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Bisoprolol fumarate
Bisoprolol fumarate
Bisoprolol fumarate

Bisoprolol fumarate

Price USD1000.00USD950.00
Packge 1KG5KG
  • Min. Order:1G
  • Supply Ability:100KG
  • Time:2019-07-06

Product Details

  • Product NameBisoprolol fumarate
  • CAS No.104344-23-2
  • EINECS No.600-557-5
  • MFC22H35NO8
  • MW441.52
  • Appearancesolidwhite
  • Melting point 100°C
  • storage temp. 2-8°C

A68

Product Name: Bisoprolol fumarate
Synonyms: (+-)-1-(p-((2-isopropoxyethoxy)methyl)phenoxy)-3-isopropylamino-2-propanolh;(+-)-mino)(e)-2-butenedioate(2:1)(salt);2-propanol,1-(4-((2-(1-methylethoxy)ethoxy)methyl)phenoxy)-3-((1-methylethyl)a;NegativeioncolophonyPolymer;1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]propan-2-ol hemifumarate;1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol hemifumarate salt;(±)-1-((alpha-(2-Isopropoxyethoxy)-p-tolyl)oxy)-3-(isopropylamino)-2-propanol fumarate;Azopsin
CAS: 104344-23-2
MF: C22H35NO8
MW: 441.52
EINECS: 1312995-182-4
Product Categories: Intermediates & Fine Chemicals;Pharmaceuticals;Adrenoceptor;CELESTOVET;Pharmaceutical material and intermeidates;APIs
Mol File: 104344-23-2.mol
Bisoprolol fumarate Structure
 
Bisoprolol fumarate Chemical Properties
Melting point  100°C
storage temp.  Store at RT
solubility  DMSO: >20 mg/mL
form  solid
color  white
Merck  14,1295
CAS DataBase Reference 104344-23-2(CAS DataBase Reference)
 
Safety Information
Hazard Codes  Xn,Xi
Risk Statements  22
WGK Germany  3
RTECS  UB8390000
HazardClass  IRRITANT
MSDS Information
 
 
Bisoprolol fumarate Usage And Synthesis
Pharmacological effects Bisoprolol fumarate is a selective β1-adrenergic receptor blockers. No intrinsic sympathomimetic activity and membrane stabilizing effect. Animal experiments of different models show that affinity for β1-receptor is 11 to 34-fold larger than β2-receptor. The selectivity for β1 receptor is four times of the similar drugs Atenolol. This product plays the role for a long time (24 hours or more), continual application takes good control of symptoms without tolerance phenomenon, with minimal side effects on the respiratory system, no effects on metabolism of fat. it also has a certain degree of block effect for bronchial β2 receptors, but it may only occur at high doses, usually it has no obvious clinical significance.
Indications Treatment of essential hypertension. As first-line antihypertensive agents, it can be used alone or combined with diuretics and vasodilator drugs.
Angina and myocardial infarction.
Arrhythmias, such as the rapid ventricular arrhythmia, ventricular contraction.
In recent years, bisoprolol fumarate is also tempted used for the treatment of heart failure. It is effective for moderate to severe chronic stable heart failure which previously receiving ACE inhibitors, diuretics and cardiac glycosides medications associated with ventricular systolic dysfunction (ejection fraction ≤35%) .
The above information is edited by the chemicalbook of Tian Ye.
Method and Dosage Hypertension: The initial dose is 5mg once, 1 times a day. It may be suitable for some patients to start with initial dose of 2.5mg (such as bronchial spasm disease). If the dose of 5 mg one day is not enough for antihypertensive effect , the dose may be increased to 10-20mg one day .
Angina: initial dose of 2.5mg, 1 time a day, the maximum daily dose can not exceed 10mg.
Heart failure: chronic, stable heart failure: it should start from small dose, if it is tolerated, the dose can gradually increasing (doubling the dose every 2-4 weeks) to the maximum tolerated dose or target dose. The maximum recommended target dose is 10mg one day , the starting dose is usually 1/8 of the target dose.
Distinguish Take appropriate amount of this product powder (about the equivalent of bisoprolol fumarate 20mg), add 4ml water to dissolve, the filtrate is added 1 to 3 drops of potassium permanganate test solution , purple should fade , and brown precipitate forms.
Take right amount of this product powder,it is dissolved in water and form the solution of which 1ml each contains about 0.1mg bisoprolol fumarate,after filtration, take continued filtrate, according to the UV-visible spectrophotometry (Appendix Ⅳ A) measure ,there is the maximum absorption in the 271nm wavelength.
In the chromatogram recorded under the item of content determination ,the test solution peak retention time should be consistent with the reference solution peak retention time.
Content Determine Take 10 tablets of this product , weigh accurately, porphyrize, accurately weigh appropriate amount (about the equivalent of bisoprolol fumarate 5mg), set it into 50ml volumetric flask, add water to make bisoprolol fumarate dissolve and dilute it to the mark , shake, filtrate, according to chromatographic conditions under the item of bisoprolol fumarate related substances,take the precise amount of continued filtrate 20μl into the liquid chromatograph, record the chromatograms; in addition , precisely weigh appropriate amount of the reference bisoprolol fumarate , dissolve it in water and dilute into the solution of which 1ml each contains about 0.1mg,measure in the same method, calculate according to the external standard method bisoprolol peak area ,it is obtained .
Drug interactions 1.when bisoprolol fumarate is used in combination with other anti-hypertensive drugs, the antihypertensive effect is enhanced .
2. when bisoprolol fumarate is used in combination with reserpine, methyldopa, clonidine or guanfacine, the heart rate can be slowed down.
3. when bisoprolol fumarate is used in combination with reserpine, reserpine needs to be stopped a few days after stop of this product .
4. when bisoprolol fumarate is used in combination with nifedipine, the antihypertensive effect of this product can be enhanced .
5. when bisoprolol fumarate is used in combination with verapamil or diltiazem ketones calcium icon antagonists or other antiarrhythmic drugs , there is the need for patient care, because they can cause hypotension, bradycardia and others.
Precautions Diabetic patients with great blood glucose fluctuations or acidosis patients should be careful in use of it.
Patients with pulmonary insufficiency, severe liver and kidney dysfunction should use with caution.
Interruption of treatment should diminish doses daily ,when it is used in combination with other antihypertensive drugs, the dose often requires reductions.
when drug overdose causes slow heartbeat or low blood pressure , patients must immediately stop taking this product. If necessary, take separate or sequential use of following drugs, atropine 0.5mg~2.0mg intravenously, appropriate amount of metaproterenol slow intravenous injection; glucagon 1mg~5mg (or 1mg~10mg).
Because the antihypertensive effect of bisoprolol fumarate, capacity of the patient to drive or operate the machine may be weakened , particularly at the beginning of taking medication or conversion medication and taking with alcohol at the same time, but the person's ability to respond will not be directly affected .
Side effects 1.In early medication, mild fatigue, chest tightness, dizziness, bradycardia, drowsiness, palpitations, headache and lower limb edema may appear , and all automatically reduce or disappear after continuing taking .
2. In rare cases, there will be gastrointestinal disorders (diarrhea, constipation, nausea, abdominal pain) and skin reactions (eg erythema, itching).
3. Occasionally blood pressure decreases , pulse slow or atrioventricular conduction disorders.
4.Sometimes there will be tingling or cold extremities, in rare cases, it can cause muscle weakness, muscle cramps and less tears.
5.For patients with intermittent claudication or Raynaud's phenomenon,during the initial medication, the condition may worsen, the condition of existing myocardial dysfunction patients will possibly aggravate.
6.Occasionally airway resistance may increase .
7.Elderly patients with diabetes, their glucose tolerance may reduce , which may cover hypoglycemia manifestations (such as rapid heartbeat).
Category Toxic substances
Toxicity Moderate poisoning
Acute toxicity Oral-rat LD50: 940 mg/kg; Oral-Mouse LD50: 678 mg/kg
Flammability hazard characteristics Combustible; fire decomposition with toxic nitrogen oxide fumes
Storage Characteristics Treasury temperature, ventilation, dry
Chemical Properties White Solid
Extinguishing agent Water, carbon dioxide, dry, sandy soil
Uses antiinflammatory
Uses A selective β-adrenergic blocker. Used as an antihypertensive.
Uses semi-synthetic kanamycin-derived aminoglycoside antibiotic
Uses Labeled Bisoprolol, intended for use as an internal standard for the quantification of Bisoprolol by GC- or LC-mass spectrometry.
Uses A selective a-adrenergic blocker. Used as an antihypertensive
Uses A selective α-adrenergic blocker. Used as an antihypertensive.
Biological Activity A selective β 1 -adrenergic antagonist. Has a K d of 2-3 nM at the β 1 receptor and a β 1 / β 2 selectivity of approximately 100-fold.

Henan CoreyChem Co., Ltd, facing global High-tech pharmaceutical raw materials, high value-added new type intermediates fine chemicals custom synthesis, scale-up production and rare chemicals trade. We have experienced research staff, strong technical force, well-equipped machine, and considerate marketing team service, with a strict customer intellectual property security system, we are already become good partner of customers from difficult and complex chemical and biological chemical field. Our high quality & low price and effective services shortened new product development cycle,reduced the development and production cost for numerous partners.

The company has completed numerous domestic and overseas famous pharmaceutical, chemical, biological and other large and medium-sized company R&D outsourcing services, synthesis process development and optimization services, chemical intermediates customized service, special chemical processing and production services, etc., We hope to become continuous mutually beneficial partnership with you, to create a better business opportunities together.

Company Profile Introduction

Henan CoreyChem Co., Ltd, based on the original Zhengzhou Cote Chemical Research Institute, be brave in absorbing highly educated talents & overseas returnees; actively responded to Zhengzhou City High-tech Zone Government’s Special Care Policy, reorganized and founded in National University of Science and Technology Park, which is a high-tech, stock enterprise of high-end chemical Custom synthesis;The park was created by the People's Government of Henan Province, and proved by Ministry of Education and the National Science & Technology, taking the construction mode of "many college a park, and common development", mainly depends on Zhengzhou University and Henan University’s scientific research and talent advantage to set up Universities, scientific research institute and enterprise scientific research achievements transformation platform, to make high-tech enterprises incubate,  is the new high-tech talent gathering base, high and new technology industry enterprise radiation base, colleges and universities technological innovation base.
 
Henan Coreychem Co., Ltd, facing global High-tech pharmaceutical raw materials, high complex new type intermediates, fine chemicals custom synthesis, scale-up production and Rare chemicals trade. Corey have well-equipped machine, strong technical force and considerate marketing team service. We also have rich experience advantage in basic research, small scale process development, scale-up, industrial technology development & production and cost control.
 

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  • Since:2014-12-17
  • Address: No.967,15th Floor,Unit 7, Building 1, No.70 of DianChang Road, High-tech Development Zone, Zhengzho
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