RU2354355C2 - Antimicrobial means of vegetable origin and method of obtaining it - Google Patents

Abstract

FIELD: pharmacology.

SUBSTANCE: invention relates to pharmaceutical industry, in particular to production of medications used in case of upper airways diseases (rhinitis, pharyngitis, laryngitis, tracheitis); in case of neuralgia (myalgia, artralgia, migraine, cardioneurosis), stenocardia (light forms), itching dermatosis. Medication contains: menthol, eucalyptus oil, lump sugar, sodium salt of carboxymethylcellulose, talc, stearic acid or its salts, additionally containing black mint oil and aerosyl with definite component ratio. Also claimed is method of obtaining said medication.

EFFECT: increase of tablet strength, increase of tablet disintegration time.

2 cl, 2 tbl

Description

The invention relates to the pharmaceutical industry, in particular to the production of medicines used in inflammatory diseases of the upper respiratory tract (runny nose, pharyngitis, laryngitis, tracheitis); with neuralgia (myalgia, arthralgia, migraine, cardioneurosis), angina pectoris (mild forms), pruritic dermatosis.

Known suction tablets Septolete (1), including, wt.%: Benzalkonium chloride 0.08; menthol 0.1; peppermint oil 0.08; eucalyptus oil 0.05; thymol 0.05; caramel mass - up to 100. The disadvantages of such quality of tablets are the relatively high toxicity of benzalkonium chloride, which leads to vomiting and nausea in case of an overdose of daily intake, as well as allergic reactions in humans to this drug.

Known antiseptic sucking tablets (ATS) (1), representing a caramel mass containing an antiseptic, menthol, peppermint oil and thymol, as an antiseptic - miramistin, in the following ratios of components, wt.%:

Miramistin 0.05-0.10 Menthol 0.08-0.12 Peppermint Essential Oil 0.06-0.1 Eucalyptus Essential Oil 0.04-0.06 Thymol 0.04-0.06 Caramel mass up to 100

From this mass tablets (lozenges, lozenges) weighing from 1 g to 1.5 g are formed.

ATS are known in which anatole and 2,4-dichlorobenzene alcohol (Antisept of Dr. Thys), liquid thyme extract (Bronchicum lozenges for coughs), sage extract with vitamin C (Dr. Thys lozenges), diclonin hydrochloride (Coldrex Lary) are used as active substances Plus), dichlorobenzyl alcohol and amylmethacresol (Faringopils).

Peppermint tablets containing peppermint oils of 0.0025 g, sugar of 0.5 g are known. They are used for nausea, vomiting, smooth muscle spasms. Known drugs based on secondary alcohols dissolved in esters: Validol - a solution of menthol in isovalerian-menthol ether (2).

Closest to the claimed composition are Pectusin tablets (2) containing 0.004 g of menthol, 0.0005 g of eucalyptus oil; up to 0.8 g of sugar and other fillers.

Composition per 1 tablet (FS 42-137-72) (3):

Menthol  0.0040 g Eucalyptus oil  0,0005 g Powdered sugar  0.75 g Carboxymethyl Cellulose Sodium  0.0120 g Talc Medical  0.03 g Calcium stearate  0.0035 g

The disadvantages of the prototype are: fast disintegration of the tablets (15 min) and the deterioration of the quality of the tablets during storage. During storage, menthol, which is in the composition, crystallizes on the surface of the tablets and disappears. This affects the quality of the lek. means: authenticity, taste and medicinal properties.

The purpose of the invention is improving the quality of tablets. The goal is solved by introducing Aerosil into the drug and partially replacing menthol with peppermint oil.

The technical result of the proposed invention is expressed in the composition of the combined drug Pectusin tablets containing menthol, eucalyptus oil and peppermint oil as active substances; refined sugar, sodium carboxymethyl cellulose, talc, aerosil, stearic acid or its salts as auxiliary substances in the following ratios of components (parts by weight):

Menthol  0.187-0.313 Eucalyptus oil  0,047-0,078 Peppermint oil in terms of menthol  0.375-0.625 Rafinated sugar  70.93-118.22 Carboxymethyl Cellulose Sodium  0.320-1.720 Talc  0,500-3,000 Aerosil  0,500-4,000 Stearic acid or its salts  0,500-1,000

The claimed ratio of the components is found experimentally and provides the required quality of Pectusin tablets in industrial production.

According to the invention, it is preferable that the composition contains eucalyptus oil in an amount of 0.047-0.078 mass parts, the introduction of which has a bactericidal antimicrobial effect; used as an antiseptic.

According to the invention, it is preferable that the composition contains peppermint oil in an amount of 0.375-0.625 mass parts, the introduction of which improves the quality of the tablets, prevents crystallization and volatilization of menthol from the composition of the tablets. As an active ingredient, it is included as a refreshing and antiseptic with a mild analgesic effect.

According to the invention, it is preferable that the composition contains menthol in an amount of 0.187-0.313 mass parts, the introduction of which has an analgesic distracting effect. The distracting effect helps to reduce pain, local action is accompanied by a narrowing of blood vessels, a feeling of cold.

According to the invention, it is preferable that the composition contains Aerosil in an amount of 0.500-4.000 mass parts, the introduction of which leads to the achievement of the necessary disintegration of the tablets.

The problem is also solved by the method of manufacturing this dosage form, in accordance with which the preparation of an antimicrobial agent includes the preparation of raw materials, obtaining a mass for tabletting by mixing the ingredients, moistening them, wet granulation, drying the tablet mass, and after the dry granulation stage, the granules are moistened with a menthol solution, eucalyptus oil and peppermint oil in ethyl alcohol, followed by dusting with a mixture of stearic acid or its salts and talc. Then, the tabletting step is carried out.

The method is as follows.

Example.

The prepared ingredients are loaded into the mixer in the following sequence:

Powdered sugar  96,406 kg Sodium Salt CMC  1.53 kg Aerosila  1.007 kg

Stirred for 15 minutes, then 0.5-0.7 kg of purified water is added to moisturize; mix again for 5 minutes The wet mass is granulated and dried at a temperature of 45-50 ° C for 25 minutes, alternating drying with stirring, to a residual moisture of 0.8-1.3%.

The dried granules are cooled to room temperature and dry granulation is carried out.

Then an alcohol solution of menthol, peppermint and eucalyptus oil is prepared. To do this, take 0.319 kg of menthol, 0.426 kg of peppermint oil (in terms of menthol - 0.638 kg depending on the menthol content in peppermint oil), 0.064 kg of eucalyptus oil. Measure out 0.64 l of rectified ethyl alcohol 90% (volume fraction). A weighed amount of crystalline menthol is mixed with ethanol until the menthol is completely dissolved. Then add peppermint oil, eucalyptus oil and mix thoroughly.

The required amount of peppermint oil is recounted depending on the menthol content in peppermint oil according to the results of the analytical sheet.

Recalculation example.

Peppermint oil was received with a quantitative content of total menthol - 74.85%.

0.638 × 50: 74.85 = 0.426 kg must be taken into the load of peppermint oil.

The solution is prepared for each download separately.

The filtered alcohol solution of menthol, peppermint and eucalyptus oil is poured evenly over the entire surface of the granules, mix thoroughly for 5-7 minutes. Then they make dusting. To dust, they take talcum powder 1,755 kg and magnesium stearate 0,6 kg. The dusting mixture is scattered over the entire surface of the granules and again stirred for 7 to 10 minutes, then the mass is tableted.

The presence of a stage of moistening the obtained granules with a solution of menthol, eucalyptus oil and peppermint oil in ethyl alcohol after the stage of dry granulation allows you to keep menthol in the composition of the tablets for the prescribed shelf life of the tablets.

From sources of information it is known that peppermint oil has an anti-inflammatory, capillary-strengthening effect and acts antispasmodically. The main active ingredient of peppermint oil is menthol, the content of which, depending on the type of peppermint, is up to 70%. When peppermint oil enters the mucous membranes, it irritates the nerve endings, causing sensations of cold and tingling sensation. With the excitation of cold receptors, the surface vessels narrow and the inner vessels expand reflexively. This explains the decrease in pain under the influence of menthol in angina pectoris. Peppermint oil has vasoactive properties: it regulates arteriovenous tone, prevents an increase in the tone of intracranial veins. When peppermint oil is taken inside, the receptors of the mucous membrane of the stomach and intestines are irritated, menthol enhances peristalsis, and has an antiseptic effect. Menthol is also prescribed orally as a sedative.

Eucalyptus oil has an antiseptic, anti-inflammatory and sedative effect, it is used for infectious and inflammatory diseases of the pharynx and upper respiratory tract (pharyngitis, laryngitis, tracheitis, catarrhal and purulent bronchitis). The aroma of eucalyptus stimulates mental abilities, strengthens memory, improves mood, is a powerful psychocorrection remedy. The biological activity of the substances contained in eucalyptus oil helps to relieve pain, soothes skin irritations.

To confirm these properties of menthol, peppermint and eucalyptus oil, a combined preparation was tested - Pectusin tablets made using peppermint oil for 20 patients with infectious and inflammatory diseases of the pharynx and upper respiratory tract, neuralgia, mild angina and skin diseases. Surveys of patients after treatment confirmed an improvement.

LITERATURE

1. Patent No. 2184534. Antiseptic pills. Rudko A.P., Krivoshein Yu.S.

2. Mashkovsky M.D. Medicines, 15th ed., New Wave, 2005, p.331-333.

3. FS 42-137-72. Pectusin tablets.

4. FSP 42-0015322802. Pectusin lozenges. OAO Tatkhimpharmpreparaty.

5. The journal "Pharmacy", No. 6, 1968, S. 73-74.

6. Synthetic and biological polymers in pharmacy. M., 1990, p. 58.

7. Industrial regulations of OAO Tatkhimpharmpreparaty for the production of Pectusin tablets for resorption, No. PR 00480750-29-04.

8. GF X, p. 387, 475.

9. GOST 14992-77 - Aerosil.

10. Research And About JSC "Tatkhimpharmpreparaty".

11. Paid FIPS database on the Internet.

12. Information from the Internet on essential oils.

Claims (2)

1. An antimicrobial agent of plant origin for the treatment of inflammatory diseases of the upper respiratory tract, neuralgia, angina pectoris (mild forms), containing menthol, eucalyptus oil, refined sugar, sodium carboxymethyl cellulose, talc, stearic acid or its salts, characterized in that it is additional contains aerosil and peppermint oil in the following ratio of components, wt.%:
menthol 0.187-0.313 eucalyptus oil 0.047-0.078 peppermint oil in terms of menthol 0.375-0.625 rafinated sugar 70.93-118.22 sodium salt carboxymethyl cellulose 0.320-1.720 talc 0,500-3,000 aerosil 0,500-4,000 stearic acid or its salts 0,500-1,000 2. The method of obtaining the antimicrobial agent according to claim 1, including preparing the raw materials, mixing the ingredients, moistening them, wet granulation, drying the tablet mass, characterized in that after the dry granulation stage, the granules are moistened with a solution of menthol, eucalyptus oil and peppermint oil in ethyl alcohol, followed by dusting with a mixture of stearic acid or its salts and talc and tabletting.