Method for ointment production based on lipophilic fraction from solid coconut husk

FIELD: pharmaceutical industry, in particular production of ointment having antiinflammation and antimicrobial activity.

SUBSTANCE: method for ointment production includes grinding of plant raw materials namely solid coconut husk up to certain particle size; extraction with chloroform during certain time followed by solvent removing and isolation of lipophilic fraction. Further emulsifier, lipophilic fraction and coconut oil are fused under specific conditions; mixture is cooled to certain temperature and blended with celandine juice heated up to certain temperature.

EFFECT: ointment of increased antiinflammation and antimicrobial activity.

3 tbl, 15 ex

 

The invention relates to medicine and relates to methods of obtaining drugs from plant material, which can be used as an external anti-inflammatory drugs on the basis of which can be obtained ointment for topical treatment of cuts, burns, etc.

Known anti-inflammatory ointment, composed of herbal preparations used to treat cuts, burns: calendula ointment, liniment aloe and other [RLS-Pharmacist / edited Krylov .F. - M., 2001. - 1584 S.; Sokolov, SJ Herbal medicine and phytopharmacology - M., 2000. - S-228].

The closest prototype is the ointment of calendula, characterized by anti-inflammatory, wound healing, antibacterial (against Staphylococcus, Streptococcus) action.

The method of obtaining ointment with calendula is mixing 90 g of the emulsion consistent with 20 g of tincture of calendula [Mashkovsky PPM Medicines. 2 T. - M.: Medicine, 1988. - Vol.2. - S]. The grease emulsion consists of water, vaseline, emulsifier T-2, taken in the ratio of 30:60:10. [Ants I.A. Technology of drugs. 2 T. - M.: Medicine, 1980. - Vol.2. - S]. Tincture of calendula (1:10) get alcohol (70% ethanol) extraction of flowers and flower baskets nails [Mashkovsky PPM Medicines: In 2 T. - M.: Medicine, 1988. - Vol.2. - S.].

The lack of calendula ointment is is low antibacterial activity. For this reason, when infected skin lesions usually practiced by the combined application of the ointment "Marigold" and ointments with antibiotics. The use of ointments with antibiotics is often accompanied by dermatitis, allergies, candidiasis [Mashkovsky PPM Medicines: In 2 T. - M.: Medicine, 1988. - Vol.2.- S-222]. In addition, it is known that petroleum jelly is as ointment base can have an irritating effect on the skin and cause pasalindami [ANCOVA A.I., Walnut V.M. Modern aspects of research and production of ointments. - M.: Medicine, 1980. - P.31]

However, the list of extracts obtained from vegetable raw materials and have anti-inflammatory action, and ointments on their basis is limited [RLS-Pharmacist / edited Krylov .F. - M., 2001. - S. 1584]. Therefore, expanding Arsenal of herbal drugs for external use characterized by anti-inflammatory action, is an important task.

The aim of the invention is to develop methods of obtaining funds for outdoor use, consisting of lipophilic fraction solid shell coconut (Cocos nucifera), characterized by anti-inflammatory action; and ointments, consisting of lipophilic fraction of solid coconut shell, coconut oil, emulsifier T-2 and juice from traicionera, characterized by anti-inflammatory and antimicrobial action.

This object is achieved in that for obtaining the target product lipophilic fraction of the hard shell coconut secrete circulating extraction with chloroform for 7-10 hours with the subsequent removal of solvent. In further to obtain Masi mix coconut oil (oil industrial production), emulsifier T-2, lipophilic fraction of the hard shell coconut, juice of celandine in the ratio of 50:9:1:40.

In the literature there are no data regarding the potential application of lipophilic fraction from solid coconut shell as anti-inflammatory agents, and in the composition of ointments, providing anti-inflammatory and antimicrobial effects. Lipophilic fraction of solid coconut shell composed of soft medicinal forms can be used in medical practice for the treatment of cuts, burns, wounds, accompanied by infection of the skin. These properties are not explicitly derived for the expert from the prior art. Thus, the proposed solution meet the criteria of the invention is a "novelty", "inventive step", "industrially applicable".

Use as a solvent of chloroform ensures maximum extraction of lipophilic FR the functions of the solid shell of the coconut. Temperature, duration of extraction identified experimentally and guarantee the optimality of the process.

To highlight the lipophilic fraction of the solid shell coconut crushed raw material is extracted with chloroform in apparatus of the type "Soxhlet" for 7-10 hours to complete depletion of raw materials. After which the chloroform is removed by evaporation under vacuum at a temperature of 30-35°C. In a porcelain or enameled vessel at a temperature of 70-75°alloy 9.0 parts of emulsifier T-2; 1.0 part of the lipophilic fraction of the hard shell coconut; 50.0 parts of coconut oil. The mixture is cooled to a temperature of 50-55°and mixed with 40.0 parts of celandine juice, heated to a temperature of 50-55°C.

The juice of celandine get by known techniques [Ants I.A. Technology of drugs. 2 T. - M.: Medicine, 1980. 1. - S].

A specific example of the method.

An analytical sample of the raw material is crushed to a particle size not greater than 0.25 mm to About 200 g hard shell coconut (accurately weighed) weigh (accurately weighed). Raw materials extracted in an apparatus of the type "Soxhlet" for 7-10 hours to complete extraction of lipids and negative reactions with 0.1% solution of Sudan III or absence of blue fluorescence in UV-light.

In parallel to determine the moisture content of raw materials. All change is possible is carried out with accuracy is 0.0002,

The extract evaporated under vacuum to remove the chloroform. The extract yield is 6.4% by weight of air-dry raw material.

In varicellae Cup at a temperature of 70-75°alloy 9.0 g of emulsifier T-2; 1.0 g of lipophilic fraction of the hard shell coconut; 50.0 g of coconut oil. The mixture is cooled to a temperature of 50-55°and mixed with 40,0 g celandine juice, heated to a temperature of 50-55°C.

When studying anti-inflammatory, wound healing, antimicrobial properties of the target product for comparison studied: lipophilic fraction of solid peel coconut, coconut oil, ointment, No. 1 (ointment with lipophilic fraction peel coconut and juice of celandine), ointment No. 2 (ointment with lipophilic fraction peel coconut and purified water), ointment "Calendula" 10% industrial production, and perform 3 series of the experiment.

Ranozazivluchee activity of the target product was studied on thermal burn model in rats [burns and burn disease / Huber E.V., etc. // Modeling of diseases. - M., 1973. - P.59-78; Wounds and their treatment in Tibetan medicine / Basaev ACTING, Nazarov-Ragdale WE, Batorova S.M., Lonshakova HP - Novosibirsk: Nauka, 1990. - P.106-108]. The experiment was carried out on outbred rats of both sexes contained in obsasyvaniem mode, weighing 200-220 g At the back of the animals was vestigal above the feature area of 4 cm 2. Then mow the skin caused thermal contact method using a flat-bottomed tubes (the area of the bottom 3 cm2with water heated on a water bath to 100°C. the exposure Time is 20 seconds. The contours of the wound surface was transferred onto tracing paper and cut out. Pieces of tracing paper was weighed on a torsion balance. In the experimental group animals immediately after application of a thermal burn caused investigational medicinal forms (lipophilic fraction of solid peel coconut, coconut oil, ointment # 1 - ointment with lipophilic fraction peel coconut and juice of celandine, ointment No. 2 - ointment with lipophilic fraction peel and coconut water purified, ointments Calendula" 10% of industrial production), without rubbing. The control group remained untreated. To apply the ointment was performed during the week.

Statistical processing of results of all series of experiments was performed using the student coefficient. The research results presented in examples 1-5 and table 1.

Example 1.

Treatment of burn wounds in animals using lipophilic fraction from solid coconut shell led on the 2nd day to the reduction of the area of the wound by 32.0% compared to control, on the 8th day to the reduction of the area of the wound by 66.4% compared to control (table 1).

Example 2.

Treatment of burn wounds in animals using Kok is spot oil led on the 2nd day to the reduction of the area of the wound by 16.0% compared with control, on the 8th day to the reduction of the area of the wound 50.8% compared with the control (table 1).

Example 3.

Treatment of burn wounds in animals using ointments No. 1 (coconut oil 50 h, emulsifier T-2 9 h, lipophilic fraction of the hard shell coconut 1 h, the juice of celandine 40 h) led on the 2nd day to the reduction of the area of the wound by 26.0% compared with the control, on the 8th day to the reduction of the area of the wound on 55,0% compared with the control (table 1).

Example 4.

Treatment of burn wounds in animals using ointments No. 2 (coconut oil 50 h, emulsifier T-2 9 h, lipophilic fraction of the hard shell coconut 1 h, purified water 40 h) led on the 2nd day to the reduction of the area of the wound of 24.0% compared with the control, on the 8th day to the reduction of the area of the wound by 53.3% compared to the control (table 1).

Example 5.

Treatment of burn wounds in animals with ointment "Calendula" led on the 2nd day to increase the area of the wound by 4% compared to control, on the 8th day to the decline in the area of the wound by 8% compared with the control (table 1).

Anti-inflammatory activity of the target product was studied on the model of the kaolin edema in rats [hazura V.V. Methods of primary pharmacological studies. - M.: Medicine, 1974. - S]. The experiment was carried out on outbred rats of both sexes contained in obsasyvaniem mode, weighing 200-220 g as f is hogenova agent used a 10% suspension of kaolin and introduced her subplantar. The study ointment (lipophilic fraction of solid peel coconut, coconut oil, ointment # 1 - ointment with lipophilic fraction peel coconut and juice of celandine, ointment No. 2 - ointment with lipophilic fraction peel and coconut water purified, ointments Calendula" 10% of industrial production) was applied without rubbing, prior to the introduction of kaolin before each measurement, and after measuring the volume of the paws. The control group remained untreated. The volume of the limbs of the rats was measured using the instrument "Oncamera" before and after injection of kaolin after 5, 24, 48 hours. Anti-inflammatory effect of ointments was assessed by the volume of liquid displaced when submerged in the rat paw.

Statistical processing of results of all series of experiments was performed using the student coefficient. The results are shown in examples 6-10 and table 2.

Example 6.

In the treatment of lipophilic fraction of the hard shell coconut magnitude of the swelling of the paws of rats after 5 hours of observations decreased 1.4-fold after 24 hours 1.8 times compared with the control group. In the hours that followed the experience of the comparative picture remained (table 2).

Example 7.

On the background of treatment with coconut oil the amount of swelling of the paws of rats after 5 hours of observations decreased by 1.2 times, 24 hours 1.6 times compared with the control group. the subsequent hours of the experiment comparative picture remained (table 2).

Example 8.

On the background of treatment with ointment No. 1 (coconut oil 50 h, emulsifier T-2 9 h, lipophilic fraction of the hard shell coconut 1 h, the juice of celandine 40 h) the amount of swelling of the paws of rats after 5 hours of observations decreased 1.5 times, 24 hours 1.9 times compared with the control group. In the hours that followed the experience of the comparative picture remained (table 2).

Example 9.

On the background of treatment with ointment No. 2 (coconut oil 50 h, emulsifier T-2 9 h, lipophilic fraction of the hard shell coconut 1 h, purified water 40 h) the amount of swelling of the paws of rats after 5 hours of observations decreased 1.5 times, 24 hours 1.9 times compared with the control group. In the hours that followed the experience of the comparative picture remained (table 2).

Example 10.

On the background of treatment with ointment "Calendula" the amount of swelling of the paws of rats after 5 hours of observations increased 1.2 times, 24 hours 1.1 times as compared with the control group. In the hours that followed the experience of the comparative picture remained (table 2).

In the study of antimicrobial activity of the target product used method is based on the ability of drugs to diffuse into the agar, the infected test-cultures of microorganisms and inhibit the growth of the last [Handbook of microbiological and virological methods studies the study, Ed. Mourer. - M.: Medicine, 1982. - P.172-177]. Determination of the activity of the studied compounds ointments were carried out in Petri dishes of the same diameter with a smooth and flat bottom. In Cup, set horizontally, poured into 15 ml of molten nutrient agar. A layer of agar in a Petri dish filled in 1-2 ml of a suspension of the test organism in physiological solution. Then over the suspension were completely removed, dried the surface of the agar for 30 minutes. Then drill (6 mm diameter) were prosurvival 4-6 holes (wells) at a distance of 2.5 cm from the centre and the same distance from each other "wells" was filled with samples of ointments. The Cup was left at room temperature for 30 minutes, after which the Cup was placed in a thermostat at a temperature of 37°With, without turning, horizontally, to get round the area. After 16 hours was measured by zone of inhibition. The results of the experiment are presented in table 3 and examples 11 to 15.

Example 11

Lipophilic fraction of solid coconut shell does not cause inhibition of growth of microorganisms Staphylococcus abony risk 103/39; Staphylococcus aureus ATTC 6538-P; Candida albicans ATCC 885-653; Aspergillus niger BKMF 1119; Esherichia coli ATCC 25922; Pseudomonas aemginosa risk 453 (table 3).

Example 12.

Coconut oil does not cause inhibition of growth of microorganisms Staphylococcus abony risk 103/39; Staphylococcus aureus ATTC 6538-P; Candida albicans ATCC 885-653; Aspergillus niger BKMF 1119; Esherichia coli ATCC 25922; Pseudomonasaeruginosa risk 453 (table 3).

Example 13.

Ointment No. 1 cause inhibition of growth of microorganisms Staphylococcus abony risk 103/39 18±2 mm; Staphylococcus aureus ATTC 6538-P 19±1 mm; Candida albicans ATCC 885-653 18±2 mm; Aspergillus niger BKMF 1119 22±3 mm; Esherichia coli ATCC 25922 16±2 mm; Pseudomonas aeruginosa GISC 453 17±2 mm (table 3).

Example 14.

Ointment No. 2 does not cause inhibition of growth of microorganisms Staphylococcus abony risk 103/39; Staphylococcus aureus ATTC 6538-P; Candida albicans ATCC 885-653; Aspergillus niger BKMF 1119; Esherichia coli ATCC 25922; Pseudomonas aeruginosa GISC 453 (table 3).

Example 15.

Ointment Calendula does not inhibit the growth of microorganisms Staphylococcus abony risk 103/39; Staphylococcus aureus ATTC 6538-P; Candida albicans ATCC 885-653; Aspergillus niger BKMF 1119; Esherichia coli ATCC 25922; Pseudomonas aeruginosa GISC 453 (table 3).

The method of obtaining ointment with anti-inflammatory and antimicrobial activity, by extraction of plant raw materials and the subsequent mixing of the extract with emulsifier-T2, wherein the plant material - hard shell coconut crushed to particle size of not more than 0.25 mm and extracted with chloroform within 7-10 h, removed the solvent and produce lipophilic fraction, then at 70-75°alloys emulsifier T-2, lipophilic fraction, Coco the TV oil, taken in the ratio of 9:1:50, and then the mixture is cooled to a temperature of 50-55°and mixed with 40 parts of celandine juice, heated to a temperature of 50-55°C.



 

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25 cl, 3 tbl, 135 ex

FIELD: veterinary science.

SUBSTANCE: the present innovation deals with treating and preventing acute and chronic septic processes of any localization in animals, especially in case of inflammatory diseases of reproductive organs if females and, firstly, in cattle. It has been suggested a new homeopathic antiphlogistic veterinary preparation that contains Lachesis mutus, Pulsatilla, Sabina, Sepia and ACD-2 taken at equal ratios at the following dilutions of components: Pulsatilla D15, Sepia D6, Lachesis mutus D8,Sabina D3, ACD-2 D9. The innovation provides broadened variety of veterinary homeopathic antiphlogistic preparations.

EFFECT: higher efficiency of therapy.

3 ex, 4 tbl

FIELD: medicine.

SUBSTANCE: invention relates to pharmaceutical composition preferably in ointment form for treatment of skin lesions containing as active ingredient dexpanthenol and target additives such as fatty additives, namely solid, soft and liquid additives, emulsifier and water. As emulsifier cetostearyl alcohol is used. Composition of present invention has storage time not less than 2 years.

EFFECT: composition of improved quality and prolonged storage time.

8 cl, 2 tbl, 6 ex

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