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Compound composition of obeticholic acid and berberine and applications thereof

A kind of technology of obeticholic acid and berberine hydrochloride

Active Publication Date: 2015-12-23
BEIJING KAWIN TECH SHARE HLDG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent application No. 201380043964 discloses the C-type crystal of obeticholic acid, which clearly admits that it will cause side effects such as lowering high-density lipoprotein; and Chinese patent application No. 201510384385 discloses the chemical synthesis method of obeticholic acid , none of which involve combination medication
[0004] In addition, even in the compositions that list dozens or even hundreds of parallel drugs like the international patent applications WO2012100248 and WO2009045443, it is very difficult to select the combination of chenodeoxycholic acid and berberine, and the goose deoxycholic acid and berberine are among them. Oxycholic acid was also not revealed to be obeticholic acid

Method used

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  • Compound composition of obeticholic acid and berberine and applications thereof
  • Compound composition of obeticholic acid and berberine and applications thereof
  • Compound composition of obeticholic acid and berberine and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Drug efficacy experiment of embodiment 1 liver cirrhosis model rat

[0028] Take clean grade SD rats (body weight 180-220g) and divide them into sham operation group and model group at random. After the rats are given 10% chloral hydrate solution (300mg / kg) intraperitoneal injection anesthesia, open the abdomen along the midline of the abdomen, find And the common bile duct was exposed. In the sham operation group, only the common bile duct was separated and then the abdomen was closed. After the common bile duct was ligated at the proximal end around the hilar bile duct in the model group, the abdomen was routinely closed. Penicillin 400,000 units per mouse was injected continuously for 3 days after operation. feed.

[0029] The liver cirrhosis model rats with successful modeling were randomly divided into model group (administered only 1% methylcellulose), berberine group (administered BBR, 100mg.kg -1 .d -1 ), obeticholic acid group (administration of OCA, 10mg.kg ...

Embodiment 2

[0033] Example 2 Drug efficacy experiment on rats with abnormal liver and blood indicators caused by high-fat diet

[0034] Get SD rats and feed with basal feed for one week as the adaptation period, and then randomly divide them into 6 groups: (1) normal group (control), fed with low-fat diet; (2) high-fat diet group, fed with high-fat diet (78.85 % raw grain, 21% lard, 0.15% cholesterol) feeding; (3) BBR group, high-fat feed (same as above) feeding+berberine (gavage, 180mg / kg, qd); (4) OCA group, high-fat feed (same as above) feeding+obeticholic acid (gavage, 10mg / kg, qd); (5) OCA+BBR high-dose group, high-fat feed (same as above) feeding+obeticholic acid combined with berberine high-dose group (gavage Stomach, 10mg / kg+180mg / kg, qd); (6) OCA+BBR low-dose group, high-fat diet (same as above) feeding + obeticholic acid combined with berberine high-dose group (gastric administration, 5mg / kg+90mg / kg, qd). Correspondingly, the normal group and the high-fat diet group were intr...

Embodiment 3

[0038] Example 3 Drug efficacy experiment on liver fibrosis model mice

[0039] After one week of adaptive feeding, male C57 / B6 mice were randomly divided into normal group (Control), CCL 4 group, BBR group (administration of BBR100mg / kg), OCA group (administration of OCA10mg / kg), OCA+BBR high-dose group (10mg / kg+100mg / kg), OCA+BBR low-dose group (5mg / kg+50mg / kg). Except the normal group, all other groups were intraperitoneally injected with 10% CCl three times a week 4 2μl / g, for 4 consecutive weeks, the normal group was intraperitoneally injected with the same amount of olive oil. Since the first day of modeling, the corresponding drugs were given by intragastric administration at the same time, and the normal group and the CCL 4 Groups were given an equal volume of 1% methylcellulose. After the experiment, blood was taken to detect liver function indicators such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST); liver was taken for liver HE patholo...

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Abstract

The invention provides a pharmaceutical composition which comprises obeticholic acid or pharmaceutically acceptable salts thereof and berberine or pharmaceutically acceptable salts thereof. In addition, the invention also provides preparations involved in the pharmaceutical composition and preparation methods and applications thereof and the like.

Description

technical field [0001] The invention belongs to the technical field of medicines. Specifically, the invention relates to a compound composition, a preparation, a preparation method and an application etc. comprising obeticholic acid and berberine. technical background [0002] Obeticholic acid (OCA for short), also known as 6-ethylchenodeoxycholic acid (6-ECDCA), is a natural ligand of farnesoid derivative X receptor (FXR) and an agonist of FXR . Chinese patent application No. 201380043964 discloses the C-type crystal of obeticholic acid, which clearly admits that it will cause side effects such as lowering high-density lipoprotein; and Chinese patent application No. 201510384385 discloses the chemical synthesis method of obeticholic acid , all of which do not involve drug combination. [0003] Berberine, its hydrochloride form (Berberine Hydrochloride, referred to as BBR) is commonly known as berberine, is an important alkaloid, has a significant antibacterial effect, inc...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P1/16A61P3/06A61P3/10A61P3/04A61K31/4375
CPCA61K31/4375A61K31/575
Inventor 潘海高妍杨健
Owner BEIJING KAWIN TECH SHARE HLDG
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