Preparation and medical application of ACEI (angiotensin converting enzynme inhibitor)-type berberine conjugate

The technology of a conjugate, berberine hydrochloride, is applied in blood pressure regulating products. In the field of treatment of high blood pressure, the Prism-like berberine conjugate can solve the problems of low fat solubility, poor water solubility, and malabsorption, etc.

Active Publication Date: 2016-07-06
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 poor water solubility and oral bioavailability of pril, the full play of its drug effect is limited.
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, pleil drugs and berberine have many similar pharmacological activities, they all limit their clinical use to a certain extent due to low bioavailability, so looking for a way to improve the biological activity of pleil drugs 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 ACEI (angiotensin converting enzynme inhibitor)-type berberine conjugate
  • Preparation and medical application of ACEI (angiotensin converting enzynme inhibitor)-type berberine conjugate
  • Preparation and medical application of ACEI (angiotensin converting enzynme inhibitor)-type berberine conjugate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Synthesis of Enalapril and Berberine Conjugates

[0021] Take 3.7g of berberine hydrochloride, put it into a 500ml three-neck 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 3.5g of enalapril Keep stirring at this temperature for 1-5 hours, cool down to room temperature, crystallize, filter, and dry to obtain 5.7 g of enalapril berberine conjugate with a yield of 84%.

Embodiment 2

[0023] Synthesis of Enalapril and Berberine Conjugates

[0024] Take 3.7g of berberine hydrochloride, put it into a 500ml three-neck flask, add 100ml of ethanol, adjust the pH to 7-8 with 3mol / l potassium hydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 3.7g of enalapril Keep stirring at this temperature for 1-5 hours, cool down to room temperature, crystallize, filter, and dry to obtain 6.1 g of enalapril berberine conjugate with a yield of 90%. ESI-MS (M + +H)m / zcalcdforC 20 h 18 NO 4 + 337.12found337.21; ESI-MS (M + +H)m / zcalcdforC 18 h 23 N 2 o 5 348.16found348.34.

Embodiment 3

[0026] Synthesis of imidapril and berberine conjugates

[0027] Take 3.7g of berberine hydrochloride, put it into a 500ml 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 4.3g of Midap Keep stirring at this temperature for 1-3 hours, cool down to room temperature, crystallize, filter, and dry to obtain 6.5 g of imidapril berberine conjugate with a yield of 88%. ESI-MS (M + +H)m / zcalcdforC 20 h 18 NO 4 + 337.12found337.16; ESI-MS (M + +H)m / zcalcdforC 20 h 26 N 3 o 6 405.19 found 405.27.

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PUM

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Abstract

The invention provides a preparation method of a conjugate shown as a formula (I) and application thereof serving as a drug for treating hypertension and regulating blood pressure.Pharmacological experiments find that the conjugate has drug activity of various values, especially for easiness in absorbing that ACEI (angiotensin converting enzynme inhibitor)-type drugs do not have; specifically, the conjugate presents excellent effect on regulating blood pressure of hypertensive rats in animal experiments.A main function of the conjugate is embodied in capability of blocking all angiontensins II generated through various paths from being combined with a special receptor thereof so as to weaken or block blood pressure rise effect.

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] According to the survey data in 2002, the prevalence rate of hypertension in adults over 18 years old in my country is 18.8%. It is estimated that there are about 200 million hypertensive patients in my country, and 2 out of every 10 adults suffer from high blood pressure, accounting for about 18.8% of the global high blood pressure. 1 / 5 of the total number of people with blood pressure. Among the hypertensive population in my country, the vast majority are mild to moderate hypertension (accounting for 90%), and mild hypertension accounts for more than 60%. However, the proportion of normal blood pressure (<120 / 80mmHg) in our population is less than 1 / 2. The proportion of people with normal high blood pressure in the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03C07D207/16C07K5/062A61K31/4375A61K31/401A61K38/05A61P9/12
CPCC07D207/16C07D455/03C07K5/06026
Inventor 高永好何勇封保龙
Owner HEFEI HUAFANG PHARMA SCI & TECH
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