SU786856A3 - Method of preparing escine - Google Patents

Method of preparing escine Download PDF

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Publication number
SU786856A3
SU786856A3 SU762377644A SU2377644A SU786856A3 SU 786856 A3 SU786856 A3 SU 786856A3 SU 762377644 A SU762377644 A SU 762377644A SU 2377644 A SU2377644 A SU 2377644A SU 786856 A3 SU786856 A3 SU 786856A3
Authority
SU
USSR - Soviet Union
Prior art keywords
escin
resulting
seeds
cation exchanger
concentrated
Prior art date
Application number
SU762377644A
Other languages
Russian (ru)
Inventor
Мадаус Рольф
Original Assignee
Др. Мадаус И Ко (Фирма)
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Application filed by Др. Мадаус И Ко (Фирма) filed Critical Др. Мадаус И Ко (Фирма)
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Publication of SU786856A3 publication Critical patent/SU786856A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/24Condensed ring systems having three or more rings
    • C07H15/256Polyterpene radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Rheumatology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pain & Pain Management (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

A method is provided for readily recovering water insoluble crystalline escin as the free acid from seeds of Aesculus hippocastanum, which comprises extracting crushed Aesculus hippocastanum seeds with an organic, water-miscible solvent, preferably a lower aliphatic alcohol,contacting the resulting extraction liquid with a cation exchanger in its H+ form, separating the resulting eluate from said cation exchanger, concentrating the eluate, for example by distillation, and separating the resulting crystalline deposit of escinic acid, for example by centrifuging or other filtering technique the escin is useful in medicine in view of its antiphlogistic action.

Description

Изобретение относитс  к фармацевтической промышленности и касаетс  получений фармацевтически активных веществ. Известен способ получени  эсцина путем экстракции сем н каштана конского (AescuEus hippocastanum) водным растворе низших спиртов, обработки экстракта на катионите с последующим сгущением его, очисткой и вьщеле нием целевого продукта flj. Однако известный способ не обеспечивает высокой активности целевого продукта. Целью изобретени   вл етс  повыше . ние активности целевого продукта. Эта цель достигаетс  тем, что после обработки экстракта на катион те его сгущают до соотношени  10:4, затем высушивают под вакуумом при , раствор ют при нагревании в 10-кратном количестве метанола или этанола с добавлением 5% активированного угл , далее фильтруют, сгущ ют до половины объема, добавл ют двухкратное количество деминерализо ванной воды с температурой , по лученный раствор охлаждают до комнатной температуры и после высушивани  обрабатывают триэтаноламином. Эсцин получают из AescuBus hippocas ta num. Способ включает экстракцию измельченных сем н AescuEus hippocastanum смесью воды с метанолом или этанолом, содержащей 65 об.% спирта, отделение экстракционного раствора, обработку его кислым катионитом до величины рН стекающего раствора, равной рН 3,5-3,8, сгущение раствора, взаимодействие получаемого кристаллического продукта с основанием в среде растворител  и выделение эсцината , за счет того, что сгущение раствора ведут в соотношении 10:4, получаемый сырой эсцин сушат в ва- . кууме при , раствор ют в 10-кратном количестве метанола или этанола, при добавке 5%, в пересчете на сырой эсцин, порошкообразного активированного угл , нагревают с обратным холодильником, фильтруют, раствор сгущают до половины, добавл ют двойное количество деминерализованной воды с температурой , раствор довод т до комнатной температуры и получаемый кристаллический продукт сушат с последующим взаитиодействием с триэтаноламином и выделением триэтаиоламинового эсцината .The invention relates to the pharmaceutical industry and relates to the preparation of pharmaceutically active substances. A known method of producing escin by extracting horse chestnut seeds (AescuEus hippocastanum) with an aqueous solution of lower alcohols, treating the extract on a cation resin, followed by thickening, purification and extension of the desired product flj. However, the known method does not provide a high activity of the target product. The aim of the invention is higher. the activity of the target product. This goal is achieved by the fact that after treating the extract with a cation, it is concentrated to a ratio of 10: 4, then dried under vacuum, dissolved by heating in 10 times the amount of methanol or ethanol with the addition of 5% activated carbon, then filtered, concentrated to half the volume, add twice the amount of demineralization of bath water with temperature, the resulting solution is cooled to room temperature and, after drying, treated with triethanolamine. Escine is obtained from AescuBus hippocas ta num. The method involves extraction of crushed seeds of AescuEus hippocastanum with a mixture of water with methanol or ethanol containing 65% by volume of alcohol, separating the extraction solution, treating it with an acidic cation exchanger to a pH value of flowing down solution equal to pH 3.5-3.8, thickening the solution, reacting the obtained crystalline product with a base in the medium of a solvent and the separation of the escinate, due to the fact that the concentration of the solution is carried out in a ratio of 10: 4, the resulting crude escin is dried in va-. when dissolved in 10-fold amount of methanol or ethanol, with the addition of 5%, in terms of crude escin, powdered activated carbon, heated under reflux, filtered, the solution is thickened to half, add double the amount of demineralized water with a temperature the solution is brought to room temperature and the resulting crystalline product is dried, followed by a mutual interaction with triethanolamine and isolation of the triethyolamine scinate.

Claims (1)

Формула изобретенияClaim Способ получения эсцина путем экстракции семян каштана конского § (AescuE^s hippocastanum) водным раствором низших спиртов, обработки 35 экстракта на катионите с последующим сгущением его очисткой и выделением целевого продукта, отличающийся тем, что, с целью повышения активности целевого продукта, после обработки экстракта на катионите его сгущают до соотношения 10:4, затем высушивают под вакуумом при 80°С, растворяют при нагревании в 10-кратном количестве метанола или этанола с добавлением 5% активированного угля, 45 далее фильтруют, сгущают до половины объема, добавляют двухкратное количество деминерализованной воды с температурой 90®С, полученный раствор охлаждают до комнатной температуры и по,сле высушивания обрабатывают три этаноламином.A method of producing escin by extraction of horse chestnut seeds § (AescuE ^ s hippocastanum) with an aqueous solution of lower alcohols, treatment of the extract 35 with cation exchange resin, followed by thickening it by purification and isolation of the target product, characterized in that, in order to increase the activity of the target product, after processing the extract it is concentrated on a cation exchanger to a ratio of 10: 4, then dried under vacuum at 80 ° C, dissolved by heating in a 10-fold amount of methanol or ethanol with the addition of 5% activated carbon, 45 is further filtered, concentrated to half s volume, add a double amount of demineralized water with a temperature of 90 ° C, the resulting solution is cooled to room temperature and after drying, treated with three ethanolamine.
SU762377644A 1975-07-11 1976-07-07 Method of preparing escine SU786856A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE2530941A DE2530941C2 (en) 1975-07-11 1975-07-11 Process for the production of crystalline aescin and for the production of certain aescin salts as well as triethanolammonium aescinate and medicaments containing this salt

Publications (1)

Publication Number Publication Date
SU786856A3 true SU786856A3 (en) 1980-12-07

Family

ID=5951217

Family Applications (1)

Application Number Title Priority Date Filing Date
SU762377644A SU786856A3 (en) 1975-07-11 1976-07-07 Method of preparing escine

Country Status (21)

Country Link
JP (1) JPS5234913A (en)
AR (1) AR210498A1 (en)
AU (1) AU510202B2 (en)
BE (1) BE844052A (en)
BG (1) BG27378A3 (en)
CA (1) CA1049497A (en)
CS (1) CS193077B2 (en)
DE (1) DE2530941C2 (en)
ES (1) ES449747A1 (en)
FI (1) FI63418C (en)
FR (1) FR2316962A1 (en)
GB (1) GB1551387A (en)
HK (1) HK33781A (en)
HU (1) HU175394B (en)
PH (1) PH13088A (en)
PL (1) PL99027B1 (en)
PT (1) PT65301B (en)
RO (1) RO71026A (en)
SU (1) SU786856A3 (en)
YU (1) YU39215B (en)
ZA (1) ZA764064B (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003080636A1 (en) * 2002-03-25 2003-10-02 Council Of Scientific And Industrial Research A simple process for obtaining beta-aescin from indian horse chestnut (aesculus indica)

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1095989B (en) * 1959-03-11 1960-12-29 Madaus & Co Dr Process for obtaining a crystallized acidic saponin from the seeds of the horse chestnut
FR1267224A (en) * 1960-06-07 1961-07-21 Madaus & Co Dr Process for the preparation of crystallized acid saponin from horse chestnuts
DE1667884B2 (en) * 1968-01-20 1976-09-30 Knoll Ag, Chemische Fabriken, 6700 Ludwigshafen PROCESS FOR THE EXTRACTION OF PURE AESCINE
DE2118916A1 (en) * 1971-04-19 1972-11-09 Schwabe, Willmar, Dr., 7500 Karlsruhe-Durlach Water-soluble acid saponin mixts prodn - by extraction of horse-chestnuts and complex formation with (alkyl)benzene
YU37063B (en) * 1971-12-06 1984-08-31 Lek Tovarna Farmacevtskih Process for preparing x-ray amorphous water-sulubleascin

Also Published As

Publication number Publication date
GB1551387A (en) 1979-08-30
JPS5539560B2 (en) 1980-10-13
JPS5234913A (en) 1977-03-17
FI63418C (en) 1983-06-10
PT65301B (en) 1977-12-13
RO71026A (en) 1981-09-24
DE2530941A1 (en) 1977-01-27
YU166976A (en) 1982-08-31
AR210498A1 (en) 1977-08-15
ES449747A1 (en) 1977-08-16
FI761957A (en) 1977-01-12
BG27378A3 (en) 1979-10-12
DE2530941C2 (en) 1991-10-10
ZA764064B (en) 1977-07-27
CS193077B2 (en) 1979-09-17
HU175394B (en) 1980-07-28
FR2316962B1 (en) 1979-03-02
HK33781A (en) 1981-07-24
FR2316962A1 (en) 1977-02-04
YU39215B (en) 1984-08-31
CA1049497A (en) 1979-02-27
BE844052A (en) 1977-01-12
PH13088A (en) 1979-11-23
FI63418B (en) 1983-02-28
AU1573076A (en) 1978-01-12
PL99027B1 (en) 1978-06-30
PT65301A (en) 1976-07-01
AU510202B2 (en) 1980-06-12

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