专利摘要:
A method of production of the active substance of an antilithiatic medicament, wherein ground seeds of the genus Dolichos are extracted with polar solvents, then the extract is contingently submitted to an acid hydrolysis, whereafter the acid hydrolyzate is contingently extracted with solvents immiscible with water, and then it is neutralized and contingently, is described.
公开号:SU1220563A3
申请号:SU782574202
申请日:1978-02-07
公开日:1986-03-23
发明作者:Густовски Влодзимеж;Коцур Марян;К.Аталь Ханд;Оркишэвска Алиця;Ольшэвски Рышард;Вроциньски Тадэуш
申请人:Польска Акадэмия Наук (Инопредприятие);Институт Хэмии Органичнэй (Инопредприятие);
IPC主号:
专利说明:

t
The invention relates to medicine, in particular, to methods for producing an agent active in the treatment of urinary tract lithiasis.
The purpose of the invention is the elimination of side effects and expansion of the spectrum of action.
Example 1.100 g of ground seeds of fodder beans Dolichos bif lorus, sifted through a sieve with openings of 0.65 mm, is extruded with ethyl ether into a Soxhlet apparatus for 3 hours. The halfway ether extract is dried over magnesium sulfate and then evaporated to 2 g of oily yellow product were obtained. The extract obtained is weighed into 100 g of distilled water and, in this form, is introduced into rats to which phosphate stones of human origin were introduced into the urinary bladder. A strong effect was established, inhibiting stone growth compared with the control group.
EXAMPLE 2. Ground seeds of Dolichos beans in an amount of 100 g are sieved through a sieve with openings of 0.65 mm and subjected to extraction with 1000 ml of a mixture of methyl alcohol and water in a volume ratio of 1: 1 at the boiling point of the mixture for 3 hours. Then the heating is interrupted and the mixture is set aside for 15 hours, after which the extract is filtered and the alcohol is evaporated under reduced pressure at 50-60 ° C, and the residue is added with water to the same volume. The aqueous solution is acidified with hydrochloric acid to a 3% solution. The solution is then heated at so C for 1 hour and set aside to cool. Osadora filtered. A clear, acidic, cherry-tea color hydrolyzate is obtained with a pH of 1-1.2, which is neutralized to pH 5.5 with the help of a concentrated solution of sodium hydroxide WG-1I. The precipitate was filtered and the clear solution was stabilized by addition of 0.02 g of inhibitor. The hydrolyzate thus obtained is then processed in the form of a pharmaceutical agent.
Example J3. The process is carried out as in Example 2, however, a mixture of ethyl alcohol and ethanol is admixed to extract ground bean seeds.

32
WATER In a 1: 1 ratio. The resulting hydrolyzate is evaporated to 1/4 of the volume.
Example 4. The process is carried out as in Example 2, using 1000 ml of water for extracting ground seeds of beans. The resulting hydrolysis is evaporated to dryness.
Example 5. The process is carried out according to Example 2, however, phosphoric acid is used for acid hydrolysis. The resulting hydrochloride is evaporated to 2/3 volume.
Example 6. The process is carried out according to Example 4, the resulting acidic hydrolyzate is extracted with ether, and then the ether extract is processed as Example 1.
Example 7, 100 g of ground dichose hIvIH Indian beans Dolichos, sifted through a 0.65 mm sieve, was extracted with 500 ml of ethyl acetate at ambient temperature for 7 days. The resultant extract is worked-up as in Example 1 or else ethyl acetate is evaporated under reduced pressure, and the residue is added with water to the same volume. The aqueous solution is acidified with 25% citric acid to obtain a 10% aqueous solution and heated to boiling with maintaining this temperature for 2 hours. After cooling, 100 g of sugar and 0.2 g of anise oil are added to the acidic hydrolyzate. thus, the form of the pharmaceutical preparation is prepared, or it is subjected to further processing. For this purpose, the acidic hydrolyzate is extracted with 500 ml of chloroform. After evaporation of chloroform, the residue is diluted with 300 ml of water and neutralized with a concentrated solution of potassium carbonate to a pH of 6. The resulting solution is processed into the desired pharmaceutical form.
Example 8. Ground seeds of Dolichos bean in an amount of 100 g are sieved through a sieve with openings of 0.65 mm and extracted with 500 ml of a mixture of solvents acetone - butyl alcohol, in a ratio of 1: 1 at ambient temperature. The resulting extract is filtered and the solvents are evaporated. The residue is diluted with 500 ml of water and processed into the desired form of pharmaceutical agent.
3 12205634
or the aqueous solution is acidified and the precipitate is filtered, and about
15 ml of a mixture of milk and propionic-clear solution stabilize 0.15 g
acids (weight ratio 60:40) of the oxybenzoic acid ester are left at room temperature. Thus obtained hydra for 13 days. The precipitated lysate of the filter lysate is then processed to require, and the acidic hydrolyzate of the pharmaceutical form is extracted with ethyl acetate. Benefits
the extract is concentrated under vacuum. Example 9. The process is carried out by drying, and then diluted in 500 ml of Example 8, the resulting extract
water and alkalinized usingto acid hydrolyzate is extracted
calcium hydroxide to pH 5.5. Ammonium hydroxide.
权利要求:
Claims (12)
[1]
1. METHOD FOR PRODUCING A LITHIOLYTIC ACTION PRODUCT, including extraction of plant materials with a polar solvent, characterized in that, in order to eliminate side effects and expand the spectrum of action, ground beans of Dolichos species are used as raw materials, and then the resulting extract is extracted with acid , re-extracted with solvents not miscible with water, then neutralized and concentrated.
[2]
2. The method of ποπ.Ι, with the fact that esters, esters, ketones, alcohols, water or a mixture thereof are used as polar solvents
[3]
3. The method of pop. 2, the difference between join and th is that they use ethyl ether, ethyl acetate, acetone, and alcohols with 1–5 carbon atoms.
[4]
4. The method according to PP. 2 and 3, characterized in that the polar organic solvents are used in a mixture with water at any ratio.
[5]
5. The method according to p. 1, about t. L and h, and that with the fact that the extraction is carried out at a temperature from room temperature to the boiling point of the solvent.
[6]
6. The method of pop. 1, characterized in that the treatment of the extract is carried out with a mineral or organic acid in a concentration of 0.5-25 ^, preferably 1 ~ 5 £.
[7]
7. The method according to PP. 1 or 6, characterized in that hydrochloric, phosphoric, acetic, perchloric, citric, lactic acids or mixtures thereof are used as the acid. ©
[8]
8. The method ποπ.Ι, ο τ l and h is that the acid treatment is carried out at a temperature from room temperature to the boiling point of the reaction mixture.
[9]
9. The method according to PP. 1 or 6, characterized in that the acid treatment is carried out at room temperature for 0.5-14 days, and at elevated temperatures for 0.5-8 hours.
[10]
10. The method according to p. ^ Characterized in that for repeated extraction using ethyl ether or ethyl acetate.
[11]
11. The method according to p. ^ Characterized in that the neutralization is carried out with a concentrated solution of hydroxides of alkali metals or oxides of alkaline earth metals or ammonium.
[12]
12. The method according to PP. 1 or 11, characterized in that they use sodium hydroxide or potassium hydroxide or sodium or potassium carbonate as a neutralizer.
SU „„ 1220563
1 12
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同族专利:
公开号 | 公开日
SE442952B|1986-02-10|
AT363175B|1981-07-10|
DD133897A5|1979-01-31|
SE7801520L|1978-08-10|
NL7801359A|1978-08-11|
JPS53121917A|1978-10-24|
DE2805224B2|1980-11-20|
US4156721A|1979-05-29|
DE2805224C3|1981-07-30|
ATA79978A|1980-12-15|
CS194835B2|1979-12-31|
ES467204A1|1978-11-16|
FR2380029A1|1978-09-08|
PL115321B1|1981-03-31|
PL195886A1|1979-09-10|
FR2380029B1|1980-08-29|
DE2805224A1|1978-08-10|
IN149699B|1982-03-20|
BE863522A|1978-05-16|
CH633715A5|1982-12-31|
GB1546360A|1979-05-23|
引用文献:
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JP2548111Y2|1991-12-06|1997-09-17|東京瓦斯株式会社|Protective sheet for piping|
JPH1129490A|1997-06-20|1999-02-02|Gem Energy Ind Ltd|Antidiabetic therapeutic agent of medicinal herb and its production|
EP0894499A1|1997-08-01|1999-02-03|Gem Energy Industry Limited|Herbal anti-diabetic composition|
US6866651B2|2002-03-20|2005-03-15|Corazon Technologies, Inc.|Methods and devices for the in situ dissolution of renal calculi|
EP2218455A1|2009-02-07|2010-08-18|Cognis IP Management GmbH|Dolichos biflorus extract for use in therapeutic skin treatment|
EP2216074A1|2009-02-07|2010-08-11|Cognis IP Management GmbH|Dolichos biflorus extract for use in cosmetic skin treatment|
法律状态:
优先权:
申请号 | 申请日 | 专利标题
PL1977195886A|PL115321B1|1977-02-09|1977-02-09|Method of obtaining the active component of an anticalculic remedy|
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