CN102652761A - Composition with blood uric acid adjusting function - Google Patents
Composition with blood uric acid adjusting function Download PDFInfo
- Publication number
- CN102652761A CN102652761A CN2011100500206A CN201110050020A CN102652761A CN 102652761 A CN102652761 A CN 102652761A CN 2011100500206 A CN2011100500206 A CN 2011100500206A CN 201110050020 A CN201110050020 A CN 201110050020A CN 102652761 A CN102652761 A CN 102652761A
- Authority
- CN
- China
- Prior art keywords
- uric acid
- chimonin
- poria
- blood uric
- compositions
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 title claims abstract description 62
- 239000000203 mixture Substances 0.000 title claims abstract description 49
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- TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 title abstract description 38
- 229940116269 uric acid Drugs 0.000 title abstract description 38
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention relates to the field of medicines and discloses a composition with a blood uric acid adjusting function. The composition consists of mangiferin and poria in a mass ratio of 1:0.1-100 and can be combined with conventional auxiliary materials to prepare a medicament and functional food with the blood uric acid adjusting function. The composition with the blood uric acid adjusting function can be used for remarkably improving the blood uric acid reduction effect, promoting the discharge of uric acid, compensating the shortcoming of the uric acid discharging function of the mangiferin and greatly reducing the influence on renal functions due to taking the single mangiferin reparation for a long time, and has the effect of assisting in improving the immunity. The medicament and functional food with the blood uric acid adjusting function prepared from the composition disclosed by the invention has the advantages of being simple in production process, stable in product quality, clear in functional factor, outstanding in health care effect, small in taking dosage, safe to use, free from side and toxic effects and the like, and is suitable for being taken by wide population with high uric acid.
Description
Technical field
The present invention relates to field of medicaments, relate to a kind of compositions of regulating the blood uric acid function that has specifically.
Background technology
Hyperuricemia is meant that disorder has taken place the metabolism of purine substance in the human body, and the oxidative metabolism product uric acid volume of production of purine is superfluous or drain bad accumulation in vivo, causes hyperlithic phenomenon in the blood.According to statistics, about 1.3 hundred million people of present domestic hyperuricemia patient account for 10% of total population, and hyperuricemia becomes the fourth-largest disease after hypertension, hyperlipidemia and hyperglycemia, is threatening human health.Hyperuricemia further develops and will form gout, has 10～15% hyperuricemia crowd to be prone to cause gout according to statistics at present.Gout is that uric acid level is lasting too high; Form with sodium salt is deposited in joint, soft tissue, cartilage and the kidney; Cause the foreign body inflammatory reaction of tissue, red, swollen, hot, gouty arthritis phenomenon such as have an intense pain takes place or cause diseases such as subcutaneous gout calculus, kidney stone or gouty nephropathy.The state of an illness further develops, and the difficult renal failure that reverses then occurs and threat to life.The probability of suffering from gout significantly increases along with the rising of uric acid concentration in the blood.
The medicine of treatment gout and hyperuricemia is very limited at present, mainly is allopurinol, benzbromarone and colchicine etc., and these drug side effectes are big, and patient usually can not tolerate, and has limited its use to a certain extent.Because hyperuricemia and gout are chronic disease often, administration time is longer, and gout and the antihyperuricemic disease drug of seeking novel low toxicity still are focuses of present pharmacy and functional food research.
Chimonin is the two benzene pyrrones chemical compounds of carbon glycoside, genus of tetrahydroxy pyrrone, and structural formula does
The leaf, fruit and the bark that mainly are present in mango (Mangifera indica.L), almond (Mangifera persiciformis); The root of Herba Hyperici perforati [St.Johns ' wort (H ypericum perforatum L.)] and syringa reticulata var mandshurica [Salacia reticulata (SRE)], the aerial parts of gentianaceae plant Northeastern Radix Gentianae (Gentiana manshuricaKitag), west, river Herba Swertiae bimaculatae (Swertia mussotii Franch), the liliaceous plant Rhizoma Anemarrhenae (Anemarrhenaasphodeloides Bge.), fire hose section plant Herba Pyrrosiae Calvatae [Pyrrosiaclvata (Bak) Chin] and thymelaeceae trees (Gnidia involucrata).Multiple pharmacologically actives such as existing existing report chimonin has antitussive, eliminates the phlegm, regulates immunity, antiinflammatory, analgesia, hepatic cholagogic, anti peroxidation of lipid, antiviral, antibiotic, antitumor, anti-diabetic.Patent CN200810058019.6 discloses the purposes that chimonin, Isomangiferin and mango aglycone have the hyperuricemia of preventing and treating and gout; Chimonin has the effect that reduces metabolic arthritis animal serum uric acid level; 1.9 μ mol/kg dosage promptly can obviously reduce the effect of hyperuricemia mice serum uric acid level, makes the hyperuricemia level of animal model mice return to normal level, activity is higher than allopurinol; Mechanism is relevant with the inhibition xanthine oxidase; Toxic and side effects is low, and the maximum tolerated dose of mouse stomach administration is 47mmol/kg, demonstrates characteristics efficient, low toxicity.
Yet chimonin is the active component of non-uricosuric excretion pattern uric acid resisting, aspect the uricosuric drainage effect not obvious, take chimonin merely and exist short-term to use uric acid to rebound, take for a long time the problem that renal function is had certain influence very soon.
Summary of the invention
In view of this, the present invention seeks to deficiency, a kind of compositions of regulating the blood uric acid function that has is provided to chimonin releasing uric acid function.
For realizing the object of the invention, the present invention adopts following technical scheme:
A kind of compositions with adjusting blood uric acid function is made up of chimonin and Poria, and the weight ratio of said chimonin and Poria is 1: 0.1～100.
Many researchs show that long-term heavy dose of diuretic of using can cause untoward reaction such as blood uric acid rising, gout; Conventional diuretic and uric acid resisting components compatibility tend to produce antagonism (Lukas E; Spieker, Frank T, et al; The management of hyperuricernia and gout in patient with heartfaiure; The European Journal of Heart Failure, 4 (2002)), chimonin and conventional diuretic can not play synergistic function.
Poria (Poria) is the dry sclerotia of Polyporaceae fungus Poria (Poria cocos (schw) Wolf.), but is the resource of China's Ministry of Public Health identification medicine-food two-purpose.The Poria nature and flavor are sweet, light, property is flat, are included into heart spleen lung meridian, have promoting diuresis to eliminate damp pathogen, invigorating the spleen and regulating the stomach, the effect of mind tranquilizing and the heart calming is used to treat dysuria, the edema overflow, the phlegm retention cough with dyspnea, vomit dirty, have loose bowels etc.The Poria main chemical compositions is polysaccharide, triterpene, fatty acid, sterol etc.Modern pharmacological research shows, pachyman have anticancer with increase effect such as immunity.The Poria effect is very extensive, with various compatibility of drugss, is regardless of the four seasons, regardless of cold, temperature, wind, wet all diseases, can both bring into play its unique effects, is called " 4 o'clock refreshing medicines " by ancients.Do not see as yet at present research with the compositions of regulating the blood uric acid function that contains in chimonin and Poria and products thereof is arranged.
Find the Poria combination of chimonin and 0.1～100 times of weight through a large amount of compatibility screening studies; Can significantly improve the effect of falling blood uric acid; Remedy the deficiency of chimonin releasing uric acid function; Significantly reduced because of taking the influence of chimonin for a long time, had the effect that the skeptophylaxis function improves simultaneously renal function.
In a specific embodiments, the present invention is through the influence test of said chimonin compositions to the acid of normal mouse retention, proves that chimonin compositions according to the invention do not have obvious influence to the normal mouse blood uric acid.
In a specific embodiments; The present invention is through relatively chimonin and said chimonin compositions are tested the influence of the inductive acute hyperuricemia mice of Oteracil Potassium uric acid; Prove that chimonin compositions according to the invention can significantly reduce the serum uric acid level of hyperuricemia mice; And the chimonin compositions Deng molar dose is compared with chimonin; The weight ratio of chimonin and Poria is that 1: 0.1～100 dose groups serum uric acid levels all are lower than the chimonin group, shows that the effect that blood uric acid falls in chimonin compositions according to the invention is better than the agent of chimonin list.
In another embodiment; The present invention is through comparing chimonin and said chimonin compositions to the phenol red excretory influence of normal rat; Prove that chimonin compositions according to the invention has the significance facilitation to urate excretion, and the agent of chimonin list there is not facilitation to urate excretion.
As preferably, according to the invention have a compositions of regulating the blood uric acid function, and the weight ratio of said chimonin and Poria is 1: 1～50.
Chimonin according to the invention is from leaf fruit of Anacardiaceae plant mango (Mangifera indica.L) and bark, to extract to obtain.
The present invention also provides said compositions to have the medicine of adjusting blood uric acid function and the application in the functional food in preparation.
Compositions with adjusting blood uric acid function according to the invention can be processed with the adjuvant combination of routine has the medicine of regulating the blood uric acid function, comprises oral liquid, granule, tablet, pill, powder, capsule and drop pill etc.
Compositions according to the invention can also be prepared into has the functional food of regulating the blood uric acid function.Functional food according to the invention comprises the said compositions of regulating the blood uric acid function that has.Functional food is meant that suitable specific crowd is edible, has the adjusting body function, is not purpose with the treatment disease, and human body is not produced the food of any acute, subacute or chronic hazard.Functional food according to the invention can be the bread and cheese form, also can be medicine form such as hard capsule, soft capsule, tablet, oral liquid, medicated wine, granule, powder, the bag bitter edible plant etc.
Preferably, functional food according to the invention is tablet, soft capsule, hard capsule, granule or sweet cream.
According to the invention have the compositions of regulating the blood uric acid function and combined by the Poria of chimonin and 0.1～100 times of weight and can significantly improve the effect of falling blood uric acid; Promote urate excretion; Remedied the deficiency of chimonin releasing uric acid function; Significantly reduced because of taking the influence of chimonin for a long time, had the effect that the skeptophylaxis function improves simultaneously renal function.It is simple that medicine and the functional food of regulating the blood uric acid function by having of preparation of compositions according to the invention has production technology, constant product quality, and functional factor is clear; Health-care efficacy is outstanding, and taking dose is little, and is safe in utilization; Advantage such as have no side effect, suitable vast metabolic arthritis crowd is edible.
The specific embodiment
The embodiment of the invention discloses a kind of compositions of regulating the blood uric acid function that has.Those skilled in the art can use for reference this paper content, suitably improve technological parameter and realize.Special needs to be pointed out is that all similarly replace and change apparent to those skilled in the art, they all are regarded as and are included in the present invention.Product of the present invention is described through preferred embodiment, and the related personnel obviously can change or suitably change and combination product as herein described in not breaking away from content of the present invention, spirit and scope, realizes and use technology of the present invention.
In order further to understand the present invention, the present invention is elaborated below in conjunction with embodiment.
Embodiment 1: chimonin compositions according to the invention is to the influence of normal mouse retention acid
110 of male mouse of kunming, body weight 18～22g is divided into 9 groups at random, 10 every group, is respectively: normal control group, 4 various dose groups of chimonin, chimonin: 4 various dose groups of compositions (hereinafter to be referred as chimonin compositions group) of Poria=1: 20.Test-compound is mixed with suspension with 0.5% sodium carboxymethyl cellulose (0.5%CMC-Na).The normal control group is irritated stomach and is given equal-volume solvent (0.5%CMC-Na), and chimonin group and chimonin compositions group are irritated stomach according to chimonin content 1.0,3.0,10.0,30.0mg/kg, press 10ml/kg gastric infusion every day 2 times, continuous 5 times.1h after the last administration extracts eyeball and gets blood, and the centrifugal 10min of 3000rpm gets serum, adopts the phosphotungstic acid method to measure serum uric acid level, and the result sees table 1.
5 influences of table 1 chimonin gastric infusion to normal mouse retention acid
Annotate: x ± s, n=10, (t-test) compared with the normal control group in * P＜0.05.
Visible by table 1; Behind the gastric infusion 5 times; Chimonin and chimonin compositions are except that the 30.0mg/kg dose groups reduces intact animal's serum uric acid level; All the other dose groups all do not have the effect that reduces the normal mouse serum uric acid level, show that compositions according to the invention does not influence intact animal's serum uric acid level in the therapeutic dose scope.
Embodiment 2: chimonin compositions according to the invention is to the influence of hyperuricemia mice serum uric acid
140 of healthy male Kunming mouses, body weight 18-22g provides [laboratory animal production licence number: SCXK (Yunnan) 2005-2008] by unming Medical College's Experimental Animal Center.Animal is divided into normal control group, hyperuricemia model group, chimonin at random: Poria=compositions (according to the chimonin cubage) 0.78,1.56,3.13 in 1: 0.1 and 6.25mg/kg dose groups and chimonin: Poria different proportion dose groups.Test-compound is mixed with suspension with 0.5% sodium carboxymethyl cellulose (0.5%CMC-Na), irritates stomach and gives every day 2 times, continuous 5 times.
The hyperuricemia formative method: mice is 2h lumbar injection 400mg/kg oxonic acid potassium salt before blood sampling, and it is active to suppress uricase, causes hyperuricemia mice (Pathogenesis of Gout.Annals of InternalMedicine.2005; 143 (7): 499-516.); The normal control group is then injected equal-volume 0.5%CMC-Na solution, irritates stomach behind the injection 1h and carries out the last administration, extracts eyeball behind the 2h and gets blood; The centrifugal 5min of 3000rpm; Get serum, adopt enzymic colorimetric (Zhongsheng Beikong Biological Science & Technology Co., Ltd.'s test kit) to measure serum uric acid level, the result sees table 2.
Table 2 chimonin compositions gastric infusion is to the influence of hyperuricemia mice serum uric acid level
Annotate: x ± s, n=10,
The Δ ΔP＜0.01 is compared with the normal control group (t-test check);
*P＜0.05,
*P＜0.01 is compared with the hyperuricemia model matched group (t-test check),
aP＜0.05 be with dosage such as chimonin group relatively.
Visible by table 2 result, the animal serum uric acid level significantly raises behind the lumbar injection Oteracil Potassium, compares with the normal control group, and significant difference is arranged, the hints model success.Behind the gastric infusion 5 times; Chimonin compositions (1: 0.1) group serum uric acid level is starkly lower than the hyperuricemia model group; And present dose dependent, compare significant difference, and the weight ratio of chimonin and Poria is that 1: 0.1～200 dose groups serum uric acid levels all are starkly lower than the hyperuricemia model group with the hyperuricemia model group; Significant difference (P＜0.05,0.01) is arranged.In addition; In chimonin content; Chimonin compositions Deng molar dose is compared with chimonin, and except that the weight ratio of chimonin and Poria was 1: 200 dose groups, other ratio dose groups serum uric acid level all was lower than the chimonin group; The compositions that shows chimonin according to the invention and 0.1～100 times of weight Poria can reduce the inductive acute hyperuricemia mice serum of Oteracil Potassium uric acid level, and the effect of falling blood uric acid is better than the agent of chimonin list.
Embodiment 3: chimonin compositions according to the invention is to the phenol red excretory influence of normal rat
70 of male SD rats, body weight 130～150g is divided into 7 groups at random, 10 every group; Be respectively: normal control group, 3 various dose groups of chimonin dose groups, chimonin: 3 various dose groups of compositions of Poria=1: 30, irritate stomach respectively and give equal-volume solvent (0.5%CMC-Na), chimonin and chimonin compositions (pressing the chimonin cubage) 3.0,6.0,12.0mg/kg, press 10ml/kg administration every day 1 time, totally 7 times; Reference literature (H.G Wo Geer, W.H Wo Geer writes. Du Guanhua; Li Xuejun, Zhang Yongxiang waits and translates. and pharmacological experiment guide--new drug is found and pharmacological evaluation. front page; 2001, p238-239.) method tail vein injection 3% phenol red (2.5ml/kg) behind last administration 30min, blood 20 μ L are got in injection back 15,30,60,180min docking; Add in the 0.2mL normal saline, the centrifugal 5min of 3000rpm gets supernatant 100 μ L; Add 100 μ L, 0.1% sodium carbonate liquor and 800 μ L normal saline, survey the OD value at the 546nm place, the result sees table 3.
Table 3 chimonin compositions is to the phenol red excretory influence of normal rat
Annotate: x ± s, n=10,
aP＜0.05,
bP＜0.01 is compared with the normal control group.
Visible by table 3 result, behind the phenol red 15min of tail vein injection, the phenol red OD value in each dose groups animal blood of chimonin all significantly is lower than normal control group (P＜0.05,0.01), minimizing trend is also arranged behind the 30min, but do not reach statistically-significant difference; Phenol red OD value in each dose groups animal blood of chimonin compositions all significantly is lower than normal control group (P＜0.05,0.01), and the OD value all significantly reduces behind the 30min, and with compared with normal, difference has statistical significance.The result shows that the agent of chimonin list does not have facilitation to urate excretion, and chimonin compositions according to the invention has the significance facilitation to urate excretion.
Embodiment 4: the chimonin tablet
Prescription is formed (by 1000 calculating)
Chimonin 100g
Poria 100g
Dextrin 100g
Calcium carbonate 50g
Mannitol 50g
Polyvinylpolypyrrolidone 10g
Magnesium stearate 5g
Micropowder silica gel 5g
The about 250g of 95% ethanol
Method for making:
1, Poria is beaten powder, cross 100 mesh sieves, it is subsequent use to get Poria powder.
2, chimonin, Poria, dextrin, calcium carbonate, mannitol, the polyvinylpolypyrrolidone with recipe quantity adds 6 speed stirrings in the efficient wet granulator, high-speed cutting premixing 3min.95% ethanol 250g is added in the efficient wet granulator, and 6 speed stir, high-speed cutting 3min.50 ± 5 ℃ of drying 15～25min of EAT.Sieve granulate with 1.5mm, add magnesium stearate, micropowder silica gel, the mixing of recipe quantity, subsequent use.
3, tabletting, packing, check gets product.
Embodiment 5: the chimonin capsule
Prescription is formed (by 1000 calculating)
Chimonin 50g
Poria 200g
Calcium carbonate 50g
Mannitol 20g
Pregelatinized Starch 110g
Carboxymethyl starch sodium 20g
Magnesium stearate 5g
Micropowder silica gel 2g
Method for making:
1, Poria is beaten powder, cross 100 mesh sieves, it is subsequent use to get Poria powder.
2, chimonin, Poria, calcium carbonate, mannitol, pregelatinized Starch, the carboxymethyl starch sodium with recipe quantity adds 6 speed stirrings in the efficient wet granulator, high-speed cutting premixing 3min.About 200g adds in the efficient wet granulator with 5% pregelatinized Starch slurry, and 6 speed stir, high-speed cutting 2min.50 ± 5 ℃ of drying 15～20min of EAT.Sieve granulate with 1.5mm, add magnesium stearate, micropowder silica gel, the mixing of recipe quantity, subsequent use.
3, fill out capsule, packing, check gets product.
Embodiment 6: soft capsule type chimonin functional food
Prescription is formed (by 1000 calculating)
Content: chimonin 30g
Poria 300g
Soybean oil 282g
Cera Flava 14g
Softgel shell: gelatin 102g
Glycerol 35g
Methyl parahydroxybenzoate 4g
Propyl p-hydroxybenzoate 0.1g
Milk chocolate palm fibre 1g
Purified water 100g
Method for making:
1, Poria is beaten powder, further super-refinement, it is subsequent use to get the Poria micropowder.
2, the soybean oil and the Cera Flava heating of recipe quantity are dissolved mix homogeneously, the Poria powder and the chimonin mixing of adding recipe quantity.
3, with in the gelatin of recipe quantity, glycerol, the purified water input glue jar, be heated to 75 ℃, stir 1.5h, the methyl parahydroxybenzoate, propyl p-hydroxybenzoate, the milk chocolate palm fibre that add recipe quantity stir subsequent use.
4, adopt the pressing pelleting.Through washing ball, the ball that dries in the air, drying, pick up ball, packing, check gets product.
Embodiment 7: granular pattern chimonin functional food
Prescription is formed (by 1000 bags of calculating)
Chimonin 200g
Poria 50g
Maltodextrin 20g
Water soluble starch 100g
Icing Sugar 200g
Mannitol 50g
Magnesium stearate 5g
Micropowder silica gel 5g
The about 250g of 85% ethanol
Method for making:
1, Poria is beaten powder, cross 100 mesh sieves, it is subsequent use to get Poria powder.
2, chimonin, Poria, maltodextrin, water soluble starch, Icing Sugar, the mannitol with recipe quantity adds 6 speed stirrings in the efficient wet granulator, high-speed cutting premixing 3min.85% ethanol 250g is added in the efficient wet granulator, and 6 speed stir, high-speed cutting 3min.50 ± 5 ℃ of drying 15～25min of EAT.Sieve granulate with 1.5mm, add magnesium stearate, micropowder silica gel, the mixing of recipe quantity, subsequent use.
3, packing, check gets product.
Embodiment 8: honey paste type chimonin functional food
Prescription is formed (calculating by 1000 cream)
Chimonin 10g
Poria 1000g
Refined honey is an amount of
Sucrose is an amount of
Method for making:
1, Poria is beaten powder, it is subsequent use to get Poria powder.
2, the chimonin micronization is subsequent use.
3, get Poria, decocte with water 3 times, decocting liquid filters, and filtrating merges, and being condensed into relative density is the clear paste of 1.2～1.4 (80 ℃).Every 100g clear paste adds refined honey 200g or sucrose 200g, and heating makes dissolves, mixing, and the cooling back adds chimonin powder, mixing.
4, packing, check gets product.
The explanation of above embodiment just is used for helping to understand the present invention and core concept thereof.Should be pointed out that for those skilled in the art, under the prerequisite that does not break away from the principle of the invention, can also carry out some improvement and modification to the present invention, these improvement and modification also fall in the protection domain of claim of the present invention.
Claims (7)
1. one kind has the compositions of regulating the blood uric acid function, it is characterized in that be made up of chimonin and Poria, the mass ratio of said chimonin and Poria is 1: 0.1～100.
2. according to the said compositions of claim 1, it is characterized in that the weight ratio of said chimonin and Poria is 1: 1～50.
3. claim 1 or 2 said compositionss have the medicine of adjusting blood uric acid function and the application in the functional food in preparation.
4. comprise the medicine of claim 1 or 2 said compositionss, it is characterized in that, process with conventional adjuvant combination by said compositions with adjusting blood uric acid function.
5. a functional food is characterized in that, comprises claim 1 or 2 said compositionss with adjusting blood uric acid function.
6. according to the said functional food of claim 5, it is characterized in that said functional food is tablet, soft capsule, hard capsule, granule or sweet cream.
7. according to the said functional food of claim 5, it is characterized in that each preparation unit contains chimonin 1～200mg in the said functional food.
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