• 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:
    The invention provides a novel acidic alkali citrate having the formula K6Na6H3(C607H5)5 . 2-4 H2O made by dissolving either (a) trisodium citratex2 H2O, tripotassium citratex1 H2O, and citric acid in a mole ratio of 2:2:1 in 3 to 5 times the quantity by weight of boiling demineralized water, based on the weight of the citric acid and maintaining the solution at a temperature not lower than 60 DEG C.; or (b) citric acid at 90 DEG C. while stirring in .01 to 1 times its weight of demineralized water and then adding sodium carbonate and potassium carbonate to give a mole ratio of 3:3:5 of sodium carbonate: potassium carbonate:citric acid, and quick drying the homogeneous solution obtained. Therapeutic agents for the treatment of urolithiasis and removal, or preventing recurrence, of urine stones comprising said acidic alkali citrate are provided.
    公开号:SU812167A3
    申请号:SU782625401
    申请日:1978-06-12
    公开日:1981-03-07
    发明作者:Мадаус Рольф；Штумпф Вернер；Герлер Клаус；Каркасона-Бельтран Альфонсо
    申请人:Др. Мадаус И Ко (Фирма)；
    IPC主号:
    专利说明:

    . , one ,. This invention relates to the field of organic chemistry, specifically, to a method for producing alkali metal citrate, which has pharmaceutical properties and can be used in the treatment of kidney diseases. A dry mixture of sodium citrate, kggsha citrate and citric acid is known, used in the treatment of diseases of the kidneys 1. Disadvantage a known preparation is its low storage stability, which leads to lumpiness after 2 months. A method of producing salts of the small metals of carboxylic acids is known by reacting the corresponding acid with an alkali metal compound G21. The purpose of the invention is to develop a process for producing a new highly stable biologically active compound based on lime reaction. The proposed method for the preparation of alkali metal citrate of the formula KfcNa Hz (.HD-) 5 (Z-i). It consists in the interaction of trisodium citrate -21120 / trikaliy citrate .1NdO with LEMONIC ACID at their molar ratio of 2: 2: 1, respectively, or sodium carbonate, potassium carbonate with citric acid at their molar ratio of 3: 3: 5, respectively, which solution in boiling demineralized water, the citric acid is dissolved either simultaneously with citrates or before or after dissolving carbonates, and water is taken in 3-5 times, in the case of citrates or 0.51 times the weight of citric acid in case of use anion of carbonates, and the resulting homogenous solution of the target product is sequentially cooled to 60-80 ° C and dried. The resulting citrate is a stable crystalline with a specific chemical composition. The components can be supplied both directly and in reverse order, namely, alkali metal carbonates are first introduced, and then citric acid. When using compounds of NaOH and KOH and respectively NaHCO and KNSO, the corresponding molar ratios of the starting components should be observed. The obtained compounds can be used in the case of a diagnosis of colic or haemoturia, if crystals are found in brick-urine sedimentation, a constant pH in urine is below 5.5, and the presence of serum uric acid in the amount of 5.5 mg / 100 ml in men and over 4.3 mg / 100 ml in women, X-ray determination of stones by lightening or gaps in the urogram of secretions. The proposed acid citrate (SW07. H5-) (2- |) H, 20 can be used in the formation of urate acids; . stones, when uric acid diathesis or the general danger of the formation of stones. Conducted clinical trials showed success in cases above 95%. Only in a few, especially difficult cases, namely with strongly shadowy stones (mixed stones) and uncontrolled urinary tract infection, the treatment turned out to be invalid. The only danger lies in pereklachelivanii with improper, excessively high dosages of the drug for a long time, so that the upper limit of the pH value of 7.0 is significantly higher and as a result phosphate stones are formed. By setting the urine pH to between 6.2 and 7.0, the following clinical results are obtained: disappearance of subjective ailments (feeling of pressure and tension in the kidneys, typical colic); micromathatures terminated; brick sediment is not observed. X-ray control shows a decrease, respectively, dissolution of the calculus. The length of treatment required depends on the position / shape and size and age of the stone. Obviously, the litholytic effect is the better, the greater the amount of urine that is flushing the stone.
    Example 1. 194.4 kg of Trikali citrate -IH-O, 176.4 kg of trisodium citrate 2H, and 57.6 kg of citric acid are dissolved in 210.0 l of boiling demineralized water. The temperature of the solution slowly decreases to approximately 70-80 ° C, and care should be taken that a precipitate does not form. Then the homogeneous solution is transferred to a two-drum dryer by means of a pump and dried quickly. The thickness of the layer on the rolls is 0.5-0.8 mm. Inside the drying rolls, saturated steam is admitted with an overpressure of 5-7 atm, so that the temperature of the outer surface of the rolls is 140-160 ° C. By setting the speed, the residence time of the material on the roll reaches approximately 5 seconds. Capacity is 30-35 kg of dry material per 1 m of heated surface in 1 hour. The cylinders of the rolls consist of fine-grained special gray cast iron with perliticheskom structure, while outside and
    inside they are ground, polished and firmly chromed. The final drying is carried out on tray dryers to approximately 3% Hx, O.
    Below is the composition of the anhydrous substance, wt.%.
    Found Calculated
    Potassium17.40 17.76
    10 Sodium. 10.42 10.44
    Citrate. (Whole) 11, P 71,57
    Example 2.1 050.50 kg of lipol moycid, stirring, at a temperature of approximately suspended in 675 l of demineralized water. A portion of citric acid does not dissolve at first. Then, stirring
    2Q at the same temperature, 317.97 kg of sodium carbonate (anhydrous) and 414.63 kg of potassium carbonate (anhydrous) are added. The process is terminated after the release of CO and
    5 after all substances have dissolved. The solution is processed as in Example 1. The resulting product has the same elemental analysis and X-ray diffraction spectrum as in Example 1. Rome's P 3, 317.97. Kg of sodium carbonate (anhydrous) and 414.63 kg of Cali carbonate ( anhydrous), stirring, at a temperature of 90 ° C is suspended in 675 ml of water. Then, continuing to stir and maintaining the temperature, slowly add 1
    050.50 kg of solid citric acid / until reaction is complete. CO no longer yots. The resulting product is processed as described in example 1. ... :;:, ....
    Example 4 The process is carried out analogously to Example 1, however, the temperature of the solution is reduced to and the drying is carried out to a water content of 4%.
    . Get the alkali metal citrate composition specified in example 1.
    Example 5. The process is carried out in a rough way as described in Example 1, however, the starting components are dissolved in three times the weight of lemon.
     acid boiling demineralized water, the temperature of the resulting solution is reduced to and drying is carried out to a water content of 2%. Get alkali metal citrate composition,
    5 specified in example 1.
    Example 6. The process is carried out analogously to example 1, however, the starting components are dissolved in a fivefold amount by weight of lemon.
    权利要求:
    Claims (2)
    [1]
    The Q acid of boiling demineralized water, the temperature of the resulting solution is reduced to 65 ° C and the drying is dried to a water content of 4%. Alkali metal citrate is obtained as specified in Example 1. PRIORITY 7, The process is carried out in accordance with Example 2, however, citric acid is dissolved in 6.5 times the weight of the acid boiling demineralized water and the temperature of the resulting solution reduced to 75 ° C. Next, the process is carried out as described in Example 1. Get the alkali metal citrate composition specified in example 1.. Example 8. The process is carried out analogously to Example 3, however, sodium brnnates and calnas are dissolved in a single quantity by weight of citric acid boiling demineralized water. Further, the process is carried out as described in Example 1. Get alkali metal citrate composition specified in example 1.; In examples 2 and 3 after preparing the solution, the process is then carried out as described in example 1. The invention of the method for producing citrate of alkaline chains of the formula KfeNafeH3 (C507Hy) 5- (2-4) -HaO, characterized in that either trisodium ditrate and citrate trikali are reacted with citric acid at their 2: 2: 1 molar ratio, respectively either sodium carbonate and potassium carbonate are reacted with citric acid at a molar ratio of 3: 3: 5, respectively, in a bale medium with demineralized water, while citric acid is introduced simultaneously with citrates or before or after dissolving the carbonates, and water take in - 3 to 3 times, in the case of using citrates or 0.5 - 1 times the amount by weight of citric acid, in the case of using carbonates, and the resulting homogeneous solution of the target product is sequentially cooled to 60SO c and dried. Sources of information taken into account in the examination 1.Schmidt A.W. und Planz K. .Prophylafe und Conservative Therapie der Uratscheindlathese Oer Urologe, 1965, №4, S. 159.
    [2]
    2.Kappep n. The course of organic chemistry. Ld, 1960, p. 243 (prototype un).
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    同族专利:
    公开号 | 公开日
    YU41105B|1986-12-31|
    FR2394513B1|1982-11-19|
    AU3716278A|1979-12-20|
    FR2394513A1|1979-01-12|
    NL174345C|1984-06-01|
    NL7805747A|1978-12-19|
    AU519032B2|1981-11-05|
    IT7824553D0|1978-06-14|
    SE438851B|1985-05-13|
    CA1133506A|1982-10-12|
    GR64516B|1980-04-09|
    IL54734D0|1978-07-31|
    PL118528B1|1981-10-31|
    JPS545912A|1979-01-17|
    CH634813A5|1983-02-28|
    BE868089A|1978-12-14|
    PL207657A1|1979-06-04|
    RO76941A|1981-06-22|
    SE7806684L|1978-12-17|
    PT68096A|1978-06-01|
    NL174345B|1984-01-02|
    IT1214864B|1990-01-18|
    CS208475B2|1981-09-15|
    DK270578A|1978-12-17|
    BG41657A3|1987-07-15|
    YU142778A|1982-10-31|
    IL54734A|1982-09-30|
    GB1583840A|1981-02-04|
    US4820870A|1989-04-11|
    ZA783409B|1979-07-25|
    AR219109A1|1980-07-31|
    MX4999E|1983-02-02|
    DE2727304C2|1982-12-02|
    DE2727304A1|1979-01-04|
    HK46481A|1981-09-25|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    DE968843C|1953-11-29|1958-04-03|Cassella Farbwerke Mainkur Ag|Process for the preparation of pharmacologically active magnesium salts of citric acid|
    DE1016251B|1955-01-22|1957-09-26|Adolf Christian Josef Opferman|Process for the preparation of monomagnesium dicalcium citrate for the treatment of pulmonary tuberculosis|
    US3658969A|1969-11-14|1972-04-25|Codex Sa|Pharmaceutical compositions useful in citric acid therapy|JPS6393968A|1986-10-06|1988-04-25|Fujita Corp|Underground sky parking area|
    JPH02104870A|1988-10-11|1990-04-17|Iwataro Moriyama|Parking device|
    DE4328577C2|1993-08-25|1997-09-11|Madaus Ag|Alkalicitrates and their use as pharmaceuticals|
    EP0673913B1|1994-03-23|1999-02-10|Madaus Ag|Calcium-alkali-citrate compounds and their use as medicaments|
    DE4409949C2|1994-03-23|1996-11-21|Madaus Ag|Use of calcium alkali citrates for the prophylaxis and treatment of degenerative diseases of the bone structure|
    DE4409948A1|1994-03-23|1995-09-28|Madaus Ag|New calcium alkali metal citrate salts|
    CA3041861A1|2016-10-27|2018-05-03|Stefanie A. Seixas-Mikelus|Juice beverage for prevention and treatment of renal stones|
    PL238507B1|2018-11-27|2021-08-30|Kozak Dariusz P H M Polcomm|Drill with double cutters|
    CN111116350A|2019-12-28|2020-05-08|湖南九典制药股份有限公司|Preparation method of potassium sodium hydrogen citrate|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE2727304A|DE2727304C2|1977-06-16|1977-06-16|Acid alkali citrate, its manufacture and use|
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