Tranquilliser and functional foodstuff
FIELD: medicine, pharmaceutics.
SUBSTANCE: there are offered an anxiolytic and/or antidepressant drug which contains vitamin K2 in the amount of 10 mcg to 100 mcg as an active component, a food additive for the same application and an appropriate method of treating.
EFFECT: vitamin K2 (preferentially - menaquinone-4 and/or menaquinone-7) is safe to use for a long period of time and shows tranquilising action, particularly bland, antidepressant and antistress action.
4 cl, 2 dwg
The technical field of the invention
 the Invention relates to a tranquilizer and containing functional foods. More specifically, this invention relates to safe tranquilizer foodborne-containing functional food product.
The level of technology
 the Growth of mental disorders such as depression, anxiety, impaired autonomic regulation and the like caused by excessive stress due to physical or emotional pain, has become a serious problem. For its solution have been developed and used numerous antidepressants and sedative substances, containing as an active ingredient chemicals. At the same time, it is also known that traditional medicines have side effects, are addictive, and the like.
 In this regard, it is desirable to develop a safe component of food origin. To food and food ingredients, which are known to have antidepressant and sedative effect, include GABA (GABA), ginseng, St. John's wort and extract of Apocynum venetum. Examples of food products and food ingredients, which are known to have anti-stress effects are theanine, soy peptide, polyphenol cocoa, mushroom, matsutake and Grifolafrondosa (off-patent document 1). However, their effect is quite moderate.
Off-patent document 1: Development and prospects of anti-stress food. Under the leadership of Hidehiko Yokogoshi, CMC Publishing CO., LTD (2006).
Description of the invention
 while creating a safe food ingredient or nutrients, are widely used as food and possessing anxiolytic action, such as relieving anxiety, providing antidepressant and anti-stress effect is desirable, such food ingredients currently unknown. Under these conditions, the objective of the present invention is to provide compounds having a significant anxiolytic effect and obtained from food-safe ingredient for a long time used as food.
 the inventors have found that vitamin K1 and vitamin K2 derived from food into body tissues in menechino-4 (MK-4). The inventors have tried to clarify the function of vitamin K in the brain based on the data indicative of extremely high concentrations of MK-4 in the brain. In the result of investigations, the inventors have found that vitamin K has a tranquilizing effect, in particular the terms of anxiety, has antidepressant and anti-stress effect, and has achieved the objectives of this invention. In other words, this invention is a tranquilizer that contains vitamin K.
 In the present description, the term "tranquilizer" is used as a generic term for soothing substances, antidepressant, anti-stress substances and the like.
 currently Known function of vitamin K is limited to his alleged participation in the accumulation of sphingolipids (Carrie, I. et al. / Carrie and others (2004) J. Nutr. 134, 167-172) and the metabolism of sulfatides (Denisova, NA & Booth/Denisova and Booth, SL (2005) Nutr. Rev. 63, 111-121) and still not fully understood. Accordingly, despite the assumption on the part of vitamin K in the implementation of a number of physiological functions of the brain are still not supported the hypothesis that vitamin To living beings, including humans, has a tranquilizing effect.
 Vitamin K includes vitamin K1 generated by the plants, vitamin K2 generated by the microorganisms, and vitamin K3, representing a synthetic substance. Further, the vitamin K2 is divided into MK-4 to MK-15 depending on the length of the isoprenoid side chain. Because vitamin K is converted in the body into MK-4, as described above, vitamin K1 or vitamin K2 can be used as vitamin K as a medicinal the CSO funds described in this invention. It is preferable to use vitamin K2, which has a high physiological activity, and even more preferred is the use of managenone-4 and/or managenone-7.
 furthermore, this invention is a dietary Supplement, medical food or functional food containing the tranquilizer.
 a Calming substance containing vitamin K as an active ingredient in accordance with the present invention, is a tranquilizer, very safe for the human body. While the daily requirement of the human body in vitamin K is 55-80 mcg (according to the Recommended dietary intake of Japan, 2005), tolerable upper level of intake To not installed. From this we can say that vitamin K is a safe substance. In this regard, the tranquilizer described in this invention, is superior in security known traditional substances, relieving anxiety, antidepressants and anti-stress substances.
 the Tranquilizer described in this invention also has the advantage in terms of duration of action, because vitamin K, a fat-soluble, it is easier to accumulate in the body than traditional substances, SN the occupying state of anxiety, antidepressants and anti-stress substances.
 in Addition, the tranquilizer described in this invention, is intended for the prevention of diseases such as depression, because it is extremely convenient for daily admission as a functional food and medical product supply.
Brief description of drawings
 figure 1 shows the weight change of the mice in groups, taking vitamin K, described in this invention, and in the control group (the control group who took the media), taken as a comparative example, a week, during which mice were given substance. Data are presented as mean values ± standard deviation for 10 mice. The analysis of the obtained values by the method of t-test in the control group and in groups menechino-4" or "menechino-7" significant differences were not found.
Figure 2 shows the time profile of akinesis-induced reaction of fear (every 60 seconds), for mice in groups, taking vitamin K, described in this invention, and in the control group, taken as a comparative example. Data are presented as mean values ± standard deviation for 10 mice. In the two-factor analysis of variance detected a significant decrease in time of akinesis in the group "menechino-4, and m is Nahyan-7 compared with the control group, moreover, the significance level is P<0.01 and P<0,05, respectively.
A detailed description of the preferred embodiments
 the Following describes one example of an embodiment of a tranquilizer described in this invention. First, vitamin K, appropriate for tranquilizer described in this invention, includes vitamins from K1 to K3. Vitamin K1 is abundant in green and yellow vegetables, beans, vegetable oil, seaweed, fish products, etc. Vitamin K1, which represents a light yellow fat-soluble oil, resistant to heat, but in light of the fragile. Vitamin K1 can exist in the form of oxide.
 Vitamin K1 is extracted, followed by purification using a known method (for example, Japanese laid patent No. 5-155803) of Japanese Basil, Perilla, Molokai, parsley, garland chrysanthemum, Japanese mustard spinach, spinach, Japanese viscositiy, alfalfa leaf hazelnut, chestnut leaves, young shoots of barley, young shoots of oats, cabbage, broccoli, cauliflower, tomatoes, vegetable oils (e.g. soybean oil, rapeseed oil, sesame oil, walnut oil, corn oil, safflower oil, sunflower oil, rice oil and olive oil and similar products. Vitamin K1 also receive Sint the optical path. Commercially available vitamin K1 can also be used for the purposes of the invention without limitation.
 Vitamin K2 includes homologues from managenone-15 (MC-15) to managenone-4 (MK-4) depending on the length of the isoprenoid side chain attached to naftochinona "skeleton". Vitamin K2 is generated by microorganisms and is found in large amounts in fermented soy beans and dairy products such as cheese. For example, managenone from MK-6 to MK-9 are contained in the cheese, and MK-7 is contained in large quantities in fermented soy beans. In addition, vitamin K2 is also produced by bacteria in the intestinal tract.
 Vitamin K2 is generated during the fermentation of microorganisms, such as bacillus natto, in accordance with the methods described, for example, in Japanese laid patent No. 08-073396, 11-92414, 10-295393 and 2001-136959. Commercially available vitamin K1 can also be used for the purposes of the invention without limitation.
 it is Known that the side chain of vitamin K1 or K2, obtained from food, are separated in the body, resulting in K1 or K2 becomes geranyloxy group and later in the MK-4. In this regard, I believe that MK-4 has a direct effect other than γ-carboxylation of vitamin K-dependent protein, and therefore MK-4 is also called active vitamin K. moreover, it is known that the amount of MK-4 in the brain increases more substantially, if you use MK-7, derived from fermented soybeans, and is not directly MK-4 (Rumi Ozaki et al./Rumi Ozaki and others (2006), Vitamins, 80, 203).
 Vitamin K3 is a synthetic compound. When vitamin K3 taken in large quantities, there are side effects. In this regard, it is preferable to use vitamin K1, extracted with subsequent cleaning of vegetables, and vitamin K2 extracted from substances fermented with Bacillus natto and similar microorganisms, because, as the experience of eating them, they are more secure. More preferably the use of vitamin K2, as it can easily be produced at low cost. Independent or sharing managenone-4 (MK-4) and managenone-7 (MK-7), tested as food, is especially desirable.
 in Addition to vitamin K as a main component, to the effect described in this invention can be added to one or more food ingredients or types of herbs, antidepressant and anti-stress effect which is widely known.
 in Addition to vitamin K as a main component and food ingredients and herbs, with appropriate antidepressant and anti-stress effect, to the effect described in this izobreteny is, can be added pharmacologically accessible environment, excipient and the like substances, if they do not inhibit the beneficial effect of the invention.
 Among examples of these environments include carriers or excipients, such as lactose, sucrose, fructose, glucose, hydrate glucose, soft white sugar, refined sucrose, erythritol, xylitol, sorbitol, mannitol, palatinose, shredded palatinose, powdered powdered maltose, glucose, carmellose, dextrin, starch, sugar corn, klasterizovannykh starch, partially klasterizovannykh starch, potato starch, corn starch, oxypropylated starch, amino acid, kaolin, silicon dioxide, silicic acid, aluminum silicate, sodium bicarbonate, calcium phosphate, secondary acidic calcium phosphate, calcium carbonate, magnesium oxide, aluminum hydroxide, fatty acid or its salt, monoglyceride of a fatty acid and diglyceride fatty acids, alcohol, vegetable oil, olive oil, soybean oil, corn oil, rich in oil, oils and fats, viscous paraffin, propylene glycol, ethylene glycol and glycerol; binders, such as crystalline cellulose, crystalline cellulose·nutricology, methylcellulose, hydroxypropylcellulose, hydroxypropylcellulose Snezkou the degree of substitution, hydroxyp pelletizers, phthalate of hydroxypropylmethylcellulose, acetylsuccinate hydroxypropylmethylcellulose, nutricology, ethylcellulose, karboksimetiltselljuloza, hydroxyethyl cellulose, wheat starch, rice starch, starch sugar corn, potato starch, klasterizovannykh starch, partially klasterizovannykh starch, oxypropylated starch, dextrin, pullulan, polyvinylpyrrolidone, aminoalkylation copolymer E, aminoalkylation copolymer RS, methacrylic acid copolymer L, methacrylic acid copolymer, diethylaminoacetate polyvinylacetal, polyvinyl alcohol, gum Arabic, powdered acacia, agar, gelatin, white shellac, tragant and macrogol; lubricants, such as wheat starch, rice starch, starch sugar corn, synthetic aluminum silicate dried gel aluminium hydroxide, alumosilicate magnesium, secondary acidic calcium phosphate, anhydrous dibasic calcium phosphate, wax, hydrogenated vegetable oil, polyethylene glycol, light anhydrous silicic acid, synthetic aluminum silicate, stearic acid, macrogol, talc, magnesium stearate, calcium stearate, water, silicon dioxide and an ester of a fatty acid sucrose; lubricant; dezintegriruetsja agents, such as crystalline cellulose, methylcellulose is a, hydroxypropylcellulose with a low degree of substitution, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, wheat starch, rice starch, starch sugar corn, potato starch, partially klasterizovannykh starch, oxypropylated starch, carboxymethoxy starch sodium and tragant; surfactants, such as soybean lecithin, esters of fatty acid and of sucrose, polyoxyl stearic acid, polyoxyethylene-hydrogenated castor oil, polyoxyethylene polyoxypropyleneglycol, servicesecurity, sarbatorile, servicemonitor, servicemanagement, sorbitanoleat, Polysorbate, glycerylmonostearate, sodium lauryl sulfate and lauromacrogol; emulsifying agent; solubilizing agents such as centripetal; a substance that causes or facilitates the absorption; pH regulators such as hydrochloric acid, citric acid, sodium citrate, acetic acid, tartaric acid, sodium hydroxide, potassium hydroxide, sodium bicarbonate, sodium carbonate and lactic acid; brightening agents, such as natural resin; a stabilizer; an antioxidant; a preservative; a moisturizing agent; a dye; the aroma and soothing agent.
 the Content of vitamin K in the tranquilizer described in this invention, depends on the magnitude of the received dose is. Typically, this content is in the range from 0.0001 to 100% (weight) and is preferably 0.001 to 90% (weight), more preferably from 0.01 to 70% (by weight) and more preferably from 1 to 50% (weight). If the content of vitamin K does not exceed 0,0001% (weight), the amount needed for a calming, antidepressant and/or anti-stress action, is not achieved.
 the Tranquilizer described in this invention, is processed in the form of solution, powder, granules, tablets, capsules, syrup, etc. for use as a medicine, food additives, functional food products or nutritional therapy. The preferred form of tablets or capsules, because vitamin K is soluble in fats.
 the Tranquilizer described in this invention can be directly added to the original material, if the material is processed in a traditional grocery products, such as bread, steamed rice, soup, side dishes, cakes and candy.
 Methods of use of tranquilizer described in this invention, as medicines are almost unlimited. For example, they include oral ingestion, transdermal input, infusion and injection (intramuscular, intra-abdominal, subcutaneous and intravenous). It is preferable to take the tablet or capsule is orally inside, since this reduces the load on the patient.
 the Scope of the tranquilizer described in this invention, include depression, anxiety, neuroses, state of painful anxiety, anthropophobia syndrome obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder (PTSD), acute stress, impaired autonomic regulation, crazy state, hallucination, mania, epilepsy, fatigue, tremor, convulsions, sweating, palpitations, tachycardia, acute pain, chest pain, headache, enuresis and insomnia as a result of these symptoms.
 the regimen of tranquilizer described in this invention is determined on the basis of symptoms and weight of the patient, the interval between meals and various factors that affect other clinical effects. As a rule, the daily dose of vitamin K for adult men can be in the range from 10 μg to 100 mg, preferably from 20 μg to 100 mg For therapeutic purposes vitamin K can be used in an amount of from 6 to 100 mg If you expect a stronger effect of possible dose up to 1800 mg for an adult male weighing 60 kg
 If the tranquilizer described in this invention, is used as a dietary Supplement, functional food, medical nutrition product or product PI of the project in General, the preferred daily dose of vitamin K for adult men is from 10 mg to 45 mg, and more preferably from 50 mg to 45 mg with security considerations.
 the Tranquilizer described in this invention can be used as a therapeutic or functional food with a sedative, antidepressant and/or anti-stress action not only against people, but against mammals, such as Pets. Methods include neuronally technique, for example by injection, and oral administration in the form of functional foods and mixed meals.
 Below the invention is explained in more detail on the example, it should be noted that it is not limited to Example 1.
External pulse enters the brain through the senses and sent to the amygdala and hippocampus, lateral septum, where a decision is made whether the pulse helpful or harmful. (This estimate is called a "biological value".) The parsed information is stored in the amygdala body and the hippocampus. At the same time there is a biological reaction that is visually recognized by the observer in the form of emotional manifestations. Man and animal digest (receive) information on the basis of the assessment of biological value in the course of everyday activities. Upon receipt of the same signal is compared in the almond-shaped body and the system of the hippocampus, lateral septum. The corresponding reaction is called "conditioned reflex emotional reaction". Suppose a rat or mouse was placed in a special box and exposed to an electric pulse, which is unpleasant for her. Six days later, when the premises of this rat or mouse in the same box it within a certain period of time is in a state of immobility (akinesis) despite the absence of electrical stimulation. This akinesis is called "conditioned reflex akinesis". Currently, the model animals are widely used to evaluate the sedative and antidepressant action, thus reducing the time of akinesis is used as indicator. It was confirmed that akinesis partially removed through, for example, oral administration of 30 mg/kg milnacipran hydrochloride, commercially available anti-depressant.
 using the above system assessment of anxiety was studied, does the tranquilizer described in this invention, the same effects as commercially available anti-depressant. In particular, mice with conditional reflex reaction of fear within 7 days of the force introduced by the sample, including Vita is in K and the environment, or control sample that includes only environment. The effect of the application of such sample was studied by time akinesis mice.
Methyl cellulose (product name: Metolose (registered trademark), SM-400, hereinafter referred to as "MS") for use as the environment was acquired by the company Shin-Etsu Chemical Co., Ltd. It was dissolved in the solvent for injection (production Otsuka Pharmaceutical Factory, Inc.) obtaining a solution of 0.5 g/100 ml
 Menechino-4 and menechino-7 as vitamin K, intended for use as an active component a sedative described in the invention were acquired in the company Wako Pure Chemical Industries, Ltd. After weighing a specified number of managenone-4 or managenone-7, suspended in 0.5% MC to achieve the desired concentration. Mice from the control group was given only the medium (0.5% of MS).
 the Male mice aged 10 weeks (C57BL/6NCrlCrlj, SPF-category) were acquired in the company Charles River Laboratories Japan. After a 5-day quarantine period and subsequent 5-day acclimatization once daily measured weight and monitor the overall health. For the experiment we used a mouse which was not observed weight changes or deviations of the General state from the norm.
 the Mice were divided into groups, each of which comprised 10 OS the Bay, in accordance with the method of random sampling using the computer (the CP system for pre-clinical trials) so that the average weight for individual groups was generally the same.
Upon receipt of the animals were identified by combined application of the method of ear piercing and a method of cutting hair. After the separation of the mice in groups they identified with labels on the tails of oil paint (I used paint different colors for different groups).
 Mice were grown in the chamber, which was maintained the following conditions: temperature 23°C (tolerance interval: 20-26°C), humidity 55% (valid range: 40-70%), light cycle: 12 hours (light from 6:00 to 18:00), ventilation: 12 times/hour (fresh air is fed through the system of sterilizing filtration). Animals were kept in plastic cages with a flat bottom (W: 175 × D: 245 × : 125 mm), in which the period of quarantine and acclimatization after separation of groups was posted sterilized in the autoclave litter. Each cell contained 5 mice.
 In the manger put solid food (ANG93G, Oriental Yeast Co., Ltd.) and mice have provided an opportunity to eat. Mice have also provided an opportunity to drink water from a bottle. The samples were administered orally forced through in accordance with the specified method is by using a polypropylene syringe disposable (production Terumo Corporation, Japan), which was joined by the needle disposable for mice (production Fuchigami kikai Ltd.). The sample was introduced in the process of mixing agitator. The sample was introduced so that the quantity of vitamin K was 30 mg per kg of body weight. The quantity of liquid was calculated as the ratio of 10 ml/kg based on weight at the date of admission.
 the testing Method
Observation of the General condition and the deaths of the mice was carried out once a day before taking the drug. Weight was measured once a day before taking the drug. To measure the electrical pulse and the time of akinesis system was used to measure the conditioned-reflex reactions of fear (production ActiMetrics). After placing divided into groups of mice in the measurement system conditioned reflex reactions of fear for the excitation state of fear was applied electrical pulse and simultaneously measured time akinesis. An electrical impulse value of 0.3 mA acting for one second every 15 seconds, was applied for 240 seconds. After the stimulation, the mice were given sample. After 7-day intake of mice in the control group (0.5% of MS) and from the group that took vitamin K was again placed in the measurement system conditioned reflex reactions of fear 2 hours or 2 hours and 1 minute after the last the last reception and measured time of akinesis for 4 minutes without the use of elettrostimolatore. Time akinesis was expressed in the form of a "time of immobility in %" for every 60 seconds. It should be noted that the condition in which there were no any movements except for movements of skeletal muscles and beards associated with breathing, were seen as "akinesis", and a condition in which the move was seen as "active".
 the Method of statistical analysis
The weight values, average values and standard deviations were calculated for each group. To determine the time of akinesis expected "time of immobility in %" for the entire period from 0 to 240 seconds for individual groups. Further, the expected mean values and standard deviations of "time of immobility in %" for every 60 seconds and for the entire period from 0 to 240 seconds for individual groups. Test for significant differences was performed on the basis of a comparative study of two groups, which took control group and each group taking vitamin K. a Study of significant differences for the "time of immobility in %" for every 60 seconds was performed using two-factor analysis of variance. Study of significant differences for the time of immobility in % for the entire period from 0 to 240 seconds was carried out on the basis of the sign of equality of variances using the criterion F for the control group and test group. If the Board is of dispersions used student test, and in the case of unequal variances were performed test Welsh. For all cases the comparisons were shown significance criteria (p-value). In the study, the significance level less than 5% was considered as significant. Cases with significance level less than 5% (p<0.05) and less than 1% (p<0.01) were shown separately. It should be noted that the above studies significant differences were used commercially available statistical software program (SAS ReL. 8.2 TS 020, a software package for pre-clinical trials SAS, version 5.0/ SAS Institute Japan Inc.). On the basis of the obtained results were verified histogram and normal distribution, and thus were tested methods.
To check the histogram and normal distribution was used a commercial statistical software (JMP, SAS, version 5.1.1; SAS Institute Japan Inc.).
 the Results
Deaths or deviations from normal General condition was not observed neither in the control group or in groups, taking vitamin K. As shown in figure 1, the weights remained largely constant during the entire reception period in the control group, the group "menechino-4" and "menechino-7". Differences between groups were not observed.
 the time Values conditioned reflex of akinesis caused by fear (every 60 seconds), shown in figure 2. the and figure 2 shows the percentage of time (%) during which movement for 60 seconds was observed. A higher value in % indicates that the mouse feels more strong fear, anxiety and stress.
 the Time akinesis in the control group (control group who received only the environment; the group of 0.5% MC) was 39,85-47,03%. On the other hand, the time of akinesis in the group "menechino-4" was 31,99% over a period of time from 0 to 60 seconds, which is slightly less than the corresponding figure for the control group. Further, the time of akinesis for menechino-4" gradually decreased, reaching values 22,29% for the period from 180 to 240 seconds. In the two-factor analysis of variance between the control group and the group "menechino-4 found a significant difference with a P<0,01. Meanwhile, the time of akinesis in the group "menechino-7" was 38,84% for the period from 0 to 60 seconds, which substantially coincides with the corresponding figure for the control group. In the future, the time of akinesis in the group "menechino-7 has decreased gradually to 20,83% for the period from 180 to 240 seconds, when there was a significant decrease in time of akinesis.
 as for the group that took vitamin K, the time of akinesis for menechino-4" was a little less for a period from 0 to 60 seconds of the initial measurement period compared with the corresponding figure for pin Olney group, and akinesis for menechino-7" substantially coincide with the corresponding figure for the control group. However, over time the time of akinesis continued to decline. This is probably due to the effects on mice where experienced fear induced state anxiety, but then the mouse is understood that the electrical stimulation will not follow and the disturbance appeared over time. As described above, reducing the time of akinesis, induced by conditioned-reflex reaction of fear, which is a measure of calming and antidepressant action, was observed for the group treated with vitamin K. in Addition, it was found that intake of vitamin K had a tranquilizing effect, such as sedative, antidepressant and anti-stress effect.
 To date, this invention is described in connection with its preferred embodiment. However, specialists in the art will understand that within the essence and scope of this invention, it is possible to modification and improvement with regard to the disclosure presents descriptions.
 Examples of embodiments of the invention include:
1. Tranquilizer that contains vitamin K as an active ingredient.
2. Tranquilizer described in paragraph 1, characterized in that the content is tion of vitamin K is in the range from 0.0001 to 100% (weight).
3. Tranquilizer described in paragraph 1, characterized in that, as vitamin K is vitamin K2.
4. Tranquilizer described in paragraph 1, characterized in that, as vitamin K is used menechino-4 and/or menechino-7.
5. Dietary Supplement product is a health food or functional food product containing a tranquilizer described in one of the above items.
6. Tranquilizer described in paragraph 1, which is intended for human use.
7. Dietary Supplement product is a health food or functional food, as described in paragraph 5, which is intended for human use.
8. A method of treating a state of anxiety, depression and/or stress, including acceptance of tranquilizer that contains vitamin K as an active ingredient.
9. The way to prevent a state of anxiety, depression and/or stress, including acceptance of tranquilizer that contains vitamin K as an active ingredient.
10. The use of vitamin K to produce a tranquilizer.
1. Remedy for anxiety and/or depression, which includes vitamin K2in the range from 10 μg to 100 mg as the active component.
2. The method of treatment of anxiety and/or depression, including the introduction of tools from anxiety and/or depression, with the Tav which includes vitamin K 2in the range from 10 μg to 100 mg as an active ingredient, the needy in this patient.
3. Remedy for anxiety and/or depression according to claim 1, characterized in that the vitamin K2is menechino-4 and/or menechino-7.
4. Food additive against the state of anxiety and/or depression containing a remedy for anxiety and/or depression, which includes vitamin K2in the range from 10 μg to 100 mg as an active ingredient.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, particularly to a composition for treating anxiety disorder. The pharmaceutical composition for treating anxiety disorder containing ginsenoside having Rg1 and Rb1; and a glycyrrhizic acid derivative being specified in a group consisting of glycyrrhizic acid, glycyrrhetinic acid and their combination taken in specific proportions. The pharmaceutical composition for treating anxiety disorder containing ginseng and liquorice taken in certain proportions.
EFFECT: compositions are effective for treating anxiety disorder.
8 cl, 6 dwg, 2 tbl, 22 ex
SUBSTANCE: invention relates to medicine, cardiology and cardiac surgery, and can be used for psychological rehabilitation of patients with prosthetic heart valves (PHV). Method includes studying index of development of anxious disorders in pre-operational and post-operational periods and carrying out procedures for patients who have undergone cardiosurgical operations, including drug therapy. In determination of anxiety higher level is considered to be from 31 points and higher, additionally performed are point massage and muscular relaxation successively with groups of muscles of arms, forearms, face, neck, shoulder girdle, abdomen, hips, ankles and feet. Relaxation with each group of muscles is performed for 5-10 seconds 2-3 times per week.
EFFECT: method improves results of treatment of patients with PHV due to complex impact taking into account reactive and personality anxiety.
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions relates to medicine, in particular to pharmacy. A composition for injections exhibiting tranquilising action contains the ingredients in the following proportions, wt %: crystalline β-modification of 7-brom-1,3-dihydro-5-(2-chlorphenyl)-2H-1,4-benzodiazepin-2-one - 0.05-0.15, polyvinylpyrrolidone - 0.50-1.20, "Tween-80" - 2.00-10.00, glycerine - 5.00-15.00, sodium pyrosulphite - 0.30-1.20, sodium hydrate solution - to pH 6.0-7.5, water - the rest. A method for preparing the composition consist in the fact that "Tween-80" and glycerine are mixed, heated to 70-90°C, and crystalline β-modification of 7-brom-1,3-dihydro-5-(2-chlorphenyl)-2H-1,4-benzodiazepin-2-one is dissolved. The prepared mixture is poured in the mixed aqueous solution of sodium pyrosulphite and polyvinylpyrrolidone heated to 40-90°C, cooled to room temperature, filtered, reduced to pH 6.0-7.5 with sodium hydrate solution, bottled and sterilised.
EFFECT: presented group of inventions provide a composition exhibiting improved anxiolytic action and decreased sedation in comparison with the composition based on pharmacopoeial phenazepam.
2 cl, 2 tbl, 4 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: described are novel compounds of general formula I:
(where values R1-R5, X and Z are defined in invention description), pharmaceutical composition, which contains them, and application of claimed compounds as MGLUR5 modulators for inhibition of transient relaxations of lower esophageal sphincter or for treatment or prevention of gastroesophageal reflux disease.
EFFECT: obtaining compounds for treatment or prevention of gastroesophageal reflux disease.
14 cl, 87 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: what is offered is a biologically active substance showing 5-HT3-serotonin receptor antagonist properties, 1-piperidinopropyl-2-(4-fluorophenyl)imidazo[1,2-a]benzimidazole of formula I. The compound has been known as a local anaesthetic. There are shown evident 5-HT3-antagonist properties of the compound in the macromolar concentration equal to the reference preparation ondansetron with the compound of formula I being safer.
EFFECT: new properties of the compound can be used for creating the effective agents exhibiting antiemetic, anxiolytic and analgesic activities.
2 cl, 2 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to pharmaceutical industry and medicine. Claimed is application of N-carbamoyl-4-(n-methoxyphenyl)-2-pyrrolidone of structural formula as means possessing antidepressive, anxiolytic and nootropic action. This low-toxic compound (LD50 2263.88 mg/kg) possesses high antidepressive, anxiolytic and nootropic activity, affect of which is not accompanied by hypnosedative phenomena, or reduction of mental and physical work ability.
EFFECT: demonstrated is antidepressive and anxiolytic action of compound already in its single application, which makes the medication different from most known antidepressants, requiring at least one-week long intake to develop their effect.
SUBSTANCE: invention relates to compounds of formula , where X denotes S; R1 and R2 taken together with atoms to which they are bonded form a 5-member carbocycle, substituted with up to two substitutes selected from alkyl and CF3; R3 is selected from a group consisting of a hydrogen atom and C1-8-alkyl; R3a denotes a hydrogen atom; R4 denotes a hydrogen atom; R4a denotes a hydrogen atom; R5 denotes a hydrogen atom; R5a denotes a hydrogen atom; R6 denotes a hydrogen atom; R6a denotes a hydrogen atom; R7 denotes a hydrogen atom; or pharmaceutically acceptable salts thereof. The invention also relates to compounds of the given formula, compounds selected from the group, as well as a pharmaceutical composition.
EFFECT: obtaining novel biologically active compounds which modulate serotonin receptor activity.
6 cl, 19 ex, 1 tbl
SUBSTANCE: described is a novel crystalline β-modification of 7-bromo-1,3-dihydro-5-(2-chlorophenyl)-2H-1,4-benzodiazepin-2-one (phenazepam) and synthesis method thereof, which can be used in pharmaceutical industry and medicine as a tranquilliser. Said novel crystalline β-modification of 7-bromo-1,3-dihydro-5-(2-chlorophenyl)-2H-1,4-benzodiazepin-2-one is characterised by certain interplanar spacing (A0) and corresponding intensity and parameters of the crystal lattice, given in the claims.
EFFECT: marked muscle relaxant, soporific, anticonvulsant and anxiolytic action.
2 cl, 7 ex, 2 tbl, 9 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed are dietary and/or nutriceutic pharmaceutical composition for peroral application which contains S-adenosylmethi-onine-para-toluolsulfonate (SAMe) in combination with inositol and/or ino-sitol-1-phosphate and pharmaceutically acceptable excipients, in which at least one of and pharmaceutically acceptable excipients represents magnesium oxide in concentration from approximately 1.0 to approximately 10.0% of composition weight (versions), method of its obtaining, method of stabilisation of hard food and/or nutriceutic pharmaceutical composition based on SAMe-para-toluolsulfonate by application of inositol and/or inositol-1-phosphate, application of SAMe-para-toluolsulfonate in combination with inositol and/or inositol-1-phosphate for obtaining composition for treatment of depressive states and panic syndromes.
EFFECT: inclusion of magnesium oxide into composition increases SAMe-para-toluolsulfonate stability, inositol reduces SAMe-para-toluolsulfonate hygroscopicity and contributes to its soothing and antidepressant action.
27 cl, 41 tbl, 7 ex
SUBSTANCE: compound is ((S)-1-phenyl-propyl)-amide 3-(methane sulphonyl amino)-2-phenyl- quinoline-4-carboxylic acid, stereoisomer, enantiomer or pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition based on the disclosed compound.
EFFECT: novel derivative of methyl sulphonamide quinoline which can be used to modulate the NK-3 receptor.
2 cl, 10 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions refers to medicine, cosmetology, and may be used for treating or preventing light exposure on a human or an animal. That is ensured by a photoprotective composition, including in the form of a cosmetic preparation containing the carotenoid compound diadinoxantine or its pharmaceutically acceptable prodrug or salt. There are also offered a method for diadinoxantine recovery from algae, as well as a method for producing a photoprotective or photoprotected product involving application or impregnation of said product with photoprotective composition containing diadinoxantine.
EFFECT: composition is effective in protection against light of wave length 350 to 500 nm.
21 cl, 4 tbl, 3 ex, 4 dwg
SUBSTANCE: invention refers to medicine, namely nephrology and can be used for treating the patients with IgA-nephropathies with infectious pathogens detected in renal tissue. For this purpose provided cytomegalovirus and/or Epstein-Barr virus, or their combination with Chlamidia thrahomitis bacterium are found in biopsy renal tissue, Reaferon 400000-600000 units daily and Amixin 125 mg every second day are administered; the therapeutic course is 2.5-4 months.
EFFECT: method provides higher clinical effectiveness with enabled stable and prolonged remission ensured by immediate action on etiological infectious antigen.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to chemical-pharmaceutical industry, and concerns a liquid 6-decaprenyl-2,3-dimethoxy-5-methyl-1,4-benzoquinone composition which is characterised by high bioavailability and prolonged shelf life. The composition contains an active substance - 6-decaprenyl-2,3-dimethoxy-5-methyl-1,4-benzoquinone, a nonionic surfactant, an antioxidant, a preservative agent, a fat-soluble emulsion stabiliser, water-soluble cellulose derivatives, water-soluble emulsion and water stabiliser. Also, there is offered a method for preparing the composition which consists in the fact that certain amounts of the nonionic surfactant and the antioxidant are mixed, heated to 40-120°C; the required amounts of the fat-soluble emulsion stabiliser and 6-decaprenyl-2,3-dimethoxy-5-methyl-1,4-benzoquinone are dissolved in the prepared solution; the prepared mixture is cooled to 30-60°C and in through mixing added to the mixed solution of the cellulose derivatives, the water-soluble emulsion stabiliser and the preservative agent pre-heated to 30-60°C.
EFFECT: enabled effective method for preparing the composition.
8 cl, 4 ex, 1 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to pharmaceutics and medicine, and concerns a composition for inflammatory bowel disease or irritable colon syndrome containing an effective amount of the composition of formula .
EFFECT: invention provides higher clinical effectiveness.
12 cl, 5 tbl, 5 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to medicine and describes composition of 6-decaprenyl-2,3-dimethoxy-5-methyl-1,4-benzoquinone, which contains 0.2-15% 6-decaprenyl-2,3-dimethoxy-5-methyl-1,4-benzoquinone, 0.2-40% solubilising agent and 45-99.6% water.
EFFECT: composition has high bio-availability, quickness of action and accuracy of dosing.
10 cl, 2 dwg, 2 tbl, 8 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to testosterone amplifier, to a drug which prevents, relieves and/or treats symptoms or diseases caused by testosterone deficiency and to an additive for treating menopausal disorders in males. As an active ingredient, vitamin K (vitamin K2, menaquinone-4 or menaquinone-7) 10 mcg to 100 mg is used.
EFFECT: inventions provide higher endogenous testosterone levels.
5 cl, 9 dwg, 2 ex, 2 tbl
SUBSTANCE: what is offered is application of idebenone for preparing a drug for transmucosal introductions for treating mitochondral, neurological and neuromotor diseases, and the drug is introduced through a nasal mucosa, an oral mucosa or a colon mucosa.
EFFECT: composition for transmucosal introduction enables to avoid a considerable first-pass metabolism of idebenone, to provide introduction in a lower dose, reduced risk of side effects and higher compliance.
8 cl, 2 dwg, 7 tbl, 6 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to new compounds of formula (1) in which X and Y can be oxygen or sulphur, each R1, R2 and R3 are hydrogen atom, methyl or (CH2)m-CH3, and m=1-12, n=1-12 inhibiting tumour cell growth, to a based pharmaceutical compositions (versions), and also to methods of inhibiting breast, liver and prostate cancer cell growth. The offered compounds are recovered from Antrodia camphorata.
EFFECT: production of the new compounds inhibiting tumour cell growth.
31 cl, 7 tbl, 8 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: offered is an application of 2-hydroxy-3-methyl-6-(1-methylethenyl)cyclo-hex-3-enone (compound of formula 1) as an analgesic. The agent can be produced of an available natural compound α-pinene.
EFFECT: agent exhibits high activity, low toxicity, can be used in medicine.
4 ex, 2 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed is application of 2-(2-nitro-4-trifluormethylbenzoyl)-1,3-cyclohexandione in production of medication in treatment of neurodegenerative disease, Parkinson's disease, as well as pharmaceutical compositions and sets (versions) of similar purpose, which include said compound.
EFFECT: compound inhibits 4-hydroxypyruvate dioxygenase, reduces time of recovery from catalepsy and increases availability of levodopa or increases dopamine synthesis, i.e. ensures action synergism in treatment of neurodegenerative disease, Parkinson's disease.
23 cl, 4 dwg, 7 tbl, 3 ex
FIELD: food industry.
SUBSTANCE: method for production of Lactococcus lactis strain version producing, under standard fermentation conditions, a quantity of vitamin K2 exceeding that produced by the stock/parent bacterial strain inoculated under the same conditions approximately 1.2 times, the said method including, at least: a) inoculation of the sock bacterial strain under standard fermentation conditions in a cultural medium causing a change in the oxidation-reduction state of a cell containing bacitracin or a peroxide and b) selection of the strain version if producing a quantity of vitamin K2 exceeding that produced by the stock/parent bacterial strain inoculated under the same conditions approximately 1.2 times. Lactococcus lactis subsp.cremoris 1-3557 strain deposited in Collection CNCN of Pasteur Institute on 20.01.2006 and Lactococcus lactis subsp.cremoris 1-3558 strain deposited in Collection CNCM of Pasteur Institute on 20.01.2006 produce at least 1.2 times more vitamin K2 than the stock/parent bacterial strain inoculated under the same conditions. Additionally, the invention deals with a lactic acid starter containing at least one of the above strains and to the method for preparation of a cultured milk product containing the above strain and/or the lactic acid starter.
EFFECT: invention enables increase of vitamin K2 content in the product.
11 cl, 5 tbl