• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    1. METHOD FOR OBTAINING MEANS, BRAKING INFLAMMATORY PROCESSES by mixing a derivative of a non-steroidal agent indomethacin with auxiliary substances followed by evaporation, characterized in that, in order to eliminate a side effect, use the acetalylacylide to use a mixture of substances that are used to derive a side effect.
    公开号:SU1175350A3
    申请号:SU802990201
    申请日:1980-09-24
    公开日:1985-08-23
    发明作者:Кахан Илона
    申请人:Kahan Ilona；
    IPC主号:
    专利说明:

    The invention relates to the chemical industry of the pharmaceutical industry, to the preparation of an inhibitory agent into the palette processes. The aim of the invention is to eliminate the side effects. Example 1: An injectable preparation for therapeutic purposes; prepared from the following components; Ampoule for powders — 25 mg of indomethacin; a ampoule for a solvent — 50 mg of tris (oxy methyl) -aminomethane, hydrochloride, 2 MP of distilled water. The contents of the ampoule with the powder is mixed with the contents of the ampoule with the solvent. The resulting solution has a pH of 6.8. The enzymatic activity of the synthesis of prostaglandin inhibits in vitro by this growth of „„ „„ „„ by a thief at: 7il. The therapeutic agent can be administered intravenously, intramuscularly, intra-articularly, or subconjunctivally. An action aimed at tissue damage is not observed. Der sterileiter, arising from high permeability, can be removed from the eye chamber by using a preparation prepared in the form of eye drops or by subconjunctival injection. In the eye cavity of one of the eyes of the rabbit inject arachidonic acid. As a result of the inflammatory effect of prostaglandin, synthesized from arachic acid, and due to increased permeability, the protein content in the eye fluid has increased tenfold. But when in the other eye of the rabbit the wounds were previously injected, the protein content in the eye fluid remained at a normal level. Example 2 To obtain water soluble indomethacin, which can be exhausted, 1000 g of indomethacin is dissolved in 10 liters of methyl alcohol with vigorous stirring at room temperature. Then, 1000 g of tris- (hydroxy methyl) -aminomethane are added with stirring to the solution. The solution formed in lemon-yellow color is evaporated by gentle heating on a water bath. During evaporation, the temperature of the solution should be lower. The resulting crystalline product dissolves easily in water, and at; concentration of 100 mg / ml solution has. . After recrystallization of the product from a mixture of acetone and diethyl ether, its melting point is 148 ° C. The therapeutic preparation may be used for the therapeutic purposes indicated in Example 1. However, it may also be mixed with carriers and placed in capsules for oral ingestion. EXAMPLE 3 To prepare eye drops of 50 mg of indomethacin, 36 mg of tris (oxymethyl) aminomethane, 10 mg of citric acid and 10 mg of boric acid are mixed, after which the powder mixture is placed in a dry capsule. The contents of the capsules are dissolved in 10 mp of water, with - ± A, i and the pH value is 7.3. The solution is used in therapy as eye drops. Example 4. To obtain the ointment used locally, the components indicated in example 1 were dissolved in 1 ml of distilled water. An indomethacin derivative soluble in water is obtained. The aqueous solution is mixed with 0.045 g of cholesterol, 0.090 g of vaseline oil and 2.835 g of yellow vaseline, resulting in an ointment. Indomethacin-containing ointment has a local anti-inflammatory effect and is used in sunbathing. PRI me R 5. Prepared from the components indicated in example 1, the solution of aglometzine is subjected to lyophilization. The lyophilized solution dissolved in 1 ml of water is used for the same purposes as the preparation obtained in accordance with Example 1. EXAMPLE 6 The therapeutic preparation is obtained from the following components: an ampoule for a powder 50 mg of indomethacin, a capsule for a solvent 80 mg of N - tris- (oxymethyl) -methyl-glycine, 2 mp of distilled water. The therapeutic preparation obtained by the above method can be used in therapy for the purposes described in example 1.
    权利要求:
    Claims (2)
    [1]
    1. METHOD FOR PRODUCING A BRAKING AGENT INFLAMMATORY PROCESSES by mixing a derivative of a non-steroidal agent indomethacin with auxiliary substances followed by evaporation, characterized in that, in order to eliminate side effects, an acetyloalicylic acid (acid 2 or 3-trifluoromethylanilino) -benzoic acid]], or niflumoic acid (3-trifluoromethyl-2-phenyl-aminonicotinic acid), or mofenamino acid (1 | _ 2,3-xylanthyl nyl acid ), naproxen [ob-2- (6-methoxy-2-naphthyl) propionic acid), indomethacin (1-p-chlorobenzoyl-5-methoxy-2-methylindolyl-3-acetic acid) or phenoprene ^ o-2 ( phenoxyphenyl) propionic acid]], which are mixed with a hydrophilic component, soluble in water in a polar solvent at a ratio of 1: (1-6), evaporated at
    12-30 ° C at a pH of 6-8.
    [2]
    2. The method according to p. 1, characterized in that in quality. hydrophilic component use tris- (oxymethyl) amino-methane, [bis - (2-hydroxyethyl) amino] -tris- (oxymethyl) methane- {* 1,3-bis [tris- (oxymethyl) methylamino]] -propane! N - [tris- (oxymethyl) methylamino] propane sulfonic acid, N - [tris- (oxymethyl) methylamino] ethanesulfonic acid, Y- [tris- (hydroxymethyl) methylglycine] and, as a polar solvent, methanol, ethanol and saline.
    >
    1 1175350
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    法律状态:
    优先权:
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