what is Leflunomide powder ?
Leflunomide, also known as Airuohua, Leflunomide, or Dongwa, is an imidazole immunosuppressant with anti proliferative activity. Modern pharmacology classifies this product as an antipyretic, analgesic, and anti-inflammatory drug. Due to the difficulty in adjusting the dosage of this product for organ transplant patients, it is mainly used to treat autoimmune diseases such as rheumatoid arthritis. After oral administration, Leflunomide powder is rapidly converted into active metabolites in the intestinal wall and liver, with an F of 80%. Eating does not affect absorption. The Tmax is 6-12 hours. If the first dose is given with a loading dose of 100mg, the steady-state blood concentration will be reached within 3 days, otherwise it will take several months to reach the steady-state blood concentration. The active metabolite PPB is 99.3%, mainly distributed in the liver, kidneys, and skin, with less in brain tissue. After further metabolism of active metabolites, 43% of the markers are excreted in urine and 48% in feces. T1/2 is about 2 weeks, and enterohepatic circulation is the main factor leading to a longer half-life of active metabolites. A high-fat diet does not have a significant impact on drug plasma concentration. Activated carbon or cholesteryl amine can inhibit drug absorption.
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Product name |
Leflunomide |
|
CAS |
75706-12-6 |
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|
Molecular formula |
C12H9F3N2O2 |
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Molecular weight |
270.21 |
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EINECS Number |
616-254-6 | |
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Storage condition |
2-8°C |
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Appearance |
white powder |
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Melting point |
166.5°C |
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| Density |
1.392±0.06g/cm3(rough estimate) |
What is Leflunomide powder's Mechanism of action ?
Leflunomide powder is rapidly converted into active metabolites through the cytoplasm and microsomes of the liver and intestinal wall, and its mechanism of action is mainly to inhibit the activity of a key enzyme in DNA synthesis - dihydroorotate dehydrogenase (DHODH), thereby reducing the consumption of nucleotides in B lymphocytes, terminating the biosynthesis of DNA and RNA, preventing cells from entering the S phase and ultimately preventing proliferation, thus producing anti rheumatic effects. It is suitable for the treatment of adult active rheumatoid arthritis and ankylosing spondylitis, and can slow down bone destruction, alleviate symptoms and signs. In addition, leflunomide can also inhibit the activity of tyrosine kinases, thereby suppressing the proliferation of T cells, B cells, and non immune cells. It can also exert anti-inflammatory effects by inhibiting the synthesis of prostaglandins by suppressing the biosynthesis of cyclooxygenase-2 (COX2), and can inhibit the release of histamine in mast cells and eosinophils.
What is the use and side effect of Leflunomide powder?
Leflunomide powder is a nonsteroidal anti-inflammatory drug Has immunosuppressive and anti-inflammatory effects, used to treat adult active rheumatoid arthritis.
Nausea, vomiting, diarrhoea, abdominal pain, loss of appetite or weight loss:Take medication after food to reduce the side effects. Sucking hard, sugar-free candy may reduce nausea and vomiting. Inform your doctor if symptoms are severe or if you experience loss of appetite.
Headache, dizziness, weakness:Usually improves as you get used to the medication.
Loss of hair:It is reversible when the medicine is stopped.
Increased blood pressure:Check your blood pressure regularly. Consult your doctor if high blood pressure persists.
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Product Specification
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Items |
Standards |
Results |
|
Character |
white powder |
white powder |
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Solubility |
As stipulated |
Conform |
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Identification |
Conform to standard |
Conform |
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Loss on drying |
≤0.5% |
0.13% |
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Ignition residue |
≤0.1 % |
0.09% |
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Assay test |
99.0%～101.0% |
99.5% |
What is the production method of Leflunomide powder?
Ethyl acetoacetate, triethyl orthoformate, and acetic anhydride were refluxed together until the raw materials were completely reacted, for about 5 hours. Distillation collection of 140, 150 ℃/1.87kPa fractions resulted in compound (I) with a yield of 85%. Compound (I) is dissolved in anhydrous ethanol and a mixture of hydroxylamine hydrochloride, sodium acetate, and water is added dropwise at 10-15 ℃ for 1 hour.
After dripping, react for about 8 hours. Add concentrated hydrochloric acid and glacial acetic acid, reflux for 5 hours. Concentrate to 1/2 volume under reduced pressure, cool to below 10 ℃, filter, and recrystallize from ethanol water to obtain compound (II) as a white crystalline powder with a melting point of 145-146.5 ℃ and a yield of 80%. Compound (II) is dissolved in thionyl chloride is added dropwise at 50-55 ℃ under reflux for 3 hours. Concentrate, fractionate, and collect fractions at 78-79 ℃/1.87kPa to obtain compound (III) with a yield of 75%. Dissolve trifluoromethylaniline and triethylamine in dichloromethane and add compound (III) dropwise at 0-5 ℃. React at 25-30 ℃ for 3 hours. Add water, separate the organic layer, wash with water, wash with saturated salt, and dry. Concentrate to 1/3 volume under reduced pressure, add petroleum ether, cool, filter, and recrystallize from ethyl acetate to obtain white crystalline powder of leflunomide powder with a melting point of 166-167 ℃ and a yield of 81%.
How and where to buy Leflunomide powder wholesale?
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A variety of shipping methods for you to choose
|
Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
|
3-7 days |
DHL, Germany DHL, Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
|
7-15 days |
By Air |
Suitable for more than 50kg. |
|
|
15-60 days |
By Sea |
Suitable for more than 500kg. |
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