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Preparation and medical application of diacerein berberine conjugate

A technology of berberine hydrochloride and conjugates, applied in the field of food and pharmaceuticals, can solve the problems of low water solubility, malabsorption, poor water solubility of diacetyl rhein, etc., and achieve the effect of regulating blood sugar and excellent blood sugar

Inactive Publication Date: 2016-06-22
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, due to the poor water solubility of diacetylrhein, the oral bioavailability is low, which limits the full play of its efficacy.
However, berberine hydrochloride has very little water solubility, even less fat solubility, and poor absorption in the gastrointestinal tract, resulting in low oral bioavailability, which affects its systemic therapeutic effect.
Although, diacetyl rhein drug, berberine has many similar pharmacological activities, but because of the low bioavailability, the clinical use is limited to a certain extent, so looking for a way to improve the diacetyl rhein drug and berberine The method of bioavailability and exerting the synergistic effect of the two will have very important clinical significance

Method used

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  • Preparation and medical application of diacerein berberine conjugate
  • Preparation and medical application of diacerein berberine conjugate
  • Preparation and medical application of diacerein berberine conjugate

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Synthesis of berberine conjugates of diacetylrhein

[0021] Take 3.7g of berberine hydrochloride, add it to a 500ml three-necked flask, add 100ml of 50% ethanol, adjust the pH to 7-8 with 3mol / l sodium hydroxide, heat up to 60-70°C, stir to dissolve, then add 3.7g dihydrochloride For acetylrhein, keep stirring at this temperature for 1-5 hours, cool down to room temperature, crystallize, filter, and dry to obtain 5.8 g of berberine diacetylrhein conjugate, with a yield of 82%.

Embodiment 2

[0023] Synthesis of berberine conjugates of diacetylrhein

[0024] Take 3.7g of berberine hydrochloride, put it into a 500ml three-necked flask, add 100ml of 60% ethanol, adjust the pH to 7-8 with 3mol / l potassium hydroxide, heat up to 60-70°C, stir to dissolve, then add 3.9g of dihydrochloride For acetylrhein, keep stirring at this temperature for 1-5 hours, cool down to room temperature, crystallize, filter, and dry to obtain 6.1 g of berberine diacetylrhein with a yield of 87%.

Embodiment 3

[0026] Synthesis of berberine conjugates of diacetylrhein

[0027] Take 3.7g of berberine hydrochloride, put it into a 500ml three-neck flask, add 100ml of 60% ethanol, adjust the pH to 7-8 with 3mol / l potassium carbonate, heat up to 60-70°C, stir to dissolve, then add 4.0g of diacetyl For rhein, keep stirring at this temperature for 1-5 hours, cool down to room temperature, crystallize, filter, and dry to obtain 6.3 g of berberine diacetylrhein conjugate with a yield of 89%.

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PUM

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Abstract

The invention provides a preparation method of a conjugate in formula (I) and application thereof in drugs for treating hyperglycemia, hyperlipidemia, obesity, bacterial infection, peptic ulcers, arthritis, heart failure, arrhythmia, platelet aggregation, high blood pressure and the like. In pharmacology experiments, it is found that the conjugate has drug activity of various values, especially, diacerein drugs do not have the performance that the conjugate is easily absorbed, and specifically, the conjugate has excellent mouse blood sugar adjusting and bacterial infection adjusting effects in animal experiments.

Description

technical field [0001] The invention relates to the technical field of food and pharmacy, in particular to the application of a Puril-like berberine conjugate in products for treating hypertension and regulating blood pressure. Background technique [0002] Berberine BBR (Berberine, BBR) is the main active ingredient of Coptis chinensis, and the content of BBR in Coptis chinensis is the highest, accounting for 5.2-7.69%. Coptis chinensis is bitter in taste and has the effects of clearing heat, detoxifying, purging fire and curing diabetes. In the past, it was believed that it was not easy to absorb after oral administration, and it was effective for intestinal infections caused by Shigella, Escherichia coli, Staphylococcus aureus, conjunctivitis, suppurative otitis media, etc. It is mainly used for the treatment of intestinal infections in clinical practice. With the deepening of research, in recent years, it has been found that it has pharmacological effects such as antiar...

Claims

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Application Information

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IPC IPC(8): C07D455/03C07C67/28C07C69/16A61K31/4375A61K31/22A61P31/04A61P3/10A61P3/04A61P1/04A61P9/04A61P9/06A61P7/02A61P9/12
CPCC07D455/03
Inventor 高永好何勇封保龙
Owner HEFEI HUAFANG PHARMA SCI & TECH
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