Method of local irritant and warming drug production

FIELD: medicine.

SUBSTANCE: vegetable raw is extracted, extract is mixed with vaseline and anhydrous lanoline. As a preliminary vegetable raw - white bryony roots - are crushed for fractions not more than 3 mm, defatted with mixture chloroform - ethanol (2:1) during 7-10 hours with further removal of dissolvent. Dried sovent cake is extracted with 70% ethanol at temperature 18-20°C, with proportions: extractor 1:2.0 during 144 hours in six diffusers; then at temperature 50-55°C vaseline and anhydrous lanoline are melted proportionally 85:10, mixture is cooled up to temperature 25-30°C; this mixture is combined with 5 portions of white bryony roots liquid extract.

EFFECT: drug without irritant odor.

2 tbl, 4 dwg, 8 ex

 

The invention relates to medicine and relates to methods of obtaining drugs from plant material, which can be used as external local irritant and warm remedies for diseases of the joints and muscles, to friction with neuralgia, radiculitis, myositis, lumbago, sciatica.

Known outer locally irritating and distracting means acting on nerve endings in the skin - tincture of Cayenne pepper, the products based on it: the ointment from frostbite, capsicin and others; mustard ointment "Finalgon [RLS-Pharmacist / edited Krylov Û.F. - M., 2001. - 1584; Mashkovsky PPM Medicines: In 2 T. - M.: Medicine, 1988. - T.1. - C-351].

The closest prototype is drug - ointment from frostbite on the basis of tincture of capsicum (VFS 42-1336-83) [RLS-Pharmacist / edited Krylov Û.F. - M., 1993. - S]. Ointment consists of tincture of capsicum, vaseline, fat pork, anhydrous lanolin, castor oil, oil of camphor 10%, formic acid, ammonia solution 25%, liquid soap potash and acts on the nerve endings of the skin causing local irritation and warming effect.

Irritating and warming effect due to the content in the ointment tincture of pepper (contains the alkaloid capsaicin, which causes irritation of the nerve endings [Encyclopedic word is ü medicinal plants and animal products / ed G.P. Yakovlev, CYP Blinova. - S.-Pb.: Special literature, 1999. - S.219-220]), camphor oil, formic acid.

A method of obtaining a local irritant and warm remedies, ointments from frostbite, which consists in mixing vaseline, fat pork, anhydrous lanolin, castor oil, oil of camphor 10%, tincture of capsicum (1:5), formic acid, ammonia solution 25%, 1.9 grams of soap liquid potassium ratio 71:9,45:1,3:1,0:6,2:7,4:0,3:1,45.

Tincture of capsicum derived from vegetable raw materials - fruits of capsicum. Their extracted with 90% ethanol in the ratio 1:5. As the method of extraction using percolation. The process is carried out in the same cone. [Ants I.A. Technology of drugs. 2 T. - M.: Medicine, 1980. - T.1. - S-181.]

Tincture of Cayenne pepper has a strong odor and may cause irritation to mucous membranes and upper respiratory tract and severe sneezing. [Gammerman A.F., Chadaev G.N., Yatsenko-Chmielewski A. Medicinal plants. - M.: high school, 1983. - S-346.] The camphor oil can also cause irritation of the upper respiratory tract. In this regard, the use of this ointment in people with allergic diseases and increased sensitivity to smells is limited.

However, the list of drugs with the outside local irritation and warming effect is m effect, limited [Mashkovsky PPM, 1988; radar-Pharmacist. 2001] due to the lack of an adequate base of the plants. Therefore, expanding Arsenal of drugs of plant origin, characterized by irritating and warming effect, is an important task.

The aim of the invention is to develop a method of obtaining a local irritant and a warming means from the roots of Bryonia white, characterized by the absence of irritating smell.

This object is achieved in that for obtaining the target product raw materials - low fat with a mixture of chloroform-ethanol (2:1) roots of white Bryonia (Bryonia alba L., family Cucurbitaceae) is extracted with 70% ethyl alcohol at a temperature of 18-20°s, when the ratio of raw material:solvent 1:2,0 within 144 hours in six diffusers. In further to obtain Masi mix petrolatum, anhydrous lanolin and extract of Bryonia in the ratio of 85:10:5.

In the literature there are no data on the possibility of application of the extract of Bryonia white as irritating and warming means. The proposed outer local irritant and warming means can be used in medical practice for the treatment of diseases of the joints and muscles, accompanied by pain. This property is not explicitly derived for the expert from the prior art. Thus, by offering the first solution meets the criteria of the invention - "novelty", "inventive step", "industrially applicable".

Use as extractant 70% ethyl alcohol caused the most complete extraction of active substances - cucurbitacins. Temperature, ratio of raw material:extractant, the number of diffusers, the exposure time are optimal and experimental way.

Local irritation and warming means receive the following: crushed to 3 mm, low fat roots of white Bryonia (Bryonia alba L.) and the extractant, 70% ethanol is divided into six equal parts. The first portion of the raw material is extracted with pure extractant, and every subsequent (second, third, fourth, fifth, sixth) extracted by the extract obtained by extraction of the preceding batch of raw materials. The ratio of raw material:extractant is equal to 1:2,0 taking into account the absorption of raw materials. Duration of 144 hours. The obtained extract (liquid extract) filtered through 4 layers of gauze, defend at a temperature of not higher than 10°With not less than 2 days. The extract yield of active substances is 85%. The content of cucurbitacins in preparation (extract of Bryonia 1:2,0) is 1.07±0,02%; output 81,99%. The content of cucurbitacins in raw, the roots of Bryonia white, is 2,61±0,08%. In a porcelain or enameled vessel at a temperature of 50-55°With fuse 85 is t, vaseline, 10 parts of anhydrous lanolin, cooled to a temperature of 25-30°and mixed with 5 parts of extract of Bryonia 1:2 to obtain a homogeneous mass.

A specific example of the method.

416,6 kg roots of Bryonia crushed to 3 mm, were loaded in to conventional Soxhlet extractions and were extracted with a mixture of chloroform-ethanol (2:1) for 7-10 hours. Low fat roots of Bryonia white was dried at 20°and used for the preparation of alcoholic extract.

Preparation of extract from low-fat roots of Bryonia white spent six percolator. In each of the six percolation put shredded fat-free roots of Bryonia white mass 8,35 kg. Volume of extractant introduced into the battery percolation at each stage of extraction, accounted for 32.6 L. the Volume of each extract, taken from the sixth, the head percolator was the equivalent of 16.7 liters

1 day. The work was introduced percolator # 1 and # 2. At 8 o'clock in percolator No. 1 was poured 32,6 l of extractant - 70% ethanol and left to stand for 16 hours.

In 16 hours opened the faucet percolator No. 1 and poured the extract is 16.7 l in the collection №1. In percolator No. 1 enter 32,6 l of extractant 70% ethyl alcohol and continued to drain the liquid phase to its full accumulation in the collection No. 1 volume of 32.6 HP then tap percolator No. 1 was closed, and removing from collection No. 1 was poured into percolator No. 2 Percolator No. 1 and No. 2 was left to stand until 8 a.m. the next day (about 16 hours).

day 2. The work was introduced percolator # 3 and # 4. At 8 o'clock in the morning opened the taps of percolation # 1 and # 2 and spent drain extraction on 16,7 l In percolator No. 1 was introduced 32,6 l of extractant - 70% ethyl alcohol and kept plum extract to full its accumulation in the collection No. 1 volume of 32.6 HP then tap percolator No. 1 was closed. Removing from collection No. 1 transferred in percolator No. 2 and accumulated in the collection No. 2 removing a volume of 32.6 l then closed the faucet percolator No. 2. Removing from collection No. 2 transferred in percolator No. 3 and left to stand for 16 hours.

In 16 hours opened the taps of percolation No. 1-3 and spent drain extraction - of 16.7 liters per percolator No. 1 was introduced 32,6 l of extractant - 70% ethyl alcohol and kept draining out of his savings in the collection No. 1 volume of 32.6 HP then tap percolator No. 1 was closed. Removing from collection No. 1 transferred in percolator No. 2 and accumulated in the collection No. 2 removing a volume of 32.6 l, then closed the faucet percolator No. 2. Plum extract from collection No. 2 volume of 32.6 l carried in percolator No. 3 and accumulated in the collection No. 3 remove the volume of 32.6 l, then closed the faucet percolator No. 3. Plum extract from collector No. 3 volume of 32.6 l carried in percolator No. 4. Percolator No. 1-4 left to stand until 8 a.m. the next day.

day 3. The work was injected PE the batteries No. 5 and No. 6. At 8 o'clock in the morning opened the taps of percolation No. 1-4 and spent plum extract. In percolator No. 1 was introduced 32,6 l of extractant - 70% ethyl alcohol and kept plum extract to full its accumulation in the collection No. 1 volume of 32.6 HP then tap percolator No. 1 was closed. Removing from collection No. 1 transferred in percolator No. 2 and accumulated in the collection No. 2 removing a volume of 32.6 l, then closed the faucet percolator No. 2. Removing from collection No. 2 transferred in percolator No. 3 and accumulated in the collection No. 3 remove the volume of 32.6 l, then closed the faucet percolator No. 3. Extract from collector No. 3 bore in percolator No. 4 and accumulated in the collection №4 removing a volume of 32.6 l, then closed the faucet percolator No. 4. Extract from collector No. 4 was transferred into percolator No. 5. Percolator No. 1-5 were left to stand for 16 hours.

In 16 hours opened the taps of percolation No. 1-5 and spent the drain of the 1st portion of the extract. In percolator No. 1 was introduced 32,6 l of extractant - 70% ethyl alcohol and kept plum extract to full its accumulation in the collection No. 1 volume of 32.6 HP then tap percolator No. 1 was closed. Removing from collection No. 1 transferred in percolator No. 2 and accumulated in the collection No. 2 removing a volume of 32.6 l, then closed the faucet percolator No. 2. Removing from collection No. 2 transferred in percolator No. 3 and accumulated in the btes, the Nike №3 remove the volume of 32.6 l, then close the faucet percolator No. 3. Extract from collector No. 3 bore in percolator No. 4 and accumulated in the collection №4 removing a volume of 32.6 l, then closed the faucet percolator No. 4. Extract from collector No. 4 was transferred into percolator No. 5 and accumulated in the collection No. 5 removing a volume of 32.6 l, then closed the faucet percolator No. 5.

Plum extract from collection No. 5 volume 32,6 l carried in percolator No. 6. Percolator No. 1 to 6 were left to stand for up to 8 hours the next day.

day 4. Spent eat 1 and 2 portions of the extract were taken from the work percolator # 1 and # 2. At 8 o'clock in the morning opened the taps of percolation No. 1-6 and spent drain extraction. The volume of each extract was 16.7 l Extract from collector No. 6 was transferred into a settling tank. Percolator No. 1 out of the work. Exhausted raw materials from percolator No. 1 were loaded into the flask for distillation of alcohol. Extract from collections No. 1-5, each volume of 16.7 l, transferred to the next stage of extraction, percolator No. 2-6, and left to stand for 16 hours.

In 16 hours opened the taps of percolation No. 2-6 and spent drain extraction. Extract from collector No. 6 was transferred into a settling tank. Percolator No. 2 were taken from the work. Exhausted raw materials from percolator No. 2 were loaded into the flask for distillation of alcohol. Extract from collections No. 2-5, each volume of 16.7 l, carried on ochered the second stage of extraction in percolator No. 3-6 and leave to infuse until 8 a.m. the next day.

day 5. Made eat 3 or 4 servings of the extract were taken from the work percolator # 3 and # 4. At 8 o'clock in the morning opened the taps of percolation No. 3-6 and spent drain extraction. The volume of each extract was 16.7 l Extract from collector No. 6 was transferred into a settling tank. Percolator No. 3 was unloaded, and wasted raw material was transferred into a flask for distillation of alcohol. Extract from collections No. 3-5, each volume of 16.7 l, transferred to the next stage of extraction, percolator No. 4-6, and left to stand for 16 hours.

In 16 hours opened the taps of percolation No. 4-6 and spent drain extraction. Extract from collector No. 6 was transferred into a sump drain extraction from collection No. 4 volume of 16.7 l carried in percolator No. 5. Plum extract from collection No. 5 volume of 16.7 l carried in percolator No. 6. Percolator No. 4 was unloaded, and wasted raw material was transferred into a flask for distillation of alcohol.

Percolator No. 5-6 left to stand until 8 a.m. the next day.

day 6. Made eat 5 and 6, portions of the extract were taken from the work percolator # 5 and # 6. At 8 o'clock in the morning opened the taps of percolation No. 5-6 and spent drain extraction. The volume of each extract should be of 16.7 liters of Extract from collector No. 6 was transferred into a settling tank. Percolator No. 5 were taken from the work. Exhausted raw materials from percolator No. 5 were loaded into the flask for distillation of alcohol. Isplace the Oia from collections No. 5, the volume of 16.7 l, transferred to percolator No. 6 and left to stand for 16 hours.

In 16 hours opened the faucet percolator # 6 and spent plum extract. Extract from collector No. 6, the volume of 16.7 l, was transferred to a settling tank. Percolator No. 6 were taken from the work. Exhausted raw materials from percolator No. 6 were loaded into the flask for distillation of alcohol. All six extracts were combined - 100,2 l, stirred and defended at a temperature of not higher than 10°C for 2 days, after which it was filtered and assessed the quality.

In a porcelain or enameled vessel at a temperature of 50-55°float 85 parts of petrolatum, 10 parts of anhydrous lanolin, cooled to a temperature of 25-30°and was mixed with 5 parts of extract of Bryonia until a homogeneous mass.

In the study of local irritation and warming properties of the target product for comparison studied the ointment on the basis of the extract of Bryonia white, ointment from frostbite industrial production, the ointment "Finalgon industrial production, control (base) and have 2 series of the experiment.

Locally irritating and warming properties in the first series of experiment was investigated using test chorioallantoic membrane of the chicken embryo (HAT-Contest) [Manual on experimental (preclinical) study of new pharmacological substances / edited by V.P. Fisenko.- M, 2004. - 352 C.]. Chorioallantois shell is a thin transparent membrane, intersected by a great number of blood vessels and capillaries. Model chorioallantoic membrane of chicken embryo can pre-determine the ability of substances or preparations from them annoying and mucous membranes of mammals. For the experiment used the developing embryos of eggs of hens at the age of 9-10 days. The eggs were kept in an incubator at a temperature of 37.8°and moisture content of 62.5%. Prior experience incubated eggs was kept for 24 hours in a stationary position with the blunt end up, for what, a day before the experience, they are removed from the incubator into thermostat. Before you begin the egg was fixed on a stand with the blunt end up, the shell was opened in the center of the blunt end of a dental Burr. Then the shell broke off small pieces with tweezers, gradually releasing the shell all air chamber. An open air chamber moistened isotonic sodium chloride 0.9 per cent, at a temperature of 37.8°C. the Solution was aspirated by using the pipettor and using tweezers remove chorioallantois shell. Study materials: with bryony, from frostbite, "Finalgon and the basis (vaseline:lanolin anhydrous 85:10) include solubility in water of 3 group of substances insoluble in water at which concentratie 100 g/l, why did without dissolving in water, pre-heated up to a temperature of 37.8°C. Each of the studied ointment was applied to chorioallantois shell in the amount of 0.3, the Monitoring of vessels shell under the drop of the base was carried out through a binocular microscope. The observation time was 50 seconds. Each ointment was tested in at least 5 replications. The results are shown in examples 1, 2, 3, 4 and table 1.

Examples of locally-irritating activity of the drug.

Example 1.

On chorioallantoic shell struck 0.3 g of molten base (vaseline:lanolin anhydrous 85:10). The basis for ointments (figure 1, table 1) did not violate the transparency of the thin shell. The network of blood vessels and capillaries to function properly. According to the classification of substances according to the degree of irritation the basis for ointments belongs to the class 1 - no irritation.

Example 2.

The shell struck 0.3 g of molten ointment with extract of Bryonia. Ointment with extract of Bryonia (figure 2, table 1) caused thrombosis in small vessels to stop the flow of blood and small petechial haemorrhages around the treated surface. Observed hyperemia. According to the classification of substances according to the degree of irritation ointment with extract of Bryonia belongs to the 4th class of the strong degree of irritation.

Example 3.

The shell struck 0.3 g p is fused ointment from frostbite. Ointment from frostbite (figure 3, table 1) caused thrombosis in small vessels to stop the flow of blood and small petechial haemorrhages around the treated surface. Observed hyperemia. According to the classification of substances according to the degree of irritation ointment from frostbite refers to the class 4 - a strong degree of irritation.

Example 4.

The shell struck 0.3 g of molten ointment "Finalgon. Ointment "Finalgon (figure 4, table 1) caused coagulation and lysis of small and medium-sized vessels, multiple bleeding and thrombosis, stopping blood flow. According to the classification of substances according to the degree of irritation ointment "Finalgon" refers to the class 5 - a very strong degree of irritation.

Locally irritating and warming properties in the second series of experiment was investigated using the test on the skin of warm-blooded animals [Sarnow LN. Elements of experimental pharmacology /Zernov L.N., Hazura V. M., 2000. - 352 S.; Basaev ACTING Wounds and their treatment in Tibetan medicine/ ACTING Basaev, WE Nazarov-Rigdon, S.M. Batorova, HP Lonshakova. - Novosibirsk: Nauka, 1990. - P.106-108]. The experiments were conducted on rats male weight 250,0-270,0 g Wistar rats. Under light ether anesthesia the animals shaved areas and identifies the 4 fields with a diameter of 2.5 see These three areas previously was treated with 20% aqueous solution of formaldehyde (after complete evaporation at each impact is). Then the fields using the applicator was applied in a thin layer (at a dose of 2000 mg/200,0) studied the ointment: the basis, with an extract of Bryonia, from frostbite, "Finalgon. The field was covered flannel strips for closer contact ointments to the skin of the animal. Then in the axillary region (hole) of the animal was injected with 0.25% solution Azur-a Through 5 and 16 hours wraps were removed and determined the intensity of staining of the fields in the points. The experimental results presented in examples 5, 6, 7, 8 and table 2.

Example 5.

On the skin of rats inflicted 0.3 g of molten base (vaseline:lanolin anhydrous 85:10), staining was not observed - no irritating effect (0-1 point, table 2).

Example 6.

On the skin of rats inflicted 0.3 g of molten ointment with extract of Bryonia, observed deep uniform color. Ointment with extract of Bryonia in the intensity of staining of the skin has a mild irritant effect (6 points, table 2).

Example 7.

On the skin of rats inflicted 0.3 g of molten ointment from frostbite, observed deep uniform color. Ointment from frostbite on the intensity of staining of the skin has a mild irritant effect (6 points, table 2).

Example 8.

On the skin of rats inflicted 0.3 g of molten ointment "Finalgon, watched ischemic centre with a strong blue aura. Ointment "Finalgon intensity of okrashivaemoy has a pronounced irritant effect (8 points, table 2).

Table 1
Annoying activity ointments with bryony, from frostbite, "Finalgon and foundations (vaseline:lanolin anhydrous 85:10) (HAT-Contest)
Name ointmentAnnoying activity (classes)
no experienceThe average of 5 experiments
12345
Control (vaseline:lanolin anhydrous 85:10)111111
Ointment with bryony444444
Ointment from frostbite444444
Ointment "Finalgon555555

Table 2
Annoying activity ointments with bryony, from frostbite, "Finalgon and foundations (vaseline:lanolin anhydrous 85:10) (test on the skin of warm-blooded animals alive is different - rats-males)
Name ointmentAnnoying activity (points)
no experienceThe average of 5 experiments
12345
Control (vaseline:lanolin anhydrous 85:10010110,6
Ointment with bryony666666
Ointment from frostbite666666
Ointment "Finalgon888888

The method of obtaining ointment with external irritant and warming effect, by extraction of plant raw materials and the subsequent mixing of the extract with petroleum jelly and lanolin anhydrous, wherein the plant material - the roots of Bryonia white - crushed to particle size of not more than 3 mm, degreased with a mixture of chloroform-ethanol (2:1) for 7-10 h followed by removal of solvent, then dried meal from the roots of Bryonia white extracted with 70% ethanol at t is mperature 18-20° With, when the ratio of raw material: solvent 1:2.0 V for 144 h in six diffusers, and the first portion of the raw material is extracted with pure extractant, and each subsequent second, third, fourth, fifth, sixth extracted by the extract obtained by extraction of the preceding batch of raw materials, and then at a temperature of 50-55°With melted petrolatum and anhydrous lanolin in the ratio of 85:10, the mixture is cooled to a temperature of 25-30°C, the resulting mixture is mixed with 5 parts of the obtained liquid extract from the roots of Bryonia white.



 

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EFFECT: obtaining of new biologically active compounds and pharmaceutical compounds based on them.

27 cl, 4 ex, 1 tbl

FIELD: medicine; pharmacology.

SUBSTANCE: extract of the birch bark containing the specific amount of betulin is used in prevention and treatment of Parkinson's disease.

EFFECT: extract of birch bark is efficient for prevention and treatment of Parkinson's disease.

19 dwg, 7 tbl

Antiallergic agent // 2324491

FIELD: medicine; pharmacology.

SUBSTANCE: antiallergic agent is produced by toluene extraction of the birch bark and contains the active components such as betulin, lupeol and O-caffeate taken in particular quantities.

EFFECT: agent is efficient against allergy and doesn't reveal side effects.

11 tbl, 9 ex

FIELD: medicine; veterinary.

SUBSTANCE: homeopathic drug Lyarsin is used as a pharmaceutical agent. 0.7 mL of Lyarsin per head is administered intramuscularly to the animals suffering from hepatosis, at the first trimester of pregnancy, twice in 3 days.

EFFECT: method reduces number of stillborn puppies and increases brood per pupped dam.

3 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: film dosage form sticking to mucous, containing at least on active substance from hemp. The form contains the polymeric matrix, which is used as a reservoir for the active substance and sticking to mucous. The form can have the multilayer structure. It can also contain the non-active ingredients, odorants or aromatisors. The film form is used in treatment of pain in such diseases as carcinomatosis, AIDS, trauma and other disorders.

EFFECT: invention provides better tolerance to administered substances and rapid onset of administered drug, simplifies administration procedures.

19 cl

FIELD: medicine.

SUBSTANCE: therapeutic-cosmetic agent for the external use contains pantohematogen, water, polymeric gel-forming component, as well as dimethyl sulfoxide and water. The components are taken in particular quantitative ratio.

EFFECT: agent shows stable efficiency in treatment of osteoarthrosis and spinal osteochondrosis.

7 cl, 2 dwg

FIELD: medicine.

SUBSTANCE: therapeutic-cosmetic agent for the external use contains pantohematogen, water, polymeric gel-forming component, as well as dimethyl sulfoxide and water. The components are taken in particular quantitative ratio.

EFFECT: agent shows stable efficiency in treatment of osteoarthrosis and spinal osteochondrosis.

7 cl, 2 dwg

FIELD: medicine.

SUBSTANCE: invention relates to the compositions for care of the oral cavity, which contain the components of the Indian Mulberry, known as Morinda citrifolia L., for treatment of single or multiple abnormalities of the oral cavity and dental abnormalities, including the periodontal diseases, such as gingivitis and periodontitis, tooth destruction, bad smell and other disorders and irritations of the oral cavity.

EFFECT: composition provides efficient care of the oral cavity.

36 cl, 20 tbl, 11 ex

FIELD: medicine, oncology, amino acids.

SUBSTANCE: invention relates, in particular, to the development of an antitumor preparation based on natural substances. Invention relates to an amino acid preparation comprising at least one modified essential amino acid obtained by treatment of amino acid by ultraviolet radiation (UV) at wavelength 250-350 nm for 12-80 h at temperature 15-30oC or with ozone at temperature 15-25oC. The modified amino acid has no toxicity for health cells. Also, invention relates to a method for preparing such preparation. Invention provides the development of an antitumor preparation based on modified amino acids and expanded assortment of antitumor preparations being without cytotoxicity for normal cells.

EFFECT: valuable medicinal antitumor properties of preparation.

8 cl, 4 tbl, 2 dwg, 4 ex

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