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Preparation and medical application of glinides berberine coupling compound

A technology of berberine hydrochloride and compound, applied in the field of food and pharmacy, can solve the problems of limiting the full exertion of drug effect, poor absorption, low fat solubility and the like

Inactive Publication Date: 2016-06-08
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 repaglinide, the oral bioavailability is low, which limits the full play of its drug effect.
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, glinides and berberine have many similar pharmacological activities, they are all limited to a certain extent in clinical use due to low bioavailability, so looking for a biological agent to improve glinides and berberine The method of utilizing the degree 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 glinides berberine coupling compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Synthesis of Repaglinide Berberine Conjugate

[0019] Take 3.7g of berberine hydrochloride, put it into a 100ml three-necked flask, add 100ml of ethanol, adjust the pH to 7-8 with 3mol / l sodium hydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 4.5g of repaglide Nai, keep the temperature and stir for 1-2h, cool down to room temperature, crystallize, filter and dry to obtain repaglinide berberine conjugate 6.8g, yield 86%.

Embodiment 2

[0021] Synthesis of Repaglinide Berberine Conjugate

[0022] Take 3.7g of berberine hydrochloride, put it into a 100ml three-necked flask, add 150ml of ethanol, adjust the pH to 7-8 with 3mol / l sodium hydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 4.7g of Benridge Keep stirring for 1-2 hours at this temperature, cool down to room temperature, crystallize, filter, and dry to obtain 7.1 g of repaglinide berberine conjugate, with a yield of 90%.

Embodiment 3

[0024] Synthesis of Repaglinide Berberine Conjugate

[0025] Take 3.7g of berberine hydrochloride, put it into a 100ml three-necked flask, add 100ml of ethanol, adjust the pH to 7-8 with 3mol / l sodium hydroxide, raise the temperature to 60-70°C, stir to dissolve, and then add 5.0g of repaglide Nai, keep the temperature and stir for 1-2h, cool down to room temperature, crystallize, filter, and dry to obtain repaglinide berberine conjugate 7.1g, yield 91%. ESI-MS (M + +H)m / zcalcdforC 20 h 16 NO 4 + 337.13found337.22; ESI-MS (M + +H)m / zcalcdforC 27 h 35 N 2 o 4 - 451.26found451.25.

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Abstract

The invention discloses preparation and medical application of a glinides berberine coupling compound, and belongs to the field of biological medicine. A glinides derivative and berberine are chemically synthesized into salt, and the problems that floxacin derivative medicine is poor in water solubility and low in oral administration bioavailability, and consequently full play of the medicine effect of floxacin derivative medicine is limited are solved. The problems that berberine hydrochloride is small in water solubility, smaller in lipid solubility and poor in gastrointestinal tract absorption, consequently the oral administration bioavailability of berberine hydrochloride is low, and the whole body treatment effect of berberine hydrochloride is influenced are solved. The derivatives show an excellent effect on regulating the blood glucose of 2-type diabetes rats in animal tests. The glinides berberine coupling compound mainly has the effects of being capable of improving oral glucose tolerance, promoting insulin secretion, improving insulin resistance and the like.

Description

technical field [0001] The invention relates to the technical field of food and pharmacy, in particular to the application of linide-type berberine conjugates in the preparation of products for preventing or treating diabetes, hyperlipidemia and related diseases or symptoms. Background technique [0002] At present, the number of diabetic patients in our country is increasing day by day. Among the urban, township and wealthy rural population, the diabetic patients over the age of 20 have reached 11%, and another 15% have impaired blood sugar regulation. The sum of the two accounts for about 1% of the above-mentioned population. / 4. From 2006 to 2007, the global sales of repaglinide alone was 450 million US dollars. It can be seen that the research and development of hypoglycemic drugs has great social benefits and market prospects. Linide hypoglycemic drugs are a class of synthetic non-sulfonylurea insulin secretagogues (Non-sulfonylureas, NSUR), which have positive signific...

Claims

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Application Information

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IPC IPC(8): C07D491/147A61P3/10
CPCC07D491/147
Inventor 高永好何勇吴宗好封保龙
Owner HEFEI HUAFANG PHARMA SCI & TECH
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