Pharmaceutical composition

 

(57) Abstract:

The pharmaceutical composition is intended for immunosuppressive therapy. The composition includes 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable acid additive salt as the active ingredient and lecithin in the ratio of 5 are 300 wt.h. 1 wt.h. the active ingredient. The composition may further contain a saccharide and can be prepared in the form of a liquid preparation. The composition is applied to suppress rejection in transplantation of an organ or bone marrow, for maintenance immunosuppressive therapy, for the treatment of autoimmune and allergic diseases and to reduce local inflammation. 4 C. and 7 C.p. f-crystals.

The technical scope of the invention

This invention relates to pharmaceutical compositions and to compositions for the set, which include 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable acid additive salt as an active ingredient. More precisely, this invention relates to pharmaceutical compositions containing 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable acid additive salt is CA, small intestine, etc.,) or bone marrow transplantation, for maintenance immunosuppressive therapy or for the treatment of autoimmune diseases, and which can be prepared in the form of liquid preparation.

Description of the prior

2-Amino-2-[2-(4-octylphenyl)ethyl] propane-1,3-diol and its pharmaceutically acceptable acid additive salt, are known to be useful as suppressants of rejection in transplantation of an organ or bone marrow or as a therapeutic agent in various autoimmune diseases, such as psoriasis, Behcet's disease, etc. and rheumatic diseases, as described, for example, in the publication WO 94/08943.

In the specified publication WO 94/08943 retrieves the specified connection in the form of a solution for injection and describes its solvents, which are polyethylene glycol and ethanol. However, the polyethylene glycol exerts undesirable effects such as local irritation and hemolysis, and its use should be limited. In addition, ethanol is not applicable for injection due to the fact that causes local irritation.

When the above-mentioned connection, in particular 2-amino-2-[2-(4-octylphenyl)ethyl]about what Britania), dissolved in distilled water to obtain a liquid preparation, the disadvantage of the liquid drug is hemolysis and local irritation that it causes. Even liquid product containing this compound and isotherwise agent, such as sodium chloride, as an additive, traditionally used for the liquid preparation such as an injection solution or eye drops, could not reduce hemolysis and local irritation, and the product was unsatisfactory.

In the publication of Japanese Patent Examined Publication N 48485/1975 describes that the lecithin, in particular egg yolk lecithin, shows no hemolysis. However, this publication does not indicate that lecithin reduces hemolysis using the connection, which represents the active ingredient.

In addition, in the publication of Japanese Patent Unexamined Publication N 340525/1994 describes eye drops, characteristically containing vitamin a, hydrogenated lecithin and nonionic surfactant in a specific ratio in order to stabilize the vitamin a and reduce eye irritation. The publication describes that since the non-ionic surfactant that is designed to add to vitamin a, which represents the consistent lecithin in a ratio of from 0.1 to 1 part per part of vitamin a and from 0.01 to 1 part per part of non-ionic surfactants.

Description of the invention

In view of the situation described above were conducted intensive studies in an attempt to obtain a pharmaceutical composition comprising 2-amino-2-[2-(4-octylphenyl)ethyl] propane-1,3-diol or its pharmaceutically acceptable acid additive salt, which is associated with fewer side effects such as hemolysis and local irritation, and which can be prepared in the form of a liquid preparation such as an injection solution and eye drops, during which it was discovered that the addition of lecithin ensured the achievement of the objectives that led to the creation of this invention.

Accordingly, the present invention relates to pharmaceutical compositions containing 2-amino-2-[2-(4-octylphenyl)ethyl] propane-1,3-diol or its pharmaceutically acceptable acid additive salt and lecithin, from which you can easily prepare a pharmaceutical drug, which is associated with fewer side effects such as hemolysis, and which causes less local irritation, and therefore acceptable to the liquid preparation. In connection with this invention it was also noted that the addition of the specified composition of the saccharide selected from monosaccharides, dis is farmacevticheskaja composition of the present invention, for example in the form of an injection solution, can significantly reduce the irritation on the skin, blood vessel, etc., a Pharmaceutical composition of this invention contains lecithin in the ratio of not less than 5 parts by weight, usually 5 are 300 parts by mass of the weight compounds, which are an active ingredient. By adding lecithin ratio, in particular, 5-100 parts by weight, preferably 5-50 parts by weight, more preferably 5-20 parts by mass of the weight compounds, which are an active ingredient, hemolysis and local irritation caused by connection, which represents the active ingredient, can be significantly reduced.

The pharmaceutical composition of this invention contains 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable acid additive salt as an active ingredient, lecithin and, if necessary, saccharide.

The active ingredient of the pharmaceutical compositions of the present invention is 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol and its pharmaceutically acceptable acid additive salt can be obtained by the method described in WO 94/08943. The preferred compound is 2-amino-2-the d, sulfate, acetate, fumarate, maleate, benzoate, citrate, malate, methanesulfonate and bansilalpet.

2-Amino-2-[2-(4-octylphenyl)ethyl] propane-1,3-diol or its pharmaceutically acceptable acid additive salt is added in the proportion of 0.01-20% by weight, in particular 0.1 to 10% by weight based on the total weight of the composition.

Lecithin designed for use in this invention is, for example, egg yolk lecithin, soybean lecithin, etc., or hydrogenated lecithin. For dissolving large quantities of connections, which represents the active ingredient, and for more transparency of the fluid, it is preferable lecithin with a high content of phosphatidylcholine and high iodine number, in which lysophosphatidylcholine and phosphatidylethanolamine are found in small quantities. For example, the preferred lecithin egg yolk is lecithin containing 65-95% of phosphatidylcholine and having an iodine number of approximately 60-80 in which lysophosphatidylcholine and phosphatidylethanolamine in small quantities. Among them is the most appropriate purified egg yolk lecithin, described in the publication of Japanese Pharmaceutical Codex.can be attributed to the addition of hydrogen. A typical specific example of such a hydrogenated lecithin is egg yolk lecithin and hydrogenated soy lecithin. These hydrogenated lecithins preferably have an iodine number of not less than 6. These lecithins, intended for use in this invention is added in an amount of not less than 5 parts by weight, usually 5 are 300 parts by weight, in particular 5-100 parts by weight, preferably 5-50 parts by weight, more preferably 5-20 parts by mass per part of weight of the above active ingredient.

Saccharide designed for use in this invention is selected from monosaccharides, disaccharides and sugar alcohols such as glucose, fructose, D-maltose, lactose, sucrose, D-mannitol, D-xylitol, D-sorbitol, which can be used separately or in combination. These sugars added in the amount of 1-100 parts by weight, preferably 5-80 parts by mass per part of 2-amino-2-[2-(4-octylphenyl)ethyl] propane-1,3-diol or its pharmaceutically acceptable acid additive salt.

Preparative form of pharmaceutical compositions of the present invention is a fluid which, in particular, is an injection solution, eye drops, nasal, drops in the ear, fluid in the Lee etc., with a preference for injection solution (for example, intravenous, subcutaneous, intramuscular, etc. injection), eye drops and liquid for intravenous infusion, with a special preference for solution for injection (e.g. intravenous, subcutaneous, intramuscular, etc. injection) and liquid for intravenous infusion. These preparative forms appropriately chosen in accordance with the diseases to be treated, symptoms, gender and age of the patient, the region of introduction, etc., and the preparation is prepared by a method known to a qualified specialist in this field.

The pharmaceutical composition of this invention can be supplied on sale as ready-to-liquid preparation or in the form of a kit including a powder or freeze-dried product containing the active ingredient and so on , and the liquid for dissolution. For example, a solution obtained by dissolving the active ingredient, 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable salts (in particular, the hydrochloride), purified water, sterilized by filtration and placed in a test tube, then lyophilizer under vacuum to obtain a lyophilized product. Individual is necessary, in distilled water to obtain an aqueous solution, which is a liquid for dissolution. The above dried product can be dissolved in such liquid to dissolve during use. The liquid used for dissolving in 5 to 2000 times the number (the part based on mass) relative to 2-amino-2-[2-(4-octylphenyl)ethyl] propane-1,3-diol or its pharmaceutically acceptable acid salt additive. The term "distilled water" in this description refers to distilled water for injection when the injection means. The above dried product is usually placed in a test tube and after displacing the air contained in them, their nitrogen, sealed with a rubber stopper and then sealed with an aluminium lid, which makes it possible for long-term storage at room temperature. Lecithin and saccharide, intended for adding, if necessary, can be dried product with the active ingredient, 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diola or its pharmaceutically acceptable acid salt additive, and not in the liquid for dissolution as described above. The amount of lecithin is n is more preferably 5-20 parts by mass per part of weight of the above active ingredient. The number of saccharide intended to introduce, if necessary, is 1-100 parts by weight, preferably 5-80 parts by mass per part of weight of the above active ingredient.

The pharmaceutical composition of this invention may contain in addition to the above ingredients, for example, solvents, isotherwise components, regulating the pH value, buffer funds, antioxidants, thickeners, surfactants, preservatives, wetting, odorants, colorants, etc. when this is acceptable. These additives may be added with the introduction of the compositions of this invention in a pharmaceutical drug or may be added to the liquid for dissolution provided in the above set to obtain the drug, which is used for dissolving in the application.

The pharmaceutical composition of the present invention can be used in the form of a liquid drug to suppress rejection after organ transplantation or bone marrow, immunosuppressive maintenance therapy and in the treatment of eye diseases such as Behcet's disease and uveitis, dermatitis, including psoriasis, diffuse neurodermatitis, contact dermatitis and allergic the data relevant diseases (e.g., for immunosuppression in organ transplantation or bone marrow at various autoimmune diseases, various allergic diseases, etc.,) with traditional manufacturing in the form preparations for oral administration.

The composition of this invention can be used in the form of a liquid drug for the treatment or prevention of immunity or rejection in transplantation of an organ or tissue (for example, when transplantation of heart, kidney, liver, lung, bone marrow, cornea, pancreas, small intestine, limb, muscle, nerve, brain fatty substances (fatty marrow), duodenum, skin and insular cells of the pancreas, with xenotransplantation, graft-versus-host (graft-versus-host (GvH) diseases) due to bone marrow transplantation, autoimmune diseases, such as rheumatoid arthritis, systemic lupus erythematosus, nephrotic syndrome lupus (nephrotic syndrome lupus, Hashimoto's thyroiditis (Hashimoto''s thyroiditis), multiple sclerosis, myasthenia gravis heavy psevdomatematicheskoe, diabetes mellitus type I, diabetes mellitus adult type II, uveitis, nephrotic syndrome, steroid-dependent and steroid-resistant nephrosis, pustular by pathogenic microorganisms. The composition of this invention are also useful for treating inflammatory, proliferative and hyperproliferative skin diseases and cutaneous manifestations of immunologically mediated diseases, such as psoriasis, psoriatic arthritis, atopic eczema (atopic dermatitis), contact dermatitis and other eczematous dermatitis, subarray dermatitis, lichen planus, puzyrchatka, bullous puzyrchatka, congenital bullous bullosa, urticaria, angioedema, vasculitis (vasculitides), erythema, cutaneous eosinophilia (cutaneous eosinophilias, acne (acne), alopecia areata, eosinophilic fasciitis (eosinophilic fasciitis) and atherosclerosis. In particular, the composition of the present invention is useful for reviving hair, such as in the treatment of baldness in male or female type or senile alopecia, through prevention of hair removal, development of hair and/or acceleration of the nucleation and growth of hair.

The composition of this invention are also useful in the treatment of respiratory diseases such as sarcoidosis, pneumosclerosis, idiopathic interstitial pneumonia (idiopathic interstitial pneumonia) and reversible obstructive airway disease (reversible obstructive airways disease), including the mA, hereditary asthma, acquired asthma and dust asthma, particularly chronic or incurable asthma (e.g. late asthma (late asthma and hypersensitivity of the respiratory tract (airway hyperresponsiveness)), bronchitis, etc., the Composition of this invention may also be useful for treatment of liver damage associated with ischemia. The composition of the present invention is also applicable in certain diseases of the eye such as conjunctivitis, keratoconjunctivitis, keratitis, vernal conjunctivitis, uveitis associated with Behcet's disease, keratitis, herpetic (herpetic) keratitis, conical cornea, the epithelial corneal dystrophy, keratoleukoma, eye disease (ocular pemphigus), ulcer Moray (Mooren''s ulcer, scleritis, ophthalmopathy Graves (Graves' ophthalroopathy), severe eye irritation, etc.

The composition of this invention are also useful for preventing or treating inflammation of mucosa or blood vessels (diseases mediated leukotriene B4, gastric ulcers, vascular damage caused by ischemic diseases and thrombosis, ischemic bowel disease, inflammatory bowel (such as Crohn's disease and ulcerative colitis), necrotizing enterocolitis) or damage Enya or prevention of kidney diseases, including interstitial nephritis syndrome?, hemolytic-uremic syndrome and diabetic neuropathy; nerve diseases, selected from dermatomyositis, Guillain-Barre syndrome, Meniere's disease and radiculopathy; endocrine diseases including hyperthyreoidism and graves ' disease; blood disorders, including true red cell aplasia, aplastic anemia, gipoplasticheskaya anemia, idiopathic thrombocytopenic purple, autoimmune hemolytic anemia, agranulocytosis and americaplay; bone diseases, including osteoporosis; respiratory diseases, including sarcoidosis, pneumosclerosis and idiopathic interstitial pneumonia (idiopathic interstitial pneumonia); skin diseases, including dematomyositis, ordinary vitiligo (vitiligo vulgaris, vulgaris (ichthyosis), photoallergic sensitivity and cutaneous lymphoma associated with the human virus T cell (cutaneous T cell lymphoma); diseases associated with the circulatory disorders, including atherosclerosis, Arteta, polyarthritis nadeznogo and myocardosis (amyocardosis); collagen diseases, including scleroderma, Wegener granulomatosis and Sjogren syndrome; obesity; eosinophilic fasciitis; periodontal Jerusalem.

In addition, the composition of the present invention is indicated for the prevention or treatment of diseases, including intestinal inflammation or allergies, such as abdominal disease (Coeliac disease), proctitis, eosinophilic gastroenteritis, mastocytosis, Crohn's disease and ulcerative colitis; and allegricheskih diseases associated with food, which have symptomatic manifestation remote from the gastrointestinal tract, for example migraine, rhinitis and eczema.

The active ingredient of the pharmaceutical compositions of the present invention is 2-amino-2-[2-(4-octylphenyl)ethyl] propane-1,3-diol and its pharmaceutically acceptable acid additive salt also have a restorative effect in the liver and/or activity of acceleration hypertrophy and hyperplasia of hepatocytes. Therefore, they are also useful for the treatment or prevention of liver disease such as immunogenic diseases (for example, chronic autoimmune liver diseases including autoimmune hepatitis, primary biliary cirrhosis and sclerosing cholangitis (sclerosing cholangitis)), partial liver resection, acute liver necrosis (e.g. necrosis caused by toxins, viral hepatitis, shock or hypoxia), B-virus hepatitis, non-a/non-b (non-A is otivational composition and, therefore, it can be used in the treatment of diseases caused by pathogenic microorganisms, etc., in Addition, the composition of this invention can be used for the prevention or treatment of malignant rheumatoid arthritis, amyloidosis, fulminante hepatitis, syndrome Shay-Drager, pustular psoriasis, diseases behceta, systemic lupus erythematosus, endocrine ophthalmopathy, progressive systemic sclerosis, mixed connective tissue disease syndrome Arteta (aortitis syndrome, Wegener granulomatosis, chronic active hepatitis, Evans syndrome (Evans syndrome, pollinosis, idiopathic hypoparathyroidism, Addison disease (autoimmune inflammation of the adrenal gland), autoimmune orchitis, autoimmune oophoritis, cold hemagglutinin disease (cold hemagglutinin disease), paroxysmal cold of hemoglobinuria, pernicious anemia, acute illness associated with human virus T cells (leukemia), autoimmune atrophic gastritis, lupus hepatitis, canalave-interstitial nephritis, membranous nephritis (membranous nephritis), amyotrophic lateral sclerosis, rheumatic fever, post-infarction syndrome (postmyocardial infarction syndrom) and simpat the other immunosuppressants, steroid(s) (e.g., prednisolone, methylprednisolone, dexamethasone, hydrocortisone, etc.,) or nonsteroidal anti-inflammatory agent. As another immunosuppressant" preferred immunosuppressant selected from azathioprine, brequinar sodium, cyclosporine, doxicillin, mizoribine, mycophenolate 2-morpholinoethyl, rapamycin, tacrolimus monohydrate, Leflunomide and OCT-3.

Although the subject matter varies depending on the disease to be treated, symptoms, age and sex of the patient, the introduction and so on, the composition of this invention may be preferred clinical effects through the introduction or application of the product containing this compound in a quantity within 0.00001 to 20 wt.%, preferably of 0.0001-10 wt.%, from one to several times a day (for example, 2-5 times a day).

The best variant embodiment of the invention

The invention is described below in more detail by reference to examples and comparative examples.

In the following examples and comparative examples, the ratios are given by weight, unless otherwise indicated. In the examples, the term "the connection" refers to 2-amino-2-[2-(4-about the second solution, containing the compound of this invention and having the following formulation.

This connection - 0,03%

Purified egg yolk lecithin - 1,0%

D-mannitol - 5,0%

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml). If necessary, may be added conventional additives such as preservatives.

Example 2

Get injectable solution containing this compound and having the following formulation.

This compound is 0.1%

Gererously egg yolk lecithin - 1,0%

D-mannitol - 5,0%

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml). If necessary, may be added conventional additives such as preservatives.

Example 3

Get injectable solution containing this compound and having the following formulation.

This compound is 0.1%

Purified egg yolk lecithin - 1,0%

The above composition is dissolved in distilled water for injection containing, if necessary, conventional additives such as preservatives. After m to obtain the injection solution.

Example 4

Get injectable solution containing this compound and having the following formulation.

This invention is 0.1%

Hydrogenated soy lecithin - 1,0%

The above composition is dissolved in distilled water for injection containing, if necessary, conventional additives such as preservatives. After sterilization by filtration in a test tube download total amount of 10 ml and lyophilizers the traditional way to obtain the injection solution.

Example 5

Get injectable solution containing this compound and having the following formulation.

This compound is 0.1%

Purified egg yolk lecithin - 2,0%

Sodium chloride 0.9 per cent

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml). If necessary, may be added conventional additives such as preservatives.

Example 6

Get solution for injection containing the compound and having the following formulation.

This compound is 0.01%

Purified egg yolk lecithin - a 0.05%

D-mannitol - 5,0%

Above the composition is necessary, may be added conventional additives, such as preservatives.

Example 7

Get injectable solution containing this compound and having the following formulation.

This compound is 0.01%

Purified egg yolk lecithin and 0.5%

D-mannitol - 5,0%

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml). If necessary, may be added conventional additives such as preservatives.

Example 8

Get injectable solution containing this compound and having the following formulation.

This compound is 0.1%

Purified egg yolk lecithin - 0,6%

Sucrose - 10,0%

The above composition is dissolved in distilled water for injection. After sterilization by filtration in a test tube download total amount of 2 ml and lyophilizers the traditional way to obtain the injection solution. If necessary, may be added conventional additives such as preservatives.

Example 9

Get injectable solution containing this compound and having the following formulation.

This compound is 0.1%

Purified egg yolk lecithin - 0,6%

Example 10

Get injectable solution containing this compound and having the following formulation.

This compound is 0.01%

Purified egg yolk lecithin - 1,0%

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml). If necessary, may be added conventional additives such as preservatives.

Example 11

Get injectable solution containing this compound and having the following formulation.

This compound is 0.1%

Purified egg yolk lecithin - 1,0%

D-mannitol - 5,0%

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml). If necessary, may be added conventional additives such as preservatives.

Example 12

The compositions described in examples 1-11, dissolved in sterile purified water (can be added conventional additives such as preservatives), get eye drops (total number of each solution - 10 ml).

Sravnitelnii, get injectable solution (total 10 ml).

Comparative example 2

This compound is 0.1%

Sodium chloride 0.9 per cent

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml).

Comparative example 3

This connection - 0,03%

Mannitol - 5,0%

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml).

Comparative example 4

This compound is 0.01%

D-mannitol - 5,0%

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml).

Comparative example 5

This compound is 0.1%

Mannitol - 5,0%

The above composition is dissolved in distilled water for injection, receive injectable solution (total 10 ml).

Experimental example 1

Test solution (1.0 ml) was kept at 37oC for 2 minutes and mixed with heparin person (10 U/ml) with the addition of blood (0.1 ml). After incubation for 30 minutes the mixture was cooled with water and centrifugally at 540 nm in accordance with the method, refer to the publication Inglot et al., Blochem. Pharmacol., vol. 17, p.269, (1968), on the basis of which to calculate the rate of hemolysis. As control was used distilled water for injection. From the calculation of the rate of hemolysis was found that preparations of examples 1-10 show a significant reduction of hemolysis. The preparations of comparative examples 1-4, in contrast, show hemolysis.

Experimental example 2

The preparations of examples 1 and 11 and the preparations of comparative examples 3 and 5 were injected intravenously re-LEW rats at 5 weeks of age, and the presence or absence of local irritation was determined on the basis of the rate of swelling of the tail, expressed in percent {(diameter of the tail group with the entered medication - diameter tail of the control group): the diameter of the tail control group 100}. The result was found that preparations of examples 1 and 11 gave the percentage swelling of the tail of 0.5% and 0.7%, respectively, demonstrating the significant decrease local irritation. The preparations of comparative examples 3 and 5, however, were the percentage of swelling of 15.6% and 20.5%, respectively, demonstrating the presence of local irritation.

Experimental example 3

Eye irritation can be estimated in accordance with the Method of Kr is an ants eye drops, as described in the publication Science Study Report of Ministry of Health and Welfare (1970).

Industrial applicability

Pharmaceutical composition suitable for liquid drug with less local irritation, which contains 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable acid additive salt, which is associated with fewer side effects such as hemolysis, and which can easily be entered in the pharmaceutical preparation can be provided by the addition of lecithin and, when necessary, of the saccharide to give a 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diolo or its pharmaceutically acceptable acid salt additive.

1. Pharmaceutical composition for immunosuppressive therapy, including 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable acid additive salt as the active ingredient and lecithin in the ratio of 5 are 300 wt.h. 1 wt.h. the active ingredient.

2. The pharmaceutical composition under item 1, in which the lecithin is selected from the group consisting of lecithins and of hydrogenated lecithins.

3. The pharmaceutical composition according to p. 1, further comprising saccharide.

4. Pharmaceutical corresponsabilidad, disaccharides and sugar alcohols.

5. The pharmaceutical composition under item 3 or 4, in which the saccharide is one or more members selected from the group consisting of D-mannitol, glucose, D-xylitol, D-maltose, D-sorbitol, lactose, fructose and sucrose.

6. The pharmaceutical composition under item 1, in which the active ingredient is 2-amino-2-[2-(4-octylphenyl)-ethyl]propane-1,3-diol hydrochloride.

7. Set for immunosuppressive therapy, including freeze-dried product of 2-amino-2-[2-(4-octylphenyl)ethyl] propane-1, 3-diol or its pharmaceutically acceptable acid additive salt as an active ingredient and a liquid for dissolution, which is an aqueous solution containing lecithin in the ratio of 5 are 300 wt.h. 1 wt.h. the active ingredient.

8. Set for immunosuppressive therapy, including freeze-dried product of 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable acid additive salts as the active ingredient and lecithin, taken in the ratio of 5 are 300 wt.h. 1 wt.h. the active ingredient, and liquid for dissolution containing distilled water.

9. Set under item 7 or 8, further is>/P>10. Set under item 7 or 8, in which the pharmaceutically acceptable acid additive salt of 2-amino-2-[2-octylphenyl)ethyl]propane-1,3-diol hydrochloride is.

11. Pharmaceutical composition containing 2-amino-2-[2-(4-octylphenyl)ethyl] propane-1,3-diol or its pharmaceutically acceptable acid additive salt as the active ingredient and lecithin in the ratio of 5 are 300 wt.h. 1 wt.h. the active ingredient used to suppress rejection in transplantation of an organ or bone marrow, for maintenance immunosuppressive therapy, for the treatment of autoimmune and allergic diseases and to reduce local inflammation.

 

Same patents:

The invention relates to new substituted piperidine-2,6-diones of the formula (I)

where Z is-C(R1R2)-CH2or-C(R1)=CH-; R1- phthalimid, when Z is-C(R1R2)-CH2- or one - or twofold substituted by hydroxy, methoxy or amino groups phtalimide radical when Z represents-C(R1)=CH-, R2is hydrogen or C1-6alkyl group; R3is hydrogen, C1-6an alkyl group or aromatic ring system; R4- C1-6alkyl or aromatic ring

The invention relates to pharmacology and medicine, in particular to the preparation of solid dosage forms of the drug rapamycin, which includes a core and a sugar coating

The invention relates to medicine and relates to drugs to prevent transplant rejection, monoclonal antibodies to the CD3 antigen of T-lymphocytes person, hybridoma producing these antibodies, and treatment of patients with reaction acute transplant rejection after kidney transplantation

The invention relates to medicine and organic chemistry and relates to the problem of creating new drugs, inhibiting the proliferation of lymphocytes

-position the retrieval method, industrial products, pharmaceutical composition" target="_blank">

The invention relates to salts of compounds of formula (I) in the case where these compounds contain aminopentyl, in particular with hydrochloric acid, Hydrobromic acid, nitric, sulfuric, phosphoric, acetic, formic, propionic, benzoic, maleic, fumaric, succinic, tartaric, citric, oxalic, Glyoxylic, aspartic acids, alkanesulfonyl, such as methane - and ethane-sulfonic acids, arylsulfonate, such as benzene and paratroop-sulfonic acids, and arylcarbamoyl acids, and, when the compounds of formula (I) contain an acid function, the salts of alkali, alkaline earth metals and ammonium, optionally substituted

The invention relates to medicine, in particular to the immunological treatment response graft-versus-host (GVHD)

The invention relates to medicine and relates to methods of inducing T-cell tolerance to tissue or organ transplant

The invention relates to a new derivative of 4-oxo-1,4-dihydropyrimidin, specifically: 2,6-diethyl-5-phenyl-1(5,6-dimethylbenzimidazolyl-1)-4-oxo-1,4-dihydropyrimidine (I) having immunosuppressive activity, which can find application in medicine

The invention relates to the composition of polyols for the production of tablets

The invention relates to the production of compressed forms in the food and pharmaceutical industries

The invention relates to medicine, namely to create a means for the treatment of cardiovascular diseases

The invention relates to microencapsulating secretory cells in the hydrophilic gel, therapeutic methods that are used macroencapsulation secretory cells, and to the preservation of secretory cells by macroencapsulation

The invention relates to pharmacology, specifically to dukaina lipid drug in the polar solvent, which comprises from 0.01 to 90 wt.%, preferably 0.1 to 50 wt.%, the material forming the bilayer, while the said material, forming a bilayer, is galactolipid material from cereals, consisting of at least 50% of digalactosyldiacylglycerols, and the remainder includes other polar lipids

The invention relates to chemical-pharmaceutical industry, namely, the liquid pharmaceutical compositions containing human chorionic gonadotropin (hCG)

The invention relates to pharmacology and for the treatment of burn wounds
Up!