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STUDY OF PHYSICO-CHEMICAL AND BULK-TECHNOLOGICAL PROPERTIES OF THE ACTIVE SUBSTANCE "BIOALBENDAZOLE" S.V. Shcherbakov A.M. Usubbayev Sh.M. Usubbayeva Tashkent Pharmaceutical Institute Uzbekistan, Tashkent,
e-mail shahnozau.m@mail.ru https://doi.org/10.5281/zenodo.11504122 ABSTRACT
Qabul qilindi: 01-Iyun 2024 yil Ma'qullandi: 05-Iyun 2024 yil Nashr qilindi: 06-Iyun 2024 yil
KEYWORDS
Biolbendazole, substances, drug, technology,
pharmaceutical veterinary industry, granulation method, state Pharmacopoeia.
The results of the physic-chemical and volumetric technological properties of the active substance "Bioalbendazole" are presented. The substance under study, in its physical and chemical properties such as: organoleptic properties, solubility, melting point, pH, heavy metal content and microbiological purity, meets all the requirements of regulatory documents.
One of the most important tasks of domestic pharmaceutical science is the creation of effective drugs used in veterinary practice based on the rich natural resources of Uzbekistan and their introduction into production. This is a significant factor in the development of the domestic pharmaceutical veterinary industry and in ensuring the pharmaceutical independence of the Republic in this area.
Animal helminthiases are widespread in our country and around the world, and the diseases they cause inflict significant economic damage on our country's livestock industry.
Currently, one of the main obstacles to implementing agrarian reforms aimed at more fully meeting the population's needs for affordable and quality food products is helminth infestation of livestock. Helminthiasis is often transmitted from an infected animal to its future offspring. As a result of helminthiasis, animal productivity decreases, which in turn causes significant damage to the national economy of the Republic. According to literature sources, more than 1,000 helminths parasitizing vertebrate animals have been identified in Uzbekistan, commonly affecting agricultural and domestic animals [2].
Currently, methods for treating animal helminthiases are based on the use of a wide range of anthelmintic drugs, some of which often do not provide the necessary effectiveness and can frequently cause undesirable side effects that harm the health of animals [1].
Currently, the development of new highly effective means of combating invasive diseases is relevant. These new treatments should be convenient for both individual and group application, low in toxicity, and have a broad spectrum of action [1,2].
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CENTRAL ASIAN JOURNAL OF ACADEMIC RESEARCH SJIF = 5.441 .
Another direction of innovationis the creation of new drugs based on existing anthelmintics by micronizing substances, enhancing solubility, and using excipients, stabilizers and polymers, as well as other physico-chemical method and techniques that increase bioavailability [5,6]. The improvement of pharmacological properties of drugs is achieved through targeted delivery to a specific area, organs, orcells, aswellas by controlling the rate, timing, andlocation of the drug'sactionin the body. These technologies for improving the pharmacological properties of drugs are referred to as Drug Delivery Technology in English terminology. In recent years, the share of Drug Delivery developments has become dominant in global pharmacy[1].
It is known that the biological effectiveness of most drugs depends on their water solubility. Since most biological processes occurring in the body take place in an aqueous environment, this leads to a limitation in the biological effectiveness of water-insoluble drugs. Therefore, most biologically active substances form water-soluble supramolecular complexes [2].
Based on the above, the creation of highly effective, harmless, import-substituting drugs produced from local raw materials, ensuring their quality at the level of global standards, and their introduction into veterinary practice is a pressing issue in pharmaceutical science. Scientists from the O. Sadykov Institute of Bioorganic Chemistry of the Academy of Sciences of the Republic of Uzbekistan have developed a new water-soluble anthelmintic supramolecular complex of monoammonium salt of glycyrrhizic acid and albendazole, provisionally named Biolbendazole.
Preliminary pharmacological and toxicological studies have shown that the substance "Bioalbendazole" at a dosage of 100 mg exhibits pronounced anthelmintic activity.
In our opinion, the most convenient, cost-effective, and bioavailable dosage form is tablets. Considering the above, our aim is to develop a scientifically-based composition and technology for the tablet form of "Bioalbendazole."
Experimental Part. In the first stage of our technological research, the crystalline form of the active substance "Bioalbendazole" was studied. The study of the crystalline form of active substances is of great importance in the development of tablet dosage form technology.
It is well known that the physico-chemical and technological properties of powdered substances largely depend on the size and shape of the particles. In many cases, the form and size of the active substance particles determine the properties of the compressible tablet mass
[3].
The aim of this experimental study is to determine the crystalline form of the active substance "Bioalbendazole."
The crystalline form of the active substance "Bioalbendazole" was determined by simultaneous visualization and photographing using a digital model NLCD-307B electron microscope with a monitor. The equipment featuresa 9.7" touchscreen LCD monitor-tablet and a revolving device with four objectives.
The research resultson the determination of the crystalline form of "Bioalbendazole" are presented in Figure 1. The imaging results indicate that the substance "Bioalbendazole,"
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according to crystallographic classification, belongs to the group of low-porosity substances— specifically, lamellar, flaky, and difficult-to-compress materials.
Figure 1. Crystalline form of the active substance "Albendazole"
The data obtained from experimental studies confirm the impossibility of using the direct compression methodic the preparation of "Bioalbendazole" tablets.
In the development of the composition and technology for tablet dosage forms from powdered drug substances with such crystalline structures, a scientifically grounded selection of the type and amount of excipients is necessary, along with the use of the wet granulation method [3,4].
When selecting excipients to achieve high-quality tablets based one active substances, it is essential to consider their physico-chemical and bulk-technological properties.
To theoretically justify the type and amount of excipients to be includedin the tablet masses, as well as the tablet formulation technology, the next stage of our research involved studying the physico-chemical and bulk-technological parameters of the substance underinvestigation, accordingto the methodology described in the literature [3,4]. The results of the study of the physico-chemical properties of the active substance "Bioalbendazole" are presented in Table 1.
Table 1.
Results of the Study of Physico-Chemical Properties of the Active Substance "Bioalbendazole"
№ StudiedParameters Methods Norms
1 Appearance Visual The powder is beige in color
2 Crystalline form of the substance Microscopy Low-porous, lamellar, flaky, scaly
3 Organoleptic properties Organoleptic With a distinct smell and a strong taste
4 Solubility State Pharmacopoeia 11th edition Easily soluble in water and 50% ethyl alcohol,
insoluble in organic solvents
5 Meltingpoint State Pharmacopoeia 11th edition Melting point 203-205oC With decomposition
6 pH State Pharmacopoeia 11th edition 3,0-7,0
7 Heavy metals content State Pharmacopoeia 11th edition Not more than 0.001%.
8 Microbiological purity State Pharmacopoeia 11th edition Category 1,2 B
According to the data in Table1,the substance under study meet sall the requirements of regulatory documents in terms of its physico-chemical properties such as; organoleptic properties, solubility, melting point, pH, heavy metalcontent and microbiological purity[6,7].
The volumetric and technological properties of the active substance "Bioalbendazole" were studied by the methods described in the literature. The results obtained are shown in Table 2.
According to the results of experimental studies, it is impossible to obtain tablets from the active substance "Bioalbendazole" with such a crystalline structure, physio-chemical and volumetric-technological characteristics by direct pressing [4,5].
Table 2.
(•_
№ Name of the silbst^uce lecUuglo^kEal iuj^imemsute
Fmrti.Qua! EUUttg lliiwibil Augleef Emmi C.gmmtiü Residiial Coron;
ESBJBßSfciÜSlJ deusjtj:, ttäüiol tü, amaîka llillMHÜtJI, essüüU
ix,
kg/«1 10 fkg/s % Va
Degree H
i Xîi£ Mibs.tmce "Eifialhfiftds. ink" + 2500- 2500 + 1000 21,4 - 1000 + 500 48,1 - 500 + 250 19,2 - 250 + 125 8,2 1 730 3,5 32 44,57 2,9 6,9 70
The results of studying the volumetric and technological cl^OÊÎêns^cs of the active substance
To obtain high-quality tablets from active substances with the above physio-chemical and volumetric-technological parameters, it is necessary to introduce a scientifically based type and amount of excipients into the tablets and the need to use the method of preliminary wet granulation using moisturizers.
References:
1. AkbaevM.Sh., Vasilevich F.I., Akbaev R.M., etc. Parasitology and invasive diseases of animals. M.: Kolos, 2009. 776 p.
2. Arkhipov I.A. Anthelmintics: pharmacology and application. M. 2009., 405 p
3. A.M. Usubbaev., Sh.M. Usubbaeva., Development of the scientific based composition and technology of the "Antivirus tablet" / Eurasian journal of academic research Volume 3 Issure 6, June 2023.-p 39-42
4. Ubaydullaeva Kh.A., Development of technology for obtaining dry extract from plant of polygonum aviculare. Asian journal of Pharmaceutical and biological research. 27-37 p. 2024 y. Research in the field of physico-chemical mechanics of tableting of medicinal powdered substances /: Abstract of the dis. for the degree of Doctor of Pharmaceutical Sciences. (790) / Lviv. gos. med. in-t. - Lviv : . , 1972. - 40 s
5. Khadjimetova S.R. Technology of obtaining sorbent for trypsin enzyme. Eurasian Journal of Medical and Natural Sciences, 4(3), 290-2936The State Pharmacopoeia of the USSR.- XI ed. -Moscow.: Medicine, 1987.- Issue, 1. - p. 334.
6. The State Pharmacopoeia of the USSR.- XI ed. - Moscow.: Medicine, 1989.- Issue 2. - p. 398.
