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Adenosine cyclophosphate oil in water composition for vein and preparation thereof

A technology of cyclophosphate water-in-oil composition, applied in the field of medicine, can solve the problems of poor long-term storage stability, high solution viscosity, high irritation, etc., and achieves reduction of vascular irritation and inflammatory response, and low toxicity and side effects. , the effect of reducing toxic side effects

Inactive Publication Date: 2008-12-17
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventor finds that glycerin is used as the isotonic regulator, the viscosity of the solution is relatively large, which brings great difficulties to production, and at the same time, it is more irritating and has a strong sense of pain during clinical application; the combination of soybean oil and lecithin emulsifies , the effect is poor, soybean oil is a polyunsaturated fatty acid oil, and the long-term storage stability is poor

Method used

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  • Adenosine cyclophosphate oil in water composition for vein and preparation thereof
  • Adenosine cyclophosphate oil in water composition for vein and preparation thereof
  • Adenosine cyclophosphate oil in water composition for vein and preparation thereof

Examples

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Effect test

example 1

[0023] The preparation of example 1 cyclic adenosine monophosphate lipid emulsion

[0024] (1) Mix 20g of cyclic adenosine monophosphate and 20g of polysorbate 80 into 200g of peanut oil heated to 80°C, and disperse evenly to obtain an oil phase;

[0025] (2) Dissolve 50g of sodium chloride in 500ml of water for injection to obtain an aqueous phase;

[0026] (3) Under high-speed stirring, pour the oil phase evenly into the water phase, stir to form colostrum, transfer to a high-speed homogeneous mixer for homogenization, add water for injection to 2000ml, and adjust with 1mol / L disodium hydrogen phosphate solution When the pH value reaches 6.2, add 2g of activated carbon to absorb for 20 minutes, decarburize by filtration, fine filter with a 0.22μm filter membrane, fill each tube with 2ml, and sterilize at 115°C for 30min to obtain cyclic adenosine monophosphate emulsion, the concentration of cyclic adenosine monophosphate is 10mg / ml.

example 2

[0027] The preparation of example 2 cyclic adenosine monophosphate lipid emulsion

[0028] (1) Mix 40g of cyclic adenosine monophosphate and 100g of polysorbate 80 into 800g of corn oil heated to 80°C, and disperse evenly to obtain an oil phase;

[0029] (2) Dissolve 200g of glucose in 1000ml of water for injection to obtain an aqueous phase;

[0030] (3) Under high-speed stirring, pour the oil phase evenly into the water phase, stir to form colostrum, transfer to a high-speed homogeneous mixer for homogenization, add water for injection to 4000ml, and adjust with 1mol / L disodium hydrogen phosphate solution When the pH value reaches 6.0, add 20g of activated carbon to absorb for 30 minutes, decarburize by filtration, fine filter with a 0.22μm filter membrane, fill each tube with 4ml, and sterilize at 115°C for 30min to obtain cyclic adenosine monophosphate emulsion, the concentration of cyclic adenosine monophosphate is 10mg / ml.

example 3

[0031] The preparation of example 3 cyclic adenosine monophosphate lipid emulsion

[0032] (1) Mix 20g cyclic adenosine monophosphate and 100g polysorbate 80 into 200g coconut oil heated to 80°C, and disperse evenly to obtain an oil phase;

[0033] (2) 100g of mannitol was dissolved in 500ml of water for injection to obtain an aqueous phase;

[0034] (3) Under high-speed stirring, pour the oil phase evenly into the water phase, stir to form colostrum, transfer to a high-speed homogeneous mixer for homogenization, add water for injection to 2000ml, and adjust with 1mol / L disodium hydrogen phosphate solution When the pH value reaches 6.1, add 10g of activated carbon to absorb for 20 minutes, decarburize by filtration, fine filter with a 0.22μm filter membrane, fill each tube with 2ml, and sterilize at 115°C for 30min to obtain cyclic adenosine monophosphate emulsion, the concentration of cyclic adenosine monophosphate is 10mg / ml.

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Abstract

The invention discloses an adenosine cyclophosphate oil-in-water composite for intravenous injection, which is the oil-in-water emulsion with the following ingredients and proportion: 20-40mg of adenosine cyclophosphate, 200-800mg oil for injection, 8,020-100 mg of polysorbate, 0-200mg of osmotic pressure regulator and 2-4ml water for injection; wherein, the oil for injection is selected from one or more of peanut oil, corn oil, sesame oil, olive oil, flaxseed oil, safflower oil, Chinese tung oil, polyoxyethylene hydrogenated castor oil, coconut oil or palm oil. The invention also discloses a preparation method. The adenosine cyclophosphate emulsion for intravenous injection is an excellent preparation with stable performance, low toxic and side effect and good biocompatibility.

Description

technical field [0001] The invention relates to an intravenous cyclic adenosine monophosphate composition and a preparation method, belonging to the technical field of medicine. Background technique [0002] Cyclic adenosine monophosphate is a protein kinase activator, which is a derivative of nucleotides. It is an important substance with physiological activity that widely exists in the human body. It is produced by adenosine triphosphate under the catalysis of adenylyl cyclase and can regulate various functional activities of cells. As the second collection of hormones, hormones regulate physiological functions and substance metabolism in cells, can change the function of cell membranes, and promote calcium ions in the reticulum sarcoplasm to enter muscle fibers, thereby enhancing myocardial contraction and promoting oxygenation of the respiratory chain Enzyme activities can improve myocardial hypoxia, relieve symptoms of coronary heart disease and improve electrocardiogr...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/7076A61P9/10A61P9/00
Inventor 朱正兵
Owner HAINAN LINGKANG PHARMA CO LTD