CN101559064A - Medicament capable of protecting cell membrane - Google Patents
Medicament capable of protecting cell membrane Download PDFInfo
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- CN101559064A CN101559064A CNA2008101041183A CN200810104118A CN101559064A CN 101559064 A CN101559064 A CN 101559064A CN A2008101041183 A CNA2008101041183 A CN A2008101041183A CN 200810104118 A CN200810104118 A CN 200810104118A CN 101559064 A CN101559064 A CN 101559064A
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- fructose diphosphate
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Abstract
The invention relates to a medicament capable of protecting a cell membrane, comprising main components of fructose-1,6-diphosphate or salts thereof, taurine, L-asparaginic acid or salts thereof, citric acid and vitamin. The medicament can protect the cell membrane, reduce the damage of free radicals to the cell membrane, quickly provide a large amount of energy substances, quickly repair damaged muscle, promote aerobic metabolism and avoid corresponding lactic acid accumulation. The animal experiment proves that the medicament can markedly improve and train the swimming capability of wistars and can prevent skeletal muscle contraction device from being damaged by sports. The medicament provided by the invention is convenient to use, and particularly suitable to athletes practicing endurance events.
Description
Technical field
The present invention relates to a kind of medicine, particularly a kind ofly can protect cell membrane, reduce the medicine of radical pair cell membrane infringement.
Background technology
During fierce physical exertion, the consumption of oxygen obviously increases, make body be in anoxybiotic relatively state, simultaneously, the also corresponding increase of consumption of the antioxidant of body (vitamin C, vitamin E, sulfydryl), the result of the effect of this two aspect, can make and produce a large amount of free radicals in the body, these free radicals will attack human body cell membrane in a organized way, make the lipid generation peroxidating on the cell membrane, the lipid peroxidation injury of cell membranes in tissue shows as tired generation ahead of time at the sport people body, is difficult to after the fatigue recover, thereby motor capacity is descended.In addition, owing to multiple reason, various athletic injury take place through regular meeting in sport people; the particularly damage of muscle cell membrane, pain unbearably, move damage after; sport people not only can't guarantee training, also can bring inconvenience to life, even cause lifelong disaster.Therefore be necessary to develop a kind of product that prevents the cell membrane damage after the strenuous exercise.
In recent years 1; the effect of 6-fructose diphosphate (FDP) has caused everybody attention; FDP is a kind of important intermediate product in the glucose metabolism process, has effects such as protection cell, stabilizing cell membrane, antioxidation and oxygen supply, can be in molecular level adjusted cellular metabolism some enzymatic activitys.Clinically, FDP is mainly used in diseases such as heart failure that a variety of causes causes, ischemia, cerebrovascular disease, diabetes microvascular complication, bronchial asthma, hepatitis, liver cirrhosis, respond well, toxic and side effects is less, just reported with 1 that as CN94111522.4 6-diphosphate fructose in treating diabetes, coronary heart disease, hepatitis have good effect.
General theory thinks that phosphofructose can not oral administration enter in the body, and reason is to contain a large amount of gastric acid in the human gastric juice, contains phosphate in the intestinal juice, after the phosphofructose oral administration enters the intestines and stomach, is decomposed by gastric acid and phosphate, can not enter blood.So in fact, sports team is using 1 really, 6-fructose diphosphate, and often take the intravenous injection mode to use, but injection inconvenient and illegal be self-evident.
In amino acid whose research, taurine and L-aspartic acid have been subjected to extensive attention.Taurine is as a kind of B2 aminoacid of sulfur-bearing, and every scholar proposes taurine and has biological action widely in conjunction with zoopery: the protection cell membrane, regulate osmotic pressure, to anti peroxidation of lipid, two-ways regulation Ca
2+The metabolic adjusting of transmembrane transport, involved in sugar; Taurine can also be by improving muscle glycogen and content of glycogen, and the motor capacity that the content of reduction blood lactic acid improves body has antifatigue effect; Suitable supplementation of taurine is in time eliminated exercise fatigue for keeping systema cariovasculare functional behind the hard training, and motion sickness tools such as prevention myocardial damage have certain effect.Therefore, theoretically, taurine is expected to become a kind of new effective nourishing tonic for sport, and the extensive studies application prospect is arranged.The L-aspartic acid is naturally occurring aminoacid, and its main effect has: 1) enhance vigour allaying tiredness, particularly confirmed fatigue; 2) come the liver protecting by assisting to eliminate too much blood ammonia; 3) combining formed molecular energy with other aminoacid absorbs poison and they can be removed from blood; 4) formation of helper cell running and DNA/RNA.Pharmaceutically mainly as treatment heart disease, liver function-promoter, ammonia detoxicant, tired remover, amino acid transfusion composition, also a kind of good nutritional supplement aspect food industry, and heat is low, do not lose tooth, is commonly used for the sport type beverage additive.
In vivo, vitamin B
1Participate in catabolism of carbohydrate with the coenzyme form, the effect of neuroprotective system is arranged, can also promote enterogastric peristalsis, stimulating appetite.Vitamin B
1Also the nervous tissue and the mental status there are desirable influence, are called as psychogenic vitamin.
Summary of the invention
The damage of various athletic injury, particularly muscle cell membrane takes place in sport people through regular meeting.The purpose of this invention is to provide a kind of easy to usely, can protect cell membrane, reduce the medicine of radical pair cell membrane infringement.Component that medicine of the present invention comprises and weight portion thereof are:
1,6-fructose diphosphate or its salt 30-40
Taurine 12-14
L-aspartic acid or its salt 4-6
Citric acid 1-2
Vitamin B
11-2,
Wherein 1, the weight portion of 6-fructose diphosphate salt and L-aspartate is with corresponding 1,6-fructose diphosphate, L-aspartic acid meter.
Wherein: 1,6-fructose diphosphate salt and L-aspartate are respectively the sodium salts that corresponding active component can be provided, one or more of calcium salt and magnesium salt.
1,6-fructose diphosphate (FDP), not common fructose, as glycometabolic intermediate product, it both can stimulate and quicken glycometabolic course of reaction, had shortened the glycosyloxy time again, for body provides a large amount of energy substances, to quickening skeletal muscle at the volley, many, fast, good, province's effect that the supply of post exercise energy plays, thus the muscle of damage is repaired fast.Use 1, the 6-fructose diphosphate can promote endogenic 1 of our body self, 6-fructose diphosphate, diphospho glycerate and ATP (adenosine triphosphate) increase at double, increase blood supply of cardiac muscle, and myocardial contraction is strengthened, microcirculation improvement, improve the polarized state and the activity that promotes ischemic tissue, organ of cell membrane, have antioxidation, can suppress the myocyte and produce free radical, this recovers and improves cell membrane function to play an important role to keeping the cell integrity.
The present invention adds aspartic acid by to 1 in the 6-fructose diphosphate, changes the pH value in the human stomach, makes 1, and the 6-fructose diphosphate can enter blood by the intestines and stomach smoothly.1,6-fructose diphosphate and taurine and L-aspartic acid synergism, resisting fatigue, the effect of protection cell membrane that can also further improve this medicine.
In the medicine that the present invention relates to, some intermediate products that promote aerobic metabolism have also been added, as citric acid, vitamin B
1, the blood lactic acid of accumulation is come back in the circulation of aerobic metabolism continues the oxidation energy supply.1,6-fructose diphosphate or its salt, taurine, L-aspartic acid or its salt, citric acid and vitamin B
1Synergism had both guaranteed quick energy supplement and the cytothesis effect of FDP, had avoided corresponding lactic acid to pile up again, was that the athlete recovers exercise fatigue, protection cell membrane, reduced the radical pair cell membrane and damaged one of indispensable means.
Medicine of the present invention can also comprise pharmaceutically acceptable adjuvant, with the selection of adjuvant, can be mixed with capsule, tablet, pill or other pharmaceutically acceptable dosage forms as required.Described adjuvant is selected from one or more in the pharmaceutically acceptable adjuvants such as starch, dextrin, Pulvis Talci, cane sugar powder, ethanol, hypromellose (HPMC), carboxymethyl starch sodium (CMS-Na), magnesium stearate.Protection cell membrane involved in the present invention, the various dosage forms of the medicine of reduction radical pair cell membrane infringement prepare by this area conventional method.
The preferred capsule of the pharmaceutical dosage form that the present invention relates to.
Above each batching successively according to ascending mistake 40 mesh sieves of ratio, is removed and sieved the impurity of going up in the retentate, pulverize the back after sieve with pulverizer; Then the material that part by weight is approaching, ascending in proportion order is mixed one by one, fully stirs, and pours capsule into and fills in the mould, make capsule, the powder of the capsule surface of scraping is used the medicine bottle packing, adds desiccant, Cotton Gossypii in the medicine bottle, seal electromagnetic induction film afterwards, spiral cover, sterilization obtains capsule preparations medicine of the present invention.
We find by experiment: medicine of the present invention can significantly improve the swimming exercise ability of trained rat, and the damage that can retardation motion brings to the Skeletal Muscle Contraction device.
The specific embodiment
Following examples are used to illustrate the present invention, but are not used for limiting the scope of the invention.
Embodiment 1
Get each composition following (weight is in g): 1,6-fructose diphosphate 35, taurine 14, L-aspartic acid 5.3, vitamin B
11, citric acid 1.1, and above each batching is sieved in (40 order) according to ratio is ascending successively, remove and sieve the impurity of going up in the retentate, and bulky grain is pulverized the back after sieve with pulverizer; Then the material that part by weight is approaching, ascending in proportion order is mixed one by one, fully stirs, and pours capsule into and fills in the mould, makes capsule, and the powder of the capsule surface of scraping is used the medicine bottle packing.Add desiccant, Cotton Gossypii in the medicine bottle, seal electromagnetic induction film afterwards, spiral cover, sterilization gets protection cell membrane of the present invention, reduces 1 of radical pair cell membrane infringement, 6-fructose diphosphate capsule preparations.
Embodiment 2
Get each composition following (weight is in g): 1,6-fructose diphosphate 40, taurine 14, L-aspartic acid 4, vitamin B
11, citric acid 1, starch 20, dextrin 20, cane sugar powder 20, and with above each batching ascending successively sieving (40 order), Impurity removal in the retentate on the sieve, bulky grain is pulverized the back after sieve with pulverizer.Then the material that part by weight is approaching, ascending in proportion order is mixed one by one, fully stirs, the ethanol of use 80% is as adhesive, make suitable soft material, above soft material is waved the granulator granulation through the YK-160 type of 12 mesh sieve eyes, make wet granular; The wet granular component is divided, treat ethanol volatilization fully after, material is inserted in the multi-functional granulator of DPL-30 type in batches, 50 ℃ of airpillow-dry one hour, makes the final products moisture Control in 5%; Carry out granulate and packing again, obtain protection cell membrane of the present invention, reduce 1 of radical pair cell membrane infringement, 6-fructose diphosphate granular preparation.
Embodiment 3
Get each composition following (weight is in g): 1,6-fructose diphosphate 30, taurine 12, L-aspartic acid 6, vitamin B
12, citric acid 2, starch 5, dextrin 7, and with above each batching ascending successively sieving (40 order), Impurity removal in the retentate on the sieve, bulky grain is pulverized the back after sieve with pulverizer.Then the material that part by weight is approaching, ascending in proportion order is mixed one by one, fully stirs, add the HPMC of above-mentioned material gross weight 1% and 1.5% CMS-Na, with all above-mentioned mixing of materials, the ethanol water of adding 60% fully stirs, and makes soft material; Above soft material is waved the granulator granulation through the YK-160 type of 12 mesh sieve eyes, make wet granular; The wet granular component is divided, treat ethanol volatilization fully after, material is inserted in the multi-functional granulator of DPL-30 type in batches, at 60 ℃ of airpillow-dry, makes dried granule; With adding an amount of magnesium stearate in the granule, be pressed into tablet with tablet machine and get protection cell membrane of the present invention, reduce 1 of radical pair cell membrane infringement, 6-fructose diphosphate tablet.
Embodiment 4
Get embodiment 1 gained capsule and carry out animal experiment.
One, experimental subject and method
1. object of study
76 of male Wistar rats, average weight 166.6 ± 16.6g (providing) by Department Of Medicine, Peking University's Experimental Animal Center, rat is divided into quiet matched group (Con), training group (Train), the additional active sugar of training (compound recipe 1,6-fructose diphosphate) group (TFdp) at random after laboratory adapts to three days.Every group of rat is divided into two groups according to slaughtering the difference of time after the final motion again, and specifically grouping situation sees Table 1.
Table 1 rat grouping situation
2. train and additional project
The mode of rat motor is swimming, and 30 ± 1 ℃ of water temperatures have current, and water velocity is 6 cubic metres/hour.Rat carries out adaptability swimming in three days, about 15 minutes every days before carrying out swimming instruction.Rat carries out the swimming exercise training in 6 weeks by a definite date by following scheme (seeing Table 2), trains Saturday, day rest weekly 5 days.Rat finally carries out a power and exhausts swimming exercise.
Table 2 rats'swimming training program
3. draw materials and processing method
By lumbar injection pentobarbital solution anesthetized animal, anaesthesia dosage is the 0.25g/Kg body weight.Taken a blood sample by ventral aorta, anticoagulant heparin is with 4 ℃ of refrigerated centrifuger insulations, 3000 rev/mins of rotating speeds centrifugal 10 minutes, are got blood plasma, and adding alpha-mercapto ethanol (final concentration is 5mmol/L) and EGTA (final concentration is 7.5mmol/L) ,-80 ℃ of cryogenic refrigerators store up to detection.Get the homonymy musculus soleus, put into 3% glutaraldehyde fixative rapidly, fix 2 hours, in order to making the ultramicroscope section.
The ultramicroscope section is prepared: (1) routine is drawn materials, and 3% glutaraldehyde is fixed 2 hours; Fix 1.5 hours behind (2) the 1% 4 oxidation blades of a sword; (3) 50%～100% ethanol dewater step by step, and each is 10 minutes; (4) epoxy resin: pure acetone (1: 1) soaked into 2 hours; (5) epon 812+815 embeddings; (6) with Leica ultramicrotome section (50nm); (7) after the plumbous dyeing of uranium, observe with the JEM-100 ultramicroscope.
4. detect index and instrument and equipment
Plasma CK gross activity: enzyme kinetics method.The CK detectable that Beijing Zhongsheng Biological Engineering High Technology Company produces.Japan HITACHI7170A type automatic clinical chemistry analyzer.
Plasma CK isozyme: agarose gel electrophoresis method for detecting.CK isozyme electrophoresis film and reagent that Helena Laboratories company produces.Helena Rep-I type electrophresis apparatus.
Rat power exhausts the electron microscopic observation of musculus soleus degree of impairment behind the swimming exercise: the musculus soleus of every group of optional two rats prepares the ultramicroscope section, for each ultramicroscope section, at first in the low power field of 2000 times of amplifications, determine viewing area, then according to the imaging readability, in the visual field of 8000～10000 times of amplifications, observe myofibrillar degree of impairment, main regular degree of observing sarcostyle and muscle segment arrangement, the complete situation and the position relation of muscle segment oolemma (I band) and blanking bar (A band).This research reflects the degree of injury of skeletal muscle by the unusual rate of skeletal muscle fiber Z line.Z line ANOMALOUS VARIATIONS comprises that Z linear flow, Z line blur, the Z line twists and the Z heading line off, and the Z line that has above-mentioned any situation to occur all be can be regarded as unusual Z line.The percentage rate that unusual Z line number accounts for observed Z line sum promptly is the unusual rate of Z line.The observed Z line sum of every animal is more than 1500.Ultramicroscope is the JEOLJEM-100CX II scanning electron microscope that Japanese HITACHI company produces.
Power exhausts the swimming exercise time: with the rats'swimming exercise not harmony, the struggle shape appears, and the underwater of the submerging standard that do not emerge and exhaust for swimming exercise power 5 seconds.
5. data statistics
All data all use CASIO fx-100 computer and SAS statistical software to calculate and statistical disposition.To each group data owner will being described property statistics, t check and variance analysis.Showing property level is P＜0.05.
Two, result of study
1. rat power exhausts behind the swimming exercise Plasma CK and isozyme changes
By table 3 as seen, the activity level of Plasma CK at once that Con group rat power exhausts behind the swimming exercise is the highest, but respectively organizes the corresponding Plasma CK activity level of rat there was no significant difference with other; Each is organized rat and recovered through 36 hours, and Plasma CK and isozyme activated water thereof average significantly (P＜0.05) are lower than the level of its immediate postexercise.
Table 3 rat power exhausts behind the swimming exercise and exercise recovery Plasma CK activity change after 36 hours
Significance level (P＜0.05): a1b1, a2b2, a3b3, a4b4, c1d1, c2d2, c3d3, c4d4, e1f1, e2f2, e3f3, e4f4.
2. the variation of the unusual rate of musculus soleus fiber Z line after rat power exhausts the swimming exercise time and moves
By table 4 as seen, it is the longest that TFdp group rat power exhausts time of swimming exercise, its level not only remarkable (P＜0.05) is longer than the movement time of Con group rat, and significantly (P＜0.05) is longer than the movement time of Train group rat, the movement time of Train group rat is longer than the movement time of Con group rat, but does not meet the requirements of significance level.
The variation of the unusual rate of musculus soleus fiber Z line after table 4 rat power exhausts the swimming exercise time and moves
Significance level (P＜0.05): ny py dhjh
TfdpI group rat power exhaust the unusual rate of musculus soleus Z line behind the swimming exercise respectively significantly (P＜0.05) be lower than the unusual rate of musculus soleus Z line behind ConI and the TrainI group rat motor; And respectively organize behind the rat motor the unusual rate of musculus soleus Z line at once and recovered in 36 hours after the unusual rate of musculus soleus Z line do not have significant difference.
Three, conclusion
The time that the trained rat power of replenishing active sugar in this research exhausts swimming exercise not only significantly (P＜0.05) power of being longer than non-trained rat exhaust swimming time, and than the movement time of trained rat significantly (P＜0.05) increase.This result shows, replenishes the swimming exercise ability that this invention preparation can significantly improve trained rat.The rat power of replenishing this invention preparation exhaust the unusual rate of motion back musculus soleus Z line significantly (P＜0.05) result of being lower than the unusual rate of trained rat motion back musculus soleus Z line show the damage that said preparation can retardation motion brings to the Skeletal Muscle Contraction device.
Claims (7)
1, a kind of medicine, it contains the active ingredient of following weight portion:
1,6-fructose diphosphate or its salt 30-40
Taurine 12-14
L-aspartic acid or its salt 4-6
Citric acid 1-2
Vitamin B
11-2,
Wherein 1, the weight portion of 6-fructose diphosphate salt and L-aspartate is with corresponding 1,6-fructose diphosphate, L-aspartic acid meter.
2, medicine as claimed in claim 1 is characterized in that, it contains the active ingredient of following weight portion:
1,6-fructose diphosphate or its salt 35
Taurine 14
L-aspartic acid or its salt 5.3
Citric acid 1
Vitamin B
11.1,
Wherein 1, the weight portion of 6-fructose diphosphate salt and L-aspartate is with corresponding 1,6-fructose diphosphate, L-aspartic acid meter.
3, medicine as claimed in claim 1 is characterized in that 1, and 6-fructose diphosphate salt is 1, the corresponding sodium salt of 6-fructose diphosphate, calcium salt, one or more of magnesium salt and organic salt.
4, medicine as claimed in claim 1 is characterized in that the L-aspartate is the corresponding sodium salt of L-aspartic acid, calcium salt, one or more of magnesium salt and organic salt.
5, medicine as claimed in claim 1 is characterized in that, also contains to be selected from starch, dextrin, Pulvis Talci, cane sugar powder, ethanol, magnesium stearate, HPMC, CMS-Na or other the pharmaceutically acceptable adjuvant one or more.
As the arbitrary described medicine of claim 1～5, it is characterized in that 6, it is tablet, capsule, pill or other pharmaceutically acceptable dosage form.
As the described medicine of claim 1～5, it is characterized in that 7, it is a capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101041183A CN101559064A (en) | 2008-04-15 | 2008-04-15 | Medicament capable of protecting cell membrane |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101041183A CN101559064A (en) | 2008-04-15 | 2008-04-15 | Medicament capable of protecting cell membrane |
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| CN101559064A true CN101559064A (en) | 2009-10-21 |
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|---|---|---|---|
| CNA2008101041183A Pending CN101559064A (en) | 2008-04-15 | 2008-04-15 | Medicament capable of protecting cell membrane |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013118136A1 (en) * | 2012-02-09 | 2013-08-15 | Zota Health Care Ltd | Stable taurine oral composition |
-
2008
- 2008-04-15 CN CNA2008101041183A patent/CN101559064A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013118136A1 (en) * | 2012-02-09 | 2013-08-15 | Zota Health Care Ltd | Stable taurine oral composition |
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Open date: 20091021 |