CN1475224A - Compound preparation of levocarnitin and adenosine triphosphate - Google Patents
Compound preparation of levocarnitin and adenosine triphosphate Download PDFInfo
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- CN1475224A CN1475224A CNA031477151A CN03147715A CN1475224A CN 1475224 A CN1475224 A CN 1475224A CN A031477151 A CNA031477151 A CN A031477151A CN 03147715 A CN03147715 A CN 03147715A CN 1475224 A CN1475224 A CN 1475224A
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Abstract
A composite medicine is prepared from levocarnitine or its physiologically receptable salt 0.05-5.0g and atenen or its physiologically receptable salt 1-100mg.
Description
Technical field:
The present invention relates to a kind of compound medicinal formulation, particularly levocarnitine and combine the compound preparation made from adenosine triphosphate disodium salt, and the application of this compound preparation in medical treatment.
Background technology:
Levocarnitine is the essential cofactor of fatty acid metabolism, and it is the cofactor that several enzymes comprise carnitine translocase, acetylcarnitine transferase I and II.It is essential that these enzymes change acetylcarnitine into and are transferred to mitochondrion by long-chain fatty acid, thereby this this material is that to enter tricarboxylic acid cycle behind beta oxidation energy-producing.Acyl-CoA the bulk deposition that when ischemia, anoxia, in the beta oxidation process, is generated, Intramitochondrial long-chain acyl carnitine is also piled up, the free carnitine of q.s can make accumulation acyl-CoA enter in the mitochondrion, reducing its inhibition to acenine nucleotide translocase, is that oxidative phosphorylation is smooth.Levocarnitine is the especially main energy source of myocardial cell of muscle cell, and many histoorgans such as brain, kidney are also mainly by the fatty acid oxidation energy supply.Be mainly used in former and secondary levocarnitine shortage at present clinically.Shock, acute, chronic cardiac insufficiency, ischemic cardiomyopathy, myocarditis, arrhythmia, angina pectoris, myocardial infarction; Chronic hepatic insufficiency, liver cirrhosis, the auxiliary treatment of chronic, acute hepatitis; Ischemic cerebrovascular, amyotrophy; Diabetes; The patient that chronic uremia is dialysed especially for a long time; Total parenteral nutrition and wound.Be used to reduce the toxicity of antitumor drug to cardiac toxicity and minimizing valproic acid.The neonate malnutrition.The bad auxiliary treatment effect of uterine contraction in puerperal.
Adenosine triphosphate disodium salt is the metabolic a kind of coenzyme of human body, and the effect that improves body is arranged, and participates in the metabolism of body fat, protein, sugar, nucleic acid and nucleotide.Be the main source of energy i (in vivo) simultaneously, when absorption in the body, secretion, muscle contraction and carry out biochemical synthetic reaction etc. when needing energy, adenosine triphosphate promptly resolves into two phosphorus adenosine and phosphates, gives off energy simultaneously.Be applicable to the disease that goes down and cause because of cellular enzymes after the cell injury.Now be used for heart failure, myocarditis, myocardial infarction, cerebral arteriosclerosis, coronary atherosclerosis, acute poliomyelitis, progressive myatrophy illness clinically.Animal experiment can suppress the slow flow of calcium ions of long response time fiber, cloudy stagnate or delay atrioventricular node analyse forward conduction in the approach of returning, heavy dose of preceding sentence or the antidromic conduction that also may block or delay bypass.In addition, also have the vagal effect of of short duration strong enhancing, thereby can stop atrioventricular node and analyse and return the arrhythmia that causes with the bypass foldback mechanism.Being applied to treat quick type supraventricular arrhythmia total effective rate is 82%, the multiple rate of tool soon, advantage such as reusable in a short time.
The metabolism of long-chain fatty acid is the main source of each histoorgan institute energy requirement of human body in the human body, and the fatty acid oxidation degraded was divided into for three stages: (1) activation (carrying out in Cell sap); (2) beta oxidation (in mitochondrion); (3) tricarboxylic acid cycle (in mitochondrion).Activation stage a part fatty acid need consume two energy-rich phosphate bonds and could activate and be acyl-CoA, replenish the metabolism that a certain amount of three bowls of adenosines help to accelerate and strengthen fatty acid to human body, more energy is provided for each histoorgan of human body, slows down or eliminate patients' such as heart failure, myocarditis, myocardial infarction, cerebral arteriosclerosis, coronary atherosclerosis misery.But in the fatty acid oxidation process, acyl-CoA that activation stage generates in Cell sap.Must be under the assistance of carnitine, just can change over to through the catalysis of carnitine acyltransferase and to enter tricarboxylic acid cycle in the mitochondrion.Lead the ATP level in ischemia, anoxia and descend, cell membrane and subcellular fraction membrane permeability raise, and the acyl-CoA of accumulation can cause membrane structure and change, film phase disintegrate and cause cell death.In addition, based on sugared anerobic glycolysis, accumulations such as fatty acid cause acidosis during anoxia, ion imbalances, aqtocytolysis death.The free carnitine of q.s can make the acyl-CoA of accumulation enter in the mitochondrion, reduces its inhibition to acenine nucleotide translocase, makes oxidative phosphorylation smooth.
Levocarnitine and adenosine triphosphate disodium salt are as two kinds of important coenzyme in the fatty acid oxidation process, divided at present and else made the medicine listing, the discovery that the inventor is surprised, when replenishing adenosine triphosphate to human body, replenish a certain amount of levocarnitine, can make both bring into play synergism, single one of using, better effects if, and reduce single with some side effect that one brought.Therefore, the inventor proposes levocarnitine and adenosine triphosphate are mixed and made into new compound preparation.
Summary of the invention:
The invention provides a kind of compound medicinal formulation, preparation contains active component a: levocarnitine or its physiologically acceptable salt and b: adenosine triphosphate disodium salt.
Its physiologically acceptable salt of described levocarnitine can be a free form, it also can be the form of its various physiologically acceptable salt, as: alkali metal salt, alkali salt or acid salt etc. also can be the forms of his inner salt or fat, and the form of any its active derivant of reservation.Preparation of the present invention removes above-mentioned two kinds of active component, also can add pharmaceutically acceptable auxiliary element, described medicine acceptable carrier comprises, solubilizing agent, cosolvent, antiseptic, filler, disintegrating agent, fluidizer, diluent and any adjuvant that needs when making pharmaceutical preparation, these can be: water, soil temperature class material, starch, sucrose, fructose, lactose, mannose, mannitol, mannitol, sorbitol, benzoic acid, sodium benzoate, benzyl alcohol, ethanol, the spans material, cellulose and derivant thereof, gelatin, polyvinylpyrrolidone, Polyethylene Glycol, Pulvis Talci, magnesium stearate etc.
Pharmaceutical preparation of the present invention can be made any pharmaceutical dosage forms, and preferably injection and oral liquid also can be other dosage forms, as: tablet, capsule, granule, electuary, infusion solutions, freeze-dried powder etc.The per unit preparation can contain levocarnitine or its physiologically acceptable salt 0.05-5.0g, adenosine triphosphate or its physiologically acceptable salt 1mg-100mg.Preferably the per unit preparation can contain levocarnitine or its physiologically acceptable salt 1.0-2.0g, adenosine triphosphate or its physiologically acceptable salt 10mg-25mg.Described unit formulation is meant that each preparation unit is as every tablet of tablet, every capsules, every injection, every bottle of oral liquid etc.In use also can refer to each taking dose, be levocarnitine or its physiologically acceptable salt 1.0-2.0g as each use amount, adenosine triphosphate or its physiologically acceptable salt 10mg-25mg.For pharmaceutical preparation, can add the medicine acceptable carrier, can not add yet, take by weighing a certain amount of active component, mix homogeneously is according to making compound preparation according to the agent routine techniques.
The present invention finds, preparation of the present invention could stable existence under alkaline environment, and therefore when preparation compound injection of the present invention and compound oral liquid, pH value has significant impact to injection and oral liquid and stability.The present invention has compared the stability of injection under identical prescription, the different PH condition when this compound injection of preparation.
Under identical prescription condition, the pH value of four kinds of injections is transferred to 5.5,7.5,8.5,9.5 respectively.Get four kinds of each 5ml of injection and inject the brown ampoule bottle of 10ml respectively, 121 ℃ of pressure sterilizings 1 hour place accelerated test under 100 ℃ of high temperature, 92.5% hot conditions with four kinds of injections respectively again.Experimental result shows, PH＞7.5 o'clock, and injection is stable, no catabolite appearance, outward appearance, character no change.Consider that human body can connect resident pH value scope, thus the stable PH of this compound preparation of selection to scope be 8.0-9.5.
The alkali that the present invention is used to regulate pH value is physiologically-acceptable organic alkali or inorganic base, is selected from sodium hydroxide, potassium hydroxide, sodium bicarbonate, potassium bicarbonate, sodium hydrogen phosphate, dipotassium hydrogen phosphate etc.
Preparation of the present invention, curative effect are single to significantly improve with levocarnitine or adenosine triphosphate disodium salt, has synergism, and easy to use, economical and practical.
The specific embodiment:
Below in conjunction with embodiment the present invention is described in detail:
Embodiment 1:
Prescription:
Triphosphoric acid adenosine monophosphate disodium 20g
Levocarnitine 1000g
Water for injection 500ml
0.1mol/L an amount of technology of sodium hydroxide solution:
Get levocarnitine 1000g, adenosine triphosphate 20g, add 5000ml water for injection, regulate pH value to 8.0-9.0 with an amount of 0.1mol/L sodium hydroxide solution, fully mix, filling bottle (every bottle of 5ml) promptly gets compound injection of the present invention.
Embodiment 2: prescription:
Adenosine triphosphate disodium salt 40g
Levocarnitine 2000g
Water for injection 10000ml
0.1mol/L an amount of technology of sodium hydroxide solution:
Get levocarnitine 1000g, adenosine triphosphate 20g, add 10000ml water for injection, regulate pH value to 8.0-9.0 with an amount of 0.1mol/L sodium hydroxide solution, fully mix, filling bottle (every bottle of 10ml) promptly gets compound oral liquid of the present invention.
Claims (10)
1, a kind of compound medicinal formulation is characterized in that, said preparation contains active component a: levocarnitine or its physiologically acceptable salt and b: adenosine triphosphate disodium salt.
2, the compound preparation of claim 1 can be any pharmaceutically acceptable dosage form.
3, the compound preparation of claim 1 is a liquid preparation.
4, the compound preparation of claim 1, the amount that contains levocarnitine or its physiologically acceptable salt in every dose are that the amount of 0.05-5.0g, adenosine triphosphate disodium salt is 1mg-100mg.
5, the compound preparation of claim 1, the amount that contains levocarnitine or its physiologically acceptable salt in every dose are that the amount of 1.0-2.0g, adenosine triphosphate disodium salt is 10mg-25mg.
6, the compound preparation of claim 3, contain physiologically acceptable alkali and/or other make the needed carrier of liquid preparation, wherein active component accounts for the 0.1-99.9% of total formulation weight amount, makes the 0.1-99.9% that the needed carrier of preparation accounts for the total formulation weight amount.
7, the compound preparation of claim 4, its pH value is greater than 7.
8, the compound preparation of claim 4, its pH value are 8.0-9.5.
9, the compound preparation of claim 7, wherein physiologically acceptable alkali is selected from, sodium hydroxide, potassium hydroxide, sodium bicarbonate, potassium bicarbonate, sodium hydrogen phosphate, dipotassium hydrogen phosphate.
10, the compound preparation of claim 3, per 1000 bottles contain
Triphosphoric acid adenosine monophosphate disodium 20g
Left side card Buddhist nun 1000g
Water for injection 500ml
0.1mol/L sodium hydroxide solution is made through following steps in right amount, get levocarnitine 1000g, adenosine triphosphate 20g, add the dissolving of 5000ml water for injection, regulate pH value to 8.0-9.0 with an amount of 0.1mol/L sodium hydroxide solution, fully mix filling bottle.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031477151A CN1475224A (en) | 2003-06-24 | 2003-06-24 | Compound preparation of levocarnitin and adenosine triphosphate |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031477151A CN1475224A (en) | 2003-06-24 | 2003-06-24 | Compound preparation of levocarnitin and adenosine triphosphate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1475224A true CN1475224A (en) | 2004-02-18 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031477151A Pending CN1475224A (en) | 2003-06-24 | 2003-06-24 | Compound preparation of levocarnitin and adenosine triphosphate |
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| CN (1) | CN1475224A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101336914B (en) * | 2007-07-03 | 2011-12-28 | 常州高新技术产业开发区三维工业技术研究所有限公司 | Medicine combination capable of reducing myocardial infarction area and use thereof |
-
2003
- 2003-06-24 CN CNA031477151A patent/CN1475224A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101336914B (en) * | 2007-07-03 | 2011-12-28 | 常州高新技术产业开发区三维工业技术研究所有限公司 | Medicine combination capable of reducing myocardial infarction area and use thereof |
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