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Suppositories with bee moth larvae extract and bee-glue extract for treating gynecopathies

IPC classes for russian patent Suppositories with bee moth larvae extract and bee-glue extract for treating gynecopathies (RU 2429867):
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FIELD: medicine.

SUBSTANCE: suppositories contain 5 % ethanolic extract of bee moth larvae, 5 % ethanolic extract of bee-glue, Lutrol F 68, polyethylene glycol 4000 and Cremophore RH-40 in the following proportions, g: 5 % ethanolic extract of bee moth larvae - 0.09; 5 % ethanolic extract of bee-glue - 0.09; Lutrol F 68 - 0.75; PEG 4000 - 1.0; Cremophore RH-40 - 1.25.

EFFECT: suppositories exhibits a wide spectrum of biological and medical activities: immunomodulatory, antistress, antioxidant, regenerative and antibacterial action improving microcirculation, blood rheology and utero-placental circulation, provide uniform active ingredient release, evident prolonged action and individual usability.

1 cl, 3 ex

 

The present invention relates to medicine, namely to the pharmacy, and concerns the development of medical suppositories containing extracts of large larvae of the wax moth (LBVM) and propolis, and can be used in complex treatment of inflammatory diseases of female sexual sphere (salpingoophoritis, endometritis, infertility, menopausal disorders, correction of the various manifestations of placental insufficiency in the combined treatment of threatened abortion.

Known gynecological of ovule for complex treatment of inflammatory diseases of female sexual sphere, made in the form of capsules, including gelatin, glycerin and purified water weight 2.5 g, and containing as active ingredients BHT and oil extract of propolis 15% (patent RU 2249449, 2005). The invention provides getting dosed means having a prolonged regenerative and anti-bacterial action, convenient and hygienic to use.

Know the treatment for non-inflammatory and inflammatory diseases of female pelvic organs, including complications of purulent-inflammatory processes in the form of vaginal suppositories containing the active substance 2-ethyl-6-methyl-3-oksipiridina succinate and a base selected from the group of the polyethylene shall noxid 1500, the polyethylene oxide 400, cocoa butter, hydrogenated fats (patent RU 2293558, 2007). The invention provides a prolonged release of therapeutic drug in the mucous membranes and soft tissues, and provides the action for about 12 hours, while the procedure itself is comfortable and easy to perform and can be done by patients themselves in the outpatient setting.

The prototype of the invention are suppositories for the treatment and/or prevention of gynecological diseases, characterized in that the active substances they contain pharmaceutical composition comprising propolis, naphtha, essential oils of calendula, St. John's wort, eucalyptus, cedar, tea tree, buckthorn and tocopherol acetate, the extracts of the fruits, tomatoes, currants, licorice, periwinkle, lady's bedstraw, calendula and TUI at a certain ratio of components, and as a basis they contain cocoa butter or tallow (application EN 2006132907, publ. 2008). The disadvantages of these suppositories are complexity, the complexity of the composition and process of production of a receipt.

The objective of the invention is to create a new dosed medications domestic production in the form of suppositories containing extract VVM and propolis extract, possessing a wide spectrum of biological and l the educational activity, immunomodulatory, anti-stress, antioxidant, regenerating and anti-bacterial effect, improves microcirculation, blood rheology and utero-placental circulation, with a uniform release of active substances and severe prolonged action, suitable for use by patients themselves.

The technical result - obtaining means expressed prolonged action for comprehensive treatment of patients with inflammatory diseases of female sexual sphere, convenience and hygiene applications.

This technical result is achieved in that the means in the form of suppositories for the treatment of gynecological diseases, containing propolis as active substance and vegetable oil as the basis, according to the invention as propolis contains 5% alcohol extract of propolis and additionally contains as active ingredient 5% alcohol extract of larvae of the great wax moth, and as a vegetable oil contains cremophor RH-40 and additionally as the basis contains lotrel F 68 and polyethylene glycol 400 in the following ratio of components 1 suppository, g:

5% Alcohol extract large larvae of the wax moth 0,09
5% Alcoholic extract of propolis 0,09
Lotrel F 68 0,75
Polyethylene glycol 4000 1,0
Cremophor RH-40 1,25

All components included in the suppositories allowed for medical use.

Lotrel F 68 BASF (Germany) 9003-11-6. Lutrol®F 68 - hydrophilic polymer, a block copolymer of polyoxyethylenesorbitan, available in granular form with an average particle size of about 1000 microns, while the non-crystalline active ingredients have a particle size in the range of 20-200 microns. One of the physical methods of increasing the solubility of the active ingredient is to increase surface by micronisation. Another way is the use of solubilization, such as surface-active polymers - poloxamer.

Cremophor RH-40 BASF (Germany) P # 013635/01-2002. Cremophor®RH-40 - ethoxylated hydrogenated castor oil, included in the Pharmacopoeia of the United States called "Polyoxyl 40". It is used as a solubilizer has the ability to enhance the pharmacological effect of drugs that can reduce their doses, can eliminate n the compatibility of the ingredients in the compositions. Has an absolute stability in hard water, in the majority of polling emulsifying, wetting and solubilizing ability, relatively low toxicity and other

Polyoxyethyleneglycol (PEG) 4000 TU 2483-166-05757587-2000. In the pharmaceutical industry is used as an auxiliary substance for the production of pharmaceuticals. Used as a thickener, softener, binders, moving and facilitate outflow of the agent, and as a solubilizer has no emulsifying effect.

Propolis is THE GOST 28886-90. The introduction of the suppositories drug propolis extract alcohol in the amount of 3% in combination with an extract LLVM increases antimicrobial activity, tissue regeneration, promotes the expression of analgesic, hemostatic, immunomodulating, reparative effect of the dosage form.

The alcohol extract of the larvae of the wax moth. Patent N 2038086, 1995. "A method for obtaining a biologically active product of the large larvae of the wax moth". Extract the larvae of the wax moth contains a large set of macro - and micronutrients. Among them, potassium, phosphorus, magnesium, zinc, iron, and trace elements with high biological activity - copper, manganese, selenium, chromium, molybdenum, cobalt.

The number of essential and non-essential acids of devjatnadcat is. Among them are amino acids, with the highest therapeutic effect: Proline, aspartic and glutamic acids, lysine, histidine. These amino acids necessary for protein synthesis, hormones, enzymes, etc. They also have a positive effect on tissue metabolism. Gamma-aminobutyric acid has anti-stress activity. Biological active compounds, such endogenous steroid hormones have an anabolic, adaptogenic, hypocholesterolemic action, as well as immunomodulatory, anti-stress, antioxidant effect, improves microcirculation, blood rheology, improve uteroplacental blood flow, and with a wide range of biological and therapeutic activity.

The following preparations containing alcohol extract LLVM: balsam Dr. Mukhina, complex drug "Vita" in the form of tinctures of medicinal plant raw materials containing dandelion root, motherwort, cottonweed marsh, hawthorn flowers, grass of a horsetail herb mistletoe, the leaves of the periwinkle, yarrow herb, Cystoseira bearded, herb Rue, the herb cinquefoil goose, flowers of Arnica, St. John's wort herb, caraway seeds, leaves, lemon balm, Valerian root, flowers, Lily may, grass creeping thyme, chamomile flowers, mint leaves is arachnoi, digitalis lanata, fennel, hops, grass spring Adonis in combination with an extract LLVM /Accacco, Masakova. Apitherapy. Manual for doctors. Ryazan. - 2003. - S./; balsam Dr. Rachkova, "Vetmedin"that contains honey extract LBWM, complex drug "Galery with extract LLVM /Accacco, Masakova, Trading, Ayiguenou. Perspectives and advances in the use of therapeutic and prophylactic preparations based on extracts of large larvae of the wax moth. - S-281; Apitherapy today (publication 13). Proceedings of the XIII all-Russian scientific-practical conference "Successes apitherapy". Fish. - 2008./, with a wide range of biological and therapeutic activity. therapeutic effect of these tools is not prolonged action due to liquid consistency and is used in the form of tinctures for internal use, which is inconvenient in use, the funds are not dosed for a single admission, intended for internal use and not intended for intravaginal way of introduction.

In the available scientific and medical and patent literature information about known drug for treatment of gynecological diseases in the form of suppositories containing alcohol extract large larvae of the wax moth, alcohol extract of propolis, Lutron F 68, polietilen icol 4000 and cremophor RH-40 at a certain ratio of components, not found. Thus, the claimed invention meets the criterion of "novelty".

As a result of experimental studies, it was found that the tubes have a high bioavailability and a number of advantages: they have a beautiful appearance, homogeneous, elastic, which is important for vaginal medicines; therapeutic effect of the extract VVM and propolis extract appears 5 minutes after administration; complete dissolution after 15 minutes. Suppositories are very promising for applications in gynecology. The composition suppozitornoj bases contributes to fast and then the prolonged release of active substances of the extract VVM and propolis extract. Giving the drug form of suppositories provides convenience and hygiene applications, the storage stability. Introduction in the drug extract LBVM in the amount of 3% in combination with propolis extract in the amount of 3% by weight of the basis increases antimicrobial activity, tissue regeneration, promotes the expression of analgesic, hemostatic, immunomodulating, anti-stress, antioxidant, improves microcirculation, blood rheology, improve uteroplacental blood flow, namely a wide range of biological and l the educational activity effective and efficient dosage forms. In addition to the manifestations of the known properties of each component of the proposed structure together strengthens their influence, because, obviously, the effect of their synergies. Thus, the claimed invention meets the criterion of "inventive step".

Example 1. Part 1 suppository mass of 3.0±5% g: alcohol extract large larvae of the wax moth 0,09; alcohol extract of propolis 0,09; lotrel 68-0 F,75, PEG 4000 - 1.0; cremophor RH-40 1,25.

In beaker melt lotrel F 68, PEG and cremophor RH-40 in a water bath at a temperature not exceeding 70°C. To remove air without mixing incubated for 30 minutes at a temperature of 45°C. the Extract LLVM alcohol and propolis extract alcohol injected into suppozitornyj mass, stirring constantly with a glass rod. Metal suppozitornoj form is wiped with a gauze pad moistened with vaseline oil, is cooled in a refrigerator at a temperature of 3-5°C for 5-6 minutes and pour cooked suppozitornyj mass at a temperature of 38-40°C for 1-2 seconds. Forms are placed in the refrigerator for 7-10 minutes, then frozen suppositories are removed. Quality suppositories appreciate the appearance, elasticity, homogeneity, solubility. Received suppositories correct form, solid and homogeneous. Full time dissolving 15 minutes. Have expressed prolongers the TES action due to the optimum composition framework that is, the active ingredients of propolis extract and the extract LLVM enter the body immediately and then kept on the mucosal surface for a certain period of time, provide long-term effects of drugs with intravaginal the introduction of the patient. Suppositories convenient and hygienic to use, because the proposed composition of the ingredients.

Example 2. Part 1 suppository mass of 3.0±5% g: alcohol extract large larvae of the wax moth 0,09; alcohol extract of propolis 0,09; Lutron F 68-1,0; PEG-4000-1,0; cremophor RH-40 and 1.0.

Made of medical suppositories in a similar way. Received suppositories irregular shape, the poor are removed from the forms and non-uniform.

Example 3. Part 1 suppository mass of 3.0±5% g: alcohol extract large larvae of the wax moth 0,09; alcohol extract of propolis 0,09; Lutron F 68-1,25; PEG-4000-1,25; cremophor RH-40 0,5.

Made of medical suppositories in a similar way. Received suppositories homogeneous, regular shape, the poor are removed from the forms, crumble, break.

The given examples show that the optimal from the point of view of ease of application and the effectiveness of treatment is the composition described in example 1. Receive offer suppositories and easy when using DOS is ikaetsya this technical result. Thus, the claimed invention meets the criterion of "industrial applicability".

Clinical trials have shown that the amount of released drug at a given ratio of components in one suppositories equally in patients studied. This allows the gynecologist in practical medicine, depending on the form and severity of the disease to recommend patients required number of suppositories for self-treatment, which makes the claimed suppositories promising dosage form in practical gynecology. For example, studies have been conducted on the use of suppositories in treatment of gynecological diseases of female genital sphere (salpingoophoritis, endometritis, infertility, menopausal disorders, correction of the various manifestations of placental insufficiency in the combined treatment of threatened abortion. It is possible to use suppositories sick yourself.

Means in the form of suppositories for the treatment of gynecological diseases, containing propolis as active substance and vegetable oil as the base, characterized in that the quality of propolis it contains 5%alcohol extract of propolis and additionally contains as active ingredient 5%with litovoi extract large larvae of the wax moth, and as vegetable oil contains cremophor RH-40 and additionally as the basis contains lotrel F 68 and polyethylene glycol 4000 in the following ratio of components 1 suppository, g:

5%alcohol extract large larvae of the wax moth 0,09
5%alcoholic extract of propolis 0,09
lotrel F 68 0,75
polyethylene glycol 4000 1,0
cremophor RH-40 1,25

 

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