Shaanxi Bloom Tech Co., Ltd. yog ib qho ntawm cov neeg tsim khoom thiab cov khoom lag luam ntawm coveetidine kev txhaj tshuaj nyob hauv Suav teb. Txais tos rau kev lag luam wholesale ntau cov khoom lag luam zoo nkaujetidine kom zoo rau muag ntawm no los ntawm peb lub hoobkas. Cov kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Cimetidine Kev Txhaj Tshuaj, raws li thawj tiam histamine h ₂ receptor kev thaiv, tau muaj dav kawm hauv cov qauv tsiaj rau nws cov kev tshwm sim txij li thaum nws tshwm sim hauv xyoo 1970. Mas siv rau kev kho cov kab mob uas muaj feem xyuam rau cov pa roj plab ntau dhau. Nws cov tub ntxhais tivthaiv yog coveetidine, uas muaj kev sib tw ntawm H2 receptors ntawm cov pa roj plab thiab lwm yam tshwm sim los ntawm cov pa roj ntsha thiab lwm cov tsos mob tshwm sim los ntawm cov pa roj plab ntau heev.
Cov ntaub ntawv ntxiv ntawm kev sib txuas lus:
| Khoom npe | Cimetidine Hmoov | Cimetidine ntsiav tshuaj | Cimetidine Kev Txhaj Tshuaj | CIMETIDINE CAPSULES | Cimetidine Cream |
| Khoom Yam | Hmoov | Ntsiav tshuaj | Kev txhaj tshuaj | Tsoom qab | Kua |
| Khoom Siv Purity | Ntau dua los yog sib npaug rau 99% | Ntau dua los yog sib npaug rau 99% | Ntau dua los yog sib npaug rau 99% | Ntau dua los yog sib npaug rau 99% | Ntau dua los yog sib npaug rau 99% |
| Cov Khoom Qhia Khoom Khoom | Tau sib kho | Tau sib kho | Tau sib kho | Tau sib kho | Tau sib kho |
| Khoom Pob | Tau sib kho | Tau sib kho | Tau sib kho | Tau sib kho | Tau sib kho |
Peb Cov Khoom Daim Ntawv
Cimetidine +. coa
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Daim Ntawv Pov Thawj Kev Ntsuam Xyuas |
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Compound npe |
Cimetidine | |
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Cas Tsis tau. |
51481-61-9 | |
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Teem nqi |
Kws Tshuaj Ntsuam Xyuas | |
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Qho ntau |
Me nyuam | |
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Ntim txheem ntim |
Me nyuam | |
| Tus tsim | Shaanxi Bloom Tech Co., Ltd. | |
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Lauj tsis tau. |
20250109001 |
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Mfg |
Jan 12th 2025 |
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Tus txeeb |
Jan 8th 2029 |
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Lub tsev |
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| Kuaj Tus Qauv | GB / T24768-2009 kev lag luam. Stnndard | |
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Yam |
Kev Lag Luam Kev Lag Luam |
Kev tsom xam tau |
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Kev tshwm sim |
Dawb lossis yuav luag dawb hmoov |
Hloov |
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Dej Cov Ntsiab Lus |
Tsawg dua los yog sib npaug rau 4.5% |
0.30% |
| Poob rau ziab |
Tsawg dua los yog sib npaug rau 1.0% |
0.15% |
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Cov hlau hnyav |
PB tsawg dua lossis sib npaug rau 0.5ppm |
N.D. |
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Tsawg tsawg dua li lossis sib npaug rau 0.5ppm |
N.D. | |
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Hg tsawg dua lossis sib npaug rau 0.5ppm |
N.D. | |
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CD tsawg dua lossis sib npaug rau 0.5ppm |
N.D. | |
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Purity (hplc) |
Ntau dua los yog sib npaug rau 99.0% |
99.5% |
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Ib Leeg Cav |
<0.8% |
0.48% |
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Residue ntawm ignition |
<0.20% |
0.064% |
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TAG NRHO LICBIAL COUNT |
Tsawg dua li lossis sib npaug rau 750cfu / g |
80 |
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E. coli |
Tsawg dua los yog sib npaug rau 2mpn / g |
N.D. |
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Tus ntses siav |
N.D. | N.D. |
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Ethanol (los ntawm gc) |
Tsawg dua los yog sib npaug rau 5000ppm |
400ppm |
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Chaw ntim khoom |
Khaws rau hauv ib qho chaw sib khi, qhov chaw tsaus thiab qhuav ntawm-20 degrees |
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Cov khoom no yog qhov tsim nyog rau kev kho tus duodenal mob rwj, cov pa roj plab, thiab cov neeg mob ua rau muaj kev rov qab dua tom qab kev kho mob luv dua. Rau cov neeg mob uas muaj cov kab mob pheej hmoo, tshwj xeeb yog cov uas nws cov tshuaj tiv thaiv kev tiv thaiv thiab cov tshuaj tiv thaiv tshuaj xws li antacids yog tsis muaj txiaj ntsig,Cimetidine Kev Txhaj Tshuajtuaj yeem txhim kho cov tsos mob. Ib qho ntxiv, nws tseem siv los tiv thaiv cov kev ntxhov siab rau cov kev ntxhov siab thiab los ntshav hauv cov kab mob zoo li roj ntsha (ZOLLONSOR AID SCRESSION.
1.1 h ₂ Receptor ib cheeb tsam thiab teeb liab Transduction
Hauv tsiaj lub plab zom mov, h ₂ receptors feem ntau yog muab faib rau sab nraud ntawm Parietal hlwb thiab yog rau G Protein Coupled receptor (GPC) tsev neeg. Thaum cov kab mob hedamine khi rau H ₂ receptor, nws ua kom cov GS protein, AC), catalyzing ATCLASE (AC), catalyzing ATCLATE Adenosine Monophopphate (chaw pw). Lub chaw pw ua ke ua ib tus neeg xa xov thib ob, ua kom muaj protein thib ob, ua haujlwm rau phosphorylation ntawm lub parietal cell proton (h} {} atpase) thiab pib cov pa roj plab zais pa.
Tsiaj sim ua pov thawj:
Nyob rau hauv cov kev sim vitro ntawm nas lub plab mog pov thawj uas muaj nuj nqis}
Nyob rau hauv canine powerfic fistula qauv, muaj kev txhaj tshuaj ntawm lub ntsej muag (5 mg / kg) basci acid zais pa los ntawm 70%, thiab iniscabory cov nyhuv zoo sib piv nrog kev siv ntshav ntau.
1.2 cov nqi sib tw tsis sib haum xeeb
CIMETIDINE Blocks cov nyhuv zoo siab ntawm cov histamine los ntawm kev nyob hauv lub tsev h ₂ receptor. Nws cov cwj pwm inhibition yog manifested li:
Reversible khi: Hauv kev sim ntawm Guinea npua mob hlwb, qhov kev khi tau zoo sib xws los ntawm cov yam ntxwv ntawm kev sib tw ntawm kev tawm tsam.
Subtype selectivity: Radioligand binding experiments have confirmed that the affinity of cimetidine for H ₂ receptors (Kd=42 nM) is significantly higher than that for H ₁ receptors (Kd>10 μ M) and H3 receptors (Kd>100 μ m), piav qhia nws cov kev phiv tshuaj antichitygyergic.
1.3 cov kev cai sib cais ntawm cov pa roj acid zais
Inhibition ntawm basal gastric acid zais cia:
Nyob rau hauv lub plab hnyuv plab zom mov hauv cov dev, txuas ntxiv ntawm cov ciaj sia (2 mg / kg / h) tuaj yeem txo cov pa roj plab los ntawm 85%, thiab cov nyhuv kav ntev dua 8 teev.
Nyob rau hauv cov kev sim vitro ntawm nas lub plab zom mov pom tias qhov kev cuam tshuam ntawm bastric patidic acid tso tawm los ntawm Cimetidine yog qhov siab yog qhov kev xav tau, nrog EC ₅₀ tus nqi ntawm 0.3 μ M.
Stimulating inhibition ntawm pais plab acid zais cia:
Kev sim nyob rau ntawm npua lub plab mog tuaj yeem thaiv cov pob twetidine tuaj yeem thaiv cov roj plab tsw qab los ntawm Pentagastrin (1 μ G), nrog tus nqi Inhibition ntawm 65%.
Nyob rau hauv tus qauv dev, tus nqi inhibitory ntawm cov risetidine ntawm cov pa roj hmab zais pa tawm los ntawm insulin induced hypoglycemia (0.1 u / kg IV) yog 58%, feem.
1.4 Cov kev hloov pauv hauv plab kua txiv muaj pes tsawg leeg
Ph Haum:
Cov kev sim dev tau qhia tias covePetidine (10 mg / Kg / Kg / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG / KG/9
Nyob rau hauv tus npua ua qauv ua qauv, cov kev ua mob pais plab ua rau pab pawg Cimetidine poob qis los ntawm Phem kev.
Pais plab kua lim tswj:
Cov khaub lig luav ua kom pom tias Cimetidine (50 μ m) tuaj yeem txo cov kua dej tso tawm los ntawm tub luam los ntawm kev cuam tshuam txog tubroling
2.1 qhia txog ntawm lub cev tsis muaj zog H ₂ receptors
T lymphocytes:
Ntws Cytometry tsom xam ntawm nas yauv T cell qhia tias tus lej ntawm CD4 ⁺ T cell li 65%, thiab C CL8 ⁺ t hlwb yog 42%.
Qhov kev sim ntawm Ras Lymphocyte mem cov pob txha yog qhia tau tias H ₂ receptor tau qhia tau tias lub GS protein thiab tuaj yeem tau txhawb nqa cov lus qhia ntawm IL-2 receptor tom qab kev ua kom ua kom tiav.
Macrophages:
Guinea npua peritoneal macrophage kab lis kev cai qhia tau tias H ₂ receptor ua kom muaj inhibit LPS Indicial}}}}} Cov nqi ntawm 10 μ m
Kev sim rau cov ntshav uas muaj cov dev uas muaj cov dev uas muaj cov dev uas muaj peev xwm (50 i
2.2 kev tswj hwm ntawm cov mob nrab
Cov ntaub ntawv los ntawm synthesis inhibition:
Kev sim ua kom muaj kev cuam tshuam ntawm cov nas mast cell qhia tias Cimetidine (100 μ m) tuaj yeem txo qhov l - hyipidine decarboxylase kev ua si.
Hauv cov tawv nqaij ua xua tawv ua haujlwm, pretreatment nrog Cimetidine (10 mg / kg iv) txo lub cheeb ntawm daim tawv nqaij ntawm daim tawv nqaij ntawm cov tawv nqaij los ntawm 40%.
CyTOKine Tshuav:
Nyob rau hauv nas Colitis qauv qauv, cov pab pawg kho nrog Cimetidine (50 mg / kg po}}}} Cia nce hauv tnf - qib hauv cov hnyuv.
Tus npua sib koom ua keCimetidine Kev Txhaj TshuajKev sim ua kom pom tias Cimetidine (1 mg / sib koom tes) tuaj yeem cuam tshuam nrog cov synthesis cig ntawm IL-1, nrog IC ₅₀ tus nqi ntawm 20 μ M.
2.3 kev tswjfwm ntawm lub cev tsis muaj zog ntawm tes adhesion
Inhibition ntawm xaiv cov lus qhia:
Rat Aortic endothelial cell kev cai coj ua qhia tias Cimetidine (50 μ m) tuaj yeem thaiv qhov kev qhia ntawm histamine (10 μ m), nrog tus nqi inhibition ntawm 75%.
In the canine myocardial ischemia-reperfusion model, the treatment group with cimetidine showed a 50% reduction in neutrophil infiltration, which was associated with a decrease in P-selectin expression.
Cov kev cai ntawm kev ua Vauv Khoom:
Cov nas lymphyste kev tsiv teb tsaws chaw uas pom tias Cimetidine (25 μ m) tuaj yeem Inhibit cov nplaum ntawm LFA-1, nrog tus nqi ICAM-1, nrog tus nqi IC, tus nqi ntawm 15 μ M.
Nyob rau hauv luav cauv hloov pauv qauv, lub sijhawm ciaj sia taus ntawm cov ntaub so ntawm lub ntsej muag yog txuas ntxiv los ntawm lub ntsej muag muaj kev cuam tshuam rau c cell infiltration.
Antitumor Angiogenesis: H ₂ Txais Cov Txheej Txheem Kev Nyab Xeeb
3.1 Kev cai ntawm Vegf Signaling Txoj Kev
H ₂ receptor ywj pheej inhibition:
Cov ratine hnab tshos qauv qhia tias CIMETIDINE (50 mg / kg poibret bfgf indiced bfgf indiced los ntawm h ₂ receptor agonists.
Cov nqaij qaib embryo missiono mapbrane tau paub tseeb tias Cimetidine tau lees paub tias Cimetidine (100 μ m) tuaj yeem thaiv txoj kev ua kom vegular begrees tsim los ntawm vegf, nrog tus nqi IY 30 μ M.
Vegf qhia cov kev cai:
Nyob rau hauv cov nas mis cancer mis, qib ntawm vegf mrna hauv qog nqaij ntawm CIMETIDINE Kev Kho Mob (100 mg / Kg / Kg / teev / teev.
Cell culture of canine mastocytoma showed that cimetidine (50 μ M) can inhibit histamine (10 μ M) - induced VEGF secretion with an inhibition rate of 80%.
3.2 Inhibition ntawm Odothelial cell ua haujlwm
Migration inhibition:
Kos cov kev sim ntawm tib neeg umbilical vein endothelial hlwb (25 μ m) tuaj yeem ua rau ntawm tus nqi hauv kev tiv thaiv ntawm 60%.
Kab lis kev cai ntawm nas hlwb microvielial pom tias CIMETIDIA (50 μ m) tuaj yeem thaiv matrix gel m) tuaj yeem ua rau kev tsim lumbinal tsim, nrog tus nqi IC50 ntawm 20 μ M.
Kev npau taws induction:
Kev sim ntawm ApopTosis ntawm Porcine Aortoth cov hlwb uas pom tias Cimetidine (100 μ m) tuaj yeem ua kom lub ntsej muag phev ntawm 35%.
Nyob rau hauv luav codyization qauv, tus naj npawb ntawm apoptotic lub cev nyob rau hauv cov xov tooj ntawm endotheles tau nce los ntawm 2.5 zaug hauv pawg muaj nuj nqis.
3.3 qog cell cov nplaum nplaum
Cov kev cai ntawm Castin Qhia:
Mous melanoma cell kab lis kev cai qhia tias CIMETIDINE (50 μ m) tuaj yeem downtregulate qhia ntawm v 3 integinition) ntawm 65%.
Lub Cell Adhesion sim ntawm canine lymphoma pom tias CIMETIDINE (25 μ m) tuaj yeem thaiv cov cell adiesion induced los ntawm fibronectin, nrog tus nqi IC50 ntawm 10 μ M.
Metalloproteinase inhibition:
Nyob rau hauv ib tug nas glioma qauv, kev ua haujlwm ntawm MMP-9 nyob rau hauv cov leeg ntaub so ntswg tau txo los ntawm 70% nyob rau hauv cov pab pawg kho nrog Cimetidine (100 Mg / KG / HNUB IP).
Npua Chaondrocyte kab lis kev cai qhia tau tias Cimetidine (50 μ m) tuaj yeem tiv thaiv MMP-13 Secition, nrog tus nqi IC50 ntawm 20 μ M.
4.1 CYP450 enzyme inhibition cov yam ntxwv
Enzyme kev ua assay:
Cov nas lival microscal tsom rau cov nqaijetidine (50 μ m) tuaj yeem tiv thaiv CYP1A2 thiab txo CyP3A4 kev ua si los ntawm 65%.
Hauv cov qauv ntawm cov dev, cimetidine (10 mg / kg iv) tuaj yeem nce AUC ntawm diazepam los ntawm 2.3 zaug thiab txo cov cl los ntawm 55%.
Kev Tshawb Fawb Txheej Txheem:
Cov kev sim molecular pom tias cov khoom siv ntometidine uas muaj kev sib koom ua ke ntawm CYP3A4, stabilizing cov enzyme inhibitical txoj kev nyuaj.
Ra mob siab ua kab lis kev cai qhia tau hais tias Cimetidine uas muaj cov cimetidine (25 μ m) tuaj yeem downregulate CyP2C11 MRA qhia nrog tus nqi Inhibition ntawm 70%.
4.2 Kev Sib Tham Yeeb Tshuaj
Metabolism ntawm Warfarin:
Pharcacerminetic kev sim hauv luav tau qhia tias Cimetidine (50 mg / kg / olon warfarin t ₁ / ₂ los ntawm 2.1 zaug thiab nce PT nqi los ntawm 35%.
Nyob rau hauv canine canagulation qauv, kev sib xyaw ntawm Cimetidine thiab Warfarin tau ua rau lub sijhawm ntawm 2.8
Theophylline metabolism:
Saib xyuas ntawm Theophline conctration hauv cov tshuaj txhuam nas uas muaj cov cimetidine (20 mg / kg / aph / hnub ip) los ntawm 2.5 zaug thiab AUC los ntawm 3.2 zaug.
Tus npua ua kom pom kev ua kom pom kev ua kom pom tseeb tias Cimetidine (50 μ m) tuaj yeem inhibit thehlit gluopuronidation thiab txo tus nqi tshem tawm los ntawm 60%.
Txoj kev ntawm kev nqis tes ua: Administretracninininetics
Kev Txhaj Tshuaj Tiv Thaiv Txoj Kev
Ntawm leegCimetidine Kev Txhaj Tshuaj:
Pharcaconinetic kev tshawb fawb hauv cov dev pom tias tom qab kev txhaj tshuaj tiv thaiv ntawm Cimetidine (5 mg / kg), CMAX mus txog 15 μ G / ML thiab T ₁ / ₂ yog 1.2 teev.
Nyob rau hauv tus qauv npua, intravenous Txoj kev lis ntshav (2 mg / h) tuaj yeem tswj hwm lub ece}} Lub xeev cov tshuaj lom neeg muaj kuab kom muaj kuab zais zais zais.
Txhaj tshuaj txhaj:
Cov kev sim ua ntej tau pom tias tom qab kev txawj ntse intramuscular txhaj tshuaj ntawm CIMETIDINE (10 MG / KG / KG), TMAX yog 0.5 teev thiab Bioavailability mus txog 85%.
A comparative study of rabbits showed no significant difference in AUC between intramuscular injection and intravenous injection (P>0.05).
Kev faib tawm cov yam ntxwv faib tawm
Ntshav cov protein protein khi tus nqi:
Cov nyob hauv vitro equilibrium sim qhia tau hais tias cov protein khi tus nqi ntawm CIMETIDINE hauv Dasma Dasma Dogma yog 20%, feem ntau yog los ntawm albumin.
Kev tshawb fawb txog kev faib cov ntaub so ntswg qhia tau hais tias kev sib haum xeeb ntawm lub ntsej muag ntawm lub plab mog hauv av yog 15 zaug ntawm ntshav, txhawb nws cov nyhuv.
Metabolism thiab excretion:
Lub canine bile cov kev sim ua kom pom tias lub ntsej muag cietidine yog feem ntau metabolized los ntawm daim siab, kev tsim cov neeg leej faj oxides thiab n {{{olide metabolites.
Txoj kev tshawb fawb ntawm nas tso zis ua rau cov tshuaj paub tseeb tias cov tshuaj prototype uas tau suav nrog 30% ntawm cov tshuaj, metabolites tus nqi yog 3.5 ml / min / kg.
Cimetidine Kev Txhaj TshuajMuab cov hluav taws xob los ntawm ntau txoj kev hauv txoj kev thiab hom phiaj:
Cov kev cai ntawm cov pa roj acid zais cia:
Raws li H ₂ receptor tiv thaiv, nws ncaj qha tiv thaiv cov pa roj parietal thiab tswj cov kev sib xyaw ntawm cov pa roj acid.
Kev tiv thaiv kab tiv thaiv kab mob:
Kev tswj hwm qhov sib npaug ntawm kev tiv thaiv kev tiv thaiv ntawm tes thiab cov kev kho mob ntawm H ₂ receptor nyob ntawm h ₂ receptor tseem nyob thiab tsis yog resentent archisms.
Anti qog angiogenesis:
Inhibiting vegf signaling txoj kev thiab endothelial cell ua haujlwm, thaiv cov qog angiogenesis.
Cov tshuaj metabolism tsis meej:
Raws li CyP450 enzyme inhibitor, nws alters cov yam ntxwv ntawm cov tshuaj sib xyaw ua ke.
Cim npe nrov: Cimetidine Kev Txhaj Tshuaj, Cov Neeg Siv Khoom, Chaw Tsim Tshuaj, Hoobkas, lag luam Wholesale, yuav, nqe, loj, rau muag