CN104083751B - A kind of medical composition and its use for cirrhosis treatment - Google Patents
A kind of medical composition and its use for cirrhosis treatment Download PDFInfo
- Publication number
- CN104083751B CN104083751B CN201410342881.5A CN201410342881A CN104083751B CN 104083751 B CN104083751 B CN 104083751B CN 201410342881 A CN201410342881 A CN 201410342881A CN 104083751 B CN104083751 B CN 104083751B
- Authority
- CN
- China
- Prior art keywords
- group
- cirrhosis
- salicifoline
- catechin
- pharmaceutical composition
- 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.)
- Expired - Fee Related
Links
- 208000019425 cirrhosis of liver Diseases 0.000 title claims abstract description 26
- 206010016654 Fibrosis Diseases 0.000 title claims description 15
- 230000007882 cirrhosis Effects 0.000 title claims description 14
- 239000000203 mixture Substances 0.000 title abstract description 7
- REIMFKRWHOKOHQ-UHFFFAOYSA-O Salicifoline Chemical compound COC1=CC=C(CC[N+](C)(C)C)C=C1O REIMFKRWHOKOHQ-UHFFFAOYSA-O 0.000 claims abstract description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 18
- CQOVPNPJLQNMDC-ZETCQYMHSA-N carnosine Chemical compound [NH3+]CCC(=O)N[C@H](C([O-])=O)CC1=CNC=N1 CQOVPNPJLQNMDC-ZETCQYMHSA-N 0.000 claims abstract description 15
- PFTAWBLQPZVEMU-DZGCQCFKSA-N (+)-catechin Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-DZGCQCFKSA-N 0.000 claims abstract description 12
- ADRVNXBAWSRFAJ-UHFFFAOYSA-N catechin Natural products OC1Cc2cc(O)cc(O)c2OC1c3ccc(O)c(O)c3 ADRVNXBAWSRFAJ-UHFFFAOYSA-N 0.000 claims abstract description 12
- 235000005487 catechin Nutrition 0.000 claims abstract description 12
- 229950001002 cianidanol Drugs 0.000 claims abstract description 12
- CCODQELMBJQZIT-UHFFFAOYSA-N salicifoline Natural products CC(C)C(=O)OC1(C)CC2(OC(=O)C)C(C1OC(=O)C)C(OC(=O)C)C3(O)CC4(OC4C(C)(C)C(OC(=O)C)C(OC(=O)C)C3OC(=O)C)C(C)C2=O CCODQELMBJQZIT-UHFFFAOYSA-N 0.000 claims abstract description 12
- 239000003814 drug Substances 0.000 claims abstract description 9
- 108700035912 polaprezinc Proteins 0.000 claims abstract description 8
- 229950004693 polaprezinc Drugs 0.000 claims abstract description 8
- 239000011701 zinc Substances 0.000 claims description 5
- 229910052725 zinc Inorganic materials 0.000 claims description 5
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 4
- 238000002360 preparation method Methods 0.000 claims description 3
- 229940079593 drug Drugs 0.000 abstract description 5
- VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 description 9
- 125000004403 catechin group Chemical group 0.000 description 6
- 210000004185 liver Anatomy 0.000 description 6
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- 239000007864 aqueous solution Substances 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000000835 fiber Substances 0.000 description 4
- 230000001629 suppression Effects 0.000 description 4
- 102000002260 Alkaline Phosphatase Human genes 0.000 description 3
- 108020004774 Alkaline Phosphatase Proteins 0.000 description 3
- 206010009208 Cirrhosis alcoholic Diseases 0.000 description 3
- 208000010002 alcoholic liver cirrhosis Diseases 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 210000003462 vein Anatomy 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
- 108010087806 Carnosine Proteins 0.000 description 2
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 2
- CQOVPNPJLQNMDC-UHFFFAOYSA-N N-beta-alanyl-L-histidine Natural products NCCC(=O)NC(C(O)=O)CC1=CN=CN1 CQOVPNPJLQNMDC-UHFFFAOYSA-N 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- 229930003268 Vitamin C Natural products 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000003651 drinking water Substances 0.000 description 2
- 235000020188 drinking water Nutrition 0.000 description 2
- 230000004761 fibrosis Effects 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
- 239000004006 olive oil Substances 0.000 description 2
- 235000008390 olive oil Nutrition 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 235000019154 vitamin C Nutrition 0.000 description 2
- 239000011718 vitamin C Substances 0.000 description 2
- LSHVYAFMTMFKBA-TZIWHRDSSA-N (-)-epicatechin-3-O-gallate Chemical compound O([C@@H]1CC2=C(O)C=C(C=C2O[C@@H]1C=1C=C(O)C(O)=CC=1)O)C(=O)C1=CC(O)=C(O)C(O)=C1 LSHVYAFMTMFKBA-TZIWHRDSSA-N 0.000 description 1
- UJOYFRCOTPUKAK-MRVPVSSYSA-N (R)-3-ammonio-3-phenylpropanoate Chemical compound OC(=O)C[C@@H](N)C1=CC=CC=C1 UJOYFRCOTPUKAK-MRVPVSSYSA-N 0.000 description 1
- CVOFKRWYWCSDMA-UHFFFAOYSA-N 2-chloro-n-(2,6-diethylphenyl)-n-(methoxymethyl)acetamide;2,6-dinitro-n,n-dipropyl-4-(trifluoromethyl)aniline Chemical compound CCC1=CC=CC(CC)=C1N(COC)C(=O)CCl.CCCN(CCC)C1=C([N+]([O-])=O)C=C(C(F)(F)F)C=C1[N+]([O-])=O CVOFKRWYWCSDMA-UHFFFAOYSA-N 0.000 description 1
- -1 3-aminopropionyl Chemical group 0.000 description 1
- 206010003445 Ascites Diseases 0.000 description 1
- 102000004625 Aspartate Aminotransferases Human genes 0.000 description 1
- 108010003415 Aspartate Aminotransferases Proteins 0.000 description 1
- JFRODOMNEMNAAA-UHFFFAOYSA-N C[N](C)(C)CCc(cc1O)ccc1OC Chemical compound C[N](C)(C)CCc(cc1O)ccc1OC JFRODOMNEMNAAA-UHFFFAOYSA-N 0.000 description 1
- 208000003322 Coinfection Diseases 0.000 description 1
- 206010063075 Cryptogenic cirrhosis Diseases 0.000 description 1
- 108010016626 Dipeptides Proteins 0.000 description 1
- 238000002965 ELISA Methods 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 208000000857 Hepatic Insufficiency Diseases 0.000 description 1
- 206010019663 Hepatic failure Diseases 0.000 description 1
- 206010019668 Hepatic fibrosis Diseases 0.000 description 1
- 206010019799 Hepatitis viral Diseases 0.000 description 1
- 102000004877 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 description 1
- 206010023126 Jaundice Diseases 0.000 description 1
- 241001362856 Lepisorus miyoshianus Species 0.000 description 1
- 206010027336 Menstruation delayed Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 description 1
- 101710098398 Probable alanine aminotransferase, mitochondrial Proteins 0.000 description 1
- 102000004887 Transforming Growth Factor beta Human genes 0.000 description 1
- 108090001012 Transforming Growth Factor beta Proteins 0.000 description 1
- 102000046299 Transforming Growth Factor beta1 Human genes 0.000 description 1
- 101800002279 Transforming growth factor beta-1 Proteins 0.000 description 1
- 206010046274 Upper gastrointestinal haemorrhage Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- GZCGUPFRVQAUEE-SLPGGIOYSA-N aldehydo-D-glucose Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O GZCGUPFRVQAUEE-SLPGGIOYSA-N 0.000 description 1
- 229910021529 ammonia Inorganic materials 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 230000001363 autoimmune Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 229960001948 caffeine Drugs 0.000 description 1
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 210000002808 connective tissue Anatomy 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 239000012531 culture fluid Substances 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- 208000003816 familial cirrhosis Diseases 0.000 description 1
- 150000007946 flavonol Chemical class 0.000 description 1
- HVQAJTFOCKOKIN-UHFFFAOYSA-N flavonol Natural products O1C2=CC=CC=C2C(=O)C(O)=C1C1=CC=CC=C1 HVQAJTFOCKOKIN-UHFFFAOYSA-N 0.000 description 1
- 235000011957 flavonols Nutrition 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 description 1
- 235000003969 glutathione Nutrition 0.000 description 1
- 229960003180 glutathione Drugs 0.000 description 1
- 230000002440 hepatic effect Effects 0.000 description 1
- 208000007386 hepatic encephalopathy Diseases 0.000 description 1
- 231100000753 hepatic injury Toxicity 0.000 description 1
- 206010019692 hepatic necrosis Diseases 0.000 description 1
- 230000007866 hepatic necrosis Effects 0.000 description 1
- 210000004024 hepatic stellate cell Anatomy 0.000 description 1
- 210000002989 hepatic vein Anatomy 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 229960002885 histidine Drugs 0.000 description 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
- 201000004108 hypersplenism Diseases 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 229940125396 insulin Drugs 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000005229 liver cell Anatomy 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 210000005228 liver tissue Anatomy 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 231100000614 poison Toxicity 0.000 description 1
- 230000007096 poisonous effect Effects 0.000 description 1
- 208000007232 portal hypertension Diseases 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000008929 regeneration Effects 0.000 description 1
- 238000011069 regeneration method Methods 0.000 description 1
- 201000004409 schistosomiasis Diseases 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 235000018553 tannin Nutrition 0.000 description 1
- 229920001864 tannin Polymers 0.000 description 1
- 239000001648 tannin Substances 0.000 description 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 201000001862 viral hepatitis Diseases 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention belongs to drug world, more particularly to a kind of medical composition and its use for treating liver cirrhosis.This pharmaceutical composition is made up of polaprezinc, catechin and salicifoline.The percentage by weight of described polaprezinc, catechin and salicifoline is 10～70%:10～70%:10～70%, more preferably 30～70%:20～40%:20～30%, more preferably 50%:30%:20%, it is also possible to for 60%:20%:20%.
Description
Technical field
The invention belongs to drug world, more particularly to a kind of medical composition and its use for treating liver cirrhosis.
Background technology
Liver cirrhosis is clinical common chronic progressive external hepatopathy, or repeated action long-term by one or more causes of disease is formed
Diffusivity hepatic injury.Being posthepatitic cirrhosis at China's great majority, small part is alcoholic cirrhosis and Cirrhosis In Schistosomiasis.
There are hepatic necrosis, remaining liver cell nodules regeneration, connective tissue proliferation widely with fiber every formation in histopathology
Causing lobules of liver structural deterioration and pseudolobuli to be formed, liver gradually deforms, hardening and develop into liver cirrhosis.In early days due to liver generation
Repay function more by force can non-evident sympton, stage is with liver function injury and portal hypertension for main performance, and has multisystem to get involved,
Often there are the complication such as upper gastrointestinal hemorrhage, hepatic encephalopathy, secondary infection, hypersplenism, ascites, canceration in late period.
The cause of disease causing liver cirrhosis is a lot, and viral hepatitis liver cirrhosis, alcoholic cirrhosis, metabolic liver can be divided into hard
Change, Cholestatic cirrhosis, hepatic vein backflow obstruction liver cirrhosis, autoimmune cirrhosis, poisonous substance and Drug liver are hard
Change, nutritional cirrhosis, cryptogenic cirrhosis etc..
Liver cirrhosis is to cause hepatic insufficiency because organizational structure is disorderly, there is no radical cure way at present.Essentially consist in and send out in early days
Now with prevention course advancement, extending life and holding labour force.Including vein input hypertonic glucose liquid with additional heat, transfusion
In can add vitamin C, insulin, potassium chloride etc.；Note maintaining water, electrolyte, acid-base balance；The state of an illness relatively severe one can input white
Albumen, fresh plasma；Additionally can protect the liver, drop the treatment such as enzyme, jaundice eliminating, such as glucuronolatone, vitamin C, vein is defeated if desired
Liquid is treated, such as hepatocyte growth-promoting factors, reduced glutathion, Radix Glycyrrhizae acids preparation etc..
Polaprezinc is the N-BETA-Alanyl-L-histidine complex of zinc, entitled poly-2-(S)-[μ-[N of its chemistryα(3-aminopropionyl)-L-
Histidine (2-)-N1,N2,O:Nτ]-zinc].The dipeptides that N-BETA-Alanyl-L-histidine is made up of β-Phenylalanine and L-group ammonia, it is a kind of antioxygen
Agent.Patent documentation CN200610065168 shows that it has certain anti-liver cirrhosis effect, but offer limited effectiveness.
Catechin is also known as cachou extract, tea tannin.For the derivant of flavonol, molecular formula C15H14O6.It is colourless crystallization shape
Solid；Water can be dissolved in；Its aqueous solution is heated or in the presence of a mineral acid, easily aggregates into amorphous tannin.Belong to together with caffeine
Two big important functional compositions in Folium Camelliae sinensis.Clinical experiment investigation display, catechin can enter whole body by blood circulation, add
Excitometabolic, strengthens fatty oxidation and energy expenditure thus reaches the effect that suppression is fat, especially to interior fat
Inhibitory action, can reach preferable fat-reducing effect.Its structural formula is as follows:
Salicifoline (salicifoline) is widely present in the plant such as Drymotaenium miyoshianum (Mak.) Mak., Cortex Magnoliae Officinalis, grinds its pharmacology at present
Studying carefully less, its concrete structure is as follows:
Summary of the invention
It is an object of the present invention to provide a kind of pharmaceutical composition for cirrhosis treatment, this pharmaceutical composition by
Polaprezinc, catechin and salicifoline composition.
In one embodiment of the invention, the percentage by weight of described polaprezinc, catechin and salicifoline
It is 10～70%:10～70%:10～70%；
Described percentage by weight more preferably 30～70%:20～40%:20～30%；
Described percentage by weight is more preferably 50%:30%:20%, it is also possible to for 60%:20%:20%.
The present invention also provides for the purposes of aforementioned pharmaceutical compositions, i.e. this pharmaceutical composition in preparation treatment liver cirrhosis medicine
Application.
In medical usage described above, aforementioned pharmaceutical compositions can be prepared according to the animal state of an illness and agents area
Becoming suitable pharmaceutical preparation to facilitate medication, administration time and administration number of times for analgesic of the present invention pharmaceutical composition need
Depending on the concrete diagnostic result of the state of an illness, this is within the technical scope that those skilled in the art grasp.Such as, will be to rat
The therapeutic scheme of liver cirrhosis is applied on the person, and all medicines can be by effective to mice of this medicine to the effective dose of people
Dosage converts, and this is apparent from for the person of ordinary skill of the art.
Compared with prior art, the pharmaceutical composition of the present invention has good therapeutical effect to rat cirrhosis model,
And show good synergism.And while there is synergism, hence it is evident that reduce the consumption of each monomer medicine,
Thus significantly reduce toxic and side effects, reduce untoward reaction and occur.
Detailed description of the invention
To further describe the present invention below in detail.It is pointed out that following description is only to application claims
The illustration of the technical scheme of protection, the not any restriction to these technical schemes.Protection scope of the present invention is with appended
The content that claims are recorded is as the criterion.
Embodiment 1 pharmaceutical composition causes the impact of rat cirrhosis model to carbon tetrachloride
Take SD rat, body weight 200 ± 20g, random packet (often group 20), use 50%CCl4(CCl4/ olive oil: v/v=
1/1), by every 100g body weight 0.1ml lumbar injection, 2 times a week, totally 8 weeks induced rat Hepatocirrhosis Model.
Normal group: give equal-volume olive oil；
Model group: give 50%CCl4；
Administration group: at injection 50%CCl4Gastric infusion is started, until experiment terminates after 2 weeks.
In pharmaceutical composition group, each monomeric compound weight percent composition is as follows:
| % | Polaprezinc | Catechin | Salicifoline |
| Administration group 1 | 50 | 30 | 20 |
| Administration group 2 | 60 | 20 | 20 |
| Administration group 3 | 70 | 20 | 10 |
| Administration group 4 | 40 | 30 | 30 |
Concrete outcome is as follows:
1. body weight and mortality rate
| Group | Dosage (mg/kg) | Increased weight (g) | Mortality rate (%) |
| Normal group | - | 0.78±0.05 | 0 |
| Model group | - | 0.21±0.04 | 30 |
| Polaprezinc group | 100 | 0.24±0.03 | 10 |
| Catechin group | 100 | 0.25±0.05 | 15 |
| Salicifoline group | 100 | 0.22±0.04 | 20 |
| Administration group 1 | 100 | 0.63±0.05 | 0 |
| Administration group 2 | 100 | 0.69±0.06 | 0 |
| Administration group 3 | 100 | 0.42±0.05 | 5 |
| Administration group 4 | 100 | 0.45±0.04 | 5 |
2. blood biochemistry detection
| Group | Dosage (mg/kg) | Glutamate pyruvate transaminase (ALT) | Glutamic oxaloacetic transaminase, GOT (AST) |
| Normal group | - | 42.5±6.7 | 112.5±15.9 |
| Model group | - | 417.8±59.5 | 489.7±57.8 |
| Polaprezinc group | 100 | 311.6±61.2 | 407.4±52.9 |
| Catechin group | 100 | 352.5±57.8 | 427.6±49.8 |
| Salicifoline group | 100 | 421.9±65.3 | 473.2±55.6 |
| Administration group 1 | 100 | 193.5±39.2 | 212.3±37.4 |
| Administration group 2 | 100 | 157.1±35.7 | 167.6±32.3 |
| Administration group 3 | 100 | 293.4±47.5 | 357.9±44.3 |
| Administration group 4 | 100 | 310.9±45.8 | 364.5±48.2 |
3. hepatic fibrosis assessment
Taking rat liver tissue frozen section, conventional H E dyes, and observation by light microscope is marked, by Scheuer ' s by stages
System standards of grading are as follows:
0 phase: without fibrosis
1 phase: portal area increases companion's fibrosis, but without fiber every formation；
2 phases: portal area surrounding annulus, header-portal area fiber is every formation；
3 phases: header-portal area fiber is connected with header-central vein every formation widely；
4 phases: liver cirrhosis
Result is as follows:
| Group | Dosage (mg/kg) | Average integral |
| Normal group | - | 0 |
| Model group | - | 4.0±0.0 |
| Polaprezinc group | 100 | 3.3±0.5 |
| Catechin group | 100 | 3.5±0.4 |
| Salicifoline group | 100 | 3.8±0.3 |
| Administration group 1 | 100 | 2.1±0.3 |
| Administration group 2 | 100 | 1.8±0.3 |
| Administration group 3 | 100 | 2.8±0.4 |
| Administration group 4 | 100 | 2.8±0.3 |
Embodiment 2 pharmaceutical composition causes the impact of rat cirrhosis model to thiacetamides
SD rat, random packet, normal group with normal water as drinking water, with 300mg/L thiacetamides aqueous solution as
Rat drinking water modeling, drinks 300mg/L thiacetamides aqueous solution after 10 weeks continuously, and administration group gastric infusion once a day, continues
Continue and drink 300mg/L thiacetamides aqueous solution 10 weeks, totally 20 weeks.
Concrete outcome is as follows:
1. serum alkaline phosphatase (ALP) content
| Group | Dosage (mg/kg) | ALP(u/L) |
| Normal group | - | 545±29 |
| Model group | - | 1379±99 |
| Polaprezinc group | 100 | 1164±87 |
| Catechin group | 100 | 1257±58 |
| Salicifoline group | 100 | 1355±101 |
| Administration group 1 | 100 | 754±33 |
| Administration group 2 | 100 | 647±36 |
| Administration group 3 | 100 | 958±41 |
| Administration group 4 | 100 | 942±34 |
The content of TGF-β 1 in 2.ELISA mensuration hepatic tissue
| Group | Dosage (mg/kg) | TGF-β1(ng/g) |
| Normal group | - | 11.3±0.6 |
| Model group | - | 67.8±3.5 |
| Polaprezinc group | 100 | 51.2±2.8 |
| Catechin group | 100 | 58.9±3.1 |
| Salicifoline group | 100 | 66.9±2.5 |
| Administration group 1 | 100 | 21.5±1.7 |
| Administration group 2 | 100 | 18.3±1.5 |
| Administration group 3 | 100 | 38.6±2.4 |
| Administration group 4 | 100 | 41.7±3.4 |
Embodiment 3 pharmaceutical composition inhibitory effect to HSC-T6 hepatic stellate cell proliferation
After HSC-T6 cell line is recovered, it is placed in incubator and cultivates, after passing on and stablizing, collect cell, with 1 × 104Individual/
Ml is inoculated in 96 orifice plates, and every hole adds 10 μ l acetaldehyde modelings, and normal group adds equal-volume culture fluid, after cultivating 48h, with mtt assay
Measure each group of OD value and calculate suppression ratio, often organizing 5 holes, repeating three times.
Suppression ratio=(model group OD value-administration group OD value)/(model group OD value-normal group OD value) × 100%
Concrete outcome is as follows:
| Group | Dosage (mg/L) | Suppression ratio (%) |
| Normal group | - | - |
| Model group | - | - |
| Polaprezinc group | 10 | 13.9±0.6 |
| Catechin group | 10 | 12.7±0.5 |
| Salicifoline group | 10 | -3.5±0.7 |
| Administration group 1 | 10 | 39.6±1.1 |
| Administration group 2 | 10 | 42.1±0.8 |
| Administration group 3 | 10 | 25.3±0.9 |
| Administration group 4 | 10 | 27.2±0.6 |
Present invention merely illustrates some claimed specific embodiments, one of them or more skill
Technical characteristic described in art scheme can be combined with arbitrary one or more technical schemes, and these are combined and obtain
Technical scheme also in the application protection domain, combined just as these and the technical scheme that obtains is open in the present invention
In content as concrete record.
Claims (5)
1. the pharmaceutical composition for cirrhosis treatment, it is characterised in that this pharmaceutical composition is by polaprezinc, catechin
Forming with salicifoline, the percentage by weight of wherein said described polaprezinc, catechin and salicifoline is about 60%
: 20%: 20%.
A kind of pharmaceutical composition for cirrhosis treatment the most according to claim 1, it is characterised in that described poly-
The percentage by weight of Puri zinc, catechin and salicifoline is about 70%: 20%: 10%.
A kind of pharmaceutical composition for cirrhosis treatment the most according to claim 1, it is characterised in that described poly-
The percentage by weight of Puri zinc, catechin and salicifoline is about 50%: 30%: 20%.
A kind of pharmaceutical composition for cirrhosis treatment the most according to claim 1, it is characterised in that described poly-
The percentage by weight of Puri zinc, catechin and salicifoline is about 40%: 30%: 30%.
5. the pharmaceutical composition described in claim 1-4 any one, it is characterised in that in preparation for treating the medicine of liver cirrhosis
Application in thing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410342881.5A CN104083751B (en) | 2014-07-18 | 2014-07-18 | A kind of medical composition and its use for cirrhosis treatment |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410342881.5A CN104083751B (en) | 2014-07-18 | 2014-07-18 | A kind of medical composition and its use for cirrhosis treatment |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104083751A CN104083751A (en) | 2014-10-08 |
| CN104083751B true CN104083751B (en) | 2016-08-24 |
Family
ID=51631576
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410342881.5A Expired - Fee Related CN104083751B (en) | 2014-07-18 | 2014-07-18 | A kind of medical composition and its use for cirrhosis treatment |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104083751B (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106619697A (en) * | 2016-12-21 | 2017-05-10 | 郑州莉迪亚医药科技有限公司 | Drug for treating cirrhosis with ascites, preparation method thereof and application |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1857715A (en) * | 2006-03-23 | 2006-11-08 | 恩泰柯数码科技（北京）有限公司 | Cirrhosis treating medicine |
-
2014
- 2014-07-18 CN CN201410342881.5A patent/CN104083751B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1857715A (en) * | 2006-03-23 | 2006-11-08 | 恩泰柯数码科技（北京）有限公司 | Cirrhosis treating medicine |
Non-Patent Citations (2)
| Title |
|---|
| The isolation of secondary metabolites and in vitro potent anti-cancer activity of clerodermic acid from Enicosanthum membranifolium;Mai Efdi等;《Bioorganic & Medicinal Chemistry》;20070318;第15卷;第3668页 * |
| 绿茶提取物对四氯化碳所致大鼠肝硬化的保护作用;肖继平等;《中华预防医学杂志》;20020731;第36卷(第4期);第243页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN104083751A (en) | 2014-10-08 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Martin | Therapeutic potential of KELEA activated water | |
| CN105434842A (en) | Traditional Chinese medicine composition for strengthening immunity and improving sleep as well as preparation and preparation method thereof | |
| US20180104269A1 (en) | Composition for suppressing muscular fatty change | |
| CN104083751B (en) | A kind of medical composition and its use for cirrhosis treatment | |
| CN106135906A (en) | Jilin Radix Ginseng oligopeptide purposes in the food or health food of preparation resisting fatigue | |
| CN102754834A (en) | Biological mixture for regulating emotion and relieving stress and preparation method thereof | |
| CN104000809B (en) | A kind of control treating coronary heart disease and angina pectoris compositions and application thereof | |
| CN103006622B (en) | New borneol use and lung cancer treatment drug composition | |
| CN104258034A (en) | Traditional Chinese medicine composition for boosting immunity | |
| CN100409854C (en) | Production prescription for mineral black mud eczema ointment | |
| CN104306362A (en) | Application of patchoulicalcohol in preparation of medicines for treating gastric motility disorders | |
| CN104887796A (en) | Anti-altitude-stress rhodiola rosea oral liquid and preparation method thereof | |
| US20100203146A1 (en) | Intermittent dosing strategy for treating rheumatoid arthritis | |
| CN103550569B (en) | Use of rice sprout extract in preparing medicament for treating fatty liver | |
| CN102631489B (en) | Traditional Chinese medicine composition capable of improving immunity and resisting fatigue | |
| CN105169291A (en) | Traditional Chinese medicine compound preparation for treating post-stroke depression and preparation method and application thereof | |
| CN104435043A (en) | Medicine for treating arthritis-induced arthralgia and preparation method thereof | |
| CN106138259A (en) | A kind of Chinese medicine composition treating anemopyretic cold and preparation method thereof | |
| CN105663450A (en) | Traditional Chinese medicine formula for treating acute bronchitis in children | |
| CN103446311A (en) | Traditional Chinese medicine for treating trichomonas vaginitis | |
| CN102335130A (en) | Preparation method of anti-tumor medicinal n-methylcantharidimide injection | |
| CN102631394B (en) | Traditional Chinese medicine composition capable of improving immunity and resisting fatigue | |
| Deyou et al. | The influence of IL-17, MMP-7 of Ga rats treated by tked method | |
| CN103316004B (en) | Pharmaceutical composition used for preventing and controlling metabolic syndrome and application thereof | |
| Kattan | Study the biological effect of Punica granatum and Thymus vulgaris extracts on parasite Giardia lamblia in experimentally infected white mice Balb/c |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB03 | Change of inventor or designer information |
Inventor after: Tang Ling Inventor after: Wang Yang Inventor after: Zhanxi Inventor before: Tang Ling Inventor before: Wang Jiao |
|
| COR | Change of bibliographic data | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20160824 |