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Capillary wormwood herb triynoic acid compound, pharmaceutical composition thereof and application thereof

A compound and composition technology, applied in the separation/purification of carboxylic acid compounds, active ingredients of anhydride/acid/halide, chemical instruments and methods, etc., can solve the application report of drugs for hepatitis B virus without compound pharmaceutical composition , Few studies on anti-HBV activity, and no reports of pharmaceutical compositions

Active Publication Date: 2018-09-14
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the reports on the activities of these compounds in the existing literature mainly focus on protecting the liver and promoting choleresis, and there are few studies on their anti-HBV activities. Compounds, triterpenes, flavonoids, lignin and phenolic acids have certain in vitro anti-HBV activity (Zhao Y., et al. Fitoterapia.2014, 95, 187-193.; Zhao Y., et al. J. Ethnopharmacol. -154.)
[0004] So far, there are no compounds 3S-hydroxyundeca-5,7,9-triynoic acid (S-3-hydroxyundeca-5,7,9-triynoic acid, 1) and 3S-hydroxyundeca- -5,7,9-triynoic acid 3-O-β-D-glucopyranoside (3S-Hydroxyndeca-5,7,9-triynoic acid 3-O-β-D-glucopyranoside, 2) There is no report on the pharmaceutical composition of compound 1 or / and 2 as active ingredients, and there is no report on the application of compound 1 or / and 2 pharmaceutical composition in the preparation or treatment of hepatitis B drugs

Method used

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  • Capillary wormwood herb triynoic acid compound, pharmaceutical composition thereof and application thereof
  • Capillary wormwood herb triynoic acid compound, pharmaceutical composition thereof and application thereof
  • Capillary wormwood herb triynoic acid compound, pharmaceutical composition thereof and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Preparation of Compounds 1 and 2:

[0055] Extraction and separation of compounds 1 and 2:

[0056] Take the dried whole herb of Artemisia capriculum or Artemisia chinensis, crush it, and extract twice with 90% ethanol under reflux, each time for 3 hours, combine the ethanol extracts, recover the ethanol under reduced pressure to obtain the extract. The extract is dissolved and adsorbed on silica gel with 80% ethanol, placed at room temperature to evaporate the solvent, ground and sieved, and subjected to silica gel column chromatography, using 9:1:0, 9:1:0.1, 8:2:0.2, 6: 4:0.4 chloroform-methanol-water gradient elution, to obtain 5 components A-E, component B was prepared by MCI CHP-20Pgel column medium pressure, 20:80 to 80:20 methanol-water gradient elution, to obtain 4 Fractions B-1~B-4, B-3 were eluted with 9:1 ethyl acetate-methanol through silica gel column chromatography to obtain two fractions B-3-1 and B-3-2, B-3-2 via Rp-C 18 The column was prepared under ...

Embodiment 2

[0083] Compound Combination Pharmaceutical Form - Tablet:

[0084] Compound 1 or / and 2 of the present invention is used as the preparation of the drug combination tablet of active ingredient: use compound 1 or / and 2 as drug active ingredient, use the excipient described in Table 3 as the adjuvant component of preparation combination drug tablet, Tablet samples containing 5 to 60 mg of the pharmaceutical ingredients of compound 1 or / and 2 were made according to the ratio. Table 3 shows the formula ratio of common tablets:

[0085] Table 3 The raw material and adjuvant formula of compound 1 or / and 2 combination medicine tablet of the present invention

[0086]

[0087]

[0088] The method of preparing a certain amount of compound 1 or / and 2 with excipients and auxiliary materials into tablet preparations of different doses is to uniformly mix several excipients and auxiliary materials with the raw material drug, and add 1% hydroxymethylcellulose sodium solution in an appro...

Embodiment 3

[0090] Compound Combination Pharmaceutical Form - Capsules:

[0091] Preparation of pharmaceutical combination capsule preparations containing compound 1 or / and 2 as active ingredients: use compound 1 or / and 2 samples as pharmaceutical active ingredients, use several excipients in the table as excipients for preparing combination drug capsules, according to the proportion Proportioning is made into capsule preparations containing 5-50 mg of the pharmaceutical ingredients of Compound 1 or / and 2 in each capsule, and Table 4 provides the formula ratio of common capsule preparations:

[0092] Table 4 The bulk drug and adjuvant formula of the compound drug capsule preparation

[0093]

[0094] The method for preparing a certain amount of compound 1 or / and 2 samples and excipients and auxiliary materials into capsule preparations is: mix several excipients and auxiliary materials with compound 1 or / and 2 evenly, add 1% hydroxymethyl cellulose Appropriate amount of sodium solutio...

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PUM

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Abstract

The invention provides two kinds of capillary wormwood herb triynoic acid compound of S-3-hydroxyundeca-5,7,9-triynoic acid, 1 and 3S-Hydroxyundeca-5,7,9-triynoic acid 3-O-beta-D-glucopyranoside, 2 shown in a structural formula (I), pharmaceutical composition prepared from the treating effective amount of compound 1 and / or 2 and a pharmaceutical carrier or polybutene, preparation methods of the compound 1 and / or 2 and the pharmaceutical composition of the compound 1 and / or 2 and application thereof in preparing human disease treating medicine and especially in preparing viral hepatitis B resisting medicine.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to two new triynoic acid compounds 1 and 2, a pharmaceutical composition for treating viral hepatitis B with compound 1 or / and 2 as active ingredients, their preparation method, and their use in pharmacy Application, especially the application in the preparation of anti-hepatitis B drugs. Background technique: [0002] Hepatitis B caused by hepatitis B virus (HBV) is a serious infectious disease affecting human health. In particular, chronic hepatitis B (CHB) can be carried for a long time and is the main cause of liver cirrhosis and liver cancer. According to World Health Organization (WHO) statistics, there are 2 billion HBV carriers in the world, of which about 350 million are CHB patients; as a high-incidence area, China has about 120 million HBV carriers, and more than 30 million CHB patients (Lin Yonghuan. Hepatitis B Prevention and Treatment [M]. Beijing: Sci...

Claims

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Application Information

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IPC IPC(8): C07C59/42C07C51/42C07C51/47C07H15/10C07H1/08A61K31/20A61K31/7028A61P31/20
CPCA61P31/20C07C51/42C07C51/47C07C59/42C07H1/08C07H15/10
Inventor 陈纪军耿长安黄晓燕马云保张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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