CS269580B1 - A pro-agent for disinfecting the mouth and throat, and the way it is prepared - Google Patents

Abstract

The solution concerns a preparation containing as an active ingredient an alcoholic extract of dry sage herb, which is prepared in two stages, first with diluted alcohol and then with water, with the weight ratio of the batch to the finished extract being 1:5 to 1:10, the alcohol concentration ranging from 60 to 70% by volume and is used for disinfection of the oral cavity and throat.

Description

The invention relates to a composition for disinfecting the oral cavity and throat. The composition contains a mixture of astringent, antiseptic and antiphlogistic substances obtained from the leaves of sage. The composition is intended for rinsing the oral cavity and throat in the form of gargles.

Preparations with synthetic active ingredients are used for rinsing the oral cavity and throat, for example Stopangin Spofa, which is a solution containing the active ingredient hexetidine, which, with prolonged use, sometimes causes hypersensitivity to the ingredients and preparations based on plant raw materials. Preparations are prepared from chamomile, for example Chamomilla Spofa, which often have an accompanying anti-allergic effect. Among the medicinal plant-based preparations for the treatment of the oral cavity and throat, we can also mention Salus Salbei-Tropfen by Salushaus, which is an extract of sage leaves for wine distillate and wine, Cional-Ereusler by Kreussler, which is an aqueous extract of chamomile, sage and mountain arnica with the addition of aluminum formate, Echtrosept gargle by Vogel and Weber, which is a composite preparation of essential oils, fresh juices and tinctures of medicinal plants, Kamillosan by Degussa containing chamomile extract, methyl salicylate, cineole and oils of: bergamot, mint, sage, anise and mountain ash, Salviathymol by Galenika Hetterich is a mixture of essential oils of sage, yarrow, peppermint, cinnamon, cloves, fennel and anise in combination with menthol, thymol and quajazulene and tinctures of myrrh, alchemilla and rattan root and Anginasin Spray by Opferman is hexetidine in combination with oils of rosemary, thyme, peppermint, menthol and camphor and others.

These preparations often have overcombined formulas, use demanding technological processes and contain extracts and essential oils from foreign plants, which reduces the economy of their production without significant differences in effect.

These shortcomings are eliminated by a means for disinfecting the oral cavity and throat containing an extract of sage /Salvia officinalis L./ according to the invention, the essence of which is that it contains as an active ingredient an alcoholic extract of dry sage herb /herba salviae/ containing at least 0.006% by weight of thujone, 0.001% by weight of cineole and 0.001% by weight of bomeol, based on the weight of the extract. The extract is prepared in two stages; In the first stage, the extraction of sage herb is carried out with 50 to 70% by weight, ethanol for 5 to 7 days and in the second stage with water for 12 to 24 hours, while the weight ratio of the drug to ethanol is 1:5 to 1:7 and to water 1:2 to 1:3. The two-stage extraction gradually leaches out almost all disinfectant-active substances of lipophilic and hydrophilic nature, which are essential oil, polyphenolic acids, tannins, flavonoids, triterpenes as well as other unspecified substances that exert their synergistic effects. The high content of disinfectant-active thujone is responsible for the increased antibacterial activity of the extract obtained in this way.

The main advantages of the said composition lie in its disinfectant effect, which is higher or comparable to the above-mentioned known preparations, which was achieved by an effective extract preparation technology.

Examples of the preparation of the composition according to the invention are given below.

Example 1

In a glass kettle of cylindrical shape with a capacity of 50 liters equipped with a drain on the bottom and lid of the container, 23.2 kg of 96% vol. alcohol is charged, to which 16.3 kg of distilled water is mixed. In the infusant prepared in this way, a batch of 8 kg of finely cut sage herb of sieve number II is immersed in a bag of viscocellulose porous fabric. The maceration container is closed with a lid, a polyethylene hose with a diameter of 15 mm is put on the drains, which passes from the bottom of the container through the peristaltic pump to the lid of the kettle.

CS 259 530 3t

The actual maceration is carried out by circulating the extractant through the drug batch as follows: When the drain tap at the bottom of the container is opened, the extractant starts to flow from the kettle into the hose, at the same time the peristaltic pump is switched on and the outflow speed is synchronized with the flow rate of the liquid through the peristaltic pump. This operation is carried out for 5 days with daily pumping. After the end of the extraction with alcohol, the liquid is poured into a homogenization vessel equipped with a stirrer using a peristaltic pump. 16 kg of distilled water is poured onto the infused batch in the maceration vessel and the extraction process continues for another 24 hours. The aqueous and aqueous ethanolic extracts are combined in the homogenization vessel and supplemented with 96% vol. alcohol to a final concentration of 62% by weight. After homogenization of the extract and the batch, clarification is carried out with subsequent filtration and adjustment. For the analysis of active substances in the preparation a gas chromatograph with a PID detector was used. A glass capillary column 100 m x 0.25 mm with Carbowax 20M as a stationary phase was used as a separation system. Qualitative analysis was performed using thujone, cineole and borneol standards; quantitative determinations were performed using the external standard method using an integrator. The preparation contains 0.06% by weight of thujone, 0.02% by weight of cineole and 0.01% by weight of borneol.

Example 2

Into a glass maceration vessel with a capacity of 50 liters, equipped with outlets on the bottom and lid of the vessel, to which polyethylene hoses connected to a type S pump with a variator are added 24.35 kg of 96% vol. alcohol and 15.65 kg of distilled water. After homogenization of the liquids, 6 kg of barley cut Salvia officinalis, grade II, in a bag shaped like a maceration vessel made of viscocellulose fabric is added to the vessel. The procedure is then as in Example 1, with the difference that instead of the peristaltic pump, a type S glass pump with a set flow rate of 1.2 liters/min is used and the extraction process lasts 7 days. After the extraction with alcohol is completed, 14 kg of distilled water is poured onto the extracted batch and the extraction process continues for another 12 hours. The aqueous and alcoholic extracts are combined in a homogenizing vessel and supplemented with 96% vol. alcohol to a final concentration of 61.4% by weight. The composition was analyzed by the method described in Example 1 and contains 0.08% by weight of thujone, 0.03% by weight of cineole and 0.014% by weight of borneol. The comparative composition Salus Salbei-Tropfen by Salushaus contained 0.04% by weight of thujone and 0.03% by weight of cineole.

The composition according to the invention is a brownish-green liquid, with a strong aromatic smell, a spicy, bitter to astringent taste. It mixes with water without turbidity. It meets the requirements for microbiological safety according to ČsL· 4. In a stability test under conditions of + 4 °C, normal, + 38 °C and + 60 °C after 18 months, there is no change in the contents in terms of microbiological, physical and chemical. It is stored in containers that are well closed and protected from light.

The microbiological activity of the composition according to the invention was tested in comparison with the foreign preparation Salus Salbei-Tropfen. The activity was determined in a liquid medium by the vitreous dilution method in order to determine the minimum inhibitory concentrations /MIC/, or. minimum cidal concentrations /MCC/. The results of the experiments performed on the collection strains of microorganisms are given in tab. no. 1

Table δ. I

Strain Dilution

Salus Sage Drops MIC MCC MICMCC

Escherichia coli CCM 2260 16 16 88

Bacillus subtilis .IEM 8/58 256 2 1282

EN 269 580 01

Staphylococcus aureus CCM 2022 64 32 32 1 □ Proteus vulgaris ΙΕΜ 11/70 16 8 1 6 ' 6 Pseudomonas aeruginosa IEM 70/70 32 16 32 1 6 Candida albicans 16 8 1 6 5

Efficacy on clinical isolates Table 2 microorganisms from the mouth cavities and the pharynx states table no. 2 Genus Number Means Salus Sage drops microorganism values MIC / year ice e n i e / tribes 5 10 20 40 80 5 10 20 40 30 Enterobacter 20 - 20 - - — — 20 - - - Staphylococcus. 20 - 2 2 16 - - 2 - 5 13 Klebsiella 20 18 2 - - - 17 3 - - - E. coli 22 17 5 - - - 14 8 - - - Proteus 18 16 2 - - - 16 2 - - * Hemolytic streptococci 12 - - - - 4 - - - - 4

The composition according to the invention was clinically tested at 6 workplaces and compared with the currently used preparation Chamomilla Spofa, which is an extract from chamomile. Patients were randomly assigned to both groups. The total number of patients tested was 169, of which 42 were patients after tonsillectomy and 128 with inflammatory diseases. The control group included a total of 100 patients treated with Chamomilla Spofa, of which 51 were patients after tonsillectomy and 49 with inflammatory diseases. The duration of treatment was 7 to 14 days, with patients with inflammatory diseases being treated on an outpatient basis and patients after tonsillectomy being hospitalized for 3 to 4 days, and the total treatment lasted 14 days. No side effects were recorded during the study. When evaluating microbiological examinations, in most cases normal oral flora was cultivated before and after treatment with both preparations, in 7 cases in the study group there was pathological flora before and after treatment, in 14 cases in the control group. In 4 cases, after treatment with the agent according to the invention, the normal oral flora changed to pathological, i.e. 4.12%, after treatment with Chamomilla Spofa in 2 cases, i.e. 2.9%* The antimicrobial effect was manifested in 22 cases, i.e. 20% in the study group and in 8 cases, i.e. 11.6% in the control group. Subjectively, 141 patients, i.e. 84% of the study group reported improvement after application of the agent according to the invention, 15 patients, i.e. 8%, did not report improvement by 5 percent, i.e. 3% evaluate the treatment negatively. In the control group of 76 patients, i.e. 76% report improvement, 24% i.e. 24% report no improvement and 13% i.e. 13% evaluate the treatment negatively.

Claims (2)

CS 269 580 0, 3 Staphylococcus aureus CCM 2022 64 32 32 1 o Proteus vulgaris IEM 11/70 16 8 1 ó 6 Pseudomonas aeruginosa IEM 70/70 32 16 32 1 6 Candida albicans 16 8 1 6 5 Effective clinical isolates of microorganisms of the oral cavity and pharynx is shown in Tab. No. 2 Tab. No. 2 Genus Number Salus Salbei-Tropfen Microorg. values. MIC / r e e d e n e / strains 5 10 20 40 80 5 10 20 40 30 Enterobacter 20 - 20 - - 20 Staphylococ. 20 - 2 2 16 - - 2 - 5 13 Klebsiella 20 18 2 - - 17 3 - - - E. coli 22 17 5 - - 14 8 - - - Proteus 18 16 2 - - 16 2 - - - Hemolyt. Streptococci 12 The compound of the invention was clinically clinched on 6 workplaces and compared with currently used Chamomilla Spofa, a chamomile extract. Patients were randomized to both sets. A total of 169 patients were enrolled in the trial group, 42 of whom were tonsillectomy and 128 were inflammatory diseases. In the control group, a total of 100 patients were treated with Chamomilla Spofa, of which 51 were after tonsilectomy and 49 and inflammatory diseases. The duration of treatment ranged from 7 to 14 days, while patients with inflammatory diseases were treated on an outpatient basis and patients after tonsillectomy were 3-4 days hospitalized and the total treatment was 14 days. No adverse side effects were noted during the trial. In the evaluation of microbiological examinations, the common oral flora was cultivated before and after obi-treatment in most cases, in 7 cases in the follow-up group the pathology was before and after treatment, in the control group in 14 cases. In 4 cases, after treatment with the composition according to the invention, the normal oral flora was changed to pathological ie 4.12%, after Chamomilla Spofa treatment in 2 cases, ie 2.9% <, 22 cases, ie 20% in the study file, showed antimicrobial effect and in 8 cases, ie 11.6% in the control group. The subjective 141 patients, ie 84% of the follow-up group, reported 2-post-α-admixing of the composition of the invention, 15 patients, ie 8%, did not show an improvement of 5 patients, ie 3% evaluated the negative treatment. 24, ie 24% do not indicate improvement and 13 ie 13% evaluate the treatment negative. P R E D E T OF THE INVENTION 1. Oral and throat disinfectant composition comprising salvia extract Salvia officinalis L., characterized in that the active ingredient comprises diluted alcoholic liquor of dry sage saliva / herba salviae / containing at least 4 CS'2 % Of 0.006 wt. tujóňu ;; Q, 004: mass, cineolhi βι.Ο, ΰΟΙ wt. borneolUl, in excess of the weight of the extract. 2. A process for the preparation of the composition according to item 1 by extraction of dry matter by Tekakeski and optionally by addition of adjuvants, characterized in that the extraction is carried out in the first stage with 50 to 70% by weight. ethanol: for 5 to 7 days and in the second stage for 12 to 24 hours, wherein the drug to ethanol weight ratio is 1: 5 to 1: 7 and to water 1: 2 to 1: 3.