Pub Date : 2023-11-11DOI: 10.33380/2305-2066-2023-12-4-1521
L. V. Kovalenko, A. G. Polivanova, A. P. Ilyin, I. N. Solovieva, E. I. Gorbacheva, M. S. Oshchepkov
Introduction. Retinoids are a group of endogenous and synthetic substances that regulate numerous important biological processes in normal development. The synthesis and study of the biological activity of new retinoids are a promising area of chemical biology. Text. The genomic functions of retinoids are mediated by their nuclear receptors RAR(α, β, γ) and RXR(α, β, γ), which regulate gene transcription by recruiting corepressors and coactivators. Retinoids also possess non-genomic functions by acylating proteins and other biomolecules. Regenerative medicine and stem cell biology are advanced areas of research in the biological activity of retinoids. Endogenous and synthetic retinoids are used for the treatment of skin pathologies and in oncology. There is evidence of their potential use in the therapy of lung diseases. The development of retinoids with high selectivity towards specific receptors and tissues may open new approaches to the treatment and prevention of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and others. Retinoids are necessary for the functioning of the immune system and are powerful immunomodulators. Additionally, retinoids have the potential for the therapy of various proliferative diseases. Conclusion. Long-term studies of the pharmacological activity of retinoic acid and its structural analogs aim to investigate and establish the precise mechanisms of their actions, as well as their involvement in the pathogenesis of various diseases. The synthesis of retinoids aims to design compounds with high selectivity towards specific receptors, which would exclude the multitarget action of natural regulatory molecules and the associated side effects. Synthetic retinoids devoid of teratogenic and other side effects can find application as therapeutic agents for the treatment of metabolic disorders, various malignancies, as well as kidney, lung, and CNS diseases. Furthermore, the development of prodrugs based on retinoids with controlled release of active molecules is also a promising direction in this field of medicinal chemistry.
{"title":"Medicinal Perspectives of Retinoids (Review)","authors":"L. V. Kovalenko, A. G. Polivanova, A. P. Ilyin, I. N. Solovieva, E. I. Gorbacheva, M. S. Oshchepkov","doi":"10.33380/2305-2066-2023-12-4-1521","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1521","url":null,"abstract":"Introduction. Retinoids are a group of endogenous and synthetic substances that regulate numerous important biological processes in normal development. The synthesis and study of the biological activity of new retinoids are a promising area of chemical biology. Text. The genomic functions of retinoids are mediated by their nuclear receptors RAR(α, β, γ) and RXR(α, β, γ), which regulate gene transcription by recruiting corepressors and coactivators. Retinoids also possess non-genomic functions by acylating proteins and other biomolecules. Regenerative medicine and stem cell biology are advanced areas of research in the biological activity of retinoids. Endogenous and synthetic retinoids are used for the treatment of skin pathologies and in oncology. There is evidence of their potential use in the therapy of lung diseases. The development of retinoids with high selectivity towards specific receptors and tissues may open new approaches to the treatment and prevention of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and others. Retinoids are necessary for the functioning of the immune system and are powerful immunomodulators. Additionally, retinoids have the potential for the therapy of various proliferative diseases. Conclusion. Long-term studies of the pharmacological activity of retinoic acid and its structural analogs aim to investigate and establish the precise mechanisms of their actions, as well as their involvement in the pathogenesis of various diseases. The synthesis of retinoids aims to design compounds with high selectivity towards specific receptors, which would exclude the multitarget action of natural regulatory molecules and the associated side effects. Synthetic retinoids devoid of teratogenic and other side effects can find application as therapeutic agents for the treatment of metabolic disorders, various malignancies, as well as kidney, lung, and CNS diseases. Furthermore, the development of prodrugs based on retinoids with controlled release of active molecules is also a promising direction in this field of medicinal chemistry.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"9 9","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135042718","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 : 2023-11-10DOI: 10.33380/2305-2066-2023-12-4-1573
Yu. E. Generalova, I. I. Terninko, A. B. Zelentsova
Introduction. For tablets “Malоben, 60 mg” and “Etmaben, 300 mg”, permission was received to conduct phase I clinical trials, so they required a full cycle of research and standardization. Aim. Development of a unified analytical procedure for the determination of related impurities in samples (RS, API, FPP) of Malоben and Ethmaben. Materials and methods. RSs were obtained at the Department of Organic Chemistry of the St. Petersburg State Chemical and Pharmaceutical University; the synthesis of APIs and the production of FPP were carried out on an industrial scale in pharmaceutical production. The studies were carried out on a Flexar liquid chromatograph (PerkinElmer, USA), equipped with a pump (formation of a gradient on the low-pressure side), an autosampler, a column thermostat, a UV detector and a chromatographic column Intersil® ODS-3V, 5 µm, 100 Å, 250 × 4, 6 (Phenomenex, Japan). Results and discussion. In the research, uniform optimal chromatographic conditions were selected using the HPLC method to determine the RP in RS, API and FPP of Maloben and Ethmaben. Column C18 250×4.6 mm, mobile phase 0.1% phosphoric acid and acetonitrile (gradient elution), flow rate 1 ml/min, sample volume 10 µl, UV detector (270 nm). They were validated in terms of specificity, linearity, detection limit, precision, robustness, and solution stability. Analytical concentration levels were selected for the formation of draft regulatory documents. Using the developed analytical technique, samples of RS, API and tablets of malоben and ethmaben were analyzed. Conclusion. A full cycle of research was carried out, an analytical methodology was developed and related impurities were identified in RS, API and FPP of Maloben and Ethmaben.
{"title":"End-to-end Standardization of Original Medicines when Determining Related Impurities","authors":"Yu. E. Generalova, I. I. Terninko, A. B. Zelentsova","doi":"10.33380/2305-2066-2023-12-4-1573","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1573","url":null,"abstract":"Introduction. For tablets “Malоben, 60 mg” and “Etmaben, 300 mg”, permission was received to conduct phase I clinical trials, so they required a full cycle of research and standardization. Aim. Development of a unified analytical procedure for the determination of related impurities in samples (RS, API, FPP) of Malоben and Ethmaben. Materials and methods. RSs were obtained at the Department of Organic Chemistry of the St. Petersburg State Chemical and Pharmaceutical University; the synthesis of APIs and the production of FPP were carried out on an industrial scale in pharmaceutical production. The studies were carried out on a Flexar liquid chromatograph (PerkinElmer, USA), equipped with a pump (formation of a gradient on the low-pressure side), an autosampler, a column thermostat, a UV detector and a chromatographic column Intersil® ODS-3V, 5 µm, 100 Å, 250 × 4, 6 (Phenomenex, Japan). Results and discussion. In the research, uniform optimal chromatographic conditions were selected using the HPLC method to determine the RP in RS, API and FPP of Maloben and Ethmaben. Column C18 250×4.6 mm, mobile phase 0.1% phosphoric acid and acetonitrile (gradient elution), flow rate 1 ml/min, sample volume 10 µl, UV detector (270 nm). They were validated in terms of specificity, linearity, detection limit, precision, robustness, and solution stability. Analytical concentration levels were selected for the formation of draft regulatory documents. Using the developed analytical technique, samples of RS, API and tablets of malоben and ethmaben were analyzed. Conclusion. A full cycle of research was carried out, an analytical methodology was developed and related impurities were identified in RS, API and FPP of Maloben and Ethmaben.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"96 12","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135091432","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 : 2023-11-10DOI: 10.33380/2305-2066-2023-12-4-1592
A. M. Katsev, S. L. Safronyuk, Y. V. Burtseva, S. Y. Osmanova
Introduction. Currently, the search for new antibacterial substances is an urgent task due to the growing resistance of pathogens to existing antibiotics. One of the key directions in this area is the expansion of scientific research of medicinal plants, as new sources of therapeutic agents. This article examines the possibility of using highly sensitive bioluminescent test bacteria for these purposes, which can quickly detect non-specific antimicrobial activity and can be adapted to highly effective pharmaceutical screening technologies. Aim. To study the applicability of bioluminescent bacteria for the analysis of the antibacterial activity of biologically active substances (BAS) of plant origin. Materials and methods. BAS quercetin, 8-hydroxyquinoline, gallic acid and thymoquinone, which are often found in medicinal plant raw materials and with which its antibacterial properties are associated, were used in the work. Bacteria with constitutive bioluminescence Aliivibrio fischeri F1 and Escherichia coli (pXen7), as well as recombinant bioreporter strains with inducible luminescence were used as test-objects: E. coli (pRecA-lux), E. coli (pColD-lux), reacting to nucleic acid damage; E. coli (pKatG-lux) and E. coli (pSoxS-lux), sensitive to oxidative stress. Results and discussion. It was found that the nonspecific antimicrobial activity of the studied BAS is manifested in the inhibition of bacterial bioluminescence of test-strains with constitutive glowing. It was noted that the marine test-bacteria A. fischeri F1 have significantly greater sensitivity to the action of BAS, compared with the recombinant strain of E. coli (pXen7). It has been shown that their inhibitory effect begins at concentrations of 2 mcg/ml, and bactericidal activity occurs at concentrations of more than 20 mcg/ml. The results obtained are compared with the data on MIC and MBC of gram(+) and gram(–) pathogens. The study of the induction of bioluminescence of recombinant bioreporter strains showed that the antibacterial effect of the BAS is accompanied by oxidative stress. Also, quercetin caused activation of luminescence in E. coli (pRecA-lux) and E. coli (pColD-lux), which may indicate its participation in damage to nucleic acids. Analysis of the induction factors of bioreporter strains indicates that the revealed mechanisms of antibacterial activity are not major, but may be of a secondary nature. Conclusion. It has been shown that the intensity of the glow of natural and recombinant bioluminescent bacteria can be an indicator of the antibacterial activity of BAS of natural origin. The high sensitivity of A. fischeri F1 bacteria to the action of substances such as quercetin, 8-hydroxyquinoline, gallic acid and thymoquinone has been shown. Considering that bioluminescence analysis is a quantitative instrumental method, it can be easily adapted for high-throughput pharmaceutical screening. It has been shown that the luminescence intensity of natural and recombinant biolumin
{"title":"Could Bioluminescent Bacteria be Used in the Search for New Plant-derived Antibacterial Substances?","authors":"A. M. Katsev, S. L. Safronyuk, Y. V. Burtseva, S. Y. Osmanova","doi":"10.33380/2305-2066-2023-12-4-1592","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1592","url":null,"abstract":"Introduction. Currently, the search for new antibacterial substances is an urgent task due to the growing resistance of pathogens to existing antibiotics. One of the key directions in this area is the expansion of scientific research of medicinal plants, as new sources of therapeutic agents. This article examines the possibility of using highly sensitive bioluminescent test bacteria for these purposes, which can quickly detect non-specific antimicrobial activity and can be adapted to highly effective pharmaceutical screening technologies. Aim. To study the applicability of bioluminescent bacteria for the analysis of the antibacterial activity of biologically active substances (BAS) of plant origin. Materials and methods. BAS quercetin, 8-hydroxyquinoline, gallic acid and thymoquinone, which are often found in medicinal plant raw materials and with which its antibacterial properties are associated, were used in the work. Bacteria with constitutive bioluminescence Aliivibrio fischeri F1 and Escherichia coli (pXen7), as well as recombinant bioreporter strains with inducible luminescence were used as test-objects: E. coli (pRecA-lux), E. coli (pColD-lux), reacting to nucleic acid damage; E. coli (pKatG-lux) and E. coli (pSoxS-lux), sensitive to oxidative stress. Results and discussion. It was found that the nonspecific antimicrobial activity of the studied BAS is manifested in the inhibition of bacterial bioluminescence of test-strains with constitutive glowing. It was noted that the marine test-bacteria A. fischeri F1 have significantly greater sensitivity to the action of BAS, compared with the recombinant strain of E. coli (pXen7). It has been shown that their inhibitory effect begins at concentrations of 2 mcg/ml, and bactericidal activity occurs at concentrations of more than 20 mcg/ml. The results obtained are compared with the data on MIC and MBC of gram(+) and gram(–) pathogens. The study of the induction of bioluminescence of recombinant bioreporter strains showed that the antibacterial effect of the BAS is accompanied by oxidative stress. Also, quercetin caused activation of luminescence in E. coli (pRecA-lux) and E. coli (pColD-lux), which may indicate its participation in damage to nucleic acids. Analysis of the induction factors of bioreporter strains indicates that the revealed mechanisms of antibacterial activity are not major, but may be of a secondary nature. Conclusion. It has been shown that the intensity of the glow of natural and recombinant bioluminescent bacteria can be an indicator of the antibacterial activity of BAS of natural origin. The high sensitivity of A. fischeri F1 bacteria to the action of substances such as quercetin, 8-hydroxyquinoline, gallic acid and thymoquinone has been shown. Considering that bioluminescence analysis is a quantitative instrumental method, it can be easily adapted for high-throughput pharmaceutical screening. It has been shown that the luminescence intensity of natural and recombinant biolumin","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"116 50","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135136619","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 : 2023-11-10DOI: 10.33380/2305-2066-2023-12-4-1523
K. M. Tserkovnaya, E. V. Flisyuk, Ju. M. Kotsur, I. A. Narkevich, I. E. Smekhova, D. Yu. Ivkin, N. V. Filimonova
Introduction. A personalized choice of antihypertensive combinations and doses is one of the promising trend in the field of combination therapy of arterial hypertension (AH). A polypill as a solid gelatin capsule with combination of mini-tablets can be used to realise this concept. Aim. Development of the composition and technology of Amlodipine 2,5 mg and 5 mg film-coated mini-tablets as a polypill-component for the personalized therapy of AH. Materials and methods. Active pharmaceutical ingredient (API) Amlodipine besylate (Glochem Industries Private Ltd., India) and excipients, such as diluent, disintegrant, lubricant, dye and premix for film coating, were used. Norvasc®, 5 mg tablets were used as a reference drug to estimate the release profile of Amlodipine. API and excipients were mixed in a «drunken barrel» mixer DGN-II (Shanghai Unique Machinery Technology Co., Ltd., China); mini-tablets were obtained on a DP30A laboratory automatic single-punch tablet press (Beijing Gylongli Sci. & Tech. Co., Ltd., China); film coatings on mini-tablets-cores were applied by using a BGB-1 laboratory machine (Chongqing Jinggong Pharmaceutical Machinery Co., Ltd., China). Assessment of technological characteristics of API and tablet mixtures and quality control of mini-tablets were conducted by the methods of State Pharmacopoeia of the Russian Federation XIV ed. Results and discussion. As a result of the study, the optimal composition of the excipients of the fillers group (lactose monohydrate, MCC and anhydrous calcium hydrogen phosphate in a ratio of 1 : 1 : 1) for the production of Amlodipine 2,5 mg and 5 mg mini-tablets-cores by direct compression was established. The technology of applying film coatings was developed. The equivalence of the release profiles of Amlodipine from the developed mini-tablets to the release profile of the reference drug was established. Conclusion. The composition and technology of Amlodipine 2,5 mg and 5 mg film-coated mini-tablets as a polypill-component for the personalized therapy of AH were developed.
{"title":"Development of Amlodipine Mini-tablets as a Polypill-component for the Personalized Therapy of Arterial Hypertension","authors":"K. M. Tserkovnaya, E. V. Flisyuk, Ju. M. Kotsur, I. A. Narkevich, I. E. Smekhova, D. Yu. Ivkin, N. V. Filimonova","doi":"10.33380/2305-2066-2023-12-4-1523","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1523","url":null,"abstract":"Introduction. A personalized choice of antihypertensive combinations and doses is one of the promising trend in the field of combination therapy of arterial hypertension (AH). A polypill as a solid gelatin capsule with combination of mini-tablets can be used to realise this concept. Aim. Development of the composition and technology of Amlodipine 2,5 mg and 5 mg film-coated mini-tablets as a polypill-component for the personalized therapy of AH. Materials and methods. Active pharmaceutical ingredient (API) Amlodipine besylate (Glochem Industries Private Ltd., India) and excipients, such as diluent, disintegrant, lubricant, dye and premix for film coating, were used. Norvasc®, 5 mg tablets were used as a reference drug to estimate the release profile of Amlodipine. API and excipients were mixed in a «drunken barrel» mixer DGN-II (Shanghai Unique Machinery Technology Co., Ltd., China); mini-tablets were obtained on a DP30A laboratory automatic single-punch tablet press (Beijing Gylongli Sci. & Tech. Co., Ltd., China); film coatings on mini-tablets-cores were applied by using a BGB-1 laboratory machine (Chongqing Jinggong Pharmaceutical Machinery Co., Ltd., China). Assessment of technological characteristics of API and tablet mixtures and quality control of mini-tablets were conducted by the methods of State Pharmacopoeia of the Russian Federation XIV ed. Results and discussion. As a result of the study, the optimal composition of the excipients of the fillers group (lactose monohydrate, MCC and anhydrous calcium hydrogen phosphate in a ratio of 1 : 1 : 1) for the production of Amlodipine 2,5 mg and 5 mg mini-tablets-cores by direct compression was established. The technology of applying film coatings was developed. The equivalence of the release profiles of Amlodipine from the developed mini-tablets to the release profile of the reference drug was established. Conclusion. The composition and technology of Amlodipine 2,5 mg and 5 mg film-coated mini-tablets as a polypill-component for the personalized therapy of AH were developed.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"117 2","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135136616","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 : 2023-11-10DOI: 10.33380/2305-2066-2023-12-4-1574
I. D. Kasymov, A. L. Marchenko, A. V. Basevich, M. E. Valeeva
Introduction. The article presents the results of a study of the influence of parameters of microcapsulation on the properties of microcapsules obtained by diffusion of an emulsion solvent. The results obtained made it possible to establish optimal parameters of the process, such as the mixing speed, the type of mixing device, the volume of the aqueous phase, the concentration of the polymer in the oil phase, the ratio of medicinal substance : polymer, temperature conditions. Aim. The aim of the work was to study the influence of the parameters of the microcapsulation process on the properties of microcapsules obtained by diffusion of an emulsion solvent. Materials and methods. Ibuprofen was used as a model substance for microcapsulation. Eudragit® RS 100 was chosen as the carrier polymer. To assess the shape and nature of the microcapsule surface, a microscope Levenhuk D80L LCD was used, and the size of microcapsules was determined using a laser particle analyzer Microsizer 201C (VA Instalt, Russia). Results and discussion. The influence of the parameters of the microcapsulation process on the properties of ibuprofen microcapsules as a model substance obtained by diffusion of an emulsion solvent has been studied. The optimal parameters of the technology are established, the dependences between the critical parameters of microcapsulation and the properties of the resulting microcapsules are determined. Conclusion. In the course of the study, the choice of technological parameters of microcapsulation by diffusion of an emulsion solvent was proposed and justified. The experimental data obtained on the example of ibuprofen as a model substance will be used as the basis of the experiment when preparing microcapsules based on other substances soluble in organic solvents.
{"title":"Influence of Technological Process Parameters on Microcapsulation of Substances with Unsatisfactory Technological Properties","authors":"I. D. Kasymov, A. L. Marchenko, A. V. Basevich, M. E. Valeeva","doi":"10.33380/2305-2066-2023-12-4-1574","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1574","url":null,"abstract":"Introduction. The article presents the results of a study of the influence of parameters of microcapsulation on the properties of microcapsules obtained by diffusion of an emulsion solvent. The results obtained made it possible to establish optimal parameters of the process, such as the mixing speed, the type of mixing device, the volume of the aqueous phase, the concentration of the polymer in the oil phase, the ratio of medicinal substance : polymer, temperature conditions. Aim. The aim of the work was to study the influence of the parameters of the microcapsulation process on the properties of microcapsules obtained by diffusion of an emulsion solvent. Materials and methods. Ibuprofen was used as a model substance for microcapsulation. Eudragit® RS 100 was chosen as the carrier polymer. To assess the shape and nature of the microcapsule surface, a microscope Levenhuk D80L LCD was used, and the size of microcapsules was determined using a laser particle analyzer Microsizer 201C (VA Instalt, Russia). Results and discussion. The influence of the parameters of the microcapsulation process on the properties of ibuprofen microcapsules as a model substance obtained by diffusion of an emulsion solvent has been studied. The optimal parameters of the technology are established, the dependences between the critical parameters of microcapsulation and the properties of the resulting microcapsules are determined. Conclusion. In the course of the study, the choice of technological parameters of microcapsulation by diffusion of an emulsion solvent was proposed and justified. The experimental data obtained on the example of ibuprofen as a model substance will be used as the basis of the experiment when preparing microcapsules based on other substances soluble in organic solvents.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"116 49","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135136620","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 : 2023-11-10DOI: 10.33380/2305-2066-2023-12-4-1577
K. A. Gusev, A. R. Aliev, Yu. E. Generalova, N. А. Aksenova, G. V. Rechkalov, D. N. Maimistov, G. M. Alekseeva, E. V. Flisyuk
Introduction. Ebastine is a second-generation antihistamine drug available in the form of orally disintegrating tablets and film-coated tablets. Ebastine substance exhibits high bioavailability, but low solubility in water and gastrointestinal tract media. The technology of solid dispersions based on polymer carriers by hot melt extrusion is proposed to solve the problem of ebastine low solubility. Aim. Composition development of extrudate and its production technology to create an amorphous solid dispersion of ebastine in oder to increase the recovery rate and bioavailability. Materials and methods. Ebastin micronized (JSC "Active Component", Russia); ebastin crystalline (Arevipharma GmbH, Germany); VIVAPHARM® PVP/VA 64 (JRS Pharma GMbH & Co. KG, Germany). Extrudates were obtained on a HAAKE™ miniCTW co-rotating twin-screw laboratory extruder (Thermo Fisher Scientific, Germany). Extrudates were studied by differential scanning calorimetry, synchronous thermal analysis, powder X-ray diffraction and FTIR-spectroscopy. The quantitative content of the active ingredient was determined by spectrophotometry. The content of related impurities in the amorphous solid dispersion of ebastine was determined by HPLC. Results and discussion. The technology of amorphous solid dispersion of ebastine by hot melt extrusion was developed. The pharmacokinetic properties of ebastine were significantly improved. The process of obtaining solid dispersion with 20 % of ebastine was optimized in order to reduce the content of impurities in the extrudate. Conclusion. The maximum concentration of ebastine for proper quality amorphous solid dispersion based on PVP/VA64 amounted to 20 %. Obtaining a solid dispersion by hot melt extrusion with ebastine content in PVP/VA64 higher than 30 % is impossible because the melt does not possess the glass transition property.
{"title":"Composition and Technology Development for Obtaining Amorphous Solid Dispersion of Ebastine by Hot Melt Extrusion to Increase Dissolution Rate","authors":"K. A. Gusev, A. R. Aliev, Yu. E. Generalova, N. А. Aksenova, G. V. Rechkalov, D. N. Maimistov, G. M. Alekseeva, E. V. Flisyuk","doi":"10.33380/2305-2066-2023-12-4-1577","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1577","url":null,"abstract":"Introduction. Ebastine is a second-generation antihistamine drug available in the form of orally disintegrating tablets and film-coated tablets. Ebastine substance exhibits high bioavailability, but low solubility in water and gastrointestinal tract media. The technology of solid dispersions based on polymer carriers by hot melt extrusion is proposed to solve the problem of ebastine low solubility. Aim. Composition development of extrudate and its production technology to create an amorphous solid dispersion of ebastine in oder to increase the recovery rate and bioavailability. Materials and methods. Ebastin micronized (JSC \"Active Component\", Russia); ebastin crystalline (Arevipharma GmbH, Germany); VIVAPHARM® PVP/VA 64 (JRS Pharma GMbH & Co. KG, Germany). Extrudates were obtained on a HAAKE™ miniCTW co-rotating twin-screw laboratory extruder (Thermo Fisher Scientific, Germany). Extrudates were studied by differential scanning calorimetry, synchronous thermal analysis, powder X-ray diffraction and FTIR-spectroscopy. The quantitative content of the active ingredient was determined by spectrophotometry. The content of related impurities in the amorphous solid dispersion of ebastine was determined by HPLC. Results and discussion. The technology of amorphous solid dispersion of ebastine by hot melt extrusion was developed. The pharmacokinetic properties of ebastine were significantly improved. The process of obtaining solid dispersion with 20 % of ebastine was optimized in order to reduce the content of impurities in the extrudate. Conclusion. The maximum concentration of ebastine for proper quality amorphous solid dispersion based on PVP/VA64 amounted to 20 %. Obtaining a solid dispersion by hot melt extrusion with ebastine content in PVP/VA64 higher than 30 % is impossible because the melt does not possess the glass transition property.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"117 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135136617","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 : 2023-11-07DOI: 10.33380/2305-2066-2023-12-4-1588
D. Yu. Ivkin, M. V. Krasnova, S. V. Okovity, A. A. Karpov, A. A. Kulikov, E. I. Yeletskaya
Introduction. With the emergence of empagliflozin in the pharmaceutical market, there has been an increase in publications on the primary and secondary pharmacodynamics of the drug, and the list of potential indications for the use of this sodium-glucose co-transporter inhibitor is increasing. Hypotheses about pharmacological effects and mechanisms of their implementation are tested both in large-scale clinical studies and in animal experiments. Aim. The purpose of this work was to study the effectiveness of empagliflozin by echocardiographic, histological and molecular biological analyses at the three most significant points of the dynamic transition from acute myocardial infarction to post-infarction chronic heart failure in laboratory male rats. Materials and methods. The experiment was performed on 60 male outbred rats. Myocardial infarction was modeled in narcotic animals by permanent ligation of the left coronary artery. Based on echocardiographic (EchoCG) study data, animals were randomized to two groups: control infarction: untreated pathology group treated with placebo and pathology group treated with empagliflozin 1 mg/kg per os intragastric daily from the first day of the experiment. At 10, 20 and 30 days after the operation, the animals were also subjected to EchoCG testing, and a group of 10 animals from each group were euthanized for histological examination and molecular analysis. Results and discussion. Empagliflozin use in animals after myocardial infarction modeling contributed to a significant increase in myocardial performance on days 10, 20 and 30, reaching a maximum on day 20 (47.58 ± 1.87 %). The drug promotes long-term preservation of the area of damage to the heart muscle with early formation of mature connective tissue, and also increases myocardial resistance to hypoxia by increasing the amount of HIF-1. Conclusion. Based on the studies carried out, it can be concluded that it is possible to use the sodium-glucose cotransporter type 2 empagliflozin in the formation of post-infarction chronic heart failure in the conditions of normoglycemia.
{"title":"Efficacy of Empagliflozin in the Treatment of Experimental Myocardial Infarction","authors":"D. Yu. Ivkin, M. V. Krasnova, S. V. Okovity, A. A. Karpov, A. A. Kulikov, E. I. Yeletskaya","doi":"10.33380/2305-2066-2023-12-4-1588","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1588","url":null,"abstract":"Introduction. With the emergence of empagliflozin in the pharmaceutical market, there has been an increase in publications on the primary and secondary pharmacodynamics of the drug, and the list of potential indications for the use of this sodium-glucose co-transporter inhibitor is increasing. Hypotheses about pharmacological effects and mechanisms of their implementation are tested both in large-scale clinical studies and in animal experiments. Aim. The purpose of this work was to study the effectiveness of empagliflozin by echocardiographic, histological and molecular biological analyses at the three most significant points of the dynamic transition from acute myocardial infarction to post-infarction chronic heart failure in laboratory male rats. Materials and methods. The experiment was performed on 60 male outbred rats. Myocardial infarction was modeled in narcotic animals by permanent ligation of the left coronary artery. Based on echocardiographic (EchoCG) study data, animals were randomized to two groups: control infarction: untreated pathology group treated with placebo and pathology group treated with empagliflozin 1 mg/kg per os intragastric daily from the first day of the experiment. At 10, 20 and 30 days after the operation, the animals were also subjected to EchoCG testing, and a group of 10 animals from each group were euthanized for histological examination and molecular analysis. Results and discussion. Empagliflozin use in animals after myocardial infarction modeling contributed to a significant increase in myocardial performance on days 10, 20 and 30, reaching a maximum on day 20 (47.58 ± 1.87 %). The drug promotes long-term preservation of the area of damage to the heart muscle with early formation of mature connective tissue, and also increases myocardial resistance to hypoxia by increasing the amount of HIF-1. Conclusion. Based on the studies carried out, it can be concluded that it is possible to use the sodium-glucose cotransporter type 2 empagliflozin in the formation of post-infarction chronic heart failure in the conditions of normoglycemia.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"86 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135475998","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 : 2023-11-07DOI: 10.33380/2305-2066-2023-12-4-1576
A. K. Whaley, A. O. Whaley, V. V. Novikova, V. O. Vasiliev, A. V. Klemper, R. I. Lukashov, N. I. Mandrik, N. S. Gurina, G. P. Yakovlev, V. G. Luzhanin
Introduction. The emergence of new strains of microorganisms that are multidrug resistant (MDR) in relation to the antimicrobial drugs used is one of the pressing problems of modern medicine. To prevent an increase in MDR-related deaths, the search for new antibiotics and their introduction into medical practice must be continuously ongoing. Infectious diseases are also accompanied by cell damage and the development of free radical oxidation processes, therefore the search for new antioxidants is also an important task. Considering the powerful biosynthetic potential of basidiomycetes, this group of fungi has every prospect of becoming a new source of biologically active substances in general, as well as antibiotics and antioxidants in particular. Cap mushrooms, represented mainly by basidiomycetes, number about 14,000 species and are an accessible source of raw materials for the search for promising antimicrobial compounds and antioxidants. Aim. Study of the antioxidant and antimicrobial activity of total extracts obtained from cap mushrooms against Escherichia coli , Staphylococcus aureus and Candida albicans and assessment of the suitability of cap mushrooms as a natural source of substances with antimicrobial and antioxidant activity. Materials and methods. The antifungal and antibacterial activity of the extracts was determined by the micromethod of two-fold serial dilutions in a liquid nutrient medium in 96-well plates in duplicate. The study of this type of biological activity was carried out against reference (type) strains Staphylococcus aureus ATCC 6538-P, Escherichia coli ATCC 25922, Candida albicans NCTC 885-653. To study antioxidant activity using DPPH, we used alcoholic extracts from the fruiting bodies of mushrooms obtained by maceration with 96 % ethanol at a ratio of raw materials to extractant of 1 to 8 for 24 hours, an aqueous solution of ascorbic acid (vitamin C) and an ethanol solution of Trolox. Result and discussion. In relation to S. aureus , a representative of gram-positive flora, the studied extracts of cap mushrooms showed low activity, on average about 2500 or 5000 μg/ml. In relation to E. coli , a representative of gram-negative flora, 8 % of the studied cap mushroom extracts showed an average activity of about 1250 μg/ml. The largest number of cap mushroom extracts – 19% of all studied species – showed activity against the yeast micromycete C. albicans . The highest activity against C. albicans was observed in extracts of the mushrooms Cantharellula umbonata with an MIC of 625 μg/ml, Cortinarius olivaceofuscus with an MIC of 625 μg/ml, and Hypomyces chrysospermus with an MIC of 312 μg/ml. During screening of antioxidant activity, the studied extracts were divided into three groups: with high (more than 50 % PPR), medium (from 15 to 50 % PPR) and low (less than 15 %) antioxidant activity. It was shown that the sum of phenolic compounds significantly correlates with the level of antioxidant activity in all three group
{"title":"Antimicrobial and Antioxidant Activity Screening of Mushrooms Growing in the Leningrad Region","authors":"A. K. Whaley, A. O. Whaley, V. V. Novikova, V. O. Vasiliev, A. V. Klemper, R. I. Lukashov, N. I. Mandrik, N. S. Gurina, G. P. Yakovlev, V. G. Luzhanin","doi":"10.33380/2305-2066-2023-12-4-1576","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1576","url":null,"abstract":"Introduction. The emergence of new strains of microorganisms that are multidrug resistant (MDR) in relation to the antimicrobial drugs used is one of the pressing problems of modern medicine. To prevent an increase in MDR-related deaths, the search for new antibiotics and their introduction into medical practice must be continuously ongoing. Infectious diseases are also accompanied by cell damage and the development of free radical oxidation processes, therefore the search for new antioxidants is also an important task. Considering the powerful biosynthetic potential of basidiomycetes, this group of fungi has every prospect of becoming a new source of biologically active substances in general, as well as antibiotics and antioxidants in particular. Cap mushrooms, represented mainly by basidiomycetes, number about 14,000 species and are an accessible source of raw materials for the search for promising antimicrobial compounds and antioxidants. Aim. Study of the antioxidant and antimicrobial activity of total extracts obtained from cap mushrooms against Escherichia coli , Staphylococcus aureus and Candida albicans and assessment of the suitability of cap mushrooms as a natural source of substances with antimicrobial and antioxidant activity. Materials and methods. The antifungal and antibacterial activity of the extracts was determined by the micromethod of two-fold serial dilutions in a liquid nutrient medium in 96-well plates in duplicate. The study of this type of biological activity was carried out against reference (type) strains Staphylococcus aureus ATCC 6538-P, Escherichia coli ATCC 25922, Candida albicans NCTC 885-653. To study antioxidant activity using DPPH, we used alcoholic extracts from the fruiting bodies of mushrooms obtained by maceration with 96 % ethanol at a ratio of raw materials to extractant of 1 to 8 for 24 hours, an aqueous solution of ascorbic acid (vitamin C) and an ethanol solution of Trolox. Result and discussion. In relation to S. aureus , a representative of gram-positive flora, the studied extracts of cap mushrooms showed low activity, on average about 2500 or 5000 μg/ml. In relation to E. coli , a representative of gram-negative flora, 8 % of the studied cap mushroom extracts showed an average activity of about 1250 μg/ml. The largest number of cap mushroom extracts – 19% of all studied species – showed activity against the yeast micromycete C. albicans . The highest activity against C. albicans was observed in extracts of the mushrooms Cantharellula umbonata with an MIC of 625 μg/ml, Cortinarius olivaceofuscus with an MIC of 625 μg/ml, and Hypomyces chrysospermus with an MIC of 312 μg/ml. During screening of antioxidant activity, the studied extracts were divided into three groups: with high (more than 50 % PPR), medium (from 15 to 50 % PPR) and low (less than 15 %) antioxidant activity. It was shown that the sum of phenolic compounds significantly correlates with the level of antioxidant activity in all three group","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"92 2","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135476141","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 : 2023-10-27DOI: 10.33380/2305-2066-2023-12-4-1582
B. A. Peres, A. P. Procyuk, A. B. Zelencova, I. E. Kauhova, M. V. Aroyan, E. K. Novikova
Introduction. Currently, the problem of liver diseases is widespread among the population, especially non-alcoholic fatty liver disease, as well as medicinal liver lesions. In this regard, there is a need to find new solutions in the development of hepatotropic therapy drugs. In clinical practice, several hepatoprotective agents are often used simultaneously in the form of separate drugs or combinations. The combined use of substances in one finished dosage form (FDF) can provide both an enhancement of a particular pharmacological effect and an expansion of the spectrum of hepatotropic action. Components of plant origin are often introduced into the composition of combined hepatoprotectors. Silybum marianum L. fruits contain at least 2.4 % of the amount of flavolignans in terms of silybin, which causes the hepatoprotective effect of medicines based on them and explains the prospects of using this vegetable raw material in the treatment of liver diseases. Aim. Development of technology for obtaining a dry extract of Silybum marianum L. fruit, enriched with silybin. Materials and methods. The objects of the study were Silybum marianum (L.) Gaertn. fruits from producer 2, harvested in June 2022. The quality indicators of the finished product, a dry extract of Silybum marianum (L.) fruit, were determined by the methods described in the SP XIV ed. Statistical processing of the research results was carried out in accordance with SP XIV ed., Volume I, p. 289, GM.1.1.0013.15 "Statistical processing of the results of a chemical experiment". Results and discussion. The optimal method of extraction of medicinal plant raw materials is proposed, which allows to obtain the highest yield of biologically active substances. A method of purification of ethanol-water extraction after extraction is proposed. The technology of dry extract of Silybum marianum (L.) fruit has been developed. Standardization of the obtained dry extract was carried out. Conclusion. In the course of the study, the technology of dry extract of Silybum marianum (L.) fruit was developed. The quality indicators of phytosubstantiation, dry extract of Silybum marianum (L.) fruits enriched with silybin were determined.
{"title":"Development of Technology of Phytosubstantiation of <i>Silybum marianum</i> L. Fruits as a Component of Complex Therapy of Liver Diseases","authors":"B. A. Peres, A. P. Procyuk, A. B. Zelencova, I. E. Kauhova, M. V. Aroyan, E. K. Novikova","doi":"10.33380/2305-2066-2023-12-4-1582","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1582","url":null,"abstract":"Introduction. Currently, the problem of liver diseases is widespread among the population, especially non-alcoholic fatty liver disease, as well as medicinal liver lesions. In this regard, there is a need to find new solutions in the development of hepatotropic therapy drugs. In clinical practice, several hepatoprotective agents are often used simultaneously in the form of separate drugs or combinations. The combined use of substances in one finished dosage form (FDF) can provide both an enhancement of a particular pharmacological effect and an expansion of the spectrum of hepatotropic action. Components of plant origin are often introduced into the composition of combined hepatoprotectors. Silybum marianum L. fruits contain at least 2.4 % of the amount of flavolignans in terms of silybin, which causes the hepatoprotective effect of medicines based on them and explains the prospects of using this vegetable raw material in the treatment of liver diseases. Aim. Development of technology for obtaining a dry extract of Silybum marianum L. fruit, enriched with silybin. Materials and methods. The objects of the study were Silybum marianum (L.) Gaertn. fruits from producer 2, harvested in June 2022. The quality indicators of the finished product, a dry extract of Silybum marianum (L.) fruit, were determined by the methods described in the SP XIV ed. Statistical processing of the research results was carried out in accordance with SP XIV ed., Volume I, p. 289, GM.1.1.0013.15 \"Statistical processing of the results of a chemical experiment\". Results and discussion. The optimal method of extraction of medicinal plant raw materials is proposed, which allows to obtain the highest yield of biologically active substances. A method of purification of ethanol-water extraction after extraction is proposed. The technology of dry extract of Silybum marianum (L.) fruit has been developed. Standardization of the obtained dry extract was carried out. Conclusion. In the course of the study, the technology of dry extract of Silybum marianum (L.) fruit was developed. The quality indicators of phytosubstantiation, dry extract of Silybum marianum (L.) fruits enriched with silybin were determined.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"19 6","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136261499","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 : 2023-10-20DOI: 10.33380/2305-2066-2023-12-4-1526
Ye. V. Burtseva, A. M. Katsev, E. V. Kuldyrkaeva, I. S. Mekhonoshina, L. A. Timasheva, O. A. Pekhova
Introduction. Vegetable raw materials processing products are becoming very popular. Of particular value are the products of essential oil production – aromatic waters or hydrolates. Hydrolates are widely used as cosmetics because they contain a number of biologically active water-soluble components of essential oil, but unlike the latter they have a softer effect on the skin, which allows them to be used in their pure form. Aim. To study the chemical composition, antibacterial and antioxidant activity of hydrolates. Materials and methods. Hydrolates were used as objects of research of production JSC "AEMSZ" derived from plants: Lavandula angusifolia , Hyssоpus officinаlis , Sаlvia officinаlis , Rosmarinus officinalis , Rosa damascеna × Rosa gallica . The composition was analyzed by gas-liquid chromatography. Antibacterial properties of hydrolates were studied with the use of bioluminescent marine bacteria Aliivibrio fischeri F1 and recombinant test-bacteria Escherichia coli MG1655 (pXen7). The study of the antioxidant effect was carried out by the method of Fe 3+ -induced lipid peroxidation of egg lipoprotein suspension in vitro . Results and discussion. It was found that salvia hydrolate contains α- and β-thujone, β-caryophyllene, α-terpineol; lavender hydrolate – camphene, linalool, linalyl acetate, geraniol, geranyl acetate; rosemary hydrolate – camphene, 1,8-cineol, β-pinene; rose hydrolate – phenylethanol, geraniol, citronelol, nerol; hydrolate hyssop – pinocamphone, isopinocamphone, spatulenol, β-caryophyllene. The antibacterial properties of the studied hydrolates were manifested in the inhibition of test bacteria bioluminescence and growth. Hydrolates of hyssop, lavender and rosemary were characterized by the greatest activity, rose and salvia had a lesser effect. It was also shown that hyssop and lavender hydrolates exhibited the bactericidal properties. Through the studying the antioxidant effect, the dynamics of accumulation of products of free-radical oxidation of lipids was observed, which in the presence of hyssop and rosemary hydrolates decreased by 40 and 36 %, respectively, in comparison with the control. Conclusion. As a result of the research, it was found that the studied hydrolates have pronounced antibacterial properties. Antioxidant properties of Hyssopus officinalis and Rosmarinus officinalis hydrolates were also revealed. Prospects for further research are the development of medicinal and cosmetic products based on the hydrolates of the above-stated essential oil cultures.
{"title":"Study of the Chemical Composition and Biological Effects of Aromatic Waters in a Comparative Aspect","authors":"Ye. V. Burtseva, A. M. Katsev, E. V. Kuldyrkaeva, I. S. Mekhonoshina, L. A. Timasheva, O. A. Pekhova","doi":"10.33380/2305-2066-2023-12-4-1526","DOIUrl":"https://doi.org/10.33380/2305-2066-2023-12-4-1526","url":null,"abstract":"Introduction. Vegetable raw materials processing products are becoming very popular. Of particular value are the products of essential oil production – aromatic waters or hydrolates. Hydrolates are widely used as cosmetics because they contain a number of biologically active water-soluble components of essential oil, but unlike the latter they have a softer effect on the skin, which allows them to be used in their pure form. Aim. To study the chemical composition, antibacterial and antioxidant activity of hydrolates. Materials and methods. Hydrolates were used as objects of research of production JSC \"AEMSZ\" derived from plants: Lavandula angusifolia , Hyssоpus officinаlis , Sаlvia officinаlis , Rosmarinus officinalis , Rosa damascеna × Rosa gallica . The composition was analyzed by gas-liquid chromatography. Antibacterial properties of hydrolates were studied with the use of bioluminescent marine bacteria Aliivibrio fischeri F1 and recombinant test-bacteria Escherichia coli MG1655 (pXen7). The study of the antioxidant effect was carried out by the method of Fe 3+ -induced lipid peroxidation of egg lipoprotein suspension in vitro . Results and discussion. It was found that salvia hydrolate contains α- and β-thujone, β-caryophyllene, α-terpineol; lavender hydrolate – camphene, linalool, linalyl acetate, geraniol, geranyl acetate; rosemary hydrolate – camphene, 1,8-cineol, β-pinene; rose hydrolate – phenylethanol, geraniol, citronelol, nerol; hydrolate hyssop – pinocamphone, isopinocamphone, spatulenol, β-caryophyllene. The antibacterial properties of the studied hydrolates were manifested in the inhibition of test bacteria bioluminescence and growth. Hydrolates of hyssop, lavender and rosemary were characterized by the greatest activity, rose and salvia had a lesser effect. It was also shown that hyssop and lavender hydrolates exhibited the bactericidal properties. Through the studying the antioxidant effect, the dynamics of accumulation of products of free-radical oxidation of lipids was observed, which in the presence of hyssop and rosemary hydrolates decreased by 40 and 36 %, respectively, in comparison with the control. Conclusion. As a result of the research, it was found that the studied hydrolates have pronounced antibacterial properties. Antioxidant properties of Hyssopus officinalis and Rosmarinus officinalis hydrolates were also revealed. Prospects for further research are the development of medicinal and cosmetic products based on the hydrolates of the above-stated essential oil cultures.","PeriodicalId":36465,"journal":{"name":"Drug Development and Registration","volume":"35 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135569498","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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