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1. WO2017133465 - BAICALIN MAGNESIUM, PREPARATION METHOD THEREOF AND APPLICATION OF SAME

Publication Number WO/2017/133465
Publication Date 10.08.2017
International Application No. PCT/CN2017/071616
International Filing Date 19.01.2017
IPC
C07H 23/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
23Compounds containing boron, silicon, or a metal, e.g. chelates, vitamin B12
C07H 1/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
A61K 31/7048 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7048having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61P 1/16 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 9/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 3/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
CPC
A61K 31/7048
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7048having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin ; digitoxin or digoxin
A61P 29/02
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)
02without antiinflammatory effect
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07H 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
C07H 1/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
06Separation; Purification
08from natural products
Applicants
  • 承德医学院 CHENGDE MEDICAL COLLEGE [CN]/[CN]
Inventors
  • 刘翠哲 LIU, Cuizhe
  • 王志轩 WANG, Zhixuan
  • 苗策禹 MIAO, Ceyu
  • 刘丽艳 LIU, Liyan
  • 薛禾菲 XUE, Hefei
  • 刘喜纲 LIU, Xigang
  • 杜闻杉 DU, Wenshan
  • 刘一鑫 LIU, Yixin
  • 张琳 ZHANG, Lin
  • 毛晓霞 MAO, Xiaoxia
  • 刘进军 LIU, Jinjun
  • 赵桂琴 ZHAO, Guiqin
Agents
  • 北京君智知识产权代理事务所(普通合伙) BEIJING JUNZHI INTELLECTUAL PROPERTY AGENCY (G. P.)
Priority Data
201610068926.301.02.2016CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) BAICALIN MAGNESIUM, PREPARATION METHOD THEREOF AND APPLICATION OF SAME
(FR) MAGNÉSIUM DE BAÏCALINE, SON PROCÉDÉ DE PRÉPARATION ET SON APPLICATION
(ZH) 一种黄芩苷镁化合物及其制备方法与它的用途
Abstract
(EN) The present invention relates to a baicalin magnesium and further relates to a preparation method and extraction method of the baicalin magnesium. The preparation method comprises the steps of preparing a suspension of a baicalin, preparing a suspension containing a magnesium ion, reacting, and drying. The extraction method comprises the steps of pre-processing with a macroporous adsorption resin, extracting, adsorbing and eluting, concentrating and drying, and purifying. The baicalin magnesium preparation restores the baicalin to an original form found in the Scutellaria baicalensis plant, and can be used as a substitute for the baicalin in pharmaceutical applications. Compared with the baicalin, the baicalin magnesium has greatly increased solubility, faster oral absorption rate and higher bioavailability. The baicalin magnesium can also be easily formulated as a water-soluble agent or powder agent for injection. Pharmacological experiments showed that the baicalin magnesium is more pharmacologically active than baicalin.
(FR) La présente invention concerne un magnésium de baïcaline et concerne en outre un procédé de préparation et un procédé d'extraction de magnésium de baïcaline. Le procédé de préparation comprend les étapes de préparation d'une suspension d'une baïcaline, la préparation d'une suspension contenant un ion magnésium, la réaction, et le séchage. Le procédé d'extraction comprend les étapes de prétraitement avec une résine d'adsorption macroporeuse, l'extraction, l'adsorption et l'élution, la concentration et le séchage, et la purification. La préparation de magnésium de baïcaline restaure la baïcaline sous une forme d'origine découverte dans la plante Scutellaria baicalensis, et peut être utilisée comme substitut à la baïcaline dans les applications pharmaceutiques. Comparé à la baïcaline, le magnésium de baïcaline présente une solubilité grandement améliorée, une vitesse d'absorption par voie orale plus rapide et une biodisponibilité plus grande. Le magnésium de baïcaline peut également être facilement formulé comme agent soluble dans l'eau ou agent pulvérulent pour injection. Des expérimentations pharmacologiques montraient que le magnésium de baïcaline est plus pharmacologiquement actif que la baïcaline.
(ZH) 一种黄芩苷镁化合物,还涉及黄芩苷镁化合物制备方法和提取方法。所述制备方法包括制备黄芩苷混悬液、制备含镁离子混悬液、反应与干燥等步骤;所述提取方法包括大孔吸附树脂预处理、提取、吸附与洗脱、浓缩与干燥、纯化等步骤。制备黄芩苷镁还原了黄芩苷在黄芩中的存在方式,可以代替黄芩苷入药。该黄芩苷镁化合物相比黄芩苷溶解度大大提高,口服吸收速度比黄芩苷快,生物利用度比黄芩苷高,还可以非常方便制成水溶性注射剂或粉针剂。药理实验表明,所述的黄芩苷镁的药理活性优于黄芩苷。
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