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L-carnitine pyruvate, and preparation method and application thereof

A technology of L-carnitine and pyruvate, which is applied in the field of L-carnitine pyruvate and L-carnitine pyruvate divalent metal salt, can solve the problems of poor solubility, low calcium content, low absorption rate, etc., and meet the reaction conditions Mild, simple production process, high stability effect

Inactive Publication Date: 2013-02-06
广州市奥海生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(1) Inorganic calcium fortifiers (such as CaCO3) have high calcium content, but poor solubility, and need to consume gastric acid for absorption in the body, and the absorption rate is low, so this type of calcium supplement will Increased burden on the liver and kidneys
(2) Biological calcium fortifiers (such as shell powder, pearl powder, and animal bone powder) not only have the same disadvantages as inorganic calcium supplements that are difficult to absorb, but also generally contain excessive heavy metals (lead, cadmium, mercury, zinc) question
(3) Organic calcium fortifiers (such as calcium gluconate and calcium acetate) mainly have low calcium content and varying degrees of toxicity, such as calcium gluconate, which contains only 8.9% calcium and is not suitable for diabetics; acetic acid Calcium LD50<5g / kg, high toxicity, easy to cause kidney stones, heart cramps, calcification of blood vessels and soft tissues

Method used

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  • L-carnitine pyruvate, and preparation method and application thereof
  • L-carnitine pyruvate, and preparation method and application thereof
  • L-carnitine pyruvate, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment one: the preparation of L-carnitine pyruvate

[0039] Add 1.8g (45.3mmol) of sodium hydroxide to the reaction vessel, add 50ml of methanol, stir to dissolve it, then add dropwise a methanol solution of L-carnitine chloride (containing 8.9g (45.3mmol) of L-carnitine chloride. After the addition, continue to stir the reaction at room temperature for 2h. Filter out the generated sodium chloride solid. Add a methanol solution of pyruvic acid dropwise to the filtrate (4.0g (45.3mmol) of pyruvic acid is dissolved in 30ml of methanol). After the addition is complete, continue Stir for 3h. Concentrate under reduced pressure to dryness, wash 2 times with an appropriate amount of acetone. Add 100ml of absolute ethanol, mash vigorously, and a white solid is precipitated. Continue to stir at room temperature for 2h. Filter the precipitated light yellow solid under reduced pressure, and wash with 10ml of absolute ethanol Washing. Place in an oven and dry under reduced...

Embodiment 2

[0057] Embodiment two: the preparation of L-carnitine calcium pyruvate

[0058] Add 1.6g (10mmol) of L-carnitine to the reaction vessel, add 50ml of water and 5ml of methanol, stir to dissolve, add 1.8g (10mmol) of pyruvic acid, and stir at room temperature for 2h. The temperature was raised to 70°C, and the reaction was continued for 3h. Cool to room temperature. Ca(OH)2 0.7 g was added. After the reaction was stirred at room temperature until clear, the reaction was continued for 4h. The reaction solution was filtered. The filtrate was concentrated under reduced pressure in vacuo. 50 ml of absolute ethanol was added to the concentrated residue. After stirring until solidified, continue stirring for 2h. The product was filtered under reduced pressure, and dried under reduced pressure in an oven at 70°C for 3 hours.

[0059] The product is 3.3g of light yellow solid powder, and the yield is 87%.

[0060] The structural formula of the L-carnitine calcium pyruvate of gai...

Embodiment 3

[0078] Embodiment three: the preparation of L-carnitine magnesium pyruvate

[0079]Add 1.6g (10mmol) of L-carnitine to the reaction vessel, add 50ml of water and 5ml of methanol, stir to dissolve, add 1.8g (10mmol) of pyruvic acid, and stir at room temperature for 2h. The temperature was raised to 70°C, and the reaction was continued for 3h. Cool to room temperature. Add Mg(OH) 2 0.58g (10mmol). After the reaction was stirred at room temperature until clear, the reaction was continued for 4h. The reaction solution was filtered. The filtrate was concentrated under reduced pressure in vacuo. 50 ml of absolute ethanol was added to the concentrated residue. After stirring until solidified, continue stirring for 2h. The product was filtered under reduced pressure, and dried under reduced pressure in an oven at 70°C for 3 hours.

[0080] The product is 3.1 g of light yellow solid powder, and the yield is 87%.

[0081] The structural formula of the L-carnitine magnesium py...

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Abstract

The invention provides a new L-carnitine pharmaceutically-acceptable salt, namely L-carnitine pyruvate and divalent metal salts thereof, and a preparation method and application thereof. The L-carnitine pyruvate and divalent metal salts thereof have the characteristics of higher stability and lower water absorbing tendency than the L-carnitine inner salts, can be accepted by the human body and participate in the physiologic metabolism of the human body more easily than the existing L-carnitine pharmaceutically-acceptable salts, and have stronger nutrition and treatment actions. The invention also provides application of the L-carnitine pyruvate and divalent metal salts in preparing slimming medicines or health foods, application in preparing diet / nutrition supplements and application in preparing veterinary products or feeds.

Description

technical field [0001] The invention belongs to the field of pharmaceutical intermediates and food additives, and relates to a new pharmaceutically acceptable salt of L-carnitine, in particular to a kind of L-carnitine pyruvate, especially a divalent metal salt of L-carnitine pyruvate, and the Preparation method and use of salt. Background technique [0002] With the development of the economy and the improvement of people's living standards, obesity has become a serious public health problem. In recent years, the number of obese patients in the world has increased day by day. The prevalence of obesity in developed countries is as high as 20%. Second only to smoking, the International Obesity Conference issued a report that the number of deaths from related diseases caused by obesity in the world has exceeded the number of people who died of starvation in the same period. Obesity is a multifactorial disease affected by biological, behavioral and environmental factors, and c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/20C07C227/18C07C51/41C07C59/19A61K31/205A61K31/19A61P3/04A61P3/02A23L1/29A23K1/16A23L33/00
Inventor 王景成苏军
Owner 广州市奥海生物科技有限公司
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