New self-emulsifying system for delivery of drugs

FIELD: medicine, pharmacology, pharmacy.

SUBSTANCE: invention relates to composition possessing an anti-inflammatory effect and useful for oral administration in form of emulsion preliminary concentrate. Composition comprises NO-releasing nonsteroid anti-inflammatory drug, surface-active substance, oil or semisolid fat and forms in situ emulsion of type oil-in-water after contact with aqueous medium, such as gastroenteric fluid. Also, invention relates to a medicinal formulation based on thereof, oral emulsion, set based on thereof and a method for treatment of inflammation and pain. Proposed compositions possess the improved availability.

EFFECT: improved and valuable properties of composition.

40 cl, 1 tbl, 20 ex

 



 

Same patents:

FIELD: medicine, surgery.

SUBSTANCE: since the 2nd d after operation for 2 wk one should prescribe nimesulide per 100 mg twice daily, and on the 7th - 10th d after operation - microwave therapy onto thyroid area at the power of 2.5 W for 5 min at low-thermal mode, moreover, after hemithyroidectomy one should prescribe physiotherapy since the 7th d, after resection of isthmus - since the 8th d, after subtotal resection - since the 9th d, after total thyroidectomy - since the 10th d. The method provides enhanced secretion of thyroid hormones and compensation of hypothyroidism due to physiotherapy, that enables to get rid of hormonal substitution therapy or decrease its dosage.

EFFECT: higher efficiency.

1 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivative of triazaspiro[5.5]undecane of the formula (I): wherein R1 means compound of the formula (1): or (2): wherein G represents a bond, (C1-C4)-alkylene, (C2-C4)-alkenylene or -CO-; ring A represents: (1) C5-10-membered mono- or bicarbocyclic ring or (2) 5-10-membered mono- or bicyclic heterocycle comprising 1-2 nitrogen atoms and/or 1-2 oxygen atoms; substitute R6 means the following values: (1) (C1-C4)-alkyl, (2) halogen atom, (3) nitrile group, (4) trifluoromethyl group and others; R2 represents: (1) (C1-C4)-alkyl, (2) (C2-C4)alkynyl or (3) (C1-C4)-alkyl substituted with a substitute represented in claim 1 of the invention claim; each R3 and R4 represents independently: (1) hydrogen atom, (2) (C1-C4)-alkyl or (3) (C1-C4)-alkyl substituted with 1-2 substituted taken among: (a) Cyc 2 and (b) hydroxy-group (wherein Cyc 2 represents (1) C5-6-membered monocarbocyclic ring or (2) 5-6-membered monocyclic heterocycle comprising 1-2 nitrogen atoms and/or one oxygen atom), or R3 and R4 form in common group of the formula: wherein R26 represents (C1-C4)-alkyl or Cyc 2; R5 represents hydrogen atom or (C1-C4)-alkyl, its quaternary ammonium salt, its N-oxide or its nontoxic salt. Also, invention relates to pharmaceutical composition inhibiting HIV, regulator of chemokine/chemokine receptor and agent used in treatment and prophylaxis of some diseases, such as inflammatory diseases, asthma, atopic dermatitis, nettle rash, allergic diseases, nephritis, hepatitis, arthritis and other diseases that comprise as an active component above described compound of the formula (I) or its quaternary ammonium salt, its N-oxide or its nontoxic salt. Also, invention relates to (3R)-1-butyl-2,5-dioxo-3-((1R)-1-hydroxy-1-cyclohexylmethyl)-9-(4-(4-carboxyphenyloxy)phenylmethyl)-1,4,9-triazaspiro[5.5]undecane or its pharmaceutically acceptable salt and pharmaceutical composition based on thereof, and to (3R)-1-butyl-2,5-dioxo-3-((1R)-1-hydroxy-1-cyclohexylmethyl)-9-(4-(4-carboxyphenyloxy)phenylmethyl)-1,4,9-triazaspiro[5.5]undecane hydrochloride and pharmaceutical composition based on thereof.

EFFECT: valuable medicinal properties of derivative and composition.

16 cl, 32 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention proposes phenylpyridazine compounds represented by the following formula (I): wherein R1 represents unsubstituted or substituted phenyl wherein substitutes are taken among the group comprising halogen atom, lower alkyl, lower alkoxy-group and phenylthio-group, or pyridyl; R2 represents lower alkoxy-group, lower alkylthio-group, lower alkylsulfinyl or lower alkylsolfonyl; R3 represents hydrogen atom or lower alkoxy-group; or R2 and R3 can be condensed in common forming lower alkylenedioxy-group; R4 represents cyano-group, carboxyl, unsubstituted or substituted lower alkyl wherein substitutes are taken among the group comprising hydroxyl, carboxyl and N-hydroxy-N-lower alkylaminocarbonyl; lower alkenyl; lower alkylthio-group; lower alkylsulfinyl; lower alkylsulfonyl; lower alkylsulfonyloxy; unsubstituted or substituted phenoxy-group wherein substitutes are taken among the group comprising halogen atom, lower alkoxy-, nitro-, cyano-group; unsubstituted phenylthio-group or phenylthio-group substituted with halogen atom; pyridyloxy-; morpholino-group; morpholinylcarbonyl; 1-piperazinylcarbonyl substituted with lower alkyl; unsubstituted or substituted amino-group wherein substitutes are taken among the group comprising lower alkyl, benzyl, phenyl that can be substituted with halogen atoms or lower alkoxy-groups, and n = 0, or their salts. Proposed compounds possess the excellent inhibitory activity against biosynthesis of interleukin-1β and can be used in preparing a medicinal agent inhibiting biosynthesis of interleukin-1β, in particular, in treatment and prophylaxis of such diseases as diseases of immune system, inflammatory diseases and ischemic diseases. Also, invention proposes intermediate compounds for preparing compounds of the formula (I). Except for, invention proposes a medicinal agent and pharmaceutical composition that inhibit biosynthesis of interleukin-1β and inhibitor of biosynthesis of interleukin-1β.

EFFECT: valuable medicinal properties of compounds and composition.

7 cl, 1 tbl, 66 ex

FIELD: medicine, rheumatology.

SUBSTANCE: the innovation deals with basic immunomodeling and symptomatic antiphlogistic therapy and additionally - therapy with Calcium-D3 preparation at dosage correction, duration and multiplicity of therapy course being dependent upon phase, activity degree, the nature of disease flow and mineral density of bony tissue (MDBT). At highly progressing RA and during exacerbation phase one should apply Calcium-D3 for 14 d at low degree of activity, for 21 d at average degree and for 28 d in case of high degree of activity, moreover, at MDBT being below the standard one should apply Calcium-D3 at the dosage of 400 IU cholecalciferol (vitamin D3) and 1250 mg calcium carbonate in the evening and 200 IU cholecalciferol and 1250 mg calcium carbonate in the morning. At MDBT ranged within the norm it is necessary to apply Calcium-D3 at the dosage of 800 IU cholecalciferol and 2500 mg calcium carbonate both in the evening and in the morning. At slowly progressing RA for above 2 yr and at the phase of relative remission one should apply Calcium-D3 at the dosage of 200 IU cholecalciferol and 1250 mg calcium carbonate in the evening for prolonged period of time at 1-wk-long interval during 1-2 d. In case of early RA lasted for 2 yr at unknown character of its flow it is necessary to apply Calcium-D3 at the dosage of 400 IU cholecalciferol and 1250 mg calcium carbonate in the evening for 14 d. Therapy course should be carried out in 4-6 mo. The innovation provides optimal therapy for every combination of the phase, activity, the nature of RA flow and MDBT parameters that enables to decrease the chance for relapses and increase remission duration by 1.5-1.8 times.

EFFECT: higher efficiency of therapy.

3 cl, 2 ex

FIELD: medicine, rheumatology.

SUBSTANCE: the innovation deals with therapy with metothrexate at the dosage of 7.5 mg/wk in combination with small dosages of glucocorticosteroids, up to 10 mg/d against prednisolone. Metothrexate should be once introduced at the quantity of 7.5-20 mg/wk, glucocorticosteroids - once at 3 a.m. Therapy course lasts for bout 6 mo, not less followed by decreasing the dosage of glucocorticosteroids for 6 mo up to their complete refusal at keeping maintenance therapy with metothrexate. The innovation enables to achieve maximal increase of antidestructive action at any terms of disease due to preventing the development of new articular erosions and keeping the width of articular fissura at the most physiological scheme of glucocorticosteroids' intake.

EFFECT: higher efficiency of prophylaxis.

4 cl, 12 dwg, 4 ex, 3 tbl

FIELD: pharmaceuticals.

SUBSTANCE: polyvinyl alcohol and magnesium or calcium chlorides polyhydrated complexes are obtained by dissolution of polyvinyl alcohol and magnesium or calcium chlorides in water on boiling water bath. Said components are taken in the next ratio (mass%): polyvinyl alcohol 11.5-11.6; magnesium or calcium chloride 23.2-24.0; and balance: distilled water.

EFFECT: new complex compounds having antiinflammation, resolution and analgesic action.

11 ex

Medicinal agent // 2268037

FIELD: medicine, chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to using 4-chloro-2-methylphenoxyacetic acid of the formula (I)

and its pharmacologically acceptable sodium, potassium and lithium salts (mixture of these salts, or mixture of salts and 4-chloro-2-methylphenoxyacetic acid) as a medicinal agent possessing immunomodulating, anti-inflammatory and antitumor properties, and antiviral activity also. 4-Chloro-2-methylphenoxyacetic acid and its mixtures with pharmacologically acceptable alkaline metal salts possess high effectiveness and enhanced bioavailability.

EFFECT: valuable medicinal properties of medicinal agent.

9 cl, 13 ex

FIELD: organic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to a heteroarylamino-substituted derivative of dihydropyrimido[4,5-d]pyrimidinone taken among of compounds order corresponding to the formula (I): wherein a subscript symbol n mans a whole number 1; R1 means (C1-C6)-alkyl (substituted with one or two substitutes taken among group involving hydroxy group, (C1-C6)-alkoxy group and others), piperidinyl-(C0-C4)-alkyl [wherein piperidinyl fragment is monosubstituted optionally with benzyl, carbamoyl, (C1-C4)-alkane sulfonyl, (C1-C6)-alkyl and so on], morpholinyl-(C0-C4)-alkyl, tetrahydropyranyl-(C0-C4)-alkyl, 2-oxoimidazolidinyl-(C0-C4)-alkyl, 2-oxopyrrolidinyl-(C0-C4)-alkyl or 1,1-dioxotetrahydrothienyl-(C0-C4)-alkyl, (C3-C6)-cycloalkyl (monosubstituted with monohydroxy group, (C1-C6)-alkoxy group and so on), 1,4-dioxaspiro[4,5]decane-8-yl, 2,4-dione-1,3-diazaspiro[4,5]decane-8-yl or (3-hydroxymethyl-3-methyl)-1,5-dioxaspiro[5,5]undecane-9-yl; R2 means (C1-C4)-alkyl, halogen atom; R3 means hydrogen atom, (C1-C6)-alkyl (optionally substituted with one or two substitutes taken among group involving (C1-C4)-alkoxy group, pyrrolidinyl, di-(C1-C4-alkyl)-amino-group and so on), phenyl, benzyl or piperidinyl (N-substituted optionally with (C1-C4)-alkyl); R4 means hydrogen atom, and also its individual isomers, racemic and nonracemic mixtures of isomers, prodrugs and its pharmaceutically acceptable salts. Also, invention proposes a pharmaceutical composition possessing inhibitory activity with respect to activity of p38 MAP kinase. The composition comprises a heteroalkylamino-derivative of dihydropyrimido[4,5-d]pyrimidinone of the formula (I), isomer, racemic or nonracemic mixture of isomers or its pharmaceutically acceptable salt in mixture with at least one pharmaceutically acceptable vehicle. Invention provides representing a heteroalkylamino-substituted derivative of dihydropyrimido[4,5-d]pyrimidinone possessing inhibitory activity with respect to activity of p38 MAP kinase.

EFFECT: valuable biochemical properties of compounds and composition.

14 cl, 4 tbl, 90 ex

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to derivatives of α-aminohydroxamic acid of the formula (I):

wherein R1 means hydrogen atom, (lower)-alkyl or phenyl-(lower)-alkyl; R2 means hydrogen atom or (lower)-alkyl; R3 means (lower)-alkyl or phenyl; A means (C1-C3)-alkylene; q = 1-5; R means (C2-C7)-alkyl, (C3-C7)-alkenyl, (C3-C7)-alkynyl, and its pharmaceutically acceptable salts. These compounds are inhibitors of MMP and first of all inhibitors of MMP2 and can be used in treatment of inflammatory states, proliferative arthritis, osteoarthritis, oncological and pulmonary diseases. Also, invention describes a method for preparing compounds and a pharmaceutical composition.

EFFECT: improved preparing method, valuable medicinal properties of compounds and composition.

18 cl, 1 tbl, 87 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of triazaspiro[5,5]undecane of the formula (I):

wherein values of radicals R1-R5 are given in the invention claim, ort o their quaternary ammonium salts, N-oxides or nontoxic salts. Proposed compounds possess inhibitory and regulating activity with respect to chemokine/chemokine receptors and can be useful in prophylaxis and treatment of different inflammatory diseases, such as asthma, atopic dermatitis, nettle rash, allergic diseases, nephritis, hepatitis, arthritis or proliferative arthritis and other similar diseases. Also, invention relates to pharmaceutical compositions based on compounds of the formula (I).

EFFECT: improved control method, valuable medicinal properties of compounds.

9 cl, 5 sch, 36 tbl, 70 ex

FIELD: biology, medicine, hormones.

SUBSTANCE: invention relates to composition designated for activation of epidermis lipogenesis and containing dehydroepiandrosterone (DHEA) and/or its precursors or chemical and/or biological derivatives. The composition represents emulsion of type "hydrophilic phase dispersed in lipophilic phase" and comprising the glycolic or hydroglycolic dispersed hydrophilic phase, continuous lipophilic phase and emulsifying agent with HLB value from 2 to 7 and wherein dehydroepiandrosterone (DHEA) and/or its precursors or chemical and/or biological derivatives are solubilized in glycolic or the hydroglycolic dispersed hydrophilic phase. Also, invention relates to its using. Invention provides preparing an agent relieving multiplication or metabolism of cells being live epidermal cells especially for prophylaxis or control of epidermis atrophy that confers young shape to skin.

EFFECT: valuable properties of emulsion.

26 cl, 3 tbl, 27 ex

The invention relates to a method for preparing biologically erodible polymeric microspheres or nanospheres using the method of "oil in water"
The invention relates to medicine and relates to antimicrobial compositions containing chloramphenicol, castor oil, emulsifier, preservative, sodium carboxymethyl cellulose and water

FIELD: medicine.

SUBSTANCE: method involves intragastrically introducing indometacin to rats at a dose of 4.5-5 mg/kg of mass after holding the animals without food and water during 5 days.

EFFECT: enhanced effectiveness of bleeding and perforating ulcer formation.

2 tbl

FIELD: medicine, neurooncology.

SUBSTANCE: one should carry out chemotherapy and irradiation till radical dosage. Moreover, 2-3 d before the onset of radiation therapy and during the whole course of irradiation one should indicate the intake of indometacin at daily dosage being 300 mg, and 8-14 d before the end of therapy course or the stage of radiation therapy it is necessary to conduct chemotherapeutic cycle with vincristine at total dosage being 4 mG and lomustine at total dosage 160-240 mg. At performing a split course of irradiation the intake of indometacin should be indicated between the stages. The innovation enables to increase radio sensitivity of malignant tumor, suppress angiogenesis, proliferative activity and increased cytotoxic activity of chemopreparations.

EFFECT: higher efficiency of therapy.

1 cl, 3 ex

FIELD: chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to manufacturing solid medicinal formulations of preparations. Invention proposes a medicinal formulation consisting of a core comprising the following components: indometacin, lactose, calcium phosphate, hydroxypropylcellulose, magnesium stearate, sodium croscarmellose and envelope comprising collicute MAE 100P, propylene glycol, pigment titanium dioxide, talc, collidon-30, brown sycovite-70. Also, invention discloses a method for preparing the formulation. Invention provides enhancing stability of envelope to effect of stomach juice, rapid and complete release of active substance, simultaneous simplifying the process of applying the envelope for a single step.

EFFECT: improved and valuable pharmaceutical properties of formulation.

3 cl, 1 tbl

FIELD: medicine, arthrology, pharmacy.

SUBSTANCE: invention relates to agents of topical applying used in treatment of articulation diseases. Proposed agent comprises mixture of chondroitin sulfate and glucosamine salts as a saccharide, the compound taken among the group nonsteroid anti-inflammatory agents, in particular, ibuprofen or nimesulid, or piroxicam, or meloxicam, or diclofenac salt, or indometacin, or ketoprofen, dimethylsulfoxide and an ointment base taken in the definite ratio of components. Invention provides enhancing effectiveness due to the content a mixture of low-molecular and high-molecular saccharides in it that results to increasing diffusion rate of active component to the articulation zone and also the compound taken among the group of nonsteroid anti-inflammatory agents. The combined using these agents provides the curative synergetic effect.

EFFECT: improved and valuable medicinal properties of agent.

2 cl, 14 ex

FIELD: medicine, arthrology, pharmacy.

SUBSTANCE: agent comprises glucosamine salt as saccharide, dimethylsulfoxide, ointment base and ibuprofen or nimesulide, or piroxicam, or meloxicam, or diclofenac salt, or indometacin, or ketoprofen as a nonsteroid anti-inflammatory agent. Glucosamine hydrochloride, glucosamine sulfate sodium, potassium or calcium salt is used as glucosamine, and diclofenac potassium or sodium salt is used as diclofenac salt. New ointment shows high perfusion rate of active substances to the articulation zone and enhanced effectiveness. Invention expands assortment of agents used in treatment of articulations.

EFFECT: improved, enhanced and valuable medicinal properties of agent.

2 cl, 14 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of indol-3-yl of the formula (I):

wherein each A and B represents independently of one another oxygen atom (O), NH, CONH, NHCO or a direct bond; X means (C1-C2)-alkylene or a direct bond; R1 means hydrogen atom (H); R2 means hydrogen atom (H); R3 means NHR6, -NR6-C(=NR6)-NHR6, -C(=NR6)-NHR6, -NR6-C(=NR9)-NHR6, -C(=NR9)-NHR6 or Het1; each R4 and R5 represents independently of one another hydrogen atom (H); R7 means -(CH2)o-Ar, Het, OR6; R6 means hydrogen atom (H); R7 means (C1-C10)-alkyl, (C3-C10)-cycloalkyl; R8 means Hal, NO2 (nitro-group), CN (cyano-group), Z, -(CH2)o-Ar, COOR1, OR1, CF3, OCF3, NHR1; R9 means CN or NO2; Z means (C1-C6)-alkyl; Ar means aryl that can represent unsubstituted, monosubstituted, or polysubstituted R8; Hal means F, Cl, Br, J; Het means saturated, partially or completely saturated monocyclic or bicyclic heterocyclic radical comprising from 5 to 10 ring members wherein 1 or 2 nitrogen atom (N) and/or 1 or two sulfur atom (S) present, and heterocyclic radical can be monosubstituted with phenyl; Het1 means saturated, partially or completely unsaturated monocyclic or bicyclic heterocyclic radical comprising from 5 to 10 ring members and from 1 to 4 nitrogen atoms (N) that can be unsubstituted or monosubstituted NHX, or oxo-group; n = 0, 1 or 2; m = 0, 1, 2, 3, 4, 5 or 6; o means 0, 1 or 2; and their physiologically acceptable salts and solvates. Compounds of the formula (I) elicit intergin-inhibitory effect that allows their using as components of pharmaceutical composition. Also, invention describes intermediate compounds.

EFFECT: valuable medicinal properties of compounds.

11 cl, 4 sch, 1 tbl, 34 ex

Up!