Summary of the invention
The purpose of this invention is to provide a kind of L-carnitine compositions, it can accelerate the burning of fat in the health, effectively makes the body fat oxidation Decomposition be converted into energy, replenishes the required nutrition of health, improves motor capacity.
Another object of the present invention is to provide a kind of L-carnitine preparation.
Another purpose of the present invention is to provide the preparation method of described L-carnitine preparation.
A further object of the present invention has been to provide the application in preparation raising endurance medicine of a kind of described L-carnitine compositions or preparation.
The invention provides a kind of L-carnitine compositions, by weight, comprise following raw material: L-carnitine or its pharmaceutically acceptable salt 10-300 part, glutamine 500-1500 part, branched-chain amino acid 300-600 part, soybean peptide 100-300 part and creatine 100-300 part.
Described L-carnitine compositions by weight, preferably comprises following raw material: L-carnitine or its pharmaceutically acceptable salt 25-200 part, glutamine 800-1200 part, branched-chain amino acid 400-500 part, soybean peptide 150-250 part and creatine 150-250 part.
Described L-carnitine compositions by weight, more preferably comprises following raw material: 150 parts of L-carnitine or its pharmaceutically acceptable salts, 900 parts of glutamine, 450 parts of branched-chain amino acid, 180 parts of 200 parts of soybean peptide and creatines.
Described L-carnitine compositions, the raw material that also comprises has: taurine, vitamin substances and lycopene.
Wherein, by weight, described taurine 5-60 part, vitamin substances 5-15 part, lycopene 0.5-2.5 part.Preferred taurine 15-50 part, vitamin substances 8-12 part, lycopene 1-2 part.More preferably taurine is 35 parts, 10 parts of vitamin substances, 1.5 parts of lycopenes.
Wherein, described L-carnitine pharmaceutically acceptable salt is selected from one or more in L-carnitine-L-tartrate, Carnitine Fumarate or the L-carnitine hydrochloride.
Wherein, described vitamin substances is vitamin B1, vitamin B2, vitamin C, vitamin B6 or vitamin E.
Wherein, described branched-chain amino acid is leucine, isoleucine and valine.Its weight ratio is (2.0-2.5): 1: (1.0-1.5), and preferred 2: 1: 1.
A kind of L-carnitine preparation provided by the invention is comprised of described L-carnitine compositions and pharmaceutically acceptable excipient.
Wherein, described pharmaceutically acceptable excipient is selected from one or more in diluent, binding agent, sweeting agent and the lubricant.
Wherein, described diluent is selected from one or more in lactose, mannitol, microcrystalline Cellulose, hydroxyl isomaltulose, Sorbitol, xylitol and the isomaltulose.
Wherein, described binding agent is selected from one or both in ethanol and the hydroxypropyl methylcellulose.
Wherein, described lubricant is selected from one or both in magnesium stearate and the soybean oil.
Wherein, described sweeting agent is selected from a kind of how several in Mel, white sugar and the citric acid.
Wherein, the weight portion of described pharmaceutically acceptable excipient is 10-2000 part, is preferably 10-1000 part, more preferably 300 parts.Excipient also is called adjuvant.
Described L-carnitine preparation can be solid preparation or liquid preparation.
Wherein, described solid preparation can be tablet, capsule or powder.Capsule can be made hard capsule or soft capsule.Described liquid preparation can be drink.
The unit of weight portion of the present invention can be the known unit of weights of field of medicaments such as μ g, mg, g, kg.
The preparation method of described L-carnitine preparation provided by the invention can adopt conventional method in the art to prepare, and also can by following method preparation, comprise the steps:
1) take by weighing each raw material in the described L-carnitine compositions, crushing screening, for subsequent use;
2) taking by weighing described pharmaceutically acceptable excipient, with this excipient and step 1) described each raw material is according to the equivalent method mix homogeneously that progressively increases, and is prepared into various regular dosage forms according to conventional formulation technique.
Compositions of the present invention and preparation have following beneficial effect:
L-carnitine (L-carnitine) claims again VBT, DL-carnitine chloride, and chemical name is beta-hydroxy γ-trimethylamine butanoic acid, is a kind of white crystalline lens or white transparent fine powder.L-carnitine is the moisture absorption very easily, and stable good can place in the solution of pH 3-6 more than 1 year, ability more than 200 ℃ high temperature and have preferably solubization and water absorption.L-carnitine has been applied to the fields such as medicine, health care and food at present.
L-carnitine is that a kind of fat that promotes is converted into the amino acid of energy, and red meat is the main source of L-carnitine, and human body is had no side effect.Dissimilar diets has contained the L-carnitine of 5-100 milligram, but common people can only take in 50 milligrams every day from meals, and vegetarian is taken in still less.The main Physiological Function of L-carnitine is to promote that fat changes into energy.L-carnitine and salt thereof are a kind of special acids that extensively is present in body tissue, it is lipometabolic necessary cofactor, can improve sports emotion and enhancing body vigor, increase muscular endurance and motor capacity, there is positive effect the aspects such as alleviation and resisting fatigue.
Soybean peptide is to adopt modern biological enzymolysis technology, after the soybean protein molecule is separated through enzyme action, and the small molecular protein peptide that obtains.It had both had soy proteinaceous nutritive peculiarity, had again the peculiar good biological activity of small-molecular peptides and physiological function.Supplement the nutrients rapidly, strengthen nutrition, allaying tiredness for the athlete increases muscle quantities, regains one's strength.Soybean peptide is fast in intestinal absorption, has antioxidant activity, can also promote the increase of sport people lean body mass, improves the sport people serum testosterone, reduces the tired grade of sport people, serum creatine kinase level after the motion of reduction sport people, Cell protection film.
Creatine is the natural nutrient that is present in body, and 95% creatine all is present in the skeletal muscle.The resynthesis of the ATP that consumes during the creatine of intramuscular abundance can guarantee to move reduces to greatest extent the generation of the lactic acid of muscle part, thereby people's physical ability is moved the longer time under higher intensity.This just can help human body to gain in strength, increase the acting ability, increase muscle, and makes human body fatigue can not occur too early.Studies show that creatine can increase the ability of muscle fiber panning protein.Actin and myosin all are essential for the contraction of all muscle.When human body by the picked-up creatine, when having promoted that these contractile proteins synthesize, then increased the ability that muscle is engaged in physical exertion, in the shorter time, can finish more work.Therefore creatine is good nutriment for the athlete who improves explosive force, carries out strength building.
Glutamine is in blood and the cell, the highest free amino acid of skeletal muscle intensive amount particularly, and it has consisted of 61% of skeletal muscle free amino acid pond.Recently about studies show that of glutamine and taurine, they can be when human body produces strong metabolic stress (body that causes such as exacting practice and match stress), promotes the anabolism of protein and reduces the decomposition of muscular tissue.Glutamine is the carrier of nitrogen, and has the effect of important cell increase-volume, studies show that, only replenishing glutamine 2-6g every day just has obvious positive interaction to protein metabolism and cell increase-volume.These effects all can promote the growth of the synthetic and cell of myocyte's internal protein.Also have research to find, use the low dose of glutamine can also stimulating immune system, serve as the fuel of immunocyte, correct acidosis, keep the normal pH value of blood.Yet the strength building of large intensity can make glutamine reduce by 50%, and a few hours just can return to original level after the motion.People's immunity after motion is low than usual, and this is that the decline of body glutamine level causes.If there is the problem of hypoimmunity in the athlete, in case they the flu or wound infection, the time of its recovery than under normal circumstances slowly many, this also will hinder finishing of exercise program.This shows that replenishing of glutamine is very important concerning them.
Branched-chain amino acid (leucine, isoleucine, valine) after training, recover with procedure of adaptation in bring into play pivotal role, branched-chain amino acid is the precursor substance that muscular energy produces, and also is simultaneously immune system and activates the fuel that recovers mechanism.Therefore its tired and anti-muscle protein of bioavailability, delay that helps to improve carbohydrate decomposes.
Lycopene (lycopene) is the main pigment of mature tomato, is a kind of oxygen-free carotenoid.In carotenoid, it has the strongest antioxidant activity.The effect that lycopene is removed free radical outclass other carotenoid and vitamin E, and the speed constant of its singlet-oxygen quenching is 100 times of vitamin E, is one of found powerful antioxidant of occurring in nature up to now.
Taurine is a kind of special aminoacid, is the requisite a kind of nutrient of human body, and the effect of balance health is arranged.Scientific research finds that taurine has protective effect to eyes, lung, liver, gastrointestinal etc.In addition; taurine can and generate the avirulence material in conjunction with the hypochlorous acid in the leukocyte; reduce hypochlorous acid to the destruction of leukocyte self; thereby raising body immunity; simultaneously, taurine can be kept cardiac function, makes blood circulation normalization; thereby the allaying tiredness product makes effectively produce power of body., it has the effect that alleviates and prevent myocardial damage after the motion of exhausting property of power, the motor capacity that can improve body after replenishing, it mainly is that generation by opposing body periphery fatigue realizes.
Vitamin B group can promote energy metabolism, alleviates the mental pressure of movement human.Vitamin C and vitamin E can be removed free radical, improve immunologic function, reduce the injury of radical pair body, the generation of delay fatigue.
In a word; L-carnitine compositions provided by the invention makes up L-carnitine or its pharmaceutically acceptable salt, creatine, branched-chain amino acid, glutamine, soybean peptide, can add taurine, vitamin substances and lycopene again; further, carry out in specific proportions composite.Wherein, L-carnitine is the fatty acid oxidation carrier, fat can be transferred to mitochondrion, carries out oxidation Decomposition in mitochondrion, for body provides energy; Other materials provide nutrition for body, thereby can improve the endurance of motion, slow down the generation of exercise fatigue and promote tired recovery.Especially can effectively promote body SOD to raise, strengthen the ability of body free radical resisting.
The specific embodiment
Following examples are used for explanation the present invention, but are not used for limiting the scope of the invention.
Embodiment 1: capsule
1, prescription (weight): L-carnitine-L-tartrate 25g, VITAMIN B15 g, lycopene 1g, creatine 100g, branched-chain amino acid 300g (leucine 150g, isoleucine 75g, valine 75g), glutamine 500g, taurine 5g, soybean peptide 100g, isomaltulose 100g, magnesium stearate 10g.
2, preparation method:
1) take by weighing L-carnitine-L-tartrate, vitamin B1, lycopene, creatine, branched-chain amino acid, glutamine, taurine, soybean peptide according to prescription, cross respectively 40 mesh sieves, for subsequent use;
2) take by weighing isomaltulose and magnesium stearate according to prescription, above-mentioned supplementary material by the equivalent method mix homogeneously that progressively increases, is poured in the capsule-filling mould, fill capsule, polishing, packing.
Embodiment 2: powder
1, prescription (weight): Carnitine Fumarate 300g, vitamin C 15g, lycopene 2.5g, creatine 300g, branched-chain amino acid 600g (leucine 300g, isoleucine 120g, valine 180g), glutamine 1500g, taurine 60g, soybean peptide 300g, hydroxyl isomaltulose 2000g.
2, preparation method:
1) take by weighing L-carnitine-L-tartrate, vitamin C, lycopene, creatine, branched-chain amino acid, glutamine, taurine, soybean peptide according to prescription, cross respectively 40 mesh sieves, for subsequent use;
2) take by weighing hydroxyl isomaltulose according to prescription, with above-mentioned supplementary material by the equivalent method mix homogeneously that progressively increases, packing.
Embodiment 3: tablet
1, prescription (weight): L-carnitine 150g, vitamin B
610g, lycopene 1.5g, creatine 180g, branched-chain amino acid 450g (leucine 125g, isoleucine 90g, valine 135g), glutamine 900g, taurine 35, soybean peptide 200g, microcrystalline Cellulose 700g, lactose 1200g, magnesium stearate 40g.
2, preparation method:
1) take by weighing L-carnitine-L-tartrate, vitamin B6, lycopene, creatine, branched-chain amino acid, glutamine, taurine, soybean peptide according to prescription, cross respectively 40 mesh sieves, for subsequent use;
2) take by weighing microcrystalline Cellulose, lactose, magnesium stearate according to prescription, by the equivalent method mix homogeneously that progressively increases, use 50% ethanol as binding agent above-mentioned supplementary material; soft material processed; with above-mentioned soft material granulation in the oscillating granulator of 14 eye mesh screens, granule is inserted in the multi-functional boiling drier, about 40 minutes of 50 ℃ of airpillow-dry; the control pellet moisture is 5%; then granulate adds magnesium stearate in granule, total mixed; tabletting, packing.
Embodiment 4: capsule
Preparation method is with embodiment 1, and the prescription of different is this capsule is:
L-carnitine-L-tartrate 50g, vitamin B2 8g, lycopene 1.8, creatine 150g, branched-chain amino acid 495g (leucine 275g, isoleucine 110g, valine 110g), glutamine 1000g, taurine 40g, soybean peptide 150g, microcrystalline Cellulose 100g, magnesium stearate 5g.
Embodiment 5: oral liquid
1, prescription (weight): L-carnitine-L-tartrate 12kg, glutamine 50kg, branched-chain amino acid 40kg, soybean peptide 20kg, creatine 15kg, Mel 10kg, white sugar 8kg, citric acid 1kg.
2, preparation method:
1) take by weighing supplementary material, cross respectively 40 mesh sieves, for subsequent use;
2) with above former, adjuvant except Mel according to the equivalent method mix homogeneously that progressively increases, then be dissolved in the 100kg water, add Mel and stir, be sub-packed in the aseptic bottle every bottle of 20ml after the sterilization.
Embodiment 6: powder
Preparation method is with embodiment 2, and the component of different is this powder is:
L-carnitine-L-tartrate 100g, vitamin E 12g, lycopene 1.2g, creatine 120g, branched-chain amino acid 450g (leucine 200g, isoleucine 100g, valine 150g), glutamine 700g, taurine 50g, soybean peptide 120g, microcrystalline Cellulose 100g, magnesium stearate 5g.
Embodiment 7: tablet
1, prescription (weight): L-carnitine 60g, vitamin B2 18g, lycopene 1.8g, creatine 100g, branched-chain amino acid 380 (leucine 190g, isoleucine 95g, valine 95g)) g, glutamine 1200g, taurine 45g, soybean peptide 250g; microcrystalline Cellulose 500g, magnesium stearate 10g, lactose 200g.
2, preparation method:
1) take by weighing supplementary material, cross respectively 40 mesh sieves, for subsequent use;
2) take by weighing microcrystalline Cellulose, magnesium stearate and lactose according to prescription, by the equivalent method mix homogeneously that progressively increases, use 50% ethanol as binding agent above-mentioned supplementary material; soft material processed with above-mentioned soft material granulation in the oscillating granulator of 14 eye mesh screens, is inserted granule in the multi-functional boiling drier; about 40 minutes of 50 ℃ of airpillow-dry; the control pellet moisture is 5%, and then granulate adds magnesium stearate in granule; total mixed; tabletting, packing, and get final product.
Experimental example: human experimentation
1 experimental subject and method
1 experimental subject and method
1.1 experimental subject
Take 91 man's long-distance runnings of certain sport university to athlete's (21.8 ± 0.75 years old mean age) as object of study.
1.2 experiment grouping
Grouping: 91 experimenters are divided into 7 groups at random, and blank group (N=13) is taken placebo, 4/day; Experimental group 1-5 takes respectively the prepared sample of embodiment 1-5, and contrast groups is taken the product that embodiment 6 makes in the patent 200510086556.8,2 bags/day, all takes continuously for 8 weeks.Whole experimental session, and prohibit food and the medicine that takes other raising endurance.
1.3 experimental technique
Venous blood when requiring the experimenter before test, to come laboratory on an empty stomach to get peace and quiet, carry out sports load (moving at the Monark energy meter) before the motion, the limber up 1min of elder generation (0 load), then begin with 50W power, increasing load progressively, reach 70%Hrmax (being drawn by trial test mensuration) about 3 minutes, after this namely no longer increase loading, continue 60 minutes to pedal.Centre of motion rate adopts the monitoring of Polar table.Temperature and the humidity of control laboratory.The experimenter tests after taking 8 all nutriments again.
1.4 index and method
Test index: get ear blood 1 per half an hour in the motion, surveys lactic acid.Measurement in the 3rd, 9,15 minute recovers heart rate, gets ear blood survey lactic acid after immediate postexercise, the motion.Second day extracting vein blood in early morning is measured serum superoxide dismutases (SOD) vigor.
Method of testing: blood lactic acid adopts YSI 1500SPORT LACTATE ANALYZER to measure, and method is Enzyme Electrode; Serum superoxide dismutases (SOD) vigor adopts xanthine oxidase to measure, and determining instrument is 721 type spectrophotometers.
1.5 result's statistics
Date processing adopts SPSS10.0 software, and all data represent with means standard deviation, adopt variance and the pairing T method of inspection.
2 experimental results
2.1 the comparison of blood lactate concentration
Table 1: blood lactate concentration (unit: mmoL/L)
Grouping |
Quiet |
Immediate postexercise |
3min after motion finishes |
9min after motion finishes |
15min after motion finishes |
Blank group |
1.60±0.46 |
3.22±0.42 |
3.23±0.53 |
2.21±0.52 |
1.61±0.43 |
Contrast groups |
1.59±0.45 |
2.92±0.46 |
2.66±0.54
@ |
2.01±0.53 |
1.58±0.47 |
Experimental group 1 |
1.58±0.43 |
2.74±0.43 |
1.59±0.58
** |
1.41±0.50
** |
1.46±0.53 |
Experimental group 2 |
1.61±0.51 |
2.78±0.40 |
1.62±0.54
** |
1.39±0.48
** |
1.38±0.49 |
Experimental group 3 |
1.57±0.32 |
2.65±0.46 |
1.53±0.59
** |
1.35±0.45
** |
1.32±0.58 |
Experimental group 4 |
1.58±0.34 |
2.70±0.42 |
1.58±0.56
** |
1.34±0.44
** |
1.35±0.53 |
Experimental group 5 |
1.59±0.23 |
2.80±0.41 |
1.68±0.49
** |
1.51±0.49
** |
1.45±0.48 |
*The expression experimental group is compared p<0.01 with the blank group;
@The expression contrast groups is compared p<0.05 with the blank group.
The result finds out from table 1:
Immediate postexercise, the blood lactate concentration of each experimental group slightly reduces, but does not produce significant difference;
3min after motion finishes, the blood lactate concentration of each experimental group is compared with the blank group, has utmost point significant difference (P<0.01); Contrast groups is compared with the blank group, has significant difference (P<0.05);
9min after motion finishes, the level the when blood lactate concentration of each experimental group returns to peace and quiet;
15min after motion finishes, the level when contrast groups and blank group just return to peace and quiet.
Lactic acid is the product that the metabolism of energy substance decomposition obtains in the body in the motor process, and a large amount of acidic materials accumulation cause muscle, joint acid is swollen and spirit is tired.Take the experimental group sample, help to accelerate the removing speed of blood lactic acid in the body, be conducive to prolong exercise tolerance, improve motor capacity.
2.2 motion finishes to recover in rear 3 minutes the comparison of heart rate
The heart rate of 3min test subject the results are shown in Table 2 after immediate postexercise and the motion.
Table 2: motion finishes the rear 3 minutes hearts rate that recover (inferior/as to divide)
Grouping |
At once heart rate (inferior/minute) after motion finishes |
Motion finishes the rear 3 minutes hearts rate that recover (inferior/as to divide) |
Blank group |
140.12±8.48 |
129.23±5.68 |
Contrast groups |
141.15±6.49 |
119.28±5.73
& |
Experimental group 1 |
138.45±6.99 |
107.54±6.23
** |
Experimental group 2 |
139.15±6.67 |
108.13±6.53
** |
Experimental group 3 |
142.32±7.12 |
106.57±6.74
** |
Experimental group 4 |
140.68±8.53 |
108.66±6.83
** |
Experimental group 5 |
141.35±7.26 |
110.64±7.12
** |
*The expression experimental group is compared p<0.01 , ﹠amp with the blank group; The expression contrast groups is compared p<0.05 with the blank group.
As can be seen from Table 2:
Motion finishes rear 3 minutes, and the recovery of each experimental group heart rate is compared with the blank group, highly significant (P<0.01);
Contrast groups is compared with the blank group, and heart rate recovers significantly (P<0.05).
The heart rate resume speed is fast, shows that experimental group experimenter exercise tolerance is good, and motor capacity is strong.Therefore can find out that experimental group experimenter's resisting fatigue effect is better than blank group and contrast groups.
2.3 oxidation resistance test result
M seq is measured respectively serum superoxide dismutases (SOD) vigor of blank group, contrast groups and each experimental group after the experiment, and experimental result sees Table 3.
Table 3: the rear impact on 4 groups of experimenter's oxidation resistances of experiment
Compare ※ p<0.05 with the blank group.
As shown in Table 3, the SOD vigor in five groups of experimenter mornings next day is all high than morning on the previous day, all is significantly higher than the previous day (P<0.05).And contrast groups is compared with the blank group, does not have significant difference.
Show that present patent application obtains compositions and can effectively promote body SOD to raise, and has strengthened the ability of body free radical resisting.
Discuss: motion causes that the body free radical increases, and too much free radical can cause some important metabolic enzymes because of the cross-linked polymeric inactivation, causes a series of pathological change, causes the ability to work of human body to descend and the generation feeling of fatigue.Therefore, accelerate the removing speed of free radical, improve the anti-oxidative defense function, help to improve motor capacity, promote fatigue recovery, reduce peroxidation to the damage of body.
3, conclusion
From whole experimentation, the compositions of resisting fatigue provided by the invention has the effect of Synergistic, and experimenter's blood lactic acid resume speed is accelerated, and it is also fast that heart rate recovers, this all is the key factor that is conducive to prolong exercise tolerance, is conducive to the raising of motor capacity.Motion can cause that the body free radical increases, and too much free radical can cause some important metabolic enzymes because of the cross-linked polymeric inactivation, causes a series of pathological change, causes the ability to work of human body to descend and generation fatigue.Therefore, accelerate the removing speed of free radical, improve the anti-oxidative defense function, significant to improving motor capacity.The antioxidation result of this experiment shows, takes the preparation that said composition makes and can effectively promote body SOD to raise, and can effectively improve the ability of body free radical resisting, to improving motor capacity and promoting that fatigue recovery also has certain effect.
Although, above used general explanation, the specific embodiment and test, the present invention is described in detail, on basis of the present invention, can make some modifications or improvements it, and this will be apparent to those skilled in the art.Therefore, these modifications or improvements all belong to the scope of protection of present invention without departing from theon the basis of the spirit of the present invention.