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Candesartan Cilexetil 145040-37-5
Product Specification
| Appearance: | White powder |
| Identification by IR: | IR spectrum of the sample in KBr dispersion should concordant with working standard |
| Identification by HPLC： | The retention time of the main peak in the chromatogram of the test preparation should match to that in the chromatogram of the standard preparation. |
| Water: | ≤0.5% |
| Heavy metals : | ≤20ppm |
| Residue on ignition : | ≤0.2% |
| Solvents: | Ethanol≤5000ppm、Acetone≤800ppm 、Ethyl acetate≤5000ppm、Toluene≤890ppm、Acetic acid≤5000ppm |
| Max singleImpurity： | ≤0.10% |
| Total Impurity： | ≤0.50% |
| Assay(HPLC)(On anhydrous basis)： | 99.0% ~ 102.0% |
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PRODUCT DESCRIPTION
Hypertension disease, due to its high incidence, high morbidity and high mortality as well as the resulted various kinds of issues including medical, social, family, economic, has changed from purely personal disease to serious social issues. Study and development of first-line drug treatment of hypertension has increasingly become the focus of the world's major competing focus of many major manufacturers. The main purpose of the treatment of hypertension is to minimize the total risk of cardiovascular disease death and disability with its goal being able to restore blood pressure to 140/90mmHg or less.
Currently, there are many kinds of clinical anti-hypertensive drugs and can be primarily divided into five categories, namely, diuretics, β-blockers, angiotensin-converting enzyme inhibitors (ACE-Ⅰ), calcium antagonists, and α-blockers. They all have certain limitations and side effects in use. Since the 1980s, ACE-I have been widely used to treat a variety of cardiovascular diseases and have been demonstrated to have excellent pressure-lowering effect on high blood pressure. However, since the ACE-Ⅰ also inhibits the degradation of bradykinin, and thus often resulting dry cough during the treatment of patients.
Currently, a new class of anti-hypertensive drugs-angiotensin Ⅱ receptor antagonist has been listed. A typical representative of such drugs includes losatran (Merck), valsartan (Novartis) and eprosartan (SmithKline). As the role of these drugs are more specific than the ACE-I, increasing the antihypertensive effect with reduced side effects as well as not causing cough. It also has protective effects on blood vessels, kidneys and heart. Therefore, this type of drug has become a competition protagonist in the hypertension drug market.
Candesartan cilexetil is the pro-drug of candesartan with the action strength being 10 times as high as losatran. Its action has a good selectivity (has a 10000 time higher affinity to AT1 receptor than AT2), long duration of action (take it one time daily). As a pro-drug, it can release its activity in a relatively mild way after oral administration, making it be a kind of ideal drug for treatment of hypertension.
According to the foreign prediction, the annual sales of this kind of goods can reach up to $ 2 billion so the development of this product will surely achieve good economic and social benefits.
Candesartan cilexetil(145040-37-5) is a prodrug of the potent, long-acting, and selective angiotensin II type 1 receptor AT1 antagonist, candesartan. It is rapidly hydrolyzed to candesartan during gastrointestinal absorption. After hydrolysis of candesartan cilexetil to candesartan during gastrointestinal absorption, candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 AT1 in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation. In addition, antagonism of AT1 in the adrenal gland inhibits angiotensin II-stimulated aldosterone synthesis and secretion by the adrenal cortex; sodium and water excretion increase, followed by a reduction in plasma volume and blood pressure.
Candesartan cilexetil can be used as pesticide and pharmaceutical intermediates.
It can be used as the raw material of antihypertensive drugs.
Candesartan is an angiotensin-receptor blocker (ARB)，Angiotensin receptor blockers effectively protect against the harmful effects of the activation of the renin-angiotensin-aldosterone system that occur with hypertension or diabetes.It may be used alone or with other agents to treat hypertension. Unlike angiotensin-converting enzyme (ACE) inhibitors, ARBs do not have the adverse effect of dry cough.
Candesartan may be used to treat hypertension, isolated systolic hypertension, left ventricular hypertrophy and diabetic nephropathy. It may also be used as an alternative agent for the treatment of heart failure, systolic dysfunction, myocardial infarction and coronary artery disease.