Combined antipyretic drug in form of rectal suppositories

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to combined antipyretic drug in form of rectal suppositories. Drug contains paracetamol, dimedrol and papaverine hydrochloride as active components, and lipophilic suppository base Suppocire (Suppocire NA-15) as auxiliary substance, with the following component ratio in g per 1 suppository with 2.0 g weight: paracetamol 0.3-0.5; dimedrol 0.03-0.05; papaverine hydrochloride 0.03-0.05; Suppocire (Suppocire NA-15) - the remaining part (to 2.0 g).

EFFECT: increased efficiency of paracetamol suppositories as antipyretic drugs, with absence of narcotic and psychostimulating substances in their composition.

4 tbl, 2 ex

 

The invention relates to medicine and pharmacy, in particular pharmacotherapy of inflammatory diseases of different etiology, accompanied by hyperthermia.

As a combined antipyretic drug offers rectal suppositories modern fat base Suppocire NA-15 (Supposer), containing as active ingredients nonsteroidal anti-inflammatory paracetamol, a blocker of histamine H1receptor diphenhydramine and myotropic spasmolytic agent papaverine hydrochloride.

The problem of regulation of fever is essential, because a significant increase in temperature is accompanied by the majority of infectious and inflammatory processes, including the so-called "colds". Fever as a natural protective-adaptive mechanism sometimes looms General state forms and require pharmaceutical intervention.

Paracetamol is one of the safest analgesics-antipyretics, widely used in Russia and abroad [Ovchinnikov L.K. Principles of selection of medicines at Ari / Lchulakova, Iaauineea // Russian pharmacies. - 2008. - No. 22. - P.27-31]. On chemical structure, it refers to a derivative of paraaminophenol.

The mechanism of antipyretic and analgesic effect of the paracetamol is slightly different from the mechanism of action of other nonsteroidal anti-inflammatory drugs (NSAIDs). Paracetamol is largely inhibits the synthesis of prostaglandins in the Central nervous system than in peripheral tissues [Lamica EJ Central component in the mechanism of analgesic action of NSAIDs / Eoulette, Wei // Expert. and clinically. pharmacology. - 1995. - T, No. 4. - P.59-62].

In the absence of peripheral actions, paracetamol has almost no ulcerogenic and antiplatelet actions, does not cause bronchoconstriction, does not affect the contractility of the uterus [Kukes VG Clinical pharmacology. - M.: GEOTAR-Media, 2006. - 944 S.]. He first recommended in the presence of contraindications to aspirin and other NSAIDs: in patients with bronchial asthma in patients with ulcerative disorder, in children with viral infections.

Currently it is used in febrile syndrome on the background of infectious diseases, vaccine-induced hyperthermia; pain syndrome (mild to moderate severity): arthralgia, myalgia, neuralgia, migraine, toothache and headache, algodismenoree.

Paracetamol is the drug of choice for pain and cough therapy in children [Kiselev NM Antipyretic drugs: pediatrically aspect of the application / Nmichael // Pharmacy business. - 2007. No. 1. - P.46-48]. In the latest sign of paracetamol is a security standard for NSAIDs. If necessary, you can apply Yes is e during pregnancy and in children under three months.

For a much more pronounced antipyretic, analgesic and anti-inflammatory effect of paracetamol, as well as extensions of the pharmacological spectrum produced combination medicines.

A known number of combined oral preparations containing paracetamol in combination with caffeine and/or codeine: Citropa, Solpadeine, Panadeine, Panadol-extra, Co-codamol, Andrews answer, Pentalgin ICN, Sedalgin-Neo [Mashkovsky PPM Combined analgetika-antipyretics and anti-inflammatory drugs / Medmaravis // Chem.-Pharm. Journe. - 1995. - C, No. 7. - P.46-53; RLS - "encyclopedia of drugs". - 19 release. - 2011 - electronic version]. The disadvantage of these preparations is the presence in their structure of codeine as a drug that creates a threat of abuse, excludes non-prescription status. Introduction caffeine as stimulating means in some cases it is not desirable, which can be dangerous for patients with high anxiety, hypertension, tachycardia, and in childhood and old age. The combination of paracetamol with an α-adrenoceptor agonist type of phenylephrine (Coldrex), causing vasoconstriction, has the above contraindications.

The oral medication is not possible in patients with gastropathy, nausea, vomiting, unconscious is able. In this case, shown rectal therapy and the use of suppositories.

Thus, the disadvantages of the known oral combination drugs of paracetamol are limitations associated with the presence in their composition of drugs and/or psychoactive drugs, and certain patient conditions, excluding medication per os.

Known one-component suppositories paracetamol 125 mg Panadol Baby", produced by GlaxoSmithKline Sante Grand Public" (France) on the basis of solid fat and designed for children from 6 months to 3 years. In Russia produced suppositories "Zeecon D" for children aged 3 months to 12 years, containing paracetamol in different dosages (50, 100 and 250 mg) depending on the age of the child [RLS - "encyclopedia of drugs". - 19 release. - 2011 - electronic version].

Currently, domestic suppositories paracetamol for adults are not available. In available patent literature information on combined paracetamol suppositories are missing.

Known short message on combined paracetamol suppositories [Orlov T.V., Patrusheva T.A., A.V. Nesterov / Mat. 4th scientifically conference. nauch.-method. proc. - Voronezh, 2010. - Part 2. - S.285-287], including containing psychoactive drug caffeine [Gnewikow N, Nesterov A.V., Kuzmin BV, Orlova T. / Sat. mater. Congress is a "Man and medicine". - M., 2011. - S], which is not disclosed composition suppositories and not the data on therapeutic efficacy of these drugs.

The inventive three-drug contains an effective combination of paracetamol with vasodilators (papaverine hydrochloride) and antihistamines (diphenhydramine) drug. Such combinations are suitable from a pharmacological point of view and are used in clinical practice by assigning a separate preparations of the above pharmacological groups orally or by injection. So, when detecting a "pale fever" doctors prescribe a combined reception of fever-reducing medicines with vasodilators (papaverine, Dibazol, parasol). When the counter fever shows the introduction of antihistamine drugs, including combinations with antipyretics and antispasmodics (Saltikov A.L., I.N. Zakharova., Ovsyannikova E.M. Antipyretics in practice, pediatrician: tactics of choice and rational therapy of fever in children, breast cancer. - 2000. - Vol.8. No. 13-14. - Art. No. 576).

The mechanism of efficient combinations of paracetamol and demerol can be explained as follows. When colds and other inflammatory diseases is quite active processes associated with the release of histamine and other biogenic amines. Asteroids the e anti-inflammatory drugs are able to suppress the effects of many biologically active substances (histamine, serotonin, bradykinin, norepinephrine), but to a lesser extent than their specific antagonists (diphenhydramine, diasorin, suprastin, etc.). Therefore, antihistamine drugs may be synergistic NSAIDs, and their combination with NSAIDs to be more effective [Kukes VG Clinical pharmacology. - M.: GEOTAR-Media, 2006. - 944 S.].

Diphenhydramine along with high anti-histamine activity has a moderate Central anticholinergic, sedative, and hypnotic, antiemetic action; inhibits conduction of nerve excitation in the autonomic ganglia, relaxes smooth muscles. Shows his rectal use, including children.

Papaverine hydrochloride is myotropic antispasmodic agent, which is widely used in spasms of smooth muscles of the abdominal, peripheral vascular and cerebral vessels. With persistent spasm of the blood vessels that takes place when hyperthermia, papaverine hydrochloride useful for expansion of surface vessels and increases heat loss. Recommended for use in the form of suppositories, including Pediatrics.

The technical result of the invention is to increase the efficiency of the known suppositories paracetamol as an antipyretic drugs, in the absence of their composition narcotic and psychoti Wirayuda substances.

The technical result is achieved by the fact that the proposed combined antipyretic drug in the form of rectal suppositories designed for teenagers and adults, in addition to containing paracetamol as active ingredients diphenhydramine, papaverine hydrochloride, and as excipients modern lipophilic suppozitornyj the basis of Suppocire NA-15 in the following ratio of components in g on 1 suppository mass of 2.0 g:

Paracetamol0,3-0,5
Diphenhydramine0,03-0,05
Papaverine hydrochloride0,03-0,05
Supposer (Suppocire NA-15)The rest (up to 2.0 g)

The content of drugs in suppositories corresponds therapeutic doses for adolescents and adults with oral and rectal administration. Adults is prescribed in a dose of 0.5 g up to 4 times/day (maximum single dose of 1 g, the maximum daily dose is 4 g); diphenhydramine - 0.03-0.05 g 1-3 times per day (the highest single dose of 0.1 g; the highest daily dose of 0.25 g); papaverine hydrochloride - 0.04 - 0.08 g 3 times a day (the highest single dose of 0.2 g; the highest daily dose of 0.6 g).

The act of the main components of the proposed structure refer to the List of vital and essential drugs (VED No. 2135-R dated 30.12.2009, - PharmaReg.ru).

The characteristics of the objects

Paracetamol (Paracetamolum) (FS 42-0268-07)

N-(4-hydroxyphenyl)-ndimethylacetamide. Synonyms: Acetaminophen, Panadol, Acelifen, Paracinol. White or almost white crystalline powder. Easily soluble in alcohol 96%, soluble in acetone and caustic alkali solution, sparingly soluble in water. List B. [XII of the State Pharmacopoeia of the Russian Federation "Publishing "Scientific center of expertise of medical application", Moscow, 2007. - Part 1. - S]. Antipyretic, analgesic agent. Paracetamol is well absorbed from the gastrointestinal tract (mainly in the small intestine). The maximum concentration of drug in plasma is reached after 20-30 min after administration and lasts for 90 min, followed by a gradual decrease. Paracetamol is metabolized in the liver and excreted by the kidneys as metabolites, mainly conjugates [Mashkovsky PPM Medicines / Medmaravis - 15 ed. Rev., Corr. and supplementary), RIA "New wave", 2007. - 1206 S.].

Diphenhydramine (Dimedrolum). (FS 42-0232-07)

N,N-Dimethyl-2-(diphenylmethoxy)-ethylamine hydrochloride. Synonyms: Diphenhydramine, Alledryl, Dimidril. White or almost white crystalline powder. Very easily soluble in water, easily soluble in alcohol 96% and chloroform. List B. [XII of the State Pharmacopoeia of the Russian Federation "Publishing "Scientific center of expertise of the medical products", Moscow, 2007. - Part 1. - S]. Anti-histamine (anti-allergic) tool. If ingestion is rapidly and well absorbed. Bound to plasma proteins at 98-99%. The maximum concentration in plasma is reached in 1-4 h after intake. A large part of the adopted Dimedrol metabolized in the liver. The half-life of 1-4 hours is Widely distributed in the body, passes through the blood-brain barrier and the placenta. During the day completely excreted from the body mostly in the form of benzhydrol, conjugated with glucuronic acid, and only in small quantities in an unmodified form. The maximum effect develops within 1 h after oral administration, the duration of action is 4 to 6 h [Mashkovsky PPM Medicines / Medmaravis - 15 ed. Rev., Corr. and supplementary), RIA "New wave", 2007. - 1206 S.].

Papaverine hydrochloride (Papaverini hydrochloridum) (FS-0267-07). 6,7-Dimethoxy-1-(3,4-dimethoxybenzyl)-isoquinoline hydrochloride. Synonyms: Papavin. White or almost white crystalline powder, odorless. Soluble in chloroform, sparingly soluble in water, little soluble in alcohol 96%. List B. [XII of the State Pharmacopoeia of the Russian Federation "Publishing "Scientific center of expertise of medical application", Moscow, 2007. - Part 1. - S]. Myotropic antispasmodic agent. Bydocument who is 54%. Binding to plasma proteins is 90%. Well distributed in the body, crosses the blood-tissue interfaces barriers. Metabolized in the liver. The half - life is 0.5 to 2 hours, may increase up to 24 hours is Excreted by the kidneys as metabolites [Mashkovsky PPM Medicines / Medmaravis - 15 ed. Rev., Corr. and supplementary), RIA "New wave", 2007. - 1206 S.].

Suppoter synthetic suppozitornyj framework, issued by the international company "Gattefosse". Products "Gattefosse" is produced in accordance with GMP requirements, is certified by the international quality system ISO 9001. Standard product line with the designation of N obtained by direct esterification of selected fatty acids with glycerol. Products in this line contain a balanced optimal ratio of mono-, di - and triglycerides. The composition suppocire includes a mixture With12-C18of triglycerides.

The Suppocire bases have the following advantages in comparison with some other natural or fully synthetic basics:

- exceptional safety and tolerance to slimy, due to the lack of toxicity and irritant properties, which are confirmed in experiments in vitro and in vivo, as well as long-term international experience in the use of drugs on the basis of their melting and good diffusion properties, providing ravnomernoe and efficient release of medicinal substances

chemical inertness and compatibility with the majority of the active substances

- excellent distribution of the active ingredient in suppozitornyj mass

- established physical and chemical stability: the color, the smell, the release profile of drug substances, low risk of oxidation

- optimized properties for curing, reducing physical polymorphism

- ability to use a variety of production equipment.

Suppoter. Suppocire NA-15 (Ph.Eur.)

Description. Solid wax-like mass in the form of pellets. When heated, melted in a yellowish oily liquid.

Numeric indicators. The melting point of 33.5-of 35.5°C.; an acid number of not more than 0.5; saponification number 230 - 245; iodine number of not more than 3; hydroxyl number - 5-15; peroxide value not more than 1.

Suppozitornyj basis [Excipients for Rectal and Vaginal Drug Delivary. Information materials of the company "Gattefosse". - www.gattefosse.com].

The advantage of using Suppocire as suppozitornoj bases compared to solid fat is proven in experiments in vitro in the study of the speed and completeness of the release of paracetamol suppositories.

A comparative study of suppositories made of solid confectionery fat and the basis Suppoter conducted using the test "Dissolution", which is recommended for biopharmaceut the political evaluation of solid dosage forms and are now widely used to analyze suppositories [General pharmacopoeial article "Dissolution" of the CFC 42-0003-04].

In the experiment used the device type "rotary basket". As the environment of the dissolution of the applied phosphate buffer solution with pH=7.4 and temperature (37±1)°C in a volume of 500 ml. Speed of rotation of the basket was 100 rpm

Through certain time intervals samples were taken, in which after filtration and appropriate dilution, conducted quantitative determination of paracetamol by means of UV-spectrophotometry. After collection of the sample in the vessel was adding a phosphate buffer solution in the volume of the samples with temperature (37±1)°C.

Each suppository was carried out by five independent experiments and counted the number of substances that have fallen into the midst of the dissolution to a specific point in time.

The duration of the experiment was 45 minutes Received data is statistically processed and presented in table 1.

As follows from the obtained data, solid confectionery fat is slowly and incompletely releases paracetamol on Wednesday dissolution. The output of the active substance to 45 min of the experiment amounted to 36%, while Suppoter actively and fully released paracetamol - 96,85%. Thus, the rationality of use as an excipient in the manufacture of suppositories paracetamol modern fundamentals of Suppocire NA-15.

Table 1
The release profiles of paracetamol from suppositories, depending on the type suppozitornoj bases
Time (min)View suppozitornoj bases
Solid confectionery fatSuppocire NA-15
524,96±3,7419,23±5,17
1027,90±3,4033,05±5,14
1529,57±2,8754,58±9,12
2032,26±2,8682,82±3,69
2534,44±was 2.7692,35±5,18
4536,45±2,9196,85±4,29

The studied physico-chemical quality parameters of the claimed medicinal preparation in the form of suppositories and established their compliance with the global Fund XI, ed. (table 2).

therapeutic effectiveness of the proposed combination of medicines in the decree is different doses as an antipyretic drug and the advantage compared with the known means proven in preclinical studies in laboratory animals.

In the experiment used white mongrel adult rats weighing (220±40) , the Animals were housed under standard vivarium conditions on normal mode content. The day before the experiment, rats were deprived of food with free access to water.

The experiments were carried out in strict accordance with the Rules of work with the use of experimental animals. The selection of animals in the control (without the introduction of drugs) and the experimental group had an incidental character (n=6).

The study of the antipyretic action of drugs was carried out on the model pyrogenalum fever in rats [Manual on experimental (preclinical) study of new pharmacological substances / Under the General editorship Rugarama. - M., 2005. - 832 C.]. With this purpose, animals were injected pyrogenes/m at a dose of 100 μg/kg To 2 hours since the introduction of pyrogenal animals was significantly increased temperature (up to 1.4°C), they become sluggish, frequent urination, some were observed tremor, ruffled coat. At the peak of hyperthermic reactions to the animals of the experimental groups were given medicines.

Paracetamol was administered to laboratory animals at the rate of 50 mg/kg intragastrically in a 1% suspension of starch paste or rectally in the IDA suppositories weighing 0.1 g (table 3). Suppositories composition 1 and 2 differed used to produce suppozitornyj basis. Combined suppositories were prepared on the basis of Suppoter containing paracetamol 50 mg/kg, Dimedrol, and papaverine hydrochloride, 5 mg/kg Dose and the ratio of drugs in the drugs for animals equivalent specified in the claimed composition and found by interspecies transfer of doses [Manual on experimental (preclinical) study of new pharmacological substances / Under the General editorship Rugarama. - M., 2005. - 832 S.].

Table 3
The composition of the rectal preparations for the comparative study of antipyretic action in laboratory animals
Composition 1Part 3
Paracetamol 50 mg/kgParacetamol 50 mg/kg
Solid confectionery fat q.s.Diphenhydramine 5 mg/kg
Suppoter q.s.
Part 2Part 4
Paracetamol 50 mg/kgParacetamol 50 mg/kg
Suppoter q.s.Diphenhydramine 5 mg/kg
Papaverine hydrochloride 5 mg/kg
Suppoter q.s.

The level of temperature reduction in gastric, rectal paracetamol and the use of combined suppositories are presented in table 4.

The data of table 4 indicate that rectal paracetamol (part 2) for the regulation of hyperthermia had equivalent antipyretic effect in comparison with its intragastric administration. Revealed significant differences (p≤0.05) as influenced suppozitornoj bases on the antipyretic efficacy of paracetamol. Suppositories made on the basis of Suppier (composition 2)was characterized by a higher antipyretic activity compared with those in the confectionery fat (part 1) 12-18%. This fact proves the advantage of the used suppozitornoj bases Suppoter as the basis for greater bioavailability of the active component. Introduction laboratory animal combinations of paracetamol with Dimedrol (part 3) for 1 hour, allowed to reduce the temperature in rats by 8% more than when using a single component suppositories, and for the second hour - 30%.

Even more effective was the op the food in one drug paracetamol Dimedrol and papaverine hydrochloride (composition 4). This drug has shown to 1 hour antipyretic activity equal to 66%, and for the second hour after injection - 82% and surpassed the one-component suppositories paracetamol (part 1) by efficiency in 3.38 times, and two-component (part 3) 1.21 times. Antipyretic effect of combined drug increases gradually, which is also the positive side of its pharmacodynamics.

Thus, the claimed combined drug in the form of rectal suppositories which significantly improves the efficiency of known suppositories paracetamol as an antipyretic medicines.

The invention is illustrated by the following examples.

The example 1 composition used for the regulation of hyperthermia in adolescents:

Paracetamol 0,3

Diphenhydramine 0,03

Papaverine hydrochloride 0,03

Supposer (Suppocire NA-15) - the rest (up to 2.0 g)

Example 2 the composition used for the regulation of hyperthermia in adults:

Paracetamol 0,5

Diphenhydramine 0,05

Papaverine hydrochloride 0,05

Supposer (Suppocire NA-15) - the rest (up to 2.0 g).

Combined antipyretic drug in the form of rectal suppositories containing as an active ingredient paracetamol, characterized in that the optionally contains as active ingredients diphenhydramine and papaverine hydrochloride, and as excipients - modern lipophilic suppozitornyj basis Supposer (Suppocire NA-15) in the following ratio of components, g 1 candle weighing 2.0 g:

Paracetamol0,3-0,5
Diphenhydramine0,03-0,05
Papaverine hydrochloride0,03-0,05
Supposer (Suppocire NA-15)the rest (up to 2.0 g)



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of general formula I [X]n-Y-ZR1R2, wherein the radicals are specified in the description, effective as heparan sulphate-binding protein inhibitors. The invention also refers to a pharmaceutical or veterinary composition having heparan sulphate-binding protein inhibitory activity for preventing or treating a disorder in a mammal, and to the use of these compounds and compositions for antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic therapy in a mammal.

EFFECT: preparing the new compounds of general formula I [X]n-Y-ZR1R2, wherein the radicals are specified in the description, effective as the heparan sulphate binding protein inhibitors.

10 cl, 31 ex, 11 tbl, 40 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to an aminopropylidene derivative presented by formula wherein R1 and R2, which may be identical or different, represent hydrogen or a substitute specified in the following (a)-(c), provided the case of both representing hydrogen is excluded: (a) carbonyl substituted with hydroxy, alkoxy or hydroxy alkylamino, (b) carbonylalkyl substituted by hydroxy or alkoxy, and (c) acrylic acid including its alkyl ester, R3 and R4, which may be identical or different, represent hydrogen, alkyl which may be substituted by phenyl or cycloalkyl, or R3 and R4, which together form a heterocyclic ring with a nitrogen atom bound thereto, represent pyrrolidino, piperidino, which may be substituted by oxo or piperidino, piperazinyl substituted by alkyl or penyl, morpholino or thiomorpholino; A means oxo or is absento, B represents canbon or oxygen; one of X and Y represents carbon, while the other one represents sulphur, a part represented by a dash line represents a single bond or a double bond, and a wavy line represents a cys-form and/or a transform. Also, the invention refers to a pharmaceutical composition exhibiting histamine receptor antagonist activity on the basis of said compounds.

EFFECT: there are produced new compounds and pharmaceutical compositions thereof, which can be used in medicine for treating asthma, allergic rhinitis, pollen allergy, hives and atopic dermatitis.

10 cl, 12 tbl, 58 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition for treating skin diseases. The composition contains a combination of methylprednisolone aceponate and glycoceramides and a glycoceramide complex containing cholesterol in the amount of 1-3%, and phospholipids in the amount of 25-34%, and excipients. A method for preparing the composition consists in the fact that methylprednisolone aceponate is introduced into an emulsion base containing the glycoceramide complex in the form of a solution to form a coagulation structure.

EFFECT: new pharmaceutical composition is characterised by a wide spectrum of pharmacological properties, stability, uniform distribution of the active ingredients.

9 cl, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula (I) presented below wherein the radicals and symbols have the values presented in the patent claim, and/or to its racemate, enantiomer, diastereomers or its pharmaceutically acceptable salts and/or esters. The invention also refers to a method for preparing it, using it in preparing a drug preparation and to drug preparations containing the compound of formula (I).

EFFECT: compound of formula has analgesic action and may be used as an active compound for pain management.

20 cl, 3 tbl, 33 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound having formula (I): wherein each of the groups R1, R2, R3 are independently H or C1-4 alkyl group or C2-4 acyl group; each of the groups R4 and R5 are independently H or the group of formula -SO3R6, wherein R6 is H or the C1-4 alkyl group or the C2-4 acyl group; provided at least one of the groups R4 and R5 is a group having formula -SO3R6, or a pharmaceutically acceptable salt thereof. The invention also refers to a method for preparing the specified compounds of formula (I) and a pharmaceutical composition possessing activity in the inhibition of IL-1 anti-inflammatory cytokines based on these compounds.

EFFECT: there are produced new compounds and pharmaceutical composition on their basis which can find application in medicine for treating an inflammatory or autoimmune condition.

17 cl, 4 dwg, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of biotechnology and immunology. Claimed is medication for treatment and prevention of TNF-dependent disorder, which contains molecule of TNF-binding nanobody, lyoprotector, surface-active substance and buffer, method of such medication obtaining, method of lyophilised preparation reduction and method of analysis of medication-manufacturing process, as well as method and set for treatment or prevention of TNF-dependent disorder.

EFFECT: invention ensures obtaining stable pharmaceutical preparations of TNF-binding nanobodies and can be applied in therapy of TNF-dependent diseases.

30 cl, 12 ex, 3 tbl, 32 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula I , wherein R2 means methyl, Y means carbon or nitrogen, and R1, R3 and R4 have the value specified in the patent claim. Also, the invention refers to a pharmaceutical composition for the use as a pharmaceutical drug having activity of a phosphatidylinositol-3-kinase inhibitor, to the use of the compounds of formula I for preparing the pharmaceutical drug for treating a disease mediated by phosphatidylinositol 3-kinase and to a method for preparing the compounds of formula I .

EFFECT: preparing the compounds of formula I possessing activity of the phosphatidylinositol-3-kinase inhibitor.

10 cl, 5 tbl, 51 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a method of intraocular pressure reduction and to a method of pain control involving the administration of a therapeutic compound representing , or its tautomer or stereoisomer forms wherein X represents NH; n is equal to 2 or 3; Ra, Rb, Rc and Rd represent stable functional groups independently consisting of: 0 to 4 carbon atoms, 1 to 9 hydrogen atoms; and Re represents H or C1-4alkyl. Furthermore, the invention refers to a compound represented by formula , or to its tautomer or stereoisomer form.

EFFECT: new compound is prepared; besides, the known compounds to be applied in pain and glaucoma control are studied.

8 cl, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of formula (I) or to its stereoisomers, or to a pharmaceutically acceptable salt, wherein Ra represents H or (C1-C6)alkyl; Rb is specified in an optionally substituted group consisting of -(CH2)n-aryl, -CH(CH3)-aryl, -(CH2)n-arylaryl, -(CH2)n-arylheteroaryl, -(CH2)n-(C3-C8) cycloalkyl, -(CH2)n-heteroaryl, -(CH2)n-heterocyclyl and -(C3-C8) cycloalkylaryl; or Ra and Rb taken together with a nitrogen atom form 2,3-dihydro-1H-isoindolyl, decahydroisoquinolinyl, optionally substituted piperidinyl or optionally substituted pyrrolidinyl; Y is specified in an an optionally substituted group consisting of 5,6,7,8-tetrahydro[1,6]naphthyridinyl, -NH-(CH2)n-heterocyclyl, wherein NH is attached to carbonyl, and -heterocyclylaryl, wherein heterocyclyl is attached to carbonyl; and n is equal to 0, 1 or 2; wherein each heterocyclyl represents an independent non-aromatic ring system containing 3 to 12 ring atoms, and at least one ring atom specified in a group consisting of nitrogen, oxygen and sulphur; wherein each heteroaryl represents an independent non-aromatic ring system containing 3 to 12 ring atoms and at least one ring atom specified in a group consisting of nitrogen, oxygen and sulphur; and wherein the optional substitutes are independently specified in a group consisting of C1-C6-alkyl, C1-C6-alkoxy, halogen, CN, CF3, OCF3, NH2, NH(CH3), N(CH3)2, hydroxy, cyclohexyl, phenyl, pyrrolidinyl, -C(O)-piperidinyl, -N(H)-C(O)-C1-C6-alkyl and N(H)-S(O)2-C1-C6-alkyl. The invention also describes a pharmaceutical composition having chemokine receptor antagonist activity and a method of treating such diseases, such as rheumatoid arthritis, psoriasis, lupus, etc.

EFFECT: there are prepared and described new chemical compounds that can be used as chemokine receptor antagonists and, as such, may be used in treating certain pathological conditions and diseases, particularly inflammatory pathological conditions and diseases and proliferative disorders and conditions, eg rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.

23 cl, 59 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, biotechnology, as well as to pharmaceutical, food and cosmetic industries, and concerns an agent made of sea urchin viscera being waste after edible gonads have been separated. The agent with anti-inflammatory and immunotropic activity is characterised by the fact that it represents an alcoholic extract prepared of sea urchin viscera after gonad separation, containing 10-15% of peptides, 35-45% of amino acids, 4-8% of phospholipids, trace substances, and has the following characteristics: molecular weight of the peptide fractions as determined by polyacrylamide gel electrophoresis is 19-15 kDa, 6-3,5 kDa and less than 3.5 kDa. The agent is prepared by separating gonads from sea urchins, taking the viscera, extraction in ethanol in ratio 1:1-3 at temperature 0 to plus 10°C for 2 h to 10 days, separation of a liquid portion to produce a water-alcohol extract, alcohol distillation, and drying.

EFFECT: invention provides preparing the safe agent with the evident therapeutic effect.

3 cl, 7 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, particularly to pharmacology in cardiology, particularly to a herbal tea for treating adolescents with labile arterial hypertension. The herbal tea for treating the adolescents suffering stable arterial hypertension containing dried grinded herbal raw material: quinquelobate motherwort herb, origanum herb, Baikal skullcap roots, thin-leaved milkwort roots taken in certain proportions.

EFFECT: herbal tea is effective in treating the adolescents with labile arterial hypertension.

2 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacology in cardiology, particularly to a herbal tea for treating the adolescents suffering stable arterial hypertension. The herbal tea for treating the adolescents suffering stable arterial hypertension containing dried grinded herbal raw material: creeping thyme herb, Baical woundwort herb, rose hips, Siberian patrinia roots in certain proportions.

EFFECT: herbal tea is effective for treating the adolescents suffering stable arterial hypertension.

2 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a pharmaceutical composition for treating and/or preventing depressions. The pharmaceutical composition contains an active substance presented by a selective serotonin reuptake inhibitor (SSRI) specified in a group of fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine differing by the fact that as an active substance, it additionally contains N-acetyl-5-methoxytryptamine (melatonin) in the following proportions, mg: selective serotonin reuptake inhibitor (SSRI) - 10-30 mg, melatonin - 3-8 mg. The pharmaceutical composition may be presented by a solid dosage form - a tablet, a film-coated tablet, a capsule, by a soft dosage form - a rectal suppository.

EFFECT: pharmaceutical composition provides treating depressions and has a number of additional therapeutic properties: easing falling asleep and relieving sleeping disorders, recovering circadian rhythm and seasonal rhythm with reducing a risk of side effects of SSRI.

3 cl, 14 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely producing herbal pharmaceutical preparations for treating cancerous diseases in gynaecology and andrology. The preparation for treating cancerous diseases in gynaecology and andrology contains in 1 suppository 2.0 g: ethanolic propolis extract 0.05-0.1 g; ethanolic poison hemlock extract 0.1-0.15 ml; fir essential oil 0.02-0.05 ml; melmot-berries essential oil 0.02-0.025 ml; tea tree essential oil 0.02-0.025 ml; manna gum essential oil 0.015-0.018 ml; ethanolic plumepoppy extract 0.1-0.15 ml; ethanolic potatoe sprout extract 0.1-0.15 ml; black caraway oil 0.015-0.02 ml; betulinol (powder) 0.025-0.05 g; base to 2.0 g.

EFFECT: suppositories are applicable for local use, as well as for general body effect, for prevention and/or treatment of the whole number of diseases and pathological conditions in gynaecology, urology and proctology.

3 cl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for producing pharmaceutical preparations for rectal and vaginal introduction for treating proctological and gynaecological diseases. What is presented is a method for producing an agent for treating proctological and gynaecological diseases on the basis of bee glue to be mixed with palm oil and an emulsifier with the prepared mixture constantly stirred on a water bath; then alcohol is distilled off; the prepared mixture is diluted with palm oil, cooled to temperature 35-36 degrees and added with aqueous-alcoholic extracts, essences and herbal powder extracts; thereafter the whole amount with the introduced ingredients is mixed up and poured with a dispenser into moulds 2 g made of food foil. The method is used to prepare rectal or vaginal suppositories. The suppositories are free from preserving agent and have shelf life one-two years at storage temperature 5-10 degrees Celsius.

EFFECT: suppositories produced by the given method may be used for treating proctological and gynaecological diseases, namely prostatitis, prostatic hyperplasia, haemorrhoid, anal fissures, gynaecological and andrological inflammatory diseases.

3 cl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacy and concerns a composition for inflammatory diseases of the female genital sphere. The presented suppositories contain a complex herbal extract, aerosil, emulsifier T2, cocoa butter in the following proportions, g in a suppository of 2 g. The solid complex herbal extract 0.25, Aerosil, 0.06, Emulsifier 0.02, cocoa butter 1.82. The complex herbal extract is prepared as follows: the ground herbal raw material containing cow clover blossom clusters, black elder blossom, thistle herb, nettle herb and purple Echinacea herb in 70% alcohol in equal proportion of alcohol: raw material 1:8. The material is soaked for 48 hours. The prepared total extract is condensed under vacuum to moisture 25% and mixed with a meal monger extract in proportions 8:2. The prepared total extract is condensed under vacuum to moisture 25% and mixed with a meal monger extract in proportions 8:2.

EFFECT: suppositories possess a wide spectrum of pharmacological action and improved bioavailability.

4 ex

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine, namely to urology, and can be used for treatment of patients with chronic infectious prostatitis. For this purpose, suppositories, containing 0.75 g of dense extract of licorice root on hydrophilic base with polyethylene glycol 6000 and polyethylene glycol stearate are introduced intrarectally, in dose 1 suppository with weight 2.25 g 2 times per day, daily. Course of treatment constitutes 10 days.

EFFECT: method provides efficient treatment due to antibiotic anti-inflammatory hormone-modulating and restoring sexual function action of suppositories.

6 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely pediatrics, may be used for preventing influenza and acute respiratory infections in children suffering bronchial asthma. For this purpose, 5 days before the scheduled influenza vaccination, Viferon is introduced in a child's body through rectum in the form of suppositories twice a day in the morning and in the evening, one suppository in a single dose for children aged 4 to 7 years old 150000 ME, 7 to 16 years - 500000 ME, and the second stage involves introducing the inactivated influenza vaccine.

EFFECT: use of the given method allows improving a clinical course of the post-vaccinal period ensured by reducing intercurrent ARIs in 4 times, and also decreasing the rate of influenza and ARIs of the other aetiology for the following epidemiological period in 2 times.

2 ex, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents medication for treatment of hemorrhoids, proctitis and other inflammatory proctological diseases in form of rectal suppository, characterised by the fact that it contains as active substances Juglanex and Tycveolum, as auxiliary substances contains polyethylene glycol 1500 and emulsifier T2, components in medication are in specified ratio in grams per 1 suppository, with weight 2.6 g.

EFFECT: invention ensures anti-inflammatory and regenerating action, and possesses good penetrating ability.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacy, namely technology of preparation of rectal suppositories. The suppositories with solid licorice extract consist of solid licorice extract 0.75 g on a hydrophilic base, polyethylene glycol 6000 1.25 g and polyethylene glycol polystear 0.25 g.

EFFECT: making the preparations exhibiting anti-inflammatory action, and also a positive effect on the hormonal status and the copulative function.

7 tbl

FIELD: medicine.

SUBSTANCE: invention relates to gel composition for nasal introduction of neurotransmitters. Composition includes, at least, one neurotransmitter, for instance, such as dopamine; at least, one lipophilic or partially lipophilic carrier; and compound or mixture of compounds, possessing activity with respect to reduction of superficial tension, in amount, efficient for formation of emulsion in situ when composition contacts water.

EFFECT: composition ensures high bioactivity and bioavailability of neurotransmitter in plasma and brain.

14 cl, 3 dwg, 2 tbl, 1 ex

Up!