ScienceRise: Pharmaceutical Science最新文献

{"title":"Preparation and evaluation of lipid matrix microencapsulation for drug delivery of azilsartan kamedoxomil","authors":"F. Rahi, M. Ameen, Krar Kadhim Mohammed Jawad","doi":"10.15587/2519-4852.2022.270306","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.270306","url":null,"abstract":"The aim of the work is to consolidate azilsartan-kamedoxomil (AZM) into lipid matrix controlled-release microparticles to enhance its permeability because AZM belongs to Biopharmaceutical classification (BCS) IV which characterized by poor permeability and to protect AZM from light and humidity and execute a prolonged release profile. \u0000Materials and methods. A reversed-phase HPLC method was created and validated to estimate the drug. AZM microparticles formulations were invented using melt dispersion technique and waxy materials such as carnuba wax, beeswax, stearic acid in the ratio of waxy-substance: drug ranging from 0.25: 1 to 1:1 and stabilizer namely; tween 80 and Poloxamer 407 in ratio of stabilizer: drug ranging from 0.5:1 to 1:1. Azilsartan formulations were assessed for azilsartan-medoxomil content, loading, entrapment efficiency, the zeta potential,the particle size, the morphology by scanning electronic microscopy (SEM), and in-vitro release profile. \u0000Results. Zeta potential results for microparticle formulations using beeswax and carnuba range from -21.1 mV to -26.6 mV and -20.6 mV to -26.7 mV, respectively. This difference indicates that the azilsartan microparticles containing stearic acid are better stabilized with zeta potential of 25.3 - 29.7 mV. Furthermore, the release from azilsartan microparticle formulations containing stearic acid exceeded 80 % after 8 h and remained for 24 h while release from beeswax did not exceed 65 % after the same period and less than 60 % in case of carnuba formulations \u0000Conclusions. The formulation (AZSP4) exhibited the highest zeta potential and released exceeding 80 % of AZM over the course of 8 hours and remained over a day. AZSP4 microparticles formulation containing, poloxamer 407, in a 0.8:0.8:1 drug: stearic acid: poloxamer ratio proved the ability of stearic acid microencapsulation employing poloxamer as stabilizer in a certain ratio can prolong the release of AZM","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"118 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74918998","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}

{"title":"Development of the spectrophotometric method for the determination of metoprolol in tablets by using bromophenol blue","authors":"M. Horyn, Liubomyr Kryskiw, T. Kucher, O. Poliak, N. Zarivna, Hryhorii Zahrychuk, D. Korobko, K. Peleshok, L. Logoyda","doi":"10.15587/2519-4852.2022.270311","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.270311","url":null,"abstract":"The aim of the work was to develop a simple, economical and eco-friendly spectrophotometric method for determining metoprolol tartrate in tablets based on the reaction with bromophenol blue (BPB). \u0000Material and methods: A double–beam Shimadzu UV-Visible spectrophotometer, with a spectral bandwidth of 1 nm wavelength accuracy ±0.5 nm, Model –UV 1800 (Japan), Software UV-Probe 2.62, and a pair of 1 cm matched quartz cells, was used to measure the absorbance of the resulting solution. All the chemicals were used in analytical reagent grade. Pharmacopeial standard samples of metoprolol tartrate and bromophenol blue (BPB) were provided by Sigma-Aldrich (≥ 98%, HPLC). The used dosage forms of metoprolol tartrate are tablets of Metoprolol 50 mg and 100 mg. \u0000Results and discussion: The method of spectrophotometric determination of the quantitative content of metoprolol tartrate based on its reaction with BPB in a methanol solution has been developed. The stoichiometric ratios of the reactive components as 1:1 were obtained by the methods of continuous changes and the saturation method. The developed method of quantitative determination of metoprolol tartrate was validated. The linearity regression equation was y = 0.0373x + 0.0038, and the obtained correlation coefficient was R2=0.9984. A linear relationship was found between absorbance at λmax and concentration of metoprolol tartrate in the range of 9.56-15.02 µg/mL. The LOD and LOQ values were calculated to be 0.81 µg/mL and 2.67 µg/mL. \u0000Conclusions. A simple, economical and eco-friendly spectrophotometric method has been developed for the quantitative determination of metoprolol tartrate in tablets based on the reaction with BPB. The developed method of quantitative determination of metoprolol tartrate was validated in accordance with the requirements of SPhU. We suggest our work with offered detailed and successful solutions for the mentioned aim with less sophisticated equipment for QC lab for routine manufacturing control","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"38 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81469592","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}

{"title":"Justification of the composition and technology of combined tablets for the treatment of type II diabetes.","authors":"A. Kotvitska, O. Ruban, A. Volkova, I. Kovalevska, N. Kononenko, V. Chikitkina","doi":"10.15587/2519-4852.2022.271046","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.271046","url":null,"abstract":"The aim. The aim of the work was to establish the feasibility of development, determine the optimal composition and technology, and confirm the pharmacological effectiveness of combined tablets for treating type II diabetes. \u0000Materials and methods. Analytical research of the pharmaceutical market of drugs used for the treatment of type II diabetes was carried out using content analysis of official sources of information. The subjects of the study were medicinal products used to treat type II diabetes. A set of physicochemical and technological research methods was used to determine the quality parameters of the tabletting mass and tablets based on them. \u0000Results. According to the results of previous studies, similarities in the approaches to the pharmacotherapy of type II diabetes in the countries of Southeast Asia, the Western Pacific region, and Ukraine were established, which became the basis for conducting a market study of drugs with a sugar-lowering effect, namely, based on voglibose, with the aim of further including such drugs in the range of Ukrainian manufacturers. Furthermore, according to the results of physicochemical and technological studies, the composition and rational technology of obtaining tablets were established. Also, pharmacological studies have established that tablets with voglibose and solid dispersion of quercetin significantly prevent the development of glucose metabolism disorders caused by a high-sugar diet. In terms of the expressiveness of the hypocholesterolemic effect of the tablets and their constituent components, they are reliably superior to the comparison drug - metformin. \u0000Conclusions. According to the research results, the feasibility and relevance of the development of combined tablets with voglibose and solid dispersion of quercetin have been established. Furthermore, based on the investigated physicochemical and technological indicators, combined tablets' composition and rational technology were developed, and their specific pharmacological activity was proven","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"22 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85660280","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}

{"title":"Chemical composition of essential oil of common juniper (Juniperus communis L.) branches from Estonia","authors":"A. Raal, R. Komarov, A. Orav, K. Kapp, A. Grytsyk, O. Koshovyi","doi":"10.15587/2519-4852.2022.271048","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.271048","url":null,"abstract":"For the treatment of the urinary system and kidney diseases, common juniper (Juniperus communis L.) fruits are widely used. This raw material is included in the European Pharmacopoeia (Ph.Eur.) and is one of the most popular kinds of official medicinal plant material with diuretic and uroantiseptic activity. However, the main biomass of bushes consists of green branches, which also contain a significant amount of essential oil that can be used in pharmaceutical practice. The branches become waste during bush cutting. So, it is advisable to investigate the chemical composition of essential oil isolated from common juniper branches from different regions of Estonia to prove the possibility of using this essential oil and branches in pharmaceutical practice. \u0000Aim. Therefore, the aim of the research was to determine the chemical composition of essential oil from common juniper (J. communis L.) branches from Estonia. \u0000Materials and Methods. The branches of juniper shrubs were collected in the summer months from 27 different habitats in Estonia. The essential oil was isolated from fresh juniper branches by the modified distillation method described in the European Pharmacopoeia monograph of Juniperi pseudo-fructus. GC/MS analysis was carried out using an Agilent 5975 Series MSDMSD, Agilent7890A GC (Agilent Technologies, Inc.) with two detectors (MSMS and FID) on a fused silica capillary column (30 m x 0.25 mm) with a bonded stationary phase: poly(5 %-diphenyl-95 %-dimethyl)siloxane (DB-5). The carrier gas was helium with a split ratio of 1:30, and the flow rate of 1.3 mL/min was applied. The temperature program was from 50°–240˚C at 2˚C/min and the injector temperature was 300˚C. The MS detector was operated in the EIEI mode of 70 eV and at a scan rate of 2 scans/s with a mass acquisition range of 20–400 u. \u0000Research results. The average amount of juniper essential oil in branches extracted during distillation using the Ph. Eur. method was 0.23±0.04 ml. 103 substances were identified in 27 different samples of juniper branches and quantified by the GC/MS method. The dominant components of Estonian common juniper essential oil are α-pinene (37.5-69.3 %), pinene, sabinene, β-myrcene and β-phellandrene. The juniper essential oils from Estonian raw materials were compared with Serbian, Iran, Portuguese, French and Greek ones. It was established that the common juniper growing in Estonia belongs to the α-pinene chemotype. \u0000Conclusions. Common juniper growing in Estonia belongs to the α-pinene chemotype. 103 substances were identified, and their assay was established in 27 different samples of juniper branches. The dominant components of Estonian common juniper essential oil are α-pinene (37.5-69.3 %), so it could be used as a source of a-pinene for the pharmaceutical industry. \u0000As the essential oils of common juniper branches didn’t meet all the requirements of the European Pharmacopoeia for juniper berries oil, so separate regulatory documentation must be ","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78510688","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}

{"title":"Broad-purpose antimicrobial chlorine-active polymers: suppression of multidrug-resistant microorganisms and microbial penetration resistance","authors":"B. Murashevych, I. Koshova, E. Surmasheva, D. Girenko, Vasyl Chuiko, D. Stepanskyi","doi":"10.15587/2519-4852.2022.266171","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.266171","url":null,"abstract":"The aim of the work was to evaluate the antimicrobial activity of polymeric materials with immobilized N-Chlorosulfonamide groups against multidrug-resistant hospital strains of common microorganisms and to determine the resistance to microbial penetration of these materials. \u0000Materials and methods: the studied samples were copolymers of styrene with divinylbenzene in the form of staple fibre and non-woven fabric with immobilized \u0000N-Chlorosulfonamide groups of various structures. Hospital strains of microorganisms have been isolated from clinical material; their antibiotic sensitivity has been determined by the Kirby-Bauer method. The agar diffusion method determines the antimicrobial activity of the polymers. Resistance to microbial penetration of samples of non-woven fabric has been determined by the membrane filtration method. \u0000Results: polymer samples have been synthesized with immobilized N-Chlorosulfonamide groups in the Na- and H-forms, and with the N, N-dichlorosulfonamide group, with chlorine concentration range 3.7 - 12.5 %. All samples demonstrated pronounced antimicrobial activity against both standard and hospital strains. Due to the higher specific surface area, staple fibre is generally more efficient. An increase in the zone of inhibition of the growth of microorganisms was observed with an increase in the concentration of immobilized chlorine. All the studied fabric samples are impermeable to S. aureus. The control samples containing the free sulfonamide group did not show antimicrobial properties. \u0000Conclusions: synthesized chlorine-active polymers have a pronounced antimicrobial activity against multidrug-resistant microorganisms, demonstrate high resistance to microbial penetration and therefore are promising for creating a wide range of medical products on their basis: dressings, protective masks, antimicrobial filters, etc.","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"27 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82314195","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}

{"title":"Research of biologically active substances of hemp seeds, hemp seed oil and hemp pomace","authors":"Oksana Struk, A. Grytsyk, Mikola Mikitin, Mykhailo Obodianskyi, T. Stasiv, S. Svirska","doi":"10.15587/2519-4852.2022.241249","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.241249","url":null,"abstract":"For the time being, the use of cannabis for medical purposes is more and more relevant. A review of literary sources shows that Ukrainian varieties of hemp are insufficiently studied. Therefore, the variety \"Glesia\" was chosen for the study, as it is the most promising Ukrainian variety. Fatty oil from hemp seeds is the leading pharmaceutical and food product produced from this raw material in Ukraine. During its production, the pomace remains, which is used for feeding animals. At the same time, it still contains many other BAS and can be a valuable raw material for creating pharmaceutical products. Therefore, developing technologies for the complex processing of this raw material is an urgent task of modern pharmaceutical science.\u0000The aim of this work was a phytochemical study of biologically active substances of hemp seeds, hemp seed oil and hemp pomace in order to develop the new phytoremedies.\u0000Materials and methods. Non-narcotic hemp seeds of the \"Glesia\" variety, hemp seed oil and hemp pomace were the objects of research. The elemental analysis was made using inductively coupled plasma atomic emission spectrometry - iCAP 7000 Duo; the study of amino acids was made using ion exchange chromatography; the study of fatty acids was made using gas-liquid chromatography. In addition, the content of vitamin E (α-, β- and γ-tocopherols) was studied using high-performance liquid chromatography (HPLC) with UV detection; the content of protein was studied using A.I. Ermakov method in O.O. Sozinov and F.O. Poperelia modification.\u0000Research results. The analysis of the qualitative characteristics of the obtained fatty oils shows that all indicators met the requirements of the State Standard of Ukraine. For the first time, the transition of macro- and microelements from hemp seeds of the \"Glesia\" variety into fatty oil was determined, and their residue in the pomace was established. The content of 16 amino acids was determined. The content of saturated and unsaturated fatty acids in oil samples was established. The content of α- β- γ-tocopherol in hemp seeds, hemp oil and hemp pomace was investigated using GC / MS. It was found that the protein content in the pomace was in the range of 32.8 – 34.6 %.\u0000Conclusions. We conducted a complex study of biologically active substances of non-narcotic hemp seeds of the \"Glesia\" variety that was harvested in 2019 and 2020, the hemp oil and hemp pomace. It was established that the content of macro- and microelements in the studied raw material of Cannabis sativa L. corresponds to the following order: Ca> Mg> Si> Fe> Al> Mn> Zn> Sr> B> Cu> Ba> Cr and Ni> Se> Co> Mo> Cd> Be> I> Pb. The content of 16 amino acids was determined. Of them, 7 amino acids are essential (leucine, valine, threonine, lysine, methionine, isoleucine, phenylalanine), 2 amino acids are essential for children (histidine and arginine), and 7 amino acids are replaceable (alanine, tyrosine, proline, glycine, glutamic and aspartic acids). It was found tha","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86695840","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}

{"title":"Development of the spectrophotometric method for the determination of metoprolol tartrate in tablets by using bromocresol green","authors":"M. Horyn, T. Kucher, Liubomyr Kryskiw, O. Poliak, N. Zarivna, K. Peleshok, L. Logoyda","doi":"10.15587/2519-4852.2022.266068","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.266068","url":null,"abstract":"The aim of the work was to develop and validate a spectrophotometric method for determining metoprolol tartrate in tablets based on the reaction with bromocresol green (BCG).\u0000Material and methods. Analytical equipment: two-beam UV-visible spectrophotometer Shimadzu model -UV 1800 (Japan), software UV-Probe 2.62, laboratory electronic balance RAD WAG AS 200/C, pH-meter И-160МИ. The following APIs, dosage forms, reagents and solvents were used in the work: pharmacopoeial standard sample (CRS) of metoprolol tartrate (Sigma-Aldrich, (≥ 98 %, HPLC)), BCG (Sigma-Aldrich, (≥ 98 %, HPLC)), \"Metoprolol\" tablets 50 mg (Kyivmedpreparat, series 0035415), \"Metoprolol\" 100 mg (Farmak, series 30421), methanol (Honeywell, (≥ 99.9 %, GC)), ethanol (Honeywell, (≥ 99.9 %, GC)), chloroform (Honeywell, (≥ 99.9 %, GC)), acetonitrile (Honeywell, (≥ 99.9 %, GC)), and ethyl acetate (Honeywell, (≥ 99.7 %, GC)).\u0000Results and discussion. A spectrophotometric method was developed for determining metoprolol tartrate by reaction with BCG in a methanol solution using the absorption maximum at a wavelength of 624 nm. Stoichiometric ratios of reactive components were established, which were 1:1. The developed method for the quantitative determination of metoprolol tartrate was validated following the requirements of the SPhU. The analytical method was linear in the concentration range of 5.47-38.30 μg/mL. The limit of detection and quantification were 0.41 μg/mL and 1.24 μg/mL, respectively. According to the «greenness» pictogram of the analytical method using the AGREE method, the score was 0.79, which indicates that the proposed spectrophotometric method for the determination of metoprolol was developed in compliance with the principles of «green» chemistry.Conclusions. A spectrophotometric method for determining metoprolol tartrate in tablets based on the reaction with BCG in compliance with the principles of «green» chemistry has been developed and validated. Furthermore, the developed method for the quantitative determination of metoprolol tartrate was validated following the requirements of the SPhU. In summary, the developed method has a low negative impact on the environment and can be applied for routine pharmaceutical analysis","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"99 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85904432","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}

{"title":"Test anti-aging activity in a face scrub preparation that contains coffee-grade active charcoal (Coffea arabica L.) with the addition of vitamin E","authors":"Dara Sukma Ratmelya, Julia Reveny, U. Harahap","doi":"10.15587/2519-4852.2022.265402","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.265402","url":null,"abstract":"Ageing can be caused by accumulating excess dead skin cells on the skin's surface. Coffee grounds are a by-product of the coffee brewing process. Coffee grounds can be used as activated charcoal in face scrub preparations.\u0000The purpose of this study was to formulate and test the effectiveness of anti-ageing face scrub preparations of coffee grounds activated charcoal (Coffea arabica L.) with the addition of vitamin E.\u0000Material and methods: the research method includes processing coffee grounds in the form of drying and making activated charcoal, then formulating into face scrub preparations with a concentration of 1 %; 2 %, 3 % with vitamin E, 5 % and without vitamin E and blanc (without activated charcoal). Evaluation of face scrub preparations includes homogeneity test, stability test (odour, colour, pH and consistency), cycling test, dispersion test, viscosity test, centrifugation test, hedonic test, irritation test, and effectiveness test (moisture, pores, stains, wrinkles) on facial skin using a skin analyser on 24 volunteers with application to the face once a week for 4 weeks. The experimental data were analysed using the SPSS 22 program.\u0000Results: they showed that all face scrub preparations were in the form of cream with grey-black granules, coffee-scented, homogeneous, stable for 12 weeks of storage at room temperature (20-25°C), pH value (5.0-6.0), had a spreading power of 5-7 cm, viscosity (3760-3996 mPa's), no separation occurs in the centrifugation test and does not irritate facial skin. The results of the hedonic test, the most preferred formulation, was the F3 preparation. The effectiveness test results were an increase in humidity of 27 %, a decrease in pore size of 35.8 %, stains of 40 % and wrinkles of 37.6 %.\u0000Conclusion: from the results of the study, it can be concluded that the face scrub preparation of activated charcoal coffee grounds (Coffea arabica L.) with a concentration of 3 % and vitamin E 5 % is a formula that meets the evaluation of the preparation and measures the effectiveness of anti-ageing","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"83 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77202838","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}

{"title":"Effect of the composition of emulsifiers and the dispersion medium on the properties of bases for semi-solid preparations","authors":"N. Lyapunov, E. Bezuglaya, A. Liapunova, I. Zinchenko, Oleksii Liapunov, Oleksii Lysokobylka, Yu. M. Stolper","doi":"10.15587/2519-4852.2022.266001","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.266001","url":null,"abstract":"The aim. To study the effect of cetostearyl alcohol (CSA) on the rheological properties of bases with different dispersion media, the release of propylene glycol (PG) from them, and the ability of these bases to absorb water. \u0000Materials and methods. Micelles of a non-ionic surfactant and its aggregates with CSA in a mixed solvent where the structure of water prevails, mixed solvent PG – macrogol 400 (M400) and hydrophilic bases-vehicles with different dispersion media were studied. The research was carried out by the spin probe method using a probe simulating a cationic surfactant and by rotational viscometry. The microstructure of the bases was studied by optical microscopy. The in vitro release test to study the release of PG and M400 from solutions and bases was performed using vertical diffusion chambers. The content of PG and M400 in the dialysate was determined by gas chromatography according to the validated analytical procedures. The absorption of water by solutions and bases was determined by dialysis through the membrane. \u0000Results. CSA, which was the part of the bases together with surfactants in certain ratios, was a significant factor in increasing their rheological parameters, reducing the parameters of PG release during in vitro release tests, as well as reducing water absorption. The mechanisms of such influence are different for bases with different structures of the dispersion medium. In the bases, where the structure of water prevailed, lateral phase separation occurred in the supramolecular structures of surfactant and CSA with the formation of liquid domains of surfactant and solid domains of CSA, which contributed to the formation of coagulation structures. In the mixed non-aqueous solvent PG – M400, surfactant micelles and mixed aggregates of surfactant and CSA molecules were not formed; at 25 oC, surfactants and CSA became separate dispersed phases of suspensions, which contributed to the formation of gels. When CSA was added into an aqueous solution of poloxamer 338, PG, M400 and cationic surfactant, the flow behaviour changed, and the rheological parameters increased, which led to a decrease in the release rate and extended for PG and M400 as well as in the ability to absorb water. The rate and extent of PG release from the solution were greater compared to the M400 release. \u0000Conclusions. The addition of CSA in combination with surfactants into the bases for semi-solid preparations is a significant factor for modifying their rheological parameters, the kinetics of PG release from them, and water absorption during experiments in vitro. The mechanisms of such an effect are different and depend on the composition and structure of the dispersion medium of the base","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"58 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79476978","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}

{"title":"SGLT-2 inhibitors as potential anticonvulsants: empagliflozin, but not dapagliflozin, renders a pronounced effect and potentiates the sodium valproate activity in pentylenetetrazole-induced seizures","authors":"V. Tsyvunin, S. Shtrygol’, Ihnat Havrylov, D. Shtrygol’, Artur Reus","doi":"10.15587/2519-4852.2022.266065","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.266065","url":null,"abstract":"On the way to the search for effective adjuvant medicines for epilepsy treatment, antidiabetic medicines such as sodium-glucose cotransporter-2 inhibitors, which are expressed not only in the kidneys but also in the brain, attract attention. From previous studies, it is known that dapagliflozin improves electroencephalographic parameters in rats on the model of pentylenetetrazole-induced seizures. However, the anticonvulsant potential of other medicines from this group needs to be clarified. \u0000The aim of the study is to estimate the effect of empagliflozin, dapagliflozin per se and their combinations with sodium valproate on pentylenetetrazole-induced seizures, as well as on muscle tone and motor coordination in mice. \u0000Material and methods. 42 random-bred male albino mice weighing 24-28 g were used in the experiments. Empagliflozin (20 mg/kg) and dapagliflozin (50 mg/kg) were administered intragastrically for 3 days. The classic anticonvulsant sodium valproate (150 mg/kg) per se, in combination with the medicines mentioned above, was administered in a similar regimen. On the second day, 30 minutes after administering all medicines, their effect on muscle tone and coordination of movements was determined in the rotarod test. On the third day, 30 minutes after the last administration of the medicines, their effect on pentylenetetrazole-induced (80 mg/kg subcutaneously) seizures was studied. \u0000Results. For the first time, a pronounced anticonvulsant effect of empagliflozin was established both when used alone (a significant increase in latency of the convulsions and a decrease in lethality by 43 %) and especially in combination with sodium valproate (a significant increase in latency of the convulsions, a decrease in the number and severity of seizures and a decrease in lethality by 83 %), as well as the absence of a muscle relaxant effect in both cases. Dapagliflozin has neither its anticonvulsant properties nor its effect on the action of sodium valproate. However, this medicine caused muscle relaxation, especially when combined with sodium valproate. \u0000Conclusions. The results suggest that empagliflozin, unlike dapagliflozin, has a high potential as an adjuvant medicine in treating epilepsy, as it enhances the efficacy of the classic anticonvulsant sodium valproate without muscle relaxant side effects","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"146 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76745702","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}