Problems and Perspectives of Pharmaceutics and Drug Discovery
The International Journal of Problems and Perspectives of Pharmaceutics and Drug Discovery is a peer-reviewed, open access and standard subscription online journal publishes articles which describe innovative research spanning the entire spectrum of pharmacy and pharmaceutical sciences, drug discovery, development, evaluation, and regulatory approval. ISSN (Print): 2181-1660 ISSN (Online): 2181-1679
OBTAINING A PHARMACEUTICAL COMPOSITION OF LEUKOPEMUM - A LEUKOPOIESIS STIMULATOR
This paper presents studies on the preparation of a pharmaceutical composition of leukopemum based on Cobalt-30 and mummy, which is used as a stimulant of secondary leukopenia. Experiments have shown that the pharmaceutical composition has a stimulating effect on hematopoiesis.
Development of drugs based on organic synthesis
Copyright (c) 2024 Problems and Perspectives of Pharmaceutics and Drug Discovery https://creativecommons.org/licenses/by-sa/4.0
PHYSICO-CHEMICAL PROPERTIES OF SELENIUM NANOPARTICLES SYNTHESIZED IN SODIUM-CARBOXYMETHYLCELLULOSE SOLUTIONS
In this study, the possibility of forming and controlling the size of selenium nanoparticles of different sizes and shapes by chemical reduction method with 0.1 M solution of sodium selenite in the presence of ascorbic acid in polymer solutions of different concentrations of purified sodium-carboxymethylcellulose with degree of substitution-0,85 and degree of polymerization -1015. The stability of shape and size of selenium nanoparticles synthesized in solutions of purified sodium-carboxymethylcellulose with a concentration of 2,5-3% over time was confirmed by UV-spectroscopy anddynamic lightscattering (DLS) analysis methods.The degree of dispersion and homogeneity of the synthesized selenium nanoparticles was studied in relation to the time of ultrasonic dispersant exposure.With the increase of processing time intheultrasonic disperser to 5, 10, 20, 30 minutesд decrease in selenium nanoparticle size from 113 nm to 85 nm and their monodis-persity in solution from 37% to 88% was proved by dynamic light scattering analysis.
STUDYING THE CONTENT OF GLYCYRIZIC АСШ AND ORGANOSILICON COMPOUNDS IN THE LIQUID EXTRACT «PHYTOALLERGODERM»
This report presents information on the results of studying the qualitative and quantitative content of glycyrrhizic acid and organosilicon compounds in the liquid extract «Phytoallergoderm». The authenticity of licorice roots was assessed by a qualitative reaction to glycyrrhizic acid, and a spectrophotometric method was also used to assess the authenticity and quantify glycyrrhizic acid. In the case of horsetail herb, a gravimetric method for the determination of organosilicon compounds was used, since in addition to quantitative determination, this method helps to indirectly determine the authenticity of horsetail herb. The developed methods for assessing the quality and the established standards for the content of glycyrrhizic acid and organosilicon compounds serve as the basis for standardizing the drug and forming the draft ND (Company's Pharmacopoeial Monograph).
Standardization and quality assurance of medicines
ANALYSIS OF AMINO ACIDS, MACRO- AND MICRO-ELEMENTS IN RAW MATERIALS AND DRY EXTRACT OF GINKGO BILOBA (GINKGO BILOBA L.) CULTIVATED IN UZBEKISTAN
This article presents the results of the first study of amino acids, macro- and microelements of ginkgo biloba, and the dry extract obtained on its basis. It has been established that raw and dry extracts of ginkgo biloba contain all the essential amino acids, 40macro- and microelements.
DEVELOPMENT OF SCIENTIFICALLY-GASKED COMPOSITION AND TECHNOLOGY OF TABLETS "ROMETIN"
For the first time to develop a scientifically based, optimal composition and technology of tablet dosage form based on local medicinal raw material "Rometin", the technolo^qsroper ties of the source of the active substance were studied by methods and laboratory devices given in the literature. The experiments carried out serve to determine the scientifically grounded, optimal tabletting technology. As a result of the research carried out, a scientifically substantiated composition and technology of Rometin tablets, which have antiviral activity, have been developed. "Rometin", antiviral, substance, tablet.
Pharmaceutical technology and biotechnology
STUDY OF TECHNOLOGICAL PROPERTIES OF A MIXTURE OF ANTHELMINTIC DRY EXTRACTS AND THE DEVELOPMENT OF A ENCAPSULATED DOSAGE FORM
The article presents research works on the study of the technological parameters of a mixture of dry extracts isolated separately from anthelmintic plant materials, such as the aerial part of wormwood, pumpkin seeds, tansy flowers and garlic bulbs, and on their basis the creation of a technology for encapsulated dosage forms. On the basis of the research work, ingredients for encapsulated preparations from a mixture of dry extracts and excipients were developed, and their technological parameters were studied. Optimal composition and technology for Helmint-ART capsules have been developed.
RESEARCH ON THE DEVELOPMENT OF GRANULES "SEDGRAN"
The results of a study of the kinetics of moisture absorption, terms and conditions of storage of instant granules for the preparation of suspensions based on the dry extract "Sedex" with sedative effects are presented. Based on research, it was found that the recommended instant granules are highly hygroscopic, and the types of packaging used ensure the stability of the granules for 2 years.
CREATE OF ADVANCED TECHNOLOGY AMLODIPINE TABLETS 5 AND 10 MG
Including the widespread use and large demand for amlodipine tablets, in order to increase production volumes, an improved technology for amlodipine tablets of 5 mg and 10 mg has been developed. Based on the study of the influence of various excipients on the technological properties of the pressed masses and the quality indicators of the tablets, the optimal composition was selected and a rational tableting technology for amlodipine 5 mg and 10 mg was established. Created technology of amlodipine tablets is recommended for industrial development on the basis of a domestic pharmaceutical manufacturer.
technological properties of pressed masses
MICROSCOPIC STUDY OF THE LEAVES OF ROSEMARY (ROSMARINUS OFFICINALIS L.) CULTIVATED IN UZBEKISTAN
The article is devoted to the microscopic structure of rosemary officinalis- Rosmarinus officinalis L. cultivated in Uzbekistan andthere were determined its diagnostic signs. When examining a paradermal section of a leaf under a microscope, it can be seen that the outlines of epidermal cells on the upper side are rectilinear, with slightly thickened and porous membranes, the projection is polygonal, and on the abaxial, with slightly sinuous membranes, the projection is polygonal. The cells of the upper epidermis are larger than those of the lower. These diagnostic signs can serve to identify plant raw-materials.
STANDARDIZATION OF RAW MATERIALS GINKGO BILOBA (GINKGO BILOBA L.) CULTIVATED IN UZBEKISTAN
For the first time, studies were carried out to substantiate the system of standardization of raw materials ginkgo biloba (folia ginkgo biloba L.) introduced in the Tashkent Botanical Garden named after Academician F.N.Rusanov. The studied raw materials were harvested in August and September. The qualitative and quantitative content of the main active substance, flavonoids, was studied. Scientifically based criteria for the quality of the proposed raw materials were also determined - moisture content, totalash content and ash insoluble in 10% hydrochloric acid solution, fineness, impurity content, microbiological purity
STUDY OF THE PRIMARY METABOLITS OF SEED THE LOCAL PLANT AMARANTH IDEA TA (AMARANTHUS CAUDATUS LL.)
Семена Amaranthus caudatus L. были собраны в октябре в Андижанской области Республики Узбекистан. Собранное сырье сушили на воздухе непосредственно под солнечными лучами. Экстракцию проводили гексаном в экстракторе сокслета. В этом исследовании на местном растении Amaranthus caudatus L. был изучен химический состав семян, в частности липидов, белков и углеводов.
PROTEIN-PEPTIDE AND AMINO ACID COMPOSITION OF VALVAE FRUCTUUM PHASEOLI VULGARIS L.
A total extract was obtained from the valves of the bean fruit ordinary by acid extraction. Analytical separation of the extract was carried out by RB-HPLC and protein -peptide fractions were isolated by ion exchange chromatography. The molecular weights of the obtained fractions were determined by the electrophoretic method. In addition, the amino acid composition of fruit bean valves is determined, including 20 components, i.e. 10 essential amino acids.
MARKETING ANALYSIS: ANTIEMETIC DRUGS ON THE PHARMACEUTICAL MARKET OF UZBEKISTAN
In this study, we analysed, with the help of the «State Register of Medicines, Medical Devices and Medical Equipment Permitted for Use in Medical Practice of the Republic of Uzbekistan», the number, dosage forms and cost of registered antiemetic drugs in 2016-2020 based on the DRUG AUDIT program, which offers a database of information from 2016 to 2020.
Organization and economics of pharmaceutical business
STUDYING THE ACUTE TOXICITY OF A MULTICOMPONENT DRY EXTRACT BASED ON MILK THISTLE, CORN, PEPPERMINT
Today, liver diseases are common, and the lack of effective drugs for the treatment of liver pathologies makes this problem actual. Based on the foregoing, the acute toxicity of a multicomponent dry extract (milk thistle seeds, corn stigmas, peppermint leaves) developed by employees of the Tashkent Pharmaceutical Institute was studied. The study of acute toxicity was carried out according to the standard method on white mice. As a result, it was found that dry extract is highly harmless, since LD50> 6000 mg/kg - the preparation belongs to the fifth class of toxicity (practically non-toxic). Based on the data obtained, it can be concluded that the preparation is highly harmless.
Pharmacology and clinical pharmacology. Microbiological and histological studies
EXPERIMENTAL EVALUATION OF THE EFFICIENCY OF THE BIOLOGICALLY ACTIVE FOOD SUPPLEMENT "GRACIANA"
Studies of the parameters of the effectiveness of biologically active food supplements for the correction of overweight were carried out on white outbred rats. The results of the testshowed that the use of dietary supplement "Gratsiana" in the recommended dose did not reveal significant changes in hematological parameters, relative organ mass and gravimetric coefficients in experimental rats.There was a tendency to weight loss in rats receiving dietary supplement "Gratsiana", in the same group of animals, metabolic processes in the body approached their maximum optimum against the background of an increase in total protein synthesis.
STUDY OF THE OPTIMAL TECHNOLOGY OF DRY PUMPKIN SEED EXTRACT INCLUDED IN THE COMPOSITION OF AN ANTHELMINTIC DRUG
In this study, the optimal conditions for the technology of obtaining a dry extract from pumpkin raw materials are given. Quantitative analysis of the composition of dry pumpkin extract obtained in three ways using the HPLC method was made. According to the amount of biologically active substances and the high percentage of the mass fraction of the products obtained, the optimal technology was chosen. The obtained results showed the usefulness of the chosen technology.
ABOUT ILLEGAL ABUSE 1,4-BENZODIAZEPINE GROUP SUBSTANCE AND ITS CONSEQUENCES
The article presents the results of a study of conditions caused by the non-traditional use of drugs of the 1,4-benzodiazepine group included in the list of psychotropic substances. Currently, among minors, there is an increase in the number of serious crimes caused by the use of drugs of the 1,4-benzodiazepine group for various non-medical purposes, and as a result of their abuse, an increase in mortality. According to statistics, the number of poisonings with drugs of the 1,4-benzodiazepine group is growing worldwide. The data presented in the literature on the illegal consumption of 1,4-benzodiazepine derivatives, as well as cases of poisoning by them, were studied.
Pharmaceutical and toxicological chemistry
DEVELOPMENT OF A METHOD FOR THE ANALYSIS OF THE PESTICIDE THIACLOPRID BY THE METHOD OF THIN LAYER CHROMATOGRAPHY
The optimal conditions for the analysis of e by thin layer chromatography have been developed. The sensitivity and specificity of the method have been studied. For thin-layer chromatographic analysis of thiaklaprid, a system of organic solvents, developing reagents, sorbents was selected.
DEVELOPMENT OF THE TECHNOLOGY OF COLLECTION “DIABDERM”
On the basis of local plant raw materials, the Diabderm collection has been developed, intended for external use for the prevention and treatment of diabetic dermatopathies. The composition of the collection “Diabderm” is selected taking into account the content of biologically active substances, their quantity, also taking into account the pharmacotherapeutic (regenerative) ability. Numerical indicators of the collection of "Diabderm" were studied, qualitative reactions to biologically active substances contained in the collection were carried out.
ON THE DEVELOPMENT OF GLACEMBRIN CAPSULES TECHNOLOGY
The article presents the results of research conducted at the Tashkent Pharmaceutical Institute on the development of the "Melting" test of glacembrin capsules. The experiments used a "rotating basket" device. The amount of biologically active substance released into the solvent medium (sum of flavonoids relative to pinotsembrin) was determined spectrophotometrically at a wavelength of 292 nm. According to the results of the experiments, the following conditions were selected to determine the bioavailability of capsules analyzed in vitro: purified water is used as a solvent medium to determine the dissolution profile, the volume of the medium is 500 ml, the circulation of basket speed 150 rpm, temperature 37 ± 10C.
PREPARATION AND ANTIFUNGAL PROPERTIES OF “ARGODERYL” LINIMENT BASED ON CARBOXYMETHYLCELLULOSE AND SILVER NANOPARTICLES
Silver nanoparticles (AgNP) stabilized in polymeric hydrogels from sodium carboxymethylcellulose (Na-CMC) have been synthesized, their structure, physicochemical properties, and bactericidal activity have been studied. Using transmission electron microscopy, the shape, concentration, and size of AgNP included in the Na-CMC hydrogel structure were established. Studies have shown that spherical silver nanoparticles in the Na-CMC hydrogel structure with a size of 2−45 nm have a high bactericidal activity. These studies have shown that changes in the size and shape of AgNP affect the biological activity in fungal diseases. On the basis of Na-CMC hydrogel containing AgNP, castor oil, menthol, propylene glycol and sorbic acid, “Argoderil” liniment was developed for the prevention and treatment of fungal diseases.
DEVELOPMENT OF TECHNOLOGY AND ANALYSIS OF DRY EXTRACT OF STEVIA GROWN IN THE CONDITIONS OF UZBEKISTAN
For the first time, employees of the Center for Genomics and Bioinformatics of the Academy of Sciences of the Republic of Uzbekistan (senior researcher, Doctor of Biological Sciences H.A. Ubaydullayeva) cultivated varieties of stevia resistant to the local climate (Stevia Rebaudiana Bertone). The present research is devoted to the production of a dry extract of stevia and the development of angalization methods from the aerial part of a plant grown using a new technology. In particular, the factors influencing the extraction process were studied: the degree of grinding of raw materials, the type and amount of extractant, the ratio of raw materials and extractant, as well as the time spent on extraction. The quantitative content of the sum of diterpene glycosides in the dry extract of stevia was determined by high performance liquid chromatography (HPLC).
DEVELOPMENT OF TECHNOLOGY OF DRY EXTRACT BASED ON PLANT RAW MATERIALS OF NETTLE (Urtica diorica
This article presents methods for obtaining dry extracts based on plant materials of Urtica diorica L. and Calendula officinalis L., the results of studying the factors affecting the extraction process, i.e. the nature of the extractant, the degree of grinding of raw materials and the method of extraction are given.
the ratio of raw materials and extractant
MARKETING STUDY OF THE DOSAGE FORM OF GEL ON THE PHARMACEUTICAL MARKET OF THE REPUBLIC OF UZBEKISTAN
The article presents the results of assessing the range of medicines on the pharmaceutical market of the Republic of Uzbekistan. The study used analytical methods such as data collection, grouping, comparison and marketing. The object of the study was the State Registers of Medicines, Medical Devices and Medical Equipment, permitted for use in medi-cal practice of the Republic of Uzbekistan (2019/23; 2020/24; 2021/25). Studies have shown that among the medicinal products registered by the State Register of the Republic of Uzbeki-stan, gels are represented by 198 trade names (TN) and constitute 2% (198 TN / 10257 TN) of their total number. The analysis showed that the gels are represented by 28 different pharmacotherapeutic groups in 10 types of release form in 31 foreign countries. India, Turkey, Germany and Bulgaria are the leaders among the distant foreign countries on the basis of the “producing country” of gels, and the countries from the CIS are Russia and Ukraine. The results of the analysis of the assortment of gels on the basis of the “pharmacotherapeutic group” showed that the largest share is made up of “non-steroidal anti inflammatory drugs (including combined action)”, “local anti-inflammatory drugs”, “dental drugs”, “drugs for the treatment of chronic venous insufficiency” and “remedies for the treatment of acne”. As a result of the analysis, the relevance of the direction was shown - the development of import-substituting gels based on medicinal substances obtained from local plant materials or combined preparations that have antiviral, bacteri-al, regenerating and local anesthetic effects.
ANALYSIS OF THE ASSORTMENT OF DRUGS DERIVED FROM THE PLANT OF GINKGO BILOBA L
This article contains a content analysis of the assortment of drugs obtained from the plant Ginkgo biloba (Ginkgo biloba L.), which is widely used in medical practice as a nootropic agent that improves brain function. When analyzing the assortment of drugs obtained from the plant Ginkgo biloba (Ginkgo biloba L.), the State Register of drugs and medical devices registered in the Republic of Uzbekistan was used, which is the only official source of information on the assortment of all drugs in our republic
drugs obtained from the plant Ginkgo biloba L
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ANALYSIS OF THE RANGE OF ADAPTOGENIC DRUGS REGISTERED IN THE REPUBLIC OF UZBEKISTAN
This study is devoted to the study of the registration of adaptogenic drugs. The results of the study show that the consumer market of the Republic of Uzbekistan in the field of adaptogenic drugs is usually satisfied by 91% with imported drugs, the price of which is 4-7 times higher than the cost of domestic drugs. The analysis of the registration of medicines and medical supplies of the Republic of Uzbekistan in the State Register № 25 of 2021 shows that Pakistan (59,1%) and India (8,84%) are the leaders among foreign countries. Analysis of the dosage form showed that 50% of all medications taken were in the form of syrups and tablets, 34% in the form of capsules and sachets, and 16% in the form of granules. It was found that the liquid drug form was mainly recorded by local manufacturers.
State register of medicines and medical devices of the Republic of Uzbekistan
ANALYSIS OF ANTIFUNGAL DRUGS IN THE LOCAL PHARMACEUTICAL MARKET
Studied and analyzed antifungal drugs in the domestic pharmaceutical market. As a result of the analysis, an assortment of antifungal drugs was identified, range indicators were determined, and the share of manufacturers in the production of antifungal drugs was studied and the main features of the development of this segment, the pharmaceutical industry of Uzbekistan, were identified.
DETERMINATION OF THE QUANTITY OF MACRO- AND MICROELEMENTS AND ALSO β-CAROTENOID IN RED PEPPER CAPSICUM ANNUUM L.
Capsicum annuum red pepper, which is widely used in the food industry, due to its rich chemical composition and healing properties, is one of the most widely used plants in folk medicine against microbes and worms. In our study, when analyzing macro-microelements in red pepper fruits on an optical emission spectrometer with inductively coupled plasma, 6 macro-, 11 micro- and six ultra- icroelements were found that are involved in vital processes. According to the literature data, the fruits of red pepper are rich inmvitamins A and C. Pro-vitamin of vitamin A is β-carotenoid. Photometric studies of the amount of β-carotenoids in red pepper fruits showed their content of 44.25 mg percentage, in hexane extract, in 96% alcohol solution up to 50.81%.
STUDYING THE CHEMICAL COMPOSITION AND STABILITY OF LAVENDER ESSENTIAL OILS CULTURED IN UZBEKISTAN
One of the most widely used medicinal plants in modern medical practice for the effective treatment of depression is Lavender (Lavandula angustifolia Mill). The study of the chemical composition of the essential oils of the lavender plant, which grows in the climatic and soil conditions of the Fergana Valley, and the development of stable drugs based on this are one of the unsolved problems. The essential oil was extracted from the herb lavender, which was collected from the experimental field in Andijan district, through steam distillation. The yield of essential oil amounted to 3.8 ± 0.4% in relation to the dry raw material. Triple quadrupole gas chromatography - mass spectrometry was used to determine the chemical composition of lavender essential oil. Its main bioactive components are: 1,8-cineole, cis-linalool oxide, trans-linalool oxide, linalool, terpinen-4-ol, α-terpineol, linalyl acetate, geraniol, lavandulyl acetate, geranyl acetate and α-bisabolol and their quantity is 62.76%. Lavender essential oil was stored in glass vials in a hermetically sealed refrigerator at 8°C for 60 days. During storage, it was found that the content of the main bioactive components in it decreased by 8.71%. Obtaining a supramolecular complex with oligo- and polysaccharides can give good results in increasing its stability.
CRITERIA FOR SELECTING COMPOSITION AND TECHNOLOGY FOR OBTAINING COMBINED SOLID DOSAGE FORMS BASED ON NSAIDs
The results of the study of the main criteria for selecting the composition and technology of combined shell tablets with anti-inflammatory effect are presented. The technological properties of the primary raw materials were studied and their negative indicators were identified. In order to improve this situation, a complex of excipients was selected.