Amlodipine Besylate powder is a long-acting calcium channel inhibitor with an IC50 of 1.9 nM. It is a third-generation 1,4-dihydropyridine calcium ion antagonist developed by Pfizer in the 1980s. This drug is unanimously recommended by the FDA Heart and Kidney Advisory Committee for the treatment of hypertension. It is also a common product for treating hypertension and angina pectoris in clinical practice in China.
| Test | Enterprise Standard | Results Of Analysis |
| Description | white crystals | confirm |
| solubility | Easily soluble in methanol | confirm |
| differentiate | positive reaction | confirm |
| sulfate | ≤0.2% w/w | 0.12% |
| Optical Rotation | -1°-+1° | 0.01° |
| Individual impurity | ≤0.1% | confirm |
| Total impurity | ≤0.3% | confirm |
| impurity D | ≤0.3% | negative |
| moisture content | ≤0.5% w/w | 0.28% |
| heavy metal | ≤20ppm | <20ppm |
| Fe | ≤20ppm | <20ppm |
| Melting Point | 199℃~201℃ | 199℃~ 200℃ |
| Specific Rotation | +25°~ +31° | +27° |
| Assay | 97.0~102.0% | 99.2% |
| Conclusion | The specification conform with enterprise standard |
Which effect is better, amlodipine besylate or levoamlodipine besylate?
Both amlodipine besylate and levoamlodipine besylate belong to calcium antagonist antihypertensive drugs, so there is little difference in antihypertensive effect. However, it should be noted that there are two structures of amlodipine, that is, levorotatory and dextrorotatory. In fact, levorotatory plays a major role in antihypertensive, while dextrorotatory does not. Levamlodipine besylate is a part of amlodipine besylate, and it is also an effective levorotatory structure for treating hypertension, so the side effects of drugs will be less. Clinically, using 2.5 mg of Levamlodipine besylate is equivalent to using 5 mg of amlodipine besylate.
However, compared with L-amlodipine without D-isomer, the D-isomer in amlodipine besylate powder has a certain protective effect on blood vessels, so it is more suitable for patients with heart problems.
To sum up, both of them have their own strengths, and which product to use depends on the patient's condition and physical condition. In order to meet the needs of different customers, our company often develops some products with different optical rotation directions, such as amlodipine besylate and levoamlodipine besylate. If you are interested in the research of levorotatory (S-type) and dextrorotatory (R-type), please leave us a message by email: email:sales6@faithfulbio.com
What is a calcium ion antagonist?
At the beginning, we pointed out that this product is a calcium antagonist, or calcium channel blocker, which can treat hypertension and heart disease, but many people may not quite understand the biological law on which calcium antagonists treat hypertension and heart disease.
Let's know the mechanism of action of calcium antagonists in detail. It is necessary to first explain how high blood pressure is produced. Blood pressure refers to the lateral pressure on the blood vessel wall when blood flows in the blood vessel. The vast majority of patients with hypertension (more than 90%) have no specific etiology, which is mostly caused by the weakening of vascular wall elasticity and the increase of resistance with age. There are calcium channels on the smooth muscle cell membrane of myocardium and vascular wall, which control the entry and exit of calcium ions like a gate. The increase of intracellular calcium concentration can cause the contraction of cells, increase vascular resistance and increase blood pressure. Calcium antagonists are like loyal gatekeepers. After combining with calcium channels, they prevent calcium ions from entering cells, thus relaxing blood vessels, reducing resistance and finally lowering blood pressure.
However, some calcium antagonists, such as amlodipine besylate and diltiazem, can not only relax the blood vessels of the whole body, but also directly relax the coronary arteries that supply blood to the heart, which will alleviate the problem of myocardial ischemia or treat heart disease.
At the same time, amlodipine besylate powder is the representative of the third generation calcium ion antagonist, and its molecular structure makes it a long-acting calcium ion antagonist. Studies have shown that its half-life is as long as 35-50 hours, so it can be taken once a day without using sustained-release or controlled-release dosage forms, and its blood pressure can be controlled smoothly for 24 hours. Moreover, its effect is not affected by gastrointestinal function problems, food and most other products. In addition, because its action lasts for a long time, patients will not raise their blood pressure if they miss it once occasionally.
Is there a contradiction between calcium supplementation and calcium antagonists?
We found that elderly patients with hypertension will take calcium tablets while using this product to reduce blood pressure. Many people wonder that the two products have opposite effects, and when they are used together, will their effects not cancel each other out?
We need to point out that calcium is not contradictory to calcium antagonists, and calcium supplementation is to correct negative calcium balance, prevent calcium metabolism disorder and bone calcium loss in vivo, and avoid abnormal deposition of calcium in blood vessels and soft tissues, thus reducing the occurrence of atherosclerosis. However, these calcium can not easily enter the cell, only through the special calcium ion channel on the cell membrane. Under normal circumstances, the extracellular calcium ion concentration is far greater than the intracellular calcium ion concentration, and maintaining such a concentration gradient depends on the calcium ion channel. However, if the calcium ion channel fails to regulate, a large number of calcium ions will enter the cell, causing vascular smooth muscle contraction, blood pressure will rise, and even cause hypertension, angina pectoris and myocardial infarction. Therefore, in order to maintain the concentration difference between inside and outside the cell, we need to control this channel, and proper and correct use of calcium antagonists can close the calcium channel in time and block the abnormal inflow of calcium ions.
Calcium antagonists commonly used in clinic,Such as nifedipine,Amlodipine,Lacidipine and so on are the first choice products in this area.
It can be seen that both calcium and calcium antagonists can protect cardiovascular and cerebrovascular diseases, prevent and treat hypertension, and there is no contradiction between them. And clinical research shows that if used together, calcium supplements can not only help to lower blood pressure, but also offset the hypertensive effect of high-salt diet on spontaneous hypertension. It is speculated that this phenomenon may be related to the fact that calcium supplements can prevent the increase of plasma norepinephrine concentration.
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|
Transportation Time |
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Cargo weight requirements |
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3-7 days |
DHL,Germany DHL,Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
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Suitable for more than 500kg. |
Our strengths:
Our company has passed FDA and ISO19001 quality management system certification. And we have internal cooperation agreements with multiple factories and laboratories in China, Therefore, we can provide you with the required amlodipine besylate,Levoamlodipine Besylate,
Diltiazem,Nifedipine,Amlodipine,Lacidipine and other products
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