RU2563189C1 - Liquid balsam having local irritant and anti-inflammatory action - Google Patents

Abstract

FIELD: chemistry.

SUBSTANCE: invention relates to a liquid balsam having antiseptic and local irritant action. Said balsam contains 5-36 wt % menthol-free peppermint oil, 8-43 wt % eucalyptus oil, 0.5-20 wt % pine oil, 13-57 wt % levomenthol, 1-25 wt % lavender oil, 1.5-36 wt % turpentine oil.

EFFECT: invention provides a marked antimicrobial effect without allergic reactions and phototoxic action.

2 cl, 3 tbl, 2 ex

Description

The invention relates to the field of pharmacology, in particular to medicines for external use, containing essential oils and having a distracting, locally irritating and antiseptic effect.

From literary sources it is known that essential oil plants have long been used for the treatment and prevention of many diseases (Suvorova T.Yu. Fragrances and oils for your health / Rostov-on-Donua: Phoenix, 2005. - 320 s). In acute respiratory diseases, essential oils of eucalyptus, pine, lavender, etc. are prescribed. As practice shows, a number of essential oils (lavender, etc.), having anti-inflammatory, antiseptic properties, are effectively used in the complex treatment of bronchopulmonary diseases. In the compositions, essential oils are more effective than individually.

The well-known drug "Vike Active Balm with menthol and eucalyptus" (manufactured by Procter and Gamble Manufacturing GmbH, Germany), which has a locally irritating, antiseptic and anti-inflammatory effect. For clinical purposes, an ointment for external use is produced (a polypropylene jar of 25 g; 50 g; 100 g in a cardboard box). 100 g of ointment contains active substances: levomenthol - 2.75 g; camphor - 5.0 g; eucalyptus oil - 1.5 g; turpentine oil - 5.0 g; excipients: thymol - 0.25 g; cedar oil - 0.45 g; soft white paraffin - up to 100 g (Encyclopedia of medicines and pharmacy assortment goods | http://www.rlsnet.ru/tn_index_id_47207.html).

The disadvantages of this ointment are due to the hydrophobic nature of its base. First of all, this is expressed in a decrease in bioavailability, since with a hydrophobic basis, the substance flows only from that layer of ointment that directly comes into contact with the skin. Hydrophobic ointment interferes with normal gas exchange and, thus, disrupts skin respiration. In addition, the hydrophobic base makes contact with the mucous membranes difficult, therefore the use of ointments with fatty bases on the mucosa does not give a high effect. In addition, the use of camphor externally can cause skin allergic reactions and skin irritation. Thymol, used as a natural preservative and stabilizer, can cause allergic reactions - hives, itching, skin rash, sweating, or bronchospasm.

Closest to the claimed solution is the drug "Golden Star Liquid Balsam" (manufactured by Danang Central Pharmaceutical Company No. 5, Danafa, Vietnam), which has a distracting, locally irritating and antiseptic effect. In Russia, the Golden Star balm is available in three forms: a pencil for inhalation, ointment and liquid balm. Liquid balm is available in 5 ml vials. In 1 bottle (5 ml) contains: crystalline menthol - 1400 mg; camphor - 444 mg; peppermint oil - 1145 mg; eucalyptus oil - 5 mg; clove oil - 23 mg; cinnamon oil - 19 mg (Encyclopedia of drugs and pharmacy assortment goods | http://www.rlsnet.ru/tn_index_id_23391.html).

The main disadvantage of liquid balm is that when it is applied to the skin, allergic reactions are possible. If they occur, it is necessary to wash off the remnants of the drug from the skin with warm water and soap, stop using it. Avoid contact with the drug in the eyes, on the mucous membranes, on the open wound surface. In addition, a preparation containing cinnamon and clove essential oils should not be used before going out, as they have a phototoxic effect (increases the skin's susceptibility to ultraviolet rays). Severe burns can result from improper use of these oils.

The present invention is aimed at eliminating these shortcomings and the creation of the drug solely on the basis of natural essential oils. The technical result achieved in this case is the elimination of undesirable allergic reactions and phototoxic effects, improving the absorption of active substances. An additional effect is the harmonization of the organoleptic perception of the composition.

The claimed result is achieved in that the medicinal liquid balm with antiseptic, local irritating and distracting effect, which is a 100% mixture of essential oils without the addition of auxiliary components of a hydrophobic nature, contains the following components in wt.%:

Peppermint oil without menthol 5-36 Eucalyptus oil 8-43 Fir oil 0.5-20 Levomenthol 13-57 Lavender oil 1-25 Turpentine oil 1,5-36

To harmonize the organoleptic perception of the composition, it is preferable that the essential oils be taken in the following ratio in wt.%:

Peppermint oil without menthol 14.4-21.6 Eucalyptus oil 16-24 Fir oil 2.4-3.6 Levomenthol 29.6-44.4 Lavender oil 5.6-8.4 Turpentine oil 12-18

The inventive balm contains the active components in an amount necessary to provide the necessary therapeutic effect. In addition, as noted earlier, essential oils are more effective in compositions. The authors experimentally found that it is with this ratio of components that the effect of each of the active components increases.

The pharmacological action of the components of the liquid balm is presented in table 1.

Implementation Examples:

Example 1

The antiseptic effect of a liquid balm containing: peppermint oil (without menthol) - 18.0 wt.%, Eucalyptus oil - 20.0 wt.%, Fir oil - 3.0 wt.%, Levomenthol - 37.0 wt.%, lavender oil - 7.0 wt.%, turpentine oil - 15.0 wt.%, was studied in experiments in vitro on test strains of microorganisms.

The spectrum of antimicrobial activity of the preparations was determined on the following test strains of microorganisms: Bacillus subtilis, Bacilius cereus, Eacherichia coli, Salmonella abony, Salmonella enteritidis, Proteus vulgaris, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, Aspergill.

The antimicrobial effect of the preparations was determined by the method of serial dilutions in liquid nutrient media No. 8 for bacteria and in Saburo's environment for fungi, as well as in agarized media No. 1 and No. 2 described in the State Pharmacopoeia XI, issue 2, pp. 200-208.

From a stock solution of the drug with a concentration of 100%, a series of 2-fold serial dilutions were made to a final concentration of 0.3%.

The daily broth cultures of bacteria and C. albicans were diluted 1: 1000 with a sterile 0.9% isotonic sodium chloride solution. The A.niger culture grown on Saburo mowed agar for 7 days was washed with agar with the same solution and standardized using a Goryaev chamber to a suspension concentration of 10 ³ conidia in 1 ml.

The resulting suspension of microorganisms was introduced into 0.1 ml in test tubes with a solution of the drug and the reference drug in liquid media N 8 and Saburo. Drugs were not added to control tubes.

When using agar media N 1 and N 2, dilutions of preparations in the amount of 1 ml were introduced into sterile Petri dishes, 9 ml of molten and cooled to 45-50 ° С medium N 1 or N 2 was added, thoroughly mixed and allowed to solidify. Suspensions of bacteria (on medium No. 1) and fungi (on medium No. 2) were applied to the surface of the agar. Crops on medium N 1 were incubated for 24 - 48 hours at 30-35 ° C, on medium N 2 - 48 hours - 5 days at 20-25 ° C.

Analysis of the results in liquid media was performed after 24 hours and 5 days. By the absence of bacterial and fungal growth, the minimum bacteriostatic concentration (MBsK) and the minimum bactericidal concentration (MBtsK) were determined. The data obtained are shown in Table 2. They showed a pronounced antimicrobial effect of the inventive liquid balm.

Example 2

To compare the effectiveness of the inventive liquid balm with similar antiseptic, locally irritating drugs, antimicrobial studies of the drug "Golden Star Liquid Balm" were conducted according to the method described above. Data for both balms are presented in Table 3.

Similar data were obtained by the method of serial dilutions of test strains of microorganisms in agar media.

From the data of table 2 it follows that the minimum bacteriostatic and bactericidal concentrations are quite low and correspond to those for antiseptic drugs and the inventive liquid balm (a mixture of 100% essential oils), has a more pronounced antimicrobial effect than the comparison drug "Golden Star liquid balm" , which allows us to recommend it in practical public health as an antiseptic.

Claims (2)

1. A liquid balm with antiseptic and local irritating effects, containing peppermint oil without menthol, eucalyptus oil, fir oil, levomenthol, lavender oil, turpentine oil, in the following ratio of components in wt.%:
peppermint oil without menthol 5 - 36 eucalyptus oil 8 - 43 fir oil 0.5 - 20 levomenthol 13 - 57 lavender oil 1 - 25 turpentine oil 1,5 - 36 2. Liquid balm according to claim 1, characterized in that the ratio of components in wt.%:
peppermint oil without menthol 14.4 - 21.6 eucalyptus oil 16-24 fir oil 2.4 - 3.6 levomenthol 29.6 - 44.4 lavender oil 5.6 - 8.4 turpentine oil 12 - 18