Development of Compositions and Technologies for Producing Tablets with Hydroxythyrozol-standardized Extract of Olive Leaves

Introduction. The article presents the results of a study of the physicochemical properties of dry extract of olive leaves, standardized by hydroxythyrozol - a biologically active substance that is part of the chemical composition of aerial parts of the olive tree.Aim. The purpose of the study is to develop tablet Formulations containing dry extract of olive leaves and to standardize by hydroxythyrozol by reversed-phase-HPLC method on the main substancecontent.Materials and methods. Substance of dry extract of olive leaves, microcrystalline cellulose (Avicel® PH-112), Aerosil® (Aeroperl® 300 Pharma), Ludipress® (Ludipress®), lactose, potato starch, sodium salt of carboxymethyl starch, magnesium stearate, direct pressing, HPLC.Results and discussion. Studies of the physicochemical properties of dry extract of olive leaves have been carried out. Selected excipients for the study of tablettable masses. Formulations for further tabletting have been developed. A complex of studies of the obtained tablets was carried out according to Russian Pharmacopoeia XIV for compliance with quality indicators.Conclusion. The biological properties of dry extract of olive leaves are have been studied, indicating the prospect of developing drugs based on it. Formulations of tablets with dry extract of olive leaves have been developed and their quality indicators have been investigated.

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Synthesis and physicochemical properties 4-((R))amino)-5-methyl-4H-1,2,4-triazole-3-thiols

Farmatsevtychnyi zhurnal ◽

10.32352/0367-3057.6.16.02 ◽

2018 ◽

pp. 55-59

Author(s):

T. V. Kravchenko ◽

O. I. Panasenko ◽

Ye. G. Knysh

Keyword(s):

Physicochemical Properties ◽

High Efficiency ◽

Chemical Compounds ◽

Biological Properties ◽

Biologically Active ◽

Physical Chemical ◽

Medical University ◽

New Compounds ◽

Instrumental Methods ◽

Derivatives Of

Purposeful synthesis of derivatives of 1,2,4-triazole is one of the most important branches of modern pharmaceutical science Modern pharmaceutical market of domestic medicines requires constant updates of existing range. It makes possible the synthesis of new compounds with a predicted biological activity. The main advantage of derivatives of 1,2,4-triazole is high efficiency and low toxic. That is promising factor for creation of new chemical compounds. Analysis of literary data of past few years has showed that there is not enough information about synthesis, physical, chemical and biological properties of derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol in the literature. So synthesis and further research of derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol is topical. The research took place at the Department of toxicological and inorganic Chemistry of Zaporizhzhia State Medical University (the head of the department – professor O. I. Panasenko). During the work the research were the physicochemical properties of newly synthesized of compounds in accordance with the methods described in the State Pharmacopoeia of Ukraine. As starting substance was used 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol obtained by cyclization of of potassium 2-atsetilgidrazinkarboditioata in the medium hydrazine hydrate. It is planned to research of the compounds obtained in the antimicrobial, act-protective, antioxidative and hypolipidemic activity. 9 new compounds of ylidene derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol were synthesized in a research. The structure of the new synthesized of substances was confirmed by with by means of modern of instrumental methods analysis (1H-PMR-spectroscopy, chromato-mass-spectrometry, elemental analysis). The obtained data is possible to use in purposeful synthesis for the further research of biologically active compounds.

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Influence of Incorporation of Different dn-Electron Metal Cations into Biologically Active System on Its Biological and Physicochemical Properties

International Journal of Molecular Sciences ◽

10.3390/ijms222312909 ◽

2021 ◽

Vol 22 (23) ◽

pp. 12909

Author(s):

Bartłomiej Rogalewicz ◽

Małgorzata Szczesio ◽

Ewa Poleszak ◽

Joanna Kowalczyk ◽

Bernadeta Szewczyk ◽

...

Keyword(s):

Physicochemical Properties ◽

Magnetic Measurements ◽

Biological Properties ◽

Biologically Active ◽

X Ray Diffraction ◽

Active System ◽

X Ray ◽

The Central Nervous System ◽

New Compounds ◽

The Impact

Three new compounds, namely [HL]2+[CuCl4]2−, [HL]2+[ZnCl4]2−, and [HL]2+[CdCl4]2− (where L: imipramine) were synthesized and their physicochemical and biological properties were thoroughly investigated. All three compounds form isostructural, crystalline systems, which havea been studied using Single-Crystal X-ray diffraction analysis (SC-XRD) and Fourier-transform infrared spectroscopy (FTIR). The thermal stability was investigated using thermogravimetric analysis (TGA) and melting points for all compounds have been determined. Magnetic measurements were performed in order to study the magnetic properties of the compounds. The above mentioned techniques allowed us to comprehensively examine the physicochemical properties of the newly obtained compounds. The biological activity was investigated using the number of Zebrafish tests, as it is one of the most common models for studying the impact of newly synthesized compounds on the central nervous system (CNS), since this model is very similar to the human CNS.

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The Influence of Excipients on the Physicochemical and Biological Properties of a Bactericidal, Labile Ester Prodrug in a Salt Form – A Case Study of Cefetamet Pivoxil Hydrochloride

JOURNAL OF ADVANCES IN CHEMISTRY ◽

10.24297/jac.v15i2.7560 ◽

2018 ◽

Vol 15 (2) ◽

pp. 6218-6234

Author(s):

Jakub Dzitko ◽

Przemyslaw Zalewski ◽

Daria Szymanowska ◽

Piotr Garbacki ◽

Magdalena Paczkowska ◽

...

Keyword(s):

Physicochemical Properties ◽

Bacterial Infections ◽

Ph Value ◽

Drug Carrier ◽

Methyl Cellulose ◽

Magnesium Stearate ◽

Biological Properties ◽

Pharmacological Potential ◽

Ester Prodrug

The article presents an innovative approach to a bactericidal drug design based on a cephem prodrug analogue – cefetamet pivoxil hydrochloride. The emergence of cefetamet pivoxil hydrochloride excipient systems (mannitol, hydroxypropyl methyl cellulose, pregelatinised starch, lactose monohydrate, magnesium stearate, polyvinylpyrrolidone) caused changes in the physicochemical properties of cefetamet pivoxil hydrochloride. They are significant for planning the development of an innovative pharmaceutical formulation. The biological activity profile of the prodrug was also modified. FTIR spectra were used to study interactions between cefetamet pivoxil hydrochloride and the excipients. The theoretical approach to the analysis of experimental spectra enabled precise indication of cefetamet pivoxil hydrochloride domains responsible for interaction with the excipients. The interactions between cefetamet pivoxil hydrochloride and the excipients resulted in some important physicochemical modifications: acceptor fluid-dependent changes in solubility and the dissolving rate as well as a decrease in the chemical stability of cefetamet pivoxil hydrochloride in the solid state, especially during thermolysis. The interactions between cefetamet pivoxil hydrochloride and the excipients also had biologically essential effects. There were changes in its permeability through artificial biological membranes simulating the gastrointestinal tract, which depended on the pH value of the acceptor solution. Cefetamet pivoxil hydrochloride combined with the excipient systems exhibited greater bactericidal potential against Staphylococcus aureus. Its bactericidal potential against Enterococcus faecalis, Pseudomonas aeruginosa and Proteus mirabilis doubled. The new approach provides an opportunity to develop treatment of resistant bacterial infections. It will enable synergy between the excipient and the pharmacological potential of an active pharmaceutical substance with modified physicochemical properties induced by the drug carrier.

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The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

Current Organic Synthesis ◽

10.2174/1570179416666190925162215 ◽

2019 ◽

Vol 16 (7) ◽

pp. 953-967 ◽

Cited By ~ 1

Author(s):

Ghodsi M. Ziarani ◽

Fatemeh Mohajer ◽

Razieh Moradi ◽

Parisa Mofatehnia

Keyword(s):

Biological Activities ◽

Biological Properties ◽

Biologically Active ◽

Microtubule Assembly ◽

Heterocyclic Molecules ◽

Biological Perspective ◽

Highly Active ◽

Anti Inflammatory ◽

High Yields ◽

Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

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Physicochemical properties of starch nanocomposite films enhanced by self-assembled potato starch nanoparticles

LWT ◽

10.1016/j.lwt.2016.01.053 ◽

2016 ◽

Vol 69 ◽

pp. 251-257 ◽

Cited By ~ 47

Author(s):

Suisui Jiang ◽

Chengzhen Liu ◽

Xiaojin Wang ◽

Liu Xiong ◽

Qingjie Sun

Keyword(s):

Physicochemical Properties ◽

Potato Starch ◽

Nanocomposite Films ◽

Starch Nanoparticles ◽

Self Assembled

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Analytical Methods for Quantification and Identification of Intact Glucosinolates in Arabidopsis Roots Using LC-QqQ(LIT)-MS/MS

Metabolites ◽

10.3390/metabo11010047 ◽

2021 ◽

Vol 11 (1) ◽

pp. 47

Author(s):

Kourosh Hooshmand ◽

Inge S. Fomsgaard

Keyword(s):

Mass Spectrometry ◽

Liquid Chromatography ◽

Crude Extract ◽

Matrix Effects ◽

Critical Role ◽

Reversed Phase ◽

Biologically Active ◽

Natural Soil ◽

Chromatography Method ◽

Arabidopsis Root

Glucosinolates are biologically active secondary metabolites in Brassicaceae plants that play a critical role in positive and negative interactions between plants and root-associated microbial communities. The aim of this study was to develop a reversed-phase liquid chromatography method to quantify and identify intact glucosinolates in the root of Arabidopsis thaliana (Arabidopsis) grown in non-sterile natural soil by using liquid chromatography-hybrid triple quadruple-linear ion trap (LC-QqQ(LIT)) mass spectrometry. The Synergi Fusion C18-based column was found to be effective for sufficient retention and separation of nine intact glucosinolates without the need for time-consuming desulfation or ion-pairing steps. Method validation results showed satisfactory inter-day and intra-day precision for all glucosinolates except for 4-hydroxyglucobrassicin. Good inter-day and intra-day accuracy and recovery results were observed for glucoiberin, gluconapin, glucobrassicin, 4-methoxyglucobrassicin and neoglucobrassicin. However, for 4-hydroxyglucobrassicin, glucoraphanin and glucoerucin corrections to quantification results might be necessary since the recovery and accuracy results were not optimal. Matrix effects were shown to have a negligible effect on the ionization of all target analytes. The established liquid chromatography–tandem mass spectrometry (LC-MS/MS) method was applied to quantify target intact glucosinolates in Arabidopsis root crude extract of four different wild-type accessions where differences in terms of concentration and composition of intact glucosinolates were observed. Employment of sensitive and selective precursor ion survey scan of m/z 97 in combination with the information-dependent acquisition (IDA) of the enhanced product ion (EPI) dependent scan (Prec97-IDA-EPI) using LC-QqQ(LIT) provided high confidence in structural characterization of diverse intact glucosinolate profiles in complex Arabidopsis root crude extract.

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Analytical Characterization of Water-Soluble Constituents in Olive-Derived By-Products

Foods ◽

10.3390/foods10061299 ◽

2021 ◽

Vol 10 (6) ◽

pp. 1299

Author(s):

Pablo Doménech ◽

Aleta Duque ◽

Isabel Higueras ◽

José Luis Fernández ◽

Paloma Manzanares

Keyword(s):

Olive Tree ◽

Mediterranean Area ◽

Water Soluble ◽

Olive Pomace ◽

Olive Leaves ◽

Olive Stone ◽

Olive Trees ◽

Tree Pruning ◽

By Products

Olive trees constitute one of the largest agroindustries in the Mediterranean area, and their cultivation generates a diverse pool of biomass by-products such as olive tree pruning (OTP), olive leaves (OL), olive stone (OS), and extracted olive pomace (EOP). These lignocellulosic materials have varying compositions and potential utilization strategies within a biorefinery context. The aim of this work was to carry out an integral analysis of the aqueous extractives fraction of these biomasses. Several analytical methods were applied in order to fully characterize this fraction to varying extents: a mass closure of >80% was reached for EOP, >76% for OTP, >65% for OS, and >52% for OL. Among the compounds detected, xylooligosaccharides, mannitol, 3,4-dihydroxyphenylglycol, and hydroxytyrosol were noted as potential enhancers of the valorization of said by-products. The extraction of these compounds is expected to be more favorable for OTP, OL, and EOP, given their high extractives content, and is compatible with other utilization strategies such as the bioconversion of the lignocellulosic fraction into biofuels and bioproducts.

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Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽

10.3390/molecules26123579 ◽

2021 ◽

Vol 26 (12) ◽

pp. 3579

Author(s):

Svetlana A. Popova ◽

Evgenia V. Pavlova ◽

Oksana G. Shevchenko ◽

Irina Yu. Chukicheva ◽

Aleksandr V. Kutchin

Keyword(s):

Antioxidant Activity ◽

Antioxidant Properties ◽

Biological Properties ◽

High Reactivity ◽

Biologically Active ◽

Brain Lipids ◽

Wide Range ◽

Privileged Structure ◽

Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

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