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6CHEMICAL SCIENCES
PRODUCTION OF A MEDICINE BASED ON LEVOMICETIN IN A CAPSULATED FORM
Begadilova Ai.
Master's degree of Chemistry, Chemical Technology and Ecology, Almaty Technological University
Zainullina A. PhD, associate Professor
Abstract
The article is devoted to the development of technology for obtaining a drug based on levomicetin in the form of capsules. Marketing analysis has shown the relevance of the development of medicinal preparations in the form of capsules in Kazakhstan. The main physical, chemical and technological properties of the substance samples were studied. The quality indicators of the initial raw material and the finished product are determined. Technological calculations were carried out.
Keywords: drug, non-steroidal anti-inflammatory drugs, levomicetin, encapsulated form of the drug.
Introduction
Today, the pharmaceutical industry produces huge names of medicines every year in the form of tablets, capsules and ampoules. It is worth noting the profitability of the production of medicines produced mainly in developed European countries, as well as in America, South Korea and Russia. The analysis of statistical data shows that the share of encapsulated forms of medicines in these countries is 5-17% of the total number of medicines produced. In Russia, this figure is just over five percent [1-3].
In Kazakhstan, the share of the pharmaceutical market engaged in encapsulated drugs lags behind the world level. In this regard, the development of medicines in the form of capsules is an urgent task of pharmaceutical science.
The encapsulated form of the drug has a number of advantages, which leads to its high demand and production.
Soft gelatin capsules have several advantages in the recent growth rate of their popularity in the world [4]. The encapsulated form of the drug has a number of significant advantages in comparison with other dosage forms:
4) a major role in the production of a medicinal product is played by profitability, which can be increased by reducing raw material costs. The encapsulated form of the drug allows you to reduce the dose of the biologically active substance by reducing the dose, which is due to an increase in its bioavailability.
5) the problem of maintaining the stability of medicinal components that are easily oxidized is a serious problem. The presence of a soft gelatin capsule protects the contents of the capsule from the penetration of air oxygen at low relative humidity.
6) for the production of soft gelatin capsules, mainly liquid compositions or compositions in the form of a paste are used, which reduces the likelihood of dust formation, which is important;
7) the use of the encapsulated form solves the acute problem of falsification of medicinal products, as the shell of the capsule deteriorates when opened;
8) in many cases, it is known that medications have a bitter, sometimes unpleasant taste and smell. Soft gelatin shell
9) various variants of shape and size, a wide color scheme, the ability to insert the name, signs, and numbers directly into the capsule provide the possibility of identifying the drug.
Experimental part.
Objects of research: levomycetin, food gelatin, purified water, glycerin of the brand "HCH".
The production of soft gelatin capsules (MJ) was carried out using a capsulator. Microcrystalline cellulose (CELLULOSUM microcristallinum (EP), Micro-crystalline cellulose (BP, USPNF, JP microcrystalline cellulose (MCC) is mainly used in the pharmaceutical industry as a baking powder or binder.
Aerosil is a colloidal silicon dioxide, amorphous anhydrous silicon dioxide, which belongs to the group of synthetically active highly dispersed mineral fillers. In the pharmaceutical industry, aerosil is used as a gel-forming agent, adsorbent, stabilizer, as an additive that increases the fluidity of various impurities.
Hydroxypropyl cellulose was used as an aerator.
Glycerol palmitostearate (Glycerin palmitos-tearate; glycerol palmitostearate; Precirol). Precirol is a mixture of mono -, Di-and triglycerides of fatty acids C16 and C18. It is used as an effective lubricant and filler in the production of capsules; in the production of tablet shells to mask the taste and give them strength.
The physico-chemical and technological characteristics of active and auxiliary substances are interrelated and can in a certain way affect the process of obtaining high-quality capsules with the necessary therapeutic effect.
The substance-acetylsalicylic acid and paracetamol and masses for encapsulation were subjected to physico-chemical and pharmaco - technological studies. All indicators were determined in accordance with GOST.
Results and their discussion
The drugs are produced in different countries of the world. Unfortunately, the main share of medicines
presented in the pharmaceutical market of Kazakhstan Table 1 shows the distribution of dosage forms de-
is made up of imported drugs: India (24%), Russia pending on the forms produced. (11%), and the share of Kazakhstani manufacturers is only 12%.
Table 1.
Total number of medicines registered in the State Register of the Republic ^ of Kazakhstan.
№ Forms of medicinal products registered in the GF of the Republic of Kazakhstan Specific weight of the dosage form % total number of medicinal products
1 Soft gaseous drugs 1,71 137
2 Medicinal products in a mild form 5,16 413
3 Medicinal products in liquid form 28,39 2272
4 Medicinal products in solid form 64,74 5180
From Table 1, solid medicines are in the first Table 2 shows the ratio of solid-form drugs to the
place, 64.74% of the total number of registered total number of drugs produced. medicines, followed by liquid medicines - 28.39%, soft medicines - 5.16% and gaseous medicines - 1.71%.
Table 2.
Ratio of solid medicinal products_
№ Types of medicines in solid form Dosage of the drug
1 Tablets 3433
2 Capsules 655
3 Powder 569
4 Suppositories 143
5 Granules 70
6 Powder 13
The analysis of the ratio of solid-form medicines to the total number of medicines showed that the maximum number of tablets (3412) is the total number of solid medicines (3412). The encapsulated form of the drug is in third place, despite a number of significant advantages (651). Powders, suppositories, granules, dragees are produced in small quantities: 568, 142, 69, 12, respectively.
Marketing analysis of medicines produced in various forms and for various purposes shows that the main share of medicines produced in solid form is accounted for by Film-coated tablets (55.03%).
The results obtained in Kazakhstan, i.e. in the future
indicates the need to expand and expand the pharmaceutical industry for the production of medicines.
The analysis of the pharmaceutical market of solid dosage forms of pharmaceutical drugs in Kazakhstan shows that among the anti-inflammatory drugs found on the market, drugs based on levomycetin are affordable and effective drugs.
According to the State Register of the Republic of Kazakhstan, 93.2% of medicines in capsule form belong to foreign manufacturers, and only 6.8% - to domestic manufacturers. 17 types of medicines based on levomycetin in tablet form have been registered, of which 41.2% are produced by foreign companies, and 52.8% - by domestic manufacturers. The dosage form in the form of capsules based on levomycetin is not produced by domestic manufacturers.
Table 3 shows the qualitative definition of the active substance levomycetin.
Table 3.
Specificity of levomycetin raw materials
№ Specific indicators Technical requirements Indicators
1. Appearance White crystalline powder White powder
2. Free salicylic acid "I'm sorry," she said.S (0.2%) 0.14%
3. Presence of sulfates The substance should not exceed 0.02%. 0.15%
4. Composition of chlorides The substance should not exceed 0.004%. 0.002%
5. Sulphate ash content The content of sulfate ash in 1 g of the substance should not exceed 0.1%. 0, 09 %
6. Heavy metal composition The content of heavy metals in the substance is 0.002 %. it should not exceed. 0,0014 %
7. Reducing the mass during drying Weight loss should not exceed 0.5%. 0,40%
8. Conclusion Levomycetin meets the requirements for product quality .
In the course of the study, levomycetin was characterized by the main indicators of specificity. The data presented in Table 3 indicate that the levomycetin used
meets the requirements of the state pharmacopoeia of the Republic of Kazakhstan (GF) in all its main characteristics.
Table 4.
№ Ingredient: Assignment function Number
G %
1. Chloramphenicol Active substance 0,200 40
2. Microcrystalline cellulose Filler 0,100 20
3. Silicon dioxide (Aerosil) Binding agent 0,040 8
4. Hydroxypropyl cellulose Aerator 0,005 1
5. The glycerol palmitostearate Lubricant 0,005 1
Total 0,500 100
Depending on the size of the shell, the calculated volume according to the average capacity corresponds to the size of the shell of the solid gelatin capsule No. 1 (200 to 600 mg of powder).
Thus, The conducted studies have proven that the drug meets the requirements of the state pharmacopoeia
of the Republic of Kazakhstan in all indicators (table. 5). The breakdown of capsules occurs within normal limits, on the basis of which it is possible to predict the high bioavailability of the developed drug.
Table 5.
Indicators Value
Description Solid gelatin capsules No. 1 with a green opaque body and a white opaque lid filled with white powder.
Average weight of internal capsules 0,500 ± 0,004
Mass uniformity No more than 20 capsules deviate from the average mass of the contents of no more than ± 6.5% and no more than ± 14
Decomposition ( not more than 15 min) 9,5± 1,0
Solubility (not less than 75 %) 89,6 ± 3,0
Output of dry mass or amount of water,% 2,1 ± 0.09
In the course of the work, a feasibility study was developed, taking into account the results of the material and energy balance for one series of the drug in capsules. For this purpose, the cost of production was determined from the cost of basic raw materials, auxiliary substances and other production costs.
The addition of administrative and commercial costs to this amount determined the cost of production. Then calculate the minimum estimated price of 10,000 packages (1 Series), adding a return to this amount, which is 75% of this amount. Dividing the amount by 10,000 ultimately determined the price per unit of product.
Thus, the calculations of the feasibility study for the production of capsules" levomycetin " showed that the price of one unit of production is 377.64 tenge.
Conclusions
1.the main physical and chemical characteristics of Livomycetin were determined and their compliance with the requirements of the state standard of the Republic of Kazakhstan was demonstrated.
2.solid gelatin capsules of the drug were obtained on the basis of Livomycetin. The composition of the main and auxiliary components was selected.
4.the main indicators of product quality are determined: organoleptic properties, average mass, mass uniformity, mass consumption during drying, solubility.
6.as a result of the feasibility study, the economic feasibility of industrial production of a drug based on levomycetin was proved. The cost of products amounted to 377.64 tenge.
REFERENCES:
1. Begadilova A. B., Jarylgapova D. S. Analysis of the pharmaceutical market of solid dosage forms. Materials of the MNC of students and young scientists "Farabi ALEMI", Almaty, Kazakhstan, 6-9 April 2020-p. 19.
2. Begadilova A. B., Jarylgapova D. S. Advantages of the encapsulated form of medicinal products. Materials of the MNC of students and young scientists "Farabi ALEMI", Almaty, Kazakhstan, 6-9 April 2020-p. 12.
3. Capsule turinde levomitsitin darilerdi alu . Materials of the international conference "Satpayev In-novations-2020". Almaty KazNITU named after K. I. Satpayev , 9.04.2020, p. 454-458.
4. Capsular nisanda DLC preparatory al. Materials of the international conference Satpayev Readings-2020. Almaty, KazNTU named after K. I. Satpayev,, 9.04.2020, p. 451-454
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