Agent, method for its preparing and method for prophylaxis and treatment of small pelvis organs inflammatory disease and rectum disease
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to the development of a novel vegetable-base agent that can be used in treatment of inflammatory diseases of small pelvis organs and diseases of rectum. Agent used in prophylaxis and treatment of diseases of small pelvis organs and diseases of rectum comprises long turmeric (Curcuma longa L.) rhizome dried extract standardized by curcumin, anesthetic agent and pharmaceutically acceptable excipients. Agent is made as a suppository and comprises benzocaine as an anesthetic agent and vitepsol and cacao butter as a suppository base. Method for preparing agent used in prophylaxis and treatment of diseases of small pelvis organs and diseases of rectum involves mixing long turmeric dried extract standardized by curcumin with anesthetic agent and a pharmaceutically acceptable excipient. Method for prophylaxis and treatment of diseases of small pelvis organs and diseases of rectum involves using the proposed agent.
EFFECT: improved preparing agent, valuable medicinal properties of agent.
9 cl, 3 ex
The invention relates to the creation of new tools, plant-based in the form of rectal suppositories for the prevention and treatment of inflammatory diseases of the pelvic organs and diseases of the rectum.
The known range of chemical products for the treatment of fissures, fistula and other diseases of the anus and rectum: laxatives - Bisacodyl (RLS, M., 2002, page 155), gutalac (str), kabilin (str); anticoagulants - gepatrombin (str); antiseptics - atone (str); local anesthetics - benzocaine, etc.
However, these drugs have a narrow spectrum of pharmacological action.
The present invention is the creation of preventive and curative complex tools in the form of a rectal suppository for the treatment of inflammatory diseases of small bodies pelvis (prostatitis, vesiculitis, adnexitis, metritis, oophoritis), hemorrhoids moderate and mild severity of proctitis, proctosigmoiditis and paraproctitis, as well as fissures, fistula and rectal tumours.
The problem is solved by a group of inventions combined to form a single inventive concept.
The proposed remedy for the prevention and treatment of inflammatory diseases of the pelvic organs and diseases of the rectum containing dry extract of the rhizomes of turmeric (Curcuma longa L.), standardize the p on curcumin, anesthetic and a pharmaceutically acceptable fillers.
The tool is made in the form of a suppository.
Medicine as an anesthetic contains benzocaine.
The product contains dry extract of the rhizomes of turmeric, standardized by curcumin, benzocaine and suppozitornyj basis at a ratio of 1 suppository mass of 1 g:
|dry extract of the rhizomes of turmeric||25-100 mg|
|suppozitornyj base||the rest of it.|
As suppozitornoj bases used witepsol or cocoa butter.
Method for obtaining funds for the prevention and treatment of inflammatory diseases of the pelvic organs and diseases of the rectum, which consists in the fact that the dry extract of the rhizomes of turmeric, standardized by curcumin, mixed with anesthetic and a pharmaceutically acceptable filler.
Also we propose a method for the prevention and treatment of inflammatory diseases of the pelvic organs and diseases of the rectum, including the use of the above tools.
The product is used for the prevention and treatment of diseases of the pelvic organs, prostatitis, vesiculitis, adnexitis, metritis, oophoritis.
Means so the e is used for the prevention and treatment of hemorrhoids, prostatitis, proctosigmoiditis, paraproctitis, cracks, fistulas, tumors of the rectum.
Turmeric, K. home - Curcuma longa L., C. domestica Val. - a perennial herb of the ginger family (Zingiberaceae). The aboveground part of it consists of several oblong, with long stems basal leaves up to 1 m in length. Inflorescence spicate, about 30 cm tall, densely lined green top lighter stipules, in the axils of which are in the middle of the peduncle to develop flowers. The flowers are tubular, with a three-bladed, slightly irregular contour, yellow, lip broad, yellow. The root system is complex: a bulbous, almost rounded rhizome up to 4 cm in diameter, yellowish-gray, with circular scars of leaves from the apical Bud above ground part; several lateral buds develop in the underground, relatively short (about 3-10 cm long and 0.5-1 cm in diameter) cylindrical shoots. Fruits from turmeric are formed very rarely.
Turmeric comes from Eastern India and Vietnam.
Since time immemorial it is widely cultivated throughout tropical Asia.
For food and medical purposes rhizomes of turmeric. To speed up ripening spices collected roots before drying scald with boiling water, destroying the cells with dye - curcumin. Curcumin, originally located in the EF is Amalickiah cells, in the process of further fermentation evenly permeates the entire root. At the same time contained in the root of the starch is partially hydrolyzed and partially forms a colloid. Saturated paste of the root when dried becomes a "stone", in the context of shining like a horn, very dense, it sinks in water.
The most well-studied component of turmeric is curcumin (diferuloylmethane). Raw turmeric contains from 0.3 to 5.4% of curcumin. Turmeric also contains essential oil 4-14%, including tumerone, atlantone, and zingiberone. These oils have medicinal properties and can be the primary active component of turmeric in some conditions. Turmeric also contains sugar (28% glucose, 12% arabinose), proteins and resins [Leung A. Encyclopedia of Common Natural Ingredients Used in Food, Drugs and Cosmetics. John Wiley & Sons, New York, NY, 1980:313-314, Ammon HPT, Wahl MA. Pharmacology of Curcuma longa. Planta Medica 1991; 57:1-7].
Curcumin is poorly absorbed after oral administration. It was found that it is much more active when administered parenterally than through the mouth [Ammon HPT, Wahl MA. Pharmacology of Curcuma longa. Planta Medica 1991; 57:1-7]
This difference in action between enteral and parenteral reception can occur because of several factors. Studies on animals have shown that 40-75% of curcumin passes through the digestive system unchanged [Wahlstrom Century, Blennow G. A study on the fate of curcumin in the rat. Acta Pharmacol Toxicol 1978; 43:86-92, V. Ravindranath, N. Chandrasekhara Absorption and tissue distribution of curcumin in rats. Toxicol 190; 16:259-265].
A large part of what remains in the body, is actively metabolized in the intestinal mucosa and liver [Shoba g, Joy d, Joseph T., et al. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med 1998; 64:353-356].
Only traces of curcumin were found in the blood after oral administration of a single, dvuhkrugovoy dose in humans and even large doses in rats [Ammon HPT, Wahl MA. Pharmacology of Curcuma longa. Planta Medica 1991; 57:1-7, Shoba g, Joy d, Joseph T., et al. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med 1998; 64:353-356].
Absorption with oral administration can be improved by concurrent intake of piperine (from black pepper). Piperine has been shown to increase bioavailability of orally entered curcumin up to 2% [Shoba g, Joy d, Joseph T., et al. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med 1998; 64:353-356.]. The dosages used in the referenced study, piperine increased the absorption, bioavailability and concentration of curcumin in serum as in rats, in humans without side effects. Based on clinical experience, the typical recommended dose of curcumin - 400-600 mg three times a day.
It is established that the toxicity of turmeric is very low. No toxic reactions were detected when receiving standard doses of either humans or animals. No mortality, no teratogenicity was not detected at any of the doses of turmeric, her alcoholic extracts or curcumin during the study the animals, including rats, mice, Guinea pigs and monkeys [Shankar TNB, Shantha NV, Ramesh NP, et al. Toxicity studies on turmeric (Curcuma longa): Acute toxicity studies in rats, guinea pigs, and monkeys. Indian J. Exp. Biol. 1980; 18:86-92].
In the study of in vitro and in vivo in animals turmeric showed hepatoprotective effect: however, there are no clinical trials in humans. Was ustanovleno that turmeric like silymarin protects the liver of animals from a variety of hepatotoxic substances, including carbon tetrachloride [Xiang ZX, He XQ, Zhou GF, et al. Protective effects of an ethanolic extract and essential oil of Curcuma kwangsinensis S. against experimental liver lesions in mice. Chung Kuo Chung Yao Tsa Chih 1989, 14:303-305, 320. [Article in Chinese], Deshpande UR, Gadre SG, Raste AS, et al. Protective effect of turmeric (Curcuma longa L.) extract on carbon tetrachloride-induced liver damage in rats. Indian J. Exp. Biol. 1998; 36:573-577], galactosamine [Kiso Y, Suzuki Y, Watanabe N, et al. Antihepatoxic principles of Curcuma longa rhizomes. Planta Med 1983, 49:185-187], pentobarbital, 1-chloro-2,4-dinitrobenzene, 7 4-hydroxy-nonenal [Piper JT, Singhal SS, Salameh MS, et al. Mechanisms of anticarcinogenic properties of curcumin: the effect of curcumin on glutathione linked detoxification enzymes in rat liver. Int J. Biochem. Cell Biol 1998; 30:445-456] and acetaminophen (paracetamol) [Donatus IA, Sardjoko, Vermeulen NP. Cytotoxic and cytoprotective activities of curcumin. Effects on paracetamol-induced cytotoxicity, lipid peroxidation and glutathione depletion in rat hepatocytes. Biochem. Pharmacol. 1990; 39:1869-1875].
Hepatoprotective effect of turmeric is probably due to its powerful antioxidant action. Turmeric contains several water - and fat-soluble antioxidant components, of which the most active is considered curcumin [Choiu JW, Wei HC, Chunk-Kuo. Preliminary study on the anti-oxidative components of some species grown in Taiwan. Nung Yeh Hua Hsuch Hui Chih 1983; 21:97-103, Moken Y, Xianping D, Yaoshu T. Studies on the chemical constituents of common turmeric (Curcuma longa). Zhongcoayoa 1984; 15:197-198]. The antioxidant properties of other substances turmeric is also significant. From an aqueous extract of turmeric was isolated thermostable protein which was more effective against superoxide than curcumin, and more effective in ingibirovanii oxidative DNA damage [Shalini VK, Srinivas L. Lipid peroxide induced DNA damage: Protection by turmeric (Curcuma longa). Mol. Cell. Biochem. 1987; 777:3-10, Srinivas L, Shalini VK. DNA damage by smoke: Protection by turmeric and other inhibitors of ROS. Free Radical Biol Med 1991; 11:277-283, Selvam R, Subramanian L, Gayathri R, et al. The anti-oxidant activity of turmeric (Curcuma longa). J. Ethnopharmacol. 1995; 47:59-67].
Adding turmeric to the diet of rats (one percent turmeric from the weight of food for 10 weeks), it was found that it significantly protects against iron-induced peroxide formation lipids. The activity of superoxide dismutase, catalase and glutathione peroxidase were higher (about 19, 19, and 20%, respectively) in the liver homogenates of rats fed containing turmeric diet compared with controls [Reddy AC, Lokesh BR. Effect of dietary turmeric (Curcuma longa) on iron-induced lipid peroxidation in the rat liver. Food Chem Toxicol 1994; 32:279-283 of].
Compared with other known antioxidants, including butyl of hydroxyanisol (butylated hydroxyanisole), the butyl hydroxytoluene (butylated hydroxytoluene) and ellagic acid; extra the t turmeric and curcumin have been more proactive in protecting from the action of aflatoxin B1 on the liver of rats [Soni KB, Lahiri M, Chackradeo P, et al. Protective effect of food additives on aflatoxin on-induced mutagenicity and hepatocarcinogenicity. Cancer Lett, 1997; 115:129-133].
It was also found that turmeric and curcumin fully restore caused by aflatoxin liver damage, adding to the feed aflatoxin B1 (5 micrograms/day for 14 days) for ducklings. Fatty degeneration, necrosis and hyperplasia of the gallbladder caused by aflatoxin B1 were fully restored by curcumin [Soni KB, Rajan A, Kuttan R. Reversal of aflatoxin on induced liver damage by turmeric and curcumin. Cancer Lett 1992; 66:115-121].
In addition to its antioxidant effects, curcumin has also shown the ability to enhance detoxicating liver function by increasing the activity of glutathione S-transferase [Piper JT, Singhal SS, Salameh MS, et al. Mechanisms of anticarcinogenic properties of curcumin: the effect of curcumin on glutathione linked detoxification enzymes in rat liver. Int J. Biochem. Cell. Biol. 1998; 30:445-456, Susan M, Rao MN. Induction of glutathione S-transferase activity by curcumin in mice. Arzneimittelforschung, 1992; 42:962-964], the enzyme that binds glutathione with a large number of toxins, facilitating their removal from the body.
Essential oil and curcumin showed potent anti-inflammatory effect [Chandra D, Gupta S. Anti-inflammatory and anti-arthritic activity of volatile oil of Curcuma longa (Haldi). Ind J Med Res 1972; 60:138-142, Arora R, Basu N, Kapoor V, et al. Anti-inflammatory studies on Curcuma longa (turmeric). Ind J Med Res 1971; 59:1289-1295, Mukhopadhyay A, Basu N, Ghatak N, et al. Anti-inflammatory and irritant activities of curcumin analogues in rats. Agents Actions, 1982, 12:508-515.]. Orally taken curcumin have shown such the e efficiency, as cortisone or phenylbutazone in acute inflammation and half is weaker than these drugs in chronic inflammation, but without side effects [Mukhopadhyay A, Basu N, Ghatak N, et al. Anti-inflammatory and irritant activities of curcumin analogues in rats. Agents Actions 1982; 12:508-515]. One of the mechanisms of anti-inflammatory action of curcumin is likely due to its ability to block the synthesis of Pro-inflammatory arachidonic acid. Curcumin significantly inhibited the conversion of dihomo-gamma-linolenic acid to arachidonic acid in the fungus Mortierelle alpina and in microsomes of rat liver24.
Curcumin also has a choleretic effect. In rats, the synthesis of bile acids was increased more than 100% after they were orally administered curcumin [Shimizu S, Jareonkitmongkol S, Kawashima H, et al. Inhibitory effect of curcumin on fatty acid desaturation in Mortierella alpina 1S-4 and rat liver microsomes. Lipids 1992; 27:509-512]. Curcumin also increased the synthesis of other elements of bile, including cholesterol, bile salts and bilirubin [Ramprasad S, Sirsi M. Curcuma longa and bile secretion - Quantitative changes in the bile constituents induced by sodium curcuminate. J Sci Indust Res 1957; 16C:108-110].
Curcumin and its derivatives have shown antitumor activity in in vitro tests [Kuttan R., P. Bhanumathy, Nirmala K., George M.C. Potential anti-cancer activity of turmeric (Curcuma longa). Cancer Letters 1985; 29:197-202], and animals [Mesa MD, Ramirez-Tortosa, M.C., Aguilera C.M., Ramires-Bosca A. at Gil. A. Efectos farmacologicos y nutricionales de los extractos de Curcuma longa L. de los curcuminoides. Ars Pharmaceutica 2000; 41:3,307-321].
In vitro established that the various lines of cancer differ in their sensitivity to curcumin. Cell line derived from malignant tumors, leukemia, breast, colon, hepatocellular and ovarian carcinomas, were subjected to disintegration (apoptosis) in the presence of curcumin, while the lines of tumor cells of the lung, kidney, prostate, cervix, CNS tumours and melanoma were resistant to zitostaticescoe action of curcumin [Khar A, Alt AM, Pardhasaradhi BV, Varalakshmi CH, Anjum R, Kumari AL. Induction of stress response renders human tumor cell lines resistant to curcumin-mediated apoptosis: role of reactive oxygen intermediates. Cell Stress Chaperones 2001; Vol.6(4):368-376]. In a clinical trial in 15 patients with advanced colon cancer was set high therapeutic activity of turmeric extract, equivalent to 180 mg of curcumin taken orally [Sharma, R. A., McLelland, H.R., Hill, K.A., Ireson, C.R., Euden, S.A., Manson, M.M., Pirmohamed, M., Mamett, L.J., Gescher, A.J., and Steward, W.P. Pharmacodynamic and pharmacokinetic study of oral Curcuma extract in patients with colorectal cancer. Clin. Cancer Res. 2001; 7, 1894-1900].
Antimicrobial and antifungal action: sodium salt of curcumin in vitro inhibits the growth of Micrococcus pyogenes var. aureus at a dilution of 1:1000000 [Selected medicinal plants in Vietnam / by prof edition. To Dang Hai // National institute ofmateria medica, Hanoi-Vietnam, Vol.I, 440 p. Vol.II, 460 p., 1999].
Essential oil of turmeric inhibits Mycobacterium tuberculosis in a minimum concentration at the 1 g/ml, Bacillus mycoides and Candida albicans, in the context of what entrale 1/160 and B. subtilis at 1/250. Turmerone component of the essential oil inhibits the in vitro growth of various bacteria and fungi (Mvcobactenum tuberculosis, Shigella dysenteriae, Bacillus mycoides. In subtilis, Proteus vulgaris).
Curcumin inhibits in vitro growth of Mycobacterium tuberculosis in a minimum concentration of 25 g/ml. Salmonella paratyphi - 50 g/ml, Staphylococcus aureus - 50 g/ml [Selected medicinal plants in Vietnam / by prof edition. To Dang Hai // National institute of materia medica, Hanoi-Vietnam, Vol.I, 440 p. Vol.II, 460 p., 1999].
Curcumin has protivoyazvennye effect, inhibiting Helicobacter populating pylori (Helicobacter pylori).
Part of rhizomes curcumin reduces the bad cholesterol (low density lipoprotein) in the blood and normalizes the composition of bile.
Turmeric not only cleanses and improves blood circulation, and stimulates the formation of erythrocytes. This herb regulates metabolism, correcting as redundancy, failure of metabolic processes, and promotes the absorption of protein.
Established immunomodulatory property of curcumin. Under the influence of this substance increases the total number of leukocytes and antitelomerase cells, and also increases the phagocytic activity of macrophages [Selected medicinal plants in Vietnam / by prof edition. To Dang Hai // National institute ofmateria medica, Hanoi-Vietnam, Vol.I, 440 p. Vol.II, 460 p., 1999, Mesa MD, Ramirez-Tortosa, M.C., Aguilera C.M., Ramires-Bosca A. at Gil. A. Efectos farmacologicos y nutricionales de los extractos de Curcuma longa L. de los curcuminoides. Ars Pharmaceutica 2000; 41:3, 307-321].
The invention is illustrated by the following paragraph is kerami.
The examples differ in that the content of curcumin in children's candlelight is 25 mg and 50 mg, and in adults is 100 mg
Example 1. To 925 g melted fat (cocoa butter or witepsol)heated to a temperature of 40-45°add 50 g of dry extract of the rhizomes of turmeric, containing 50% of curcumin, 25 g of anesthetic (benzocaine), and thoroughly mixed in the mixer until a uniform distribution of the substances in the basis. Received candlestick mass is poured into a cooled mould 1000 candles 1 g each.
Example 2. To 875 g melted fat (cocoa butter or witepsol)heated to a temperature of 40-45°add 100 g of dry extract of the rhizomes of turmeric, containing 50% of curcumin, 25 g of anesthetic (benzocaine), and thoroughly mixed in the mixer until a uniform distribution of the substances in the basis. Received candlestick mass is poured into a cooled mould 1000 candles 1 g each.
Example 3. To 775 g melted fat (cocoa butter or witepsol)heated to a temperature of 40-45°add 200 g of dry extract of the rhizomes of turmeric, containing 50% of curcumin, 25 g of anesthetic (benzocaine), and thoroughly mixed in the mixer until a uniform distribution of the substances in the basis. Received candlestick mass is poured into a cooled mould 1000 is eternal 1 g each.
Received suppositories orange, torpedo-shaped form, with the possible splashes of yellow.
Store in a dry place protected from light at a temperature not higher than 25°C. shelf Life: 2 years. On the expiry date of the drug not be used.
- children up to 1 year;
hypersensitivity to the drug components.
Clinical trials were conducted on volunteers.
Suppositories were prescribed to adults and children with inflammatory diseases of small bodies pelvis (prostatitis, vesiculitis, adnexitis, metritis, oophoritis), hemorrhoids average and mild severity, proctitis, proktoshigmoidit and paraproctitis, as well as fissures, fistula and rectal tumours).
Way of application and dose.
Before the introduction of the suppository will need to empty the bowel. Suppository enter into the anus pointed end, possibly deeply. For more convenient insertion of the suppository, it is recommended to bend down, sit in the squat or lie on your side, crossed his legs. When rough handling and suppositories can leave on underwear stains orange color.
Dosage and administration:
Adults appoint 1 suppository (100 mg), 2 times a day, morning and night; maximum single dose of 200 is g; the maximum daily dose of 200 mg
Children aged 1-7 years appoint 1 suppository (25 mg) 2 times a day, morning and night; maximum single dose of 50 mg; maximum daily dose is 50 mg
Children aged 7-12 years old appointed on 1 suppository (50 mg) 2 times a day, morning and night; maximum single dose of 100 mg; maximum daily dose is 100 mg
Children over 12 years take 1 suppository (100 mg), 2 times a day, morning and night; maximum single dose of 200 mg; the maximum daily dose of 200 mg
Duration of drug treatment in inflammatory diseases ranges from 7 to 30 days, depending on the severity of the disease. In cancer of the limit on the duration of the drug not.
Side effects: When used in the recommended doses, the side effects were revealed.
Interaction with other drugs: in case of simultaneous use candles weaken the effect of chlorpromazine and barbiturates.
Hypersensitivity to the drug may result in irritation of the mucous membrane of the rectum, in some cases, pain in the rectal area.
Combined preparation for local application has a pronounced anti-inflammatory, antimicrobial, immunomodulatory, reparative, anti-oxidant, about ecbolium and protivoopujolevam action.
The combination of turmeric extract with anestetikom allows to achieve high results in the treatment of such intractable diseases as cracks, ulcers and fistulas anal canal. These diseases are difficult therapeutic treatment, as is characteristic of these diseases pain symptoms causes spasm of the mouse rectum, disrupting the circulation of the body and, thereby, preventing the healing of his injuries.
Present in suppositories anesthetic (benzocaine) as a result of anesthetic action leads to muscle relaxation and, consequently, to the weakening of the peristalsis of the rectum and restore blood flow. Due to this effect slows down the advance of feces in the colon and achieved prolonged action of the second component suppositories - curcumin. Curcumin has a strong anti-inflammatory and reparative effect on povrezhdeniya tissue. This combination of pharmacological properties of the above components provides a more efficient therapeutic effect compared with plain products of similar purpose.
1. The remedy for the prevention and treatment of inflammatory diseases of the pelvic organs and diseases of the rectum, characterized in that it contains dry extract of rhizomes curcumine (Curcuma longa L.), standardized by curcumin, an anesthetic and a pharmaceutically acceptable fillers.
2. The tool according to claim 1, executed in the form of a suppository.
3. The tool according to claim 1, as an anesthetic contains benzocaine.
4. The tool according to claim 1, contains dry extract of rhizomes of turmeric, standardized by curcumin, benzocaine and suppozitornyj basis at a ratio of 1 suppository mass of 1 g:
|Dry extract of the rhizomes of turmeric||25-100 mg|
5. The tool according to claim 1, where the suppozitornoj bases contains witepsol or cocoa butter.
6. The method of obtaining funds for the prevention and treatment of diseases of the pelvic and rectal diseases, characterized in that the dry extract of the rhizomes of turmeric, standardized by curcumin mixed with anesthetic and a pharmaceutically acceptable filler.
7. The method of prevention and treatment of diseases of the pelvic and rectal diseases, characterized by the fact that they use the tool according to claim 1 or 4.
8. The method according to claim 7, the means used for the prevention and treatment of diseases of the pelvic organs, prostatitis, vesiculitis, adnex is the metritis, oophoritis.
9. The method according to claim 7, the means used for the prevention and treatment of hemorrhoids, prostatitis, proximedia, paraproctitis, cracks, fistulas, tumors of the rectum.
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel derivatives of pyrimidine of the general formula (I) that possess properties of antagonists to adenosine A2-receptors and can be effective in relieve, for example, of defecation. In compound of the general formula (I) each R1 and R2 represents hydrogen atom; R3 represents hydrogen atom, halogen atom, amino-group, cyano-group, alkyl group comprising 1-6 carbon atoms, alkoxy-group comprising 1-6 carbon atoms, alkenyloxy-group comprising 2-6 carbon atoms, phenyl group that can be substituted with halogen atom, pyridyl group, furyl group or thienyl group; R4 represents pyridyl that can be substituted with a substitute chosen from the group comprising: hydrogen atom, halogen atom, amino-group, mono- or dialkylamino-group, aminoalkylamino-group wherein each has in alkyl residue from 1 to 6 carbon atoms, alkyl group comprising from 1 to 6 carbon atoms that can be substituted with halogen atom, hydroxy-group, amino-group, mono- or dialkylamino-group, alkoxycarbonyl wherein each has in alkyl residue from 1 to 6 carbon atoms, alkoxy-group comprising in alkyl group from 1 to 6 carbon atoms substituted with phenyl or pyridyl, hydroxyalkoxy-group comprising in alkyl residue from 1 to 6 carbon atoms, hydroxycarbonyl, alkoxycarbonyl comprising from 1 to 6 carbon atoms in alkyl residue, alkenyl group comprising from 2 to 6 carbon atoms, alkynyl group comprising from 2 to 6 carbon atoms, piperidinyl group that can be substituted with hydroxyl group, or represents group of the formula (IV): R5 represents phenyl that can be substituted with halogen atom, pyridyl group, thienyl or furyl group.
EFFECT: valuable biological properties of derivatives.
16 cl, 2 tbl, 185 ex
FIELD: pharmaceutical industry, in particular antacidal and purgative tablet.
SUBSTANCE: claimed tablet for peroral administration contains particles of magnesium oxide as active ingredient, wherein 1) magnesium oxide particles containing in tablet, have average secondary size measured by laser IR-scattering of 0.5-10 mum; 2) tablet contains 99 mass % or more of magnesium oxide particles: 3) tablet is not blacked and essentially has no spots formed in pelletization process; and 4) tablet disintegration time is 10 s or less.
EFFECT: tablets with high content of magnesium oxide particles and short disintegration time.
12 cl, 6 tbl, 5 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to a purgative agent composition comprising bicyclic compound of the formula (1) and a method providing the purgative effect and using compounds of the formula (1). He composition possesses the enhanced effectiveness.
EFFECT: valuable medicinal properties of composition.
42 cl, 3 tbl, 2 ex
FIELD: pharmaceutical industry, in particular medicine X-ray contrast diagnosis agent.
SUBSTANCE: claimed pellet-shaped agent contains oxymethyl uracil, barium sulfate for fluoroscopy and potato starch in ratio of 4:1 or 6:1, wherein corn is coated with 5 % alcohol/acetone acetylphthalylcellulose solution, 10 % low molecular polyethylene solution in hexane and medical adhesive. Agent of present invention provides disintegration ability of active ingredient in intestine for 2, 4, 6 hours.
EFFECT: system for intestinal diagnosis with treating action, improved convenience and sanitary effect.
FIELD: medicine, chemical-pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates to the development of purgative agents. Invention proposes novel compositions of medicinal agents possessing the purgative effect, pleasant taste and odor and comprising components taken in the optimal ratio and with minimal doses of separate active components in simultaneous enhancing economy in preparing, providing safety and simplifying a process in using the mixture. Purgative mixture comprising mixture of dry component involves senna extract, purging buckthorn extract and licorice roots extract, and/or major plantain extract, and/or rhubarb extract, and colt's foot extract, and/or oat extract, and/or anise fruits extract, and/or fennel extract as a water-soluble finely dispersed powder or water-soluble granules, or water-soluble tablets, and comprises additionally anise oil or dill oil, or flax oil, or thyme oil, or mint oil, or rose oil, granulated sugar or sugar powder or glucose, or lactose, or fructose, or sorbitol, or xylitol, or any other correcting agent, and mixture comprises additionally a bactericidal and/or stabilizing substance as sodium benzoate, nipagin or nepasol, or sorbic acid or any other preserving agent. A purgative agent comprises a powder-like mixture of senna extract, purging buckthorn extract, licorice roots extract, anise oil, sugar powder and sodium benzoate taken in the definite ratio. Compositions possess a mild purgative effect and without adverse effect.
EFFECT: improved and valuable medicinal properties of mixture.
15 cl, 5 ex
FIELD: medicine, phytotherapy, pharmacy.
SUBSTANCE: invention relates to the development of agents of vegetable origin used as purgative agents. Invention proposes the purified form of the gel-forming component from plantain flea seeds husk, and a method for preparing the gel-forming fraction from plantain flea seeds husk. Also, invention proposes methods for applying this gel-forming fraction as a purgative agent. Proposed compositions can be made in different medicinal formulations. Compositions show pleasant taste and safety.
EFFECT: improved and valuable properties of gel fraction.
20 cl, 6 tbl, 7 ex
FIELD: organic chemistry, medicine.
SUBSTANCE: invention relates to new 2-aminopyridine derivatives of formula I , wherein R1 is cyano, carboxyl or carbamoyl; R2 is hydrogen, hydroxyl, C1-C6-alkoxy or phenyl; R3 and R4 are aromatic hydrocarbon such as phenyl or naphthyl, 5-14-membered 5-14-membered optionally substituted aromatic group, excepted cases, when (1) R1 is cyano, R2 is hydrogen, and R3 and R4 are simultaneously phenyl;(2) R1 is cyano, R2 is hydrogen, R3 is 4-pyridyl, and R4 is 1-pyridyl; (3) R1 is cyano, R2 is 4-methylphenyl, and R3 and R4 are simultaneously phenyl;(4) R1 is cyano, R2, R3 and R4 are simultaneously phenyl, or salts thereof. Derivatives of present invention have adenosine receptor antagonist activity and are useful in medicine for treatment of irritable bowel syndrome, constipation, and defecation stimulation.
EFFECT: 2-aminopyridine derivatives as adenosine receptor antagonists useful in medicine.
34 cl, 2 tbl, 179 ex
FIELD: chemical and pharmaceutical industry.
SUBSTANCE: the present innovation deals with creating medicinal preparations of plant origin and could be applied for treating functional constipations and affected biorhythm of defecation. It is suggested to apply either dry aqueous or aqueous-alcoholic extract of horse chestnut seeds of Aesculus species to prepare curative-prophylactic preparation in case of constipation and affected biorhythm of defecation. The suggested preparation should be applied in the form of powder, tablets or suppositories. Pharmaceutical composition for preventing and treating constipation and affected biorhythm of defecation contains an active substance out of medicinal plant and a pharmaceutically acceptable filling agent, moreover, this preparation is designed as suppositories and contains either dry aqueous or aqueous-alcoholic extract of horse chestnut seeds of Aesculus species and suppository hydrophobic foundation at certain content of ingredients. Dry aqueous or aqueous-alcoholic extract contains 1-50% active substance as escin. As foundation it could contain either cacao oil or vitepsol. The method for preventing and treating constipations and affected biorhythm of defecation deals with introducing the suggested pharmaceutical composition into patient's anus 5-15 min before planned act of defecation. Application of "Rectum-activ" preparation provides positive result at treating functional psychogenic constipation: in 5-15 min after introducing a suppository into anus pronounced urgency for defecation. In case of course therapy for 4 wk one should observe restoration of natural urgency for intestinal evacuation. Moreover, purgative preparation causes no unfavorable pain feelings.
EFFECT: higher efficiency.
10 cl, 6 ex
FIELD: medicine, homeopathy, pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates, in particular, to suppository possessing immunomodulating effect and comprising coneflower, accessory substances and a base, sea-buckthorn oil, arborvitae (thuja) homeopathic essence, baptisia homeopathic essence, Timalin-1C homeopathic trituratium wherein coneflower is a component of homeopathic essence. Suppository comprises anhydrous lanolin and wax as accessory substances and cacao butter as a base wherein components are taken in the definite ration in grams per one suppository of weight 2 g. Proposed suppository possesses the enhanced immunomodulating effect and allows stimulating processes of regeneration and hemogenesis and improves processes of cellular metabolism.
EFFECT: valuable medicinal properties of suppository.
FIELD: medicine, pharmaceutics.
SUBSTANCE: the present innovation deals with rectal suppositories that contain biphosphonic acids and their pharmacologically acceptable salts applied for preventing and treating diseases caused by affected calcium and magnesium balance in the body. The suggested new suppositories contain 0.1-10 weight% xydiphone and 0.5-10 weight emulsifiers, the rest - the foundation for one suppository of 1.125-2.5 g weight. Rectal xydiphone-containing suppositories could additionally contain medicinal and/or biologically active supplements, for example 0.1-1.0 weight% trisodium salt of phosphonoformic acid as medicinal additive, and, also, biologically active additive chosen out of the group of vitamin B6, B12 or carbon dioxide solution of common camomile, olive oil. The innovation provides the chance to avoid some complications occurred at applying this preparation in known forms and, also, in some cases leads to its increased efficiency.
EFFECT: higher efficiency of application.
4 cl, 4 ex, 1 tbl
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to an agent used in treatment of rheumatic arthrosis and osteoarthrosis. Proposed suppository comprises glucosamine hydrochloride, 0.475-0.525 g, and solid fat or mixture of polyethylene glycols of molecular mass 1500 and 400 Da (95:5), the balance, per one suppository of mass 2.0-2.5 g. Invention provides enhancing bioavailability of glucosamine and decreases the level of allergic reactions.
EFFECT: improved and enhanced medicinal properties of composition.
FIELD: veterinary science.
SUBSTANCE: preparation for treatment and prophylaxis of endometritis in cows comprises antibacterial substance dioxydin, gelatin, glycerol and distilled water wherein food or medicinal gelatin is used as gelatin source, distilled glycerol if the 1-st grade is used glycerol source and comprises additionally resorcinol and veterinary algalipin in the following ratio of components, g: dioxydin, 0.1-0.3; resorcinol, 0.01-0.02; veterinary algalipin, 0.9-1.1; food or medicinal gelatin, 1.5-2.0; distilled glycerol of the 1-st grade, 5.0-5.4, and distilled water, 2.1-2.6. Invention provides enhancing effectiveness of the preparation and fertilization in cows.
EFFECT: improved and valuable veterinary properties of preparation.
FIELD: veterinary pharmacology, veterinary science.
SUBSTANCE: the suggested method deals with mixing formalin with components followed by heating with subsequent cooling at the following ratio of components including: 0.8%-formalin 5 ml, analgin 1 g, Veratrum tincture 1.0 ml, glycerol 5 ml, citric acid 0.2 g, gelatin 3 g.
EFFECT: enhanced curative result, more convenient medicinal form.
1 ex, 2 tbl
FIELD: medicine, gynecology, contraceptives, pharmaceutical chemistry.
SUBSTANCE: invention proposes vaginal suppository comprising benzalconium chloride, benzoic acid, purified water and the preparation vitespol taken in the definite content of components. Invention provides the reliable inhibition of fungal microflora being especially against fungus Candida albicans and the absence of irritation and symptoms in vagina drying. Invention can be used as an individual agent for prophylaxis of undesirable pregnancy.
EFFECT: valuable properties of suppository.
FIELD: medicine, chemical-pharmaceutical industry.
SUBSTANCE: invention relates to the development of new homeopathic suppository that can be used for treatment of prostatitis, hemorrhoid, uterus cervix erosion, endometritis. Invention proposes two variants. By the first variant agent represents suppository comprising the following components, g: propolis, 0.1; sea-buckthorn, 0.2; chestnut homeopathic essences, 0.1; Ginkgo biloba homeopathic essences, 0.1; aloe homeopathic essences, 0.1; milfoil, 0.1; wax, 0.1 and a base. The second variant represents suppository comprising the following components, g: sea-buckthorn, 0.2; propolis, 0.1; rue homeopathic essences, 0.05; Hypericum (Saint-John's-wort), 0.05; Symphytum (comfrey), 0.05; Tambukan curative muddy extract, 0.2; lanolin, 0.15; wax, 0.1, and a base. Proposed suppository elicits an anti-inflammatory regenerating effect and without toxic effect.
EFFECT: valuable medicinal properties of suppository.
15 cl, 4 ex
FIELD: pharmaceutical industry.
SUBSTANCE: new urogenital drug contains 50-250 g antibacterially efficient antibiotic erythromycin, 50-250 g antifungally efficient antibiotic nistatin, antiprotozoal preparation metronidazole, and 1.5-3.5 g (to complete weight of suppository) A type solid fat as filler. Drug can be used to treat mixed urogenital infections.
EFFECT: reduced treatment time, lowered recurrence of diseases, lack of adverse effects, and lowered cost.
FIELD: medicine, proctology, pharmaceutics.
SUBSTANCE: the present innovation deals with obtaining medicinal forms as suppositories applied for treating proctological diseases. Medicinal preparation as suppositories containing active substance, anesthetic, purified water and foundation could additionally contain antiseptic and local irritating substance, as an active substance - glucocorticoid at the following ratio of components, weight%: glucocorticoid 0.0277-0.0368, anesthetic 1.8-2.2, antiseptic 2.8-3.52, local irritating substance 0.288-0.352, purified water 1.8-2.2, foundation - the rest. As glucocorticoid that inhibits the release of inflammation mediators and causes pronounced antiphlogistic and antiallergic action one should apply, for example, hydrocortisone or synaflane. As anesthetic one should apply, for example, anesthesin, lidocaine or trimecaine. As antiseptic being of astringent, drying off and analgesic actions one should apply, for example, dermatol or xeroform. As local irritating substance being of reflector, venotonic, analgesic and antiphlogistic and, also, antimicrobial actions one should apply, for example, racemic menthol or essential oils.
EFFECT: higher therapeutic efficiency.
5 cl, 3 ex, 4 tbl
FIELD: medicine and immunology, in particular treatment and prevention immunodeficiency conditions and diseases associated with bacterial or viral aggression.
SUBSTANCE: claimed method includes administration to a patient immunoglobulin drug (e.g., pharmaceutical composition containing 6-12 % of specific heterologous secreted immunoglobulin A, isolated from milk or foremilk of immunized ungulates). Administration is performed parenterally wherein single dose is at least 10 IU/kg of patient weight for treatment or at least 5 IU/kg for prophylaxis; or perorally in dose of 0.2-0.5 g and/or topically one-two times per day for 1-5 days. Method of present invention makes it possible to decrease dose of administrating immunoglobulin due to prolonged retention of its high titers in body fluids.
EFFECT: enlarged range of application and assortment of immunoglobulin drugs.
4 cl, 5 ex
FIELD: medicine, dermatology, pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates to compositions used for skin care in itching dermatosis. The composition comprises essential oils of different plants, citrosept and cedar nut oil prepared by cold pressing method. Proposed composition possesses the stable effect on allergic and inflammatory processes and can be used as an accessory agent in treatment of itching dermatosis and allergic responses after hirudotherapy.
EFFECT: valuable medicinal properties of composition.