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1. WO2020062545 - METHOD FOR PREPARING TERTIARY AMINE BASIC COMPONENTS IN RHIZOMA CORYDALIS

Publication Number WO/2020/062545
Publication Date 02.04.2020
International Application No. PCT/CN2018/118603
International Filing Date 30.11.2018
IPC
A61K 31/4375 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 36/66 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
36Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
18Magnoliophyta (angiosperms)
185Magnoliopsida (dicotyledons)
66Papaveraceae (Poppy family), e.g. bloodroot
CPC
A61K 31/4375
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 36/66
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
36Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
18Magnoliophyta (angiosperms)
185Magnoliopsida (dicotyledons)
66Papaveraceae (Poppy family), e.g. bloodroot
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
Applicants
  • 泰州医药城国科化物生物医药科技有限公司 TAIZHOU GUOKEHUAWU BIOMEDICAL TECHNOLOGIES CO., LTD [CN]/[CN]
Inventors
  • 梁鑫淼 LIANG, Xinmiao
  • 王超然 WANG, Chaoran
  • 赵耀鹏 ZHAO, Yaopeng
  • 郭秀洁 GUO, Xiujie
  • 乔健 QIAO, Jian
  • 高振华 GAO, Zhenhua
Agents
  • 南京瑞弘专利商标事务所(普通合伙) NANJING RUIHONG PATENT & TRADEMARK AGENCY (ORDINARY PARTNERSHIP)
Priority Data
201811144625.X29.09.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) METHOD FOR PREPARING TERTIARY AMINE BASIC COMPONENTS IN RHIZOMA CORYDALIS
(FR) PROCÉDÉ DE PRÉPARATION DE COMPOSANTS DE BASE D'AMINE TERTIAIRE DANS DU RHIZOMA CORYDALIS
(ZH) 一种延胡索中叔胺碱类组分的制备方法
Abstract
(EN)
Provided in the present invention is a method for preparing tertiary amine basic components in rhizoma corydalis. The method for preparing basic components provided in the present invention is: reducing berberine quaternary ammonium hydroxide in rhizoma corydalis extracts to protoberberine tertiary amine hydroxide, wherein palmatine and dehydrocorydaline, both of which are two bases with the highest content in rhizoma corydalis, are reduced to tetrahydropalmatine and corydaline respectively. Evaporating the reaction supernatant to dryness after adjusting the pH to neutral, and drying same after desalination to obtain the tertiary amine basic component, wherein the total base content is at least 50%. The preparation method has the advantages of a simple process, high efficiency, high recovery rate and low production cost, and provides good technological schemes for the development of safe, efficient and controllable rhizoma corydalis alkaloid component preparations.
(FR)
La présente invention concerne un procédé de préparation de composants de base d'amine tertiaire dans du rhizoma corydalis. Le procédé de préparation de composants de base selon la présente invention comprend : la réduction d'hydroxyde d'ammonium quaternaire de berbérine dans des extraits de rhizoma corydalis en hydroxyde d'amine tertiaire de protoberbérine, la palmatine et la déhydrocorydaline, toutes deux des bases présentant la teneur la plus élevée en rhizoma corydalis, étant réduites en tétrahydropalmatine et corydaline respectivement ; l'évaporation du surnageant réactionnel à sec après neutralisation du pH, et le séchage de celui-ci après le dessalement pour obtenir le composant de base d'amine tertiaire, la teneur totale en base étant d'au moins 50 %. Le procédé de préparation présente les avantages d'un procédé simple, d'un rendement élevé, d'un taux de récupération élevé et d'un faible coût de production, et fournit de bons procédés technologiques pour le développement de préparations de composants d'alcaloïde de rhizoma corydalis sûres, efficaces et contrôlables.
(ZH)
本发明提供了一种延胡索中叔胺碱类组分的制备方法。本发明所提供的类组分制备方法,将延胡索提取物中小檗碱类季铵碱还原为原小檗碱类叔胺碱,其中延胡索中两种含量最高的季铵碱——巴马汀和去氢紫堇碱分别被还原为延胡索乙素和延胡索甲素。反应上清液调pH至中性后蒸干,脱盐后干燥即得叔胺碱组分,其中总碱含量达到50%以上。该制备方法工艺简单,高效,回收率高,生产成本低,为"安全,有效,可控"的延胡索生物碱类组分制剂的开发提供了良好的技术方案。
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