![Open Access](https://journals.eco-vector.com/lib/pkp/templates/images/icons/text_open.png)
![Restricted Access](https://journals.eco-vector.com/lib/pkp/templates/images/icons/text_unlock.png)
![Restricted Access](https://journals.eco-vector.com/lib/pkp/templates/images/icons/text_lock.png)
Vol 71, No 8 (2022)
Pharmaceutical chemistry and pharmacognosy
Evaluation of the quality and biological activity of BioDihydroquercetin
Abstract
Introduction. BioDihydroquercetin is a natural dietary supplement made from larch wood, produced by “SibPribor” LLC using a proprietary technology under the trade mark “Baikal Legend”. BioDihydroquercetin powder is obtained with a low density and high rates of biological activity and bioavailability, accessibility. Sublingual administration ensures rapid and complete penetration of the biologically active substance into the blood.
Objectives: a comprehensive study of the composition and the biological activity of BioDihydroquercetin in connection with the peculiarities of its production technology.
Material and methods. The content of dihydroquercetin (%) was determined according to GOST 33504-2015 and pharmacopoeial monograph of the company "Taxifolia", the qualitative composition was studied using high-performance liquid chromatography. The antiradical activity of the powder to organic and inorganic radicals of natural and artificial origin was studied by spectrometry and coulometry to determine the biological activity of BioDihydroquercetin. Antioxidant potential was assessed using spectrophotometry and fluorimetry with the determination of the total antioxidant potential and the ability to absorb oxygen radicals. The iron-reducing and iron-chelating potential of BioDihydroquercetin was determined by spectrophotometry. The study of bioavailability was carried out using GIT model. In addition, the protection of the organic substrate from oxidative stress caused by lipid peroxides, as well as the anti-inflammatory and membrane-stabilizing potential, were studied by spectrophotometry.
Results and discussion. The content of dihydroquercetin in the samples was 99.2–104%. The content of dihydroquercetin according to the HPLC method is 96.84±2.03. The product of high purity, 100% consists of an active substance, an accompanying satellite of dihydroquercetin is a natural accompanying satellite of dihydroquercetin – dihydrokaempferol, the content of which does not exceed 1%. Biodihydroquercetin was shown to have antioxidant, antiradical and iron-reducing activity. The conducted studies have shown that Biodihydroquercetin is effective for protecting the biological substrate. In addition, BioDihydroquercetin has shown to be a good inactivator of nitric oxide molecules and has a pronounced inhibitory effect on the albumin coagulation process, which indicates its high anti-inflammatory activity. BioDihydroquercetin also has a pronounced membrane stabilizing potential. The special form of the powder, produced according to the author's technology, ensures high bioavailability.
Conclusion. BioDihydroquercetin is a highly active natural product, characterized as an effective antioxidant, created using an author's technology. Its high biological activity and purity indicate its effectiveness and safety, which allows it to be recommended to a wide range of the population as an antioxidant, anti-inflammatory, membrane-stabilizing and membrane-protective agent of a high degree of protection. Biodihydroquercetin can be recommended to healthy people, living in big cities as a means of preventing “diseases of civilization”, also to all people for active longevity. Besides, Biodihydroquercetin can be used as an adjuvant in complex therapy of cardio-vascular, oncological, neurological diseases as well as diabetes mellitus type 2.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Investigation of flavonoids of the herb alfalfa sickle (Medicago falcata L.)
Abstract
Introduction. Crescent alfalfa (Medicago falcata L.) is widespread in the regions of central Russia, it is a fodder and honey plant. The plant contains various classes of biologically active substances, among which flavonoids, isoflavonoids are more valuable, because. have different pharmacological efficacy, such as anti-inflammatory, anticarcinogenic, antimicrobial, antioxidant.
In this regard, the identification and qualitative determination of individual flavonoids of the herb sickle alfalfa by various methods is relevant.
Objective: study of the flavonoid compounds of the alfalfa herb by known qualitative reactions, paper chromatography and ultra performance liquid chromatography/MS.
Material and methods. The flavonoid composition of sickle alfalfa was studied using qualitative reactions, paper chromatography, ultra performance liquid chromatography/MS on a Waters Acquility chromatograph with a UV diode array detector and a TQD tandem quadrupole MS detector (Waters) in the gradient elution mode. Flavonoid compounds were extracted with 70% ethyl alcohol.
Results. The flavonoid composition of the crescent alfalfa herb is represented by derivatives of quercetin, myricetin, apigenin, mainly their methoxylated forms. A total of 10 compounds were identified, including 8 flavonols, which were divided into quercetin derivatives (rutin, 4',7-O-Dimethylquercetin-3-O-di-methylglucoside, 4',7-O-dimethylquercetin-3-O-methylglucoside) , the rest are classified as myricetin derivatives. Two compounds are classified as flavones (apigenin-7-O-methylglucoside, apigenin-7-O-acetylglucosyl, glucosylglucoside).
Conclusion. 10 flavonoid compounds, represented mainly by methoxylated compounds, were identified in the herb alfalfa sickle, and therefore it can serve as a potential source of these compounds.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Elemental composition of pectoral species No. 1 and its components
Abstract
Introduction. Medicinal herbal preparations are very popular in the complex therapy of various diseases. Many medicinal plants are able to concentrate mineral elements. Knowledge of the content of macro- and microelements in plants makes it possible to purposefully use them for the prevention and treatment of human microelementoses. Also, to assess the safety of herbal medicines, it is necessary to monitor the content of toxic elements in plant raw materials and the transition of toxic elements from raw materials to aqueous extracts.
Objectives: study of pectoral species No.1 and its components mineral elements composition and contamination with toxic elements.
Material and methods. Samples of pectoral species No.1 and its components – marshmallow roots, oregano herb, coltsfoot leaves (manufacturer: Krasnogorskleksredstva JSC) were purchased at Moscow’s pharmacy and used for analysis. The elemental composition of pectoral species No. 1 and its components was determined by inductively coupled plasma mass spectrometry (ICP-MS).
Results. 29 elements were found in pectoral species No. 1 and its components. Potassium, calcium, magnesium, sodium, aluminum, iron, strontium, zinc, manganese are the predominant elements of pectoral species No. 1 and its components.
Conclusion. The high content of potassium, calcium and magnesium in the pectoral species No. 1 can be explained by the high content of these elements in each component. The content of heavy metals in the pectoral species No. 1 and its components did not exceed the maximum permissible concentration.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Validation of the method for the quantitative determination of lapatinib in tablets during the "Dissolution" test
Abstract
Introduction. Lapatinib is used for targeted therapy of breast cancer caused by overexpression or activation of tyrosine kinase receptors of epidermal growth factor (Human epidermal growth factor receptors, HER/ErbB). For the determination of lapatinib in tablets, chromatographic methods are mainly used. However, spectrophotometry in the visible and ultraviolet regions of the spectrum can be considered as a more accessible and simple method of quantitative determination. To prove the suitability of the method for quantitative determination of lapatinib in tablets by UV spectrophotometry in the dissolution test, it is necessary to validate it.
The objective of the study was to validate the method for the quantitative determination of lapatinib during the dissolution test.
Material and methods. As an investigational drug, lapatinib tablets (film-coated tablets, 250 mg) obtained in the laboratory for the development of dosage forms of the FSBI " N.N. Blokhin National Medical Research Center of Oncology" was chosen. The "Dissolution" test was carried out in accordance with GPM.1.4.2.0014.15 "Dissolution for solid dosage forms", the quantitative determination of the released substance was carried out by UV spectrophotometry, the statistical processing of the results was carried out in accordance with GPM.1.1.0013.15 "Statistical processing of the results of a chemical experiment" and the recommendations of the Guidelines for pharmaceutical industry enterprises.
Results. When determining specificity, placebo interference was found to be less than 0,1%. A linear relationship between the concentration of lapatinib and the optical density of the solution has been proven. The values taken as true lay within the confidence intervals of the corresponding average results of analyzes obtained experimentally using validated method. When determining the repeatability, the value of the relative standard deviation (RSD, %) for the degree of dissolution of lapatinib did not exceed 2%. For the validated method, acceptable specificity, linearity, accuracy, and precision were proven in the concentration range from 0.025 mg/ml to 0.061 mg/ml, which corresponds to the range from 55% to 135%.
Conclusion. Validation of the method for lapatinib quantitative determination during the “Dissolution” test for the dosage form of film-coated tablets, 250 mg has shown the possibility of its use for quality control of the medicinal product.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Technology of medicines
Quantum-chemical calculation as a method of theoretical prediction of the physico-chemical interaction of intranasal gel components
Abstract
Introduction. An important area of pharmaceutical research is the creation of new, as well as the improvement of existing available dosage forms, using already known medicinal substances as active substances. Currently, the issues of developing drugs that activate the integrative properties and functions of the brain, as well as increase the body's resistance to aggressive influences, are relevant. A group of drugs that regulate such conditions are nootropics, namely piracetam and its analogues. The advantages of nasal dosage forms for realizing this are obvious. This is both high bioavailability and the possibility of systemic action of medicinal substances. The speed of development of the effect, as a result of the active absorption of medicinal substances that are cleaved in the gastrointestinal tract.
Objectives: selection and theoretical justification of an intranasal dosage form containing piracetam as an active ingredient and several different excipients.
Material and methods. When creating an intranasal dosage form with a nootropic effect, various research methods were used: technological, biopharmaceutical. And also, methods of molecular mechanics and quantum chemistry.
Results. Theoretical and experimental studies on the choice of excipients for intranasal dosage form have been carried out.
Conclusion. The conducted studies prove the feasibility of developing a dosage form technology – an intranasal gel with piracetam, which has nootropic activity.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Study of amino acid and elemental composition of dry extract of Samarkand immortelle
Abstract
Introduction. A comprehensive study of medicinal plants widely used in traditional medicine, in order to scientifically substantiate their use in practical medicine, is one of the urgent tasks of modern pharmacy. One of these plants is the Samarkand immortelle (Helichrysum maracandicum Popov ex Kirp.), widely distributed in Central Asia.
Objectives. Study of the amino acid and elemental composition of the dry extract of Samarkand immortelle flowers.
Material and methods. The elemental composition of the dry extract was determined by inductively coupled plasma mass spectrometry (ICP-MS), and the quantitative determination of interchangeable and essential amino acids was carried out by high-performance liquid chromatography.
Results. In the dry extract of the Samarkand immortelle, the presence of 38 micro- and macroelements has been established, of which eight are vital (essential) and five are conditionally essential. Elements such as potassium, calcium, phosphorus, magnesium, sodium, aluminum, etc. are represented in the largest amount. According to the classification of Polyanskaya (2005), the detected elements by quantitative content can be divided into the following categories:
- 2 macroelements (K, Ca);
- 9 millielements (P, Mg, Na, Al, Fe, B, Mn, Zn, Cu);
- 25 microelements (Ba, Cr, Ni, Ga, V, Li, Mo, Sr, Pb, Sc, Zr, Ag, Co, As, Ti, Tl, Se, Rb, Y, Sn, Sb, Cs, Be, Pt, Au);
- 2 nanoelements (In, Cd).
At the same time, the quantitative content of heavy metals and arsenic does not exceed the limits specified in regulatory documentation. Free amino acid analysis showed the presence of 20 amino acids in the dry extract, 10 of which are essential. The total free amino acid content is 6753.134 mcg/g, of which 29.19% are essential amino acids.
Conclusion. The research results confirm the high value of the dry extract of the Samarkand immortelle in terms of the content of amino acids, macro- and microelements. This fact testifies to its supposed pharmacotherapeutic activity, possible breadth of application in medicine and the expediency of creating drugs based on it.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Organization and economy
Analysis of the herbal drugs uses in psychiatry
Abstract
Introduction. The article provides an analysis of the use of herbal drugs (HD) in the treatment of mental disorders associated with anxiety. Throughout life, many people develop symptom complexes that allow narrow specialists to diagnose a disorder caused by anxiety and fear. ICD-11 combines disorders with anxiety or fear as the main clinical feature in this new group.
Objective. Analysis of the prescription of CH to patients with disorders caused by anxiety and fear, along with the main psycho-pharmacological therapy, taking this type of CH.
Material and methods. Analysis of CH prescriptions for patients with anxiety disorders. The article presents studies of the work of specialized departments and hospitals of the Sverdlovsk Regional Psychiatric Hospital in the context of the prescribed therapy by the specified group of CHs on nosology: mental disorders caused by anxiety and fear.
Results and discussion. In the course of the study, it was noted that in the women's, mixed departments and day hospital there are more prescriptions of CH No.2, along with the men's department, which has more prescriptions of CH No.5. Day hospital No.2, in addition to the main therapy, uses CH No.4.
Conclusion. CHs have fewer side effects, and thus, if possible, may be an alternative treatment for anxiety or as a concomitant therapy to enhance the sedative effect of psychotropic CHs. We note that CHs No. 2, No. 4, No. 5 are in high demand among doctors when prescribing concomitant therapy based on the results of the analysis.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)
Pharmacoeconomic assessment of providing patients with tableted non-narcotic opioid analgestics upon their discharge from the hospital: opportunities and realities
Abstract
The balance of the drug portfolio of healthcare facilities contributes to the prolongation of the provision of medical care at the proper level, ensuring interaction and continuity between the inpatient and outpatient stages of care, which is especially important in organizing and conducting pain syndrome therapy. Currently, the patient's need for pain therapy already at the time of discharge from the hospital before an appointment with an outpatient doctor is expressed by the legislative possibility of handing over potent drugs to the patient for a period of up to 5 days.
Objectives: justification of medicine provision with a fixed-dose combination (FDC) of Paracetamol and Tramadol to patients with pain syndrome during their transition from inpatient to outpatient care based on a pharmacoeconomic approach and to evaluate the costs of such pharmacotherapy.
Material and methods. The results of previous studies on the evaluation of the effectiveness of the analgesic action of the Paracetamol and Tramadol FDC in comparison with the injectable monodrug Tramadol product and the cost of obtaining 1 unit of effectiveness in the conditions of emergency surgical and trauma departments of a hospital, content analysis of legislation and internal regulations on the circulation of drugs of controlled groups, statistics of the bed capacity of the emergency surgery department for the period of 2021–2022.
Results and discussion. The use of Paracetamol and Tramadol FDC for pain therapy, taking into account the comparison and grouping of patients, made it possible to reduce the cost of pain syndrome therapy by 23,472.68 rubles within 4 months. Extrapolation of the obtained data for 4 months for an annual period showed the possibility of reducing the cost of treating pain syndrome by 70,418.04 rubles while ensuring a comfortable transition of patients to outpatient care.
Conclusion. The studies show the clinical and economic feasibility of using a Paracetamol and Tramadol FDC both in hospital care and when moving from a hospital to an outpatient clinic.
![pages](/img/style/pages.png)
![views](/img/style/views.png)
![](/img/style/loadingSmall.gif)