been studied in detail. This review provides an analysis of published data from 2010 to 2020 on the biological activity of St. John’s wort. At the present time H. perforatum is primarily well-known for its antidepressant-like properties, which are confirmed by numerous pharmacological studies and clinical trials. Still there is no consensus on the effective treatment of severe or even moder ate depression with St. John’s wort. This review also provides information on the neuroprotective, nootropic, antiepilep tic, anxiolytic, antimicrobial, antiviral, antiprotozoal, antitumor, cytotoxic, analgesic, anti-inflammatory and other effects of H. perforatum extracts, as well as its individual compounds. Conclusion. Despite the popularity of H. perforatum as a plant with an antidepressant-like activity, intensive research work continues to be carried out to elucidate the molecular m
贯叶连翘(St. John’s wort)是一种药用植物，已被临床医生、药理学家和化学家深入研究。它导致发表了原创文章和一些评论，专门研究其提取物的生物活性的一般谱和该物种的单独化学成分。与许多其他已知的药用植物不同，它们的药理学研究伴随着化合物新结构的建立(或重新发现)，目前对贯叶连珠的动态研究主要与对其治疗作用机制的详细研究有关，而较少与寻找新成分有关。对连翘(Hypericum perforatum L.，金丝桃科)圣约翰草(St. John’s wort, St. John’s wort)近10年来所发表的提取物及单体化合物的生物活性进行了综述和分析。材料和方法。为了收集和分析这些信息，使用了PubMed、Scopus、Web of science、Google Scholar等电子数据库和其他可用资源。在2010-2020年度数据库中检索的关键词和词组合为:贯叶连翘(Hypericum perforatum)、圣约翰草(St. John’s wort)、圣约翰草的生物活性(The biological activity of St. John’s wort)、金丝桃素(hypericin)、hyperperforin。结果。这篇综述提供了有关贯叶连翘的抗抑郁、神经保护、促智、抗焦虑、抗菌、细胞毒性、抗炎、镇痛、降糖作用和其他类型活性的信息，以及从该物种中分离出的个别化合物(金丝桃素、金丝连翘素、阿门托黄酮等)。众所周知，圣约翰草的次生代谢产物是萘醌、黄酮类化合物和其他酚类化合物，以及间苯三酚衍生物和萜类化合物等几类亲脂物质。除提取物及其组分外，还对光反应性萘dianthrone金丝桃素和间苯三酚衍生物金丝桃素的生物活性进行了详细的研究。本文对2010年至2020年发表的有关圣约翰草生物活性的数据进行了分析。目前，贯叶连翘主要以其抗抑郁的特性而闻名，这已被许多药理研究和临床试验所证实。对于用圣约翰草治疗重度甚至中度抑郁症的有效方法，目前还没有达成共识。综述了贯叶连翘提取物的神经保护、促智、抗癫痫、抗焦虑、抗菌、抗病毒、抗原虫、抗肿瘤、细胞毒、镇痛、抗炎等作用及其化合物的研究进展。结论。尽管贯叶连翘作为一种具有抗抑郁活性的植物而广受欢迎，但为了阐明其提取物和个别化合物在神经系统紊乱中的作用的分子机制，人们仍在进行深入的研究工作。研究其抗菌、抗病毒和细胞毒性活性也可能开辟一些广阔的前景，同时确定将圣约翰草用于代谢紊乱、泌尿生殖系统紊乱和其他医学领域的可能性。一磷酸;-人-无色素黑色素瘤-具有1型基序的崩解素样金属蛋白酶8,9;BDNF -脑源性神经营养因子;CaMK-IV -钙/calmod -ulin依赖性蛋白激酶;cAMP -环磷酸腺苷;-淋巴细胞白血病系;COX -环加氧酶;- cAMP元素绑定
{"title":"BIOLOGICAL ACTIVITY OF HYPERICUM PERFORATUM L. (HYPERICACEAE): A REVIEW","authors":"A. L. Budantsev, V. Prikhodko, I. V. Varganova, S. Okovityi","doi":"10.19163/2307-9266-2021-9-1-17-31","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-1-17-31","url":null,"abstract":"Hypericum perforatum L. (St. John’s wort) is a medicinal plant that has been intensively studied by clinicians, pharmacolo-gists, and chemists. It has resulted in the publication of both original articles and a number of reviews devoted to the general spectrum of the biological activity of its extracts and the separate chemical components of this species. Unlike many other known medicinal plants, the pharmacological study of which is accompanied by the establishment of new (or rediscovered) structures of chemical compounds, the dynamics of the present study of H. perforatum is mostly associated with a detailed study of the mechanisms of its therapeutic effect and less with the search for new components. The aim of this work is to review and analyze the data on the biological activity of extracts and individual compounds of Hypericum perforatum L. (Hypericaceae), or St. John’s wort, published in the scientific literature over the past 10 years. Materials and methods. To collect and analyze the information, such electronic databases as PubMed, Scopus, Web of Sci -ence, Google Scholar, and other available resources have been used. The following keywords and word combinations were used for search in the databases for 2010–2020: “ Hypericum perforatum ”, “St. John’s wort”, “the biological activity of St. John’s wort”, “hypericin”, “hyperforin”. Results. The review provides information on antidepressant, neuroprotective, nootropic, anxiolytic activity, antibacterial, cytotoxic, anti-inflammatory properties, analgesic, hypoglycaemic effects, and other types of activity of H. perforatum ex -tracts, as well as individual compounds (hypericin, hyperforin, amentoflavone, and others) isolated from this species. It is well known that the secondary metabolites of St. John’s wort are naphthodianthrons, flavonoids and other phenolic compounds, several classes of lipophilic substances including phloroglucinol derivatives and terpenoids. Apart from extracts and their fractions, the biological activity of photoreactive naphthodianthrone hypericin and hyperforin (a phloroglucinol derivative) has been studied in detail. This review provides an analysis of published data from 2010 to 2020 on the biological activity of St. John’s wort. At the present time H. perforatum is primarily well-known for its antidepressant-like properties, which are confirmed by numerous pharmacological studies and clinical trials. Still there is no consensus on the effective treatment of severe or even moder ate depression with St. John’s wort. This review also provides information on the neuroprotective, nootropic, antiepilep tic, anxiolytic, antimicrobial, antiviral, antiprotozoal, antitumor, cytotoxic, analgesic, anti-inflammatory and other effects of H. perforatum extracts, as well as its individual compounds. Conclusion. Despite the popularity of H. perforatum as a plant with an antidepressant-like activity, intensive research work continues to be carried out to elucidate the molecular m","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"15 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84949418","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-23DOI: 10.19163/2307-9266-2021-9-1-32-53
A. A. Klimenkova, L. N. Geller, A. A. Skripko, L. A. Gravchenko, E. A. Korzhavykh
The aim of the review is to provide an analysis and generalization of the main directions of research in the sphere of pharmaceutical services, and their characteristics associated with the determination of their main development trends.Materials and methods. For the analysis, the information store on the basis of scientific publications by Russian and foreign scientists, devoted to research in the field of pharmaceutical services (PSs), has been used. The search for publications was carried out in the open and accessible sources of the latest twenty years (the retrospective period of 2001-2021), located in scientific and technical libraries of institutions, as well as in electronic databases: Elibrary, Medline / PubMed, Cochrane Library, Scopus, Cyberleninka, Google-academy, J-stage. When forming the information array, the search for publications was carried out according to the following requests: pharmaceutical services (pharmaceutical care services), the provision of pharmaceutical services, the quality of pharmaceutical services. For the conceptualization of the study, 87 scientific publications obtained as a result of information retrieval, have been used.Results. In the course of the study, a logical and structural analysis of the main directions in which research in the field of providing PSs in our country is developing, has been carried out. The main trends in the study of the providing services’ activity in the sphere of drug circulation, are characterized. A comprehensive analysis of the category of "pharmaceutical service" has been carried out. The terminological content of this concept, the groups of features characterizing the economic and social essence of educational institutions have been generalized, and the most characteristic features that make up the structure and content of educational institutions, have been identified. The existing approaches to the development of the nomenclature and types of PSs have been analyzed and the systematization of pharmaceutical works and services using the process approach, have been proposed by the authors.Conclusion. The conducted study indicates the presence of several directions in the development of research in the field of providing PSs, aimed at improving the quality of services for the population in pharmaceutical organizations. However, the most important role in the research is assigned to the study and assessment of the quality of educational institutions, the development of approaches to its optimization. As evidenced by the results of the analysis and generalization, the most successful activity in the provision of services in the field of drug circulation requires the implementation of a process approach and the implementation of Quality Management Systems (QMSs).
{"title":"PHARMACEUTICAL SERVICES: STATUS AND DEVELOPMENT TRENDS","authors":"A. A. Klimenkova, L. N. Geller, A. A. Skripko, L. A. Gravchenko, E. A. Korzhavykh","doi":"10.19163/2307-9266-2021-9-1-32-53","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-1-32-53","url":null,"abstract":"The aim of the review is to provide an analysis and generalization of the main directions of research in the sphere of pharmaceutical services, and their characteristics associated with the determination of their main development trends.Materials and methods. For the analysis, the information store on the basis of scientific publications by Russian and foreign scientists, devoted to research in the field of pharmaceutical services (PSs), has been used. The search for publications was carried out in the open and accessible sources of the latest twenty years (the retrospective period of 2001-2021), located in scientific and technical libraries of institutions, as well as in electronic databases: Elibrary, Medline / PubMed, Cochrane Library, Scopus, Cyberleninka, Google-academy, J-stage. When forming the information array, the search for publications was carried out according to the following requests: pharmaceutical services (pharmaceutical care services), the provision of pharmaceutical services, the quality of pharmaceutical services. For the conceptualization of the study, 87 scientific publications obtained as a result of information retrieval, have been used.Results. In the course of the study, a logical and structural analysis of the main directions in which research in the field of providing PSs in our country is developing, has been carried out. The main trends in the study of the providing services’ activity in the sphere of drug circulation, are characterized. A comprehensive analysis of the category of \"pharmaceutical service\" has been carried out. The terminological content of this concept, the groups of features characterizing the economic and social essence of educational institutions have been generalized, and the most characteristic features that make up the structure and content of educational institutions, have been identified. The existing approaches to the development of the nomenclature and types of PSs have been analyzed and the systematization of pharmaceutical works and services using the process approach, have been proposed by the authors.Conclusion. The conducted study indicates the presence of several directions in the development of research in the field of providing PSs, aimed at improving the quality of services for the population in pharmaceutical organizations. However, the most important role in the research is assigned to the study and assessment of the quality of educational institutions, the development of approaches to its optimization. As evidenced by the results of the analysis and generalization, the most successful activity in the provision of services in the field of drug circulation requires the implementation of a process approach and the implementation of Quality Management Systems (QMSs).","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79334785","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-23DOI: 10.19163/2307-9266-2021-9-1-4-16
A. Amjad
Dendrimers are nanoparticles with unique features including globular 3D shape and nanometer size. The availability of numerous terminal functional groups and modifiable surface engineering permit modification of dendrimer surface with several therapeutic agents, diagnostic moieties and targeting substances.The aim. To enlighten the readers regarding design, development, limitations, challenges and future directions regarding anticancer bio-dendrimers.Materials and methods. The data base was represented by such systems as Medline, Cochrane Central Register of Controlled Trials, Scopus, Web of Science Core Collection, PubMed. gov, Google-Academy. A search was carried out for the following keywords and combinations: Polypropylene imine (PPI); Poly-L-lysine (PLL); polyamidoamine (PAMAM); cancer; drug delivery; dendrimers.Results. High encapsulation of drug and effective passive targeting are also among their therapeutic uses. Herein, we have described latest developments in chemotherapeutic delivery of drugs by dendrimers. For the most part, the potential and efficacy of dendrimers are anticipated to have considerable progressive effect on drug targeting and delivery.Conclusion. The newest discoveries have shown that the dendritic nanocarriers have many unique features that endorse more research and development.
树状大分子是一种具有独特特征的纳米颗粒，包括球形3D形状和纳米尺寸。许多末端官能团的可用性和可修饰的表面工程允许用几种治疗剂、诊断基团和靶向物质修饰树突表面。的目标。对抗癌生物树状大分子的设计、发展、局限性、挑战和未来发展方向进行启发。材料和方法。数据库由Medline、Cochrane Central Register of Controlled Trials、Scopus、Web of Science Core Collection、PubMed等系统代表。州长,Google-Academy。对以下关键词和组合进行了检索:聚丙烯亚胺(PPI);Poly-L-lysine(锁相环);polyamidoamine (PAMAM);癌症;药物输送;dendrimers.Results。药物的高包封性和有效的被动靶向也是它们的治疗用途之一。在此，我们描述了树状大分子在化疗药物递送方面的最新进展。在大多数情况下，预计树状大分子的潜力和功效在药物靶向和给药方面具有相当大的进行性作用。最新的发现表明，树突纳米载体有许多独特的特征，值得进一步的研究和开发。
{"title":"DENDRIMERS IN ANTICANCER TARGETED DRUG DELIVERY: ACCOMPLISHMENTS, CHALLENGES AND DIRECTIONS FOR FUTURE","authors":"A. Amjad","doi":"10.19163/2307-9266-2021-9-1-4-16","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-1-4-16","url":null,"abstract":"Dendrimers are nanoparticles with unique features including globular 3D shape and nanometer size. The availability of numerous terminal functional groups and modifiable surface engineering permit modification of dendrimer surface with several therapeutic agents, diagnostic moieties and targeting substances.The aim. To enlighten the readers regarding design, development, limitations, challenges and future directions regarding anticancer bio-dendrimers.Materials and methods. The data base was represented by such systems as Medline, Cochrane Central Register of Controlled Trials, Scopus, Web of Science Core Collection, PubMed. gov, Google-Academy. A search was carried out for the following keywords and combinations: Polypropylene imine (PPI); Poly-L-lysine (PLL); polyamidoamine (PAMAM); cancer; drug delivery; dendrimers.Results. High encapsulation of drug and effective passive targeting are also among their therapeutic uses. Herein, we have described latest developments in chemotherapeutic delivery of drugs by dendrimers. For the most part, the potential and efficacy of dendrimers are anticipated to have considerable progressive effect on drug targeting and delivery.Conclusion. The newest discoveries have shown that the dendritic nanocarriers have many unique features that endorse more research and development.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"60 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74578173","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-23DOI: 10.19163/2307-9266-2021-9-1-73-83
A. V. Matveev, E. Egorova, E. I. Konyaeva, E. Bekirova, L. A. Adjimamutova
Iron deficiency is the most common micronutrient deficiency worldwide. Prevention and treatment of iron deficiency conditions are some of the most important health problems in many countries of the world. At the same time, the main problems for it remain the timely diagnosis, elimination of the cause, as well as the choice of replacement therapy with iron-containing drugs and correction of adverse reactions (ADR) that occur during their use.The aim. This research aims to study the peculiarities of the development of antianaemic drugs ADRs in patients living in the territory of the Republic of Crimea.Materials and methods. The objects of research were cases of ADR occurrence associated with the use of a group of antianaemic drugs and revealed during the 2009-2018 period in the territory of the Republic of Crimea. The main tasks in the analysis of notification forms were the study of the ADR severity, the causality assessment for suspected drugs and ADRs, as well as analysis of particular problems associated with the use of antianaemic drugs (Drug-related problems, DRP).Results. Iron supplements in combination with other drugs became the leaders in the incidence of ADR among antianaemic drugs (28 cases, 42.4% of all cases of ADR). The largest number of cases was registered in patients aged from 18 to 30 years, with female patients prevailing. Among the clinical manifestations of ADR, the most cases were drug hypersensitivity reactions of varying severity (40 cases) and disorders of the gastrointestinal tract (18 cases). The study of the problems associated with the use of antianaemic drugs made it possible to determine that the highest rates of DRP values were observed with the use of iron preparations for parenteral use and cyanocobalamine. The minimal DRP values were observed when prescribing iron protein succinylate preparations.Conclusion. The basis of pharmacotherapy for various types of anemias is the replenishment of iron and vitamin B12 (cyanocobalamin) depots. The effectiveness of the treatment in these cases largely depends on the patient's adherence to treatment, which is, in turn, depends on the frequency and severity of ADRs that occur during the use of antianaemic drugs.
{"title":"STUDY OF THE SAFETY OF ANTIANEMIC PREPARATIONS BY METHOD OF THE SYSTEM OF PROBLEMS RELATED TO MEDICINAL PREPARATIONS","authors":"A. V. Matveev, E. Egorova, E. I. Konyaeva, E. Bekirova, L. A. Adjimamutova","doi":"10.19163/2307-9266-2021-9-1-73-83","DOIUrl":"https://doi.org/10.19163/2307-9266-2021-9-1-73-83","url":null,"abstract":"Iron deficiency is the most common micronutrient deficiency worldwide. Prevention and treatment of iron deficiency conditions are some of the most important health problems in many countries of the world. At the same time, the main problems for it remain the timely diagnosis, elimination of the cause, as well as the choice of replacement therapy with iron-containing drugs and correction of adverse reactions (ADR) that occur during their use.The aim. This research aims to study the peculiarities of the development of antianaemic drugs ADRs in patients living in the territory of the Republic of Crimea.Materials and methods. The objects of research were cases of ADR occurrence associated with the use of a group of antianaemic drugs and revealed during the 2009-2018 period in the territory of the Republic of Crimea. The main tasks in the analysis of notification forms were the study of the ADR severity, the causality assessment for suspected drugs and ADRs, as well as analysis of particular problems associated with the use of antianaemic drugs (Drug-related problems, DRP).Results. Iron supplements in combination with other drugs became the leaders in the incidence of ADR among antianaemic drugs (28 cases, 42.4% of all cases of ADR). The largest number of cases was registered in patients aged from 18 to 30 years, with female patients prevailing. Among the clinical manifestations of ADR, the most cases were drug hypersensitivity reactions of varying severity (40 cases) and disorders of the gastrointestinal tract (18 cases). The study of the problems associated with the use of antianaemic drugs made it possible to determine that the highest rates of DRP values were observed with the use of iron preparations for parenteral use and cyanocobalamine. The minimal DRP values were observed when prescribing iron protein succinylate preparations.Conclusion. The basis of pharmacotherapy for various types of anemias is the replenishment of iron and vitamin B12 (cyanocobalamin) depots. The effectiveness of the treatment in these cases largely depends on the patient's adherence to treatment, which is, in turn, depends on the frequency and severity of ADRs that occur during the use of antianaemic drugs.","PeriodicalId":20025,"journal":{"name":"Pharmacy & Pharmacology","volume":"17 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73581622","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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