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Preparation method and medical application of berberine hydrochloride conjugate
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A technology of berberine hydrochloride and acid compound, applied in the field of food and pharmacy, can solve the problems of low oral bioavailability, low fat solubility, poor absorption and the like
Inactive Publication Date: 2016-07-06
HEFEI HUAFANG PHARMA SCI & TECH
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[0004] However, due to the poor water solubility of niacin, the oral bioavailability is not high, which limits its full efficacy.
Although nicotinic acid drugs and berberine have many similar pharmacological activities, their clinical use is limited to a certain extent due to their low bioavailability. The method of utilizing the degree and exerting the synergistic effect of the two will have very important clinical significance
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Embodiment 1
[0020] Synthesis of nicotinic acid berberine conjugate
[0021] 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 0.5mol / l sodiumhydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 1.25g of nicotinic acid , keep stirring at this temperature for 1-2 hours, filter while hot, concentrate the filtrate to one-third of the original volume, cool and crystallize, filter and dry to obtain 3.9 g of nicotinic acid berberine conjugate with a yield of 85%.
Embodiment 2
[0023] Synthesis of nicotinic acid berberine conjugate
[0024] Take 3.7g of berberine hydrochloride, put it into a 100ml three-neck flask, add 150ml of ethanol, adjust the pH to 7-8 with 0.6mol / l sodiumhydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 1.3g of nicotinic acid , keep stirring at this temperature for 1-2 hours, filter while hot, concentrate the filtrate to one-third of the original volume, cool and crystallize, filter and dry to obtain 4.1 g of nicotinic acid berberine conjugate with a yield of 89.5%.
Embodiment 3
[0026] Synthesis of nicotinic acid berberine conjugate
[0027] 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 sodiumhydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 2.0g of nicotinic acid, Stir at this temperature for 1-2 hours, filter while hot, concentrate the filtrate to one-third of the original volume, cool and crystallize, filter, and dry to obtain 4.0 g of nicotinic acid berberine conjugate with a yield of 87.3%. ESI-MS (M + +H)m / zcalcdforC 20 h 16 NO 4 + 337.13found337.17; ESI-MS (M + +H)m / zcalcdforC 6 h 4 NO 2 - 122.02found122.05.
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technical field [0001] The invention relates to the technical field of food and pharmaceuticals, in particular to the application of niacin derivatives in the preparation of products for preventing or treating obesity and related diseases or symptoms. Background technique [0002] About 12 million people die of cardiovascular disease and cerebral apoplexy every year in the world, and atherosclerosis caused by hyperlipidemia is the main cause of coronary heart disease, hypertension and cerebrovascular disease. In 2002, the global annual sales of only atorvastatin (a blood lipid-lowering drug) was nearly 8 billion US dollars, becoming the world's best-selling drug that year. It can be seen that the research and development of blood lipid-lowering drugs has significant social benefits and market prospects. Nicotinic acid is converted into nicotinamide in the body, and then forms nicotinamide adenine dinucleotide (coenzyme I) and nicotinamide adenine dinucleotide phosphate (coe...
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