what is Lamivudine powder?
Lamivudine powder is a novel antiviral drug that belongs to the nucleoside reverse transcriptase inhibitor class. It has a strong inhibitory effect on hepatitis B virus (HBV) in vitro and in experimentally infected animals, and can inhibit the synthesis of HIV virus; This drug is produced by GlaxoSmithKline Group. In the early 1990s, it was used by some countries in Europe and North America to treat AIDS. In the mid-1990s, medical experts found that it had an inhibitory effect on the DNA of hepatitis B virus. In 1998, the Food Chemicalbook and the Drug Administration (FDA) of the United States first approved it as a treatment drug for hepatitis B. The State Food and Drug Administration in Chinese Mainland approved the drug to be imported mainly for the treatment of hepatitis B. and it was officially sold in Chinese Mainland in 1999. After 10 years of clinical verification, Lamivudine is the only drug that has been proven to delay the progress of hepatitis and cirrhosis, with less side effects and costs. At present, there are 2 million hepatitis B patients in China who are using it.
 |
Product name |
Lamivudine |
|
CAS |
134678-17-4 |
|
|
Molecular formula |
C8H11N3O3S | |
|
Molecular weight |
229.26 | |
|
EINECS Number |
603-844-3 | |
|
Storage condition |
2-8°C |
|
|
Appearance |
white powder |
|
|
Melting point |
177 °C | |
| Density | 1.73±0.1 g/cm3(Predicted) |
What is the mechanism of action of lamivudine powder?
Lamivudine can be metabolized into lamivudine triphosphate in HBV infected cells and normal cells. It is the active form of lamivudine and serves as both an inhibitor and substrate for HBV polymerase. Lamivudine triphosphate is incorporated into the viral DNA strand, blocking the synthesis of viral DNA without interfering with the metabolism of deoxyribonucleosides in normal cells. It has a weak inhibitory effect on mammalian DNA polymerase alpha and beta, and has almost no effect on the DNA content of mammalian cells. There is no significant toxicity to the structure, DNA content, and function of mitochondria. The serum HBV-DNA test results of most hepatitis B patients indicate that lamivudine can rapidly inhibit HBV replication, and its inhibitory effect lasts throughout the entire treatment process. Simultaneously reducing serum transaminase levels to normal, long-term use can significantly improve liver necrosis and inflammatory changes, and alleviate or prevent the progression of liver fibrosis.
What diseases and patients are suitable for using lamivudine powder?
if you need it,you can click email：sales1@faithfulbio.comHepatitis B, chronic hepatitis B virus replication.
Based on the characteristics of lamivudine's action and clinical experience, lamivudine should be used in the following situations: (1) moderate or above positive HBVDNA quantitative detection; HBeAg positive; ALT increases by 2-10 times. (2) HBeAg is negative, but HBVDNA is moderately or above positive (not based on qualitative PCR results, quantitative testing should be performed), and ALT is elevated by 2-10 times. This situation is mostly likely due to mutations in the pre-C region of viral genes.
The situations where lamivudine powder is not suitable for use mainly include: (1) HBV DNA negative or quantitative determination<105 copies/ml; (2) ALT is normal (mainly referring to asymptomatic carriers of the virus); For patients who have had ALT elevation in the past but now have normal ALT and AST, treatment can be temporarily left untreated and resumed after ALT elevation. The reason why these two types of patients are not suitable for use is not because lamivudine is harmful to these people, but because the effectiveness rate for these patients is low and does not comply with the principles of pharmacoeconomics. Lamivudine, like other drugs, can benefit most patients when used appropriately. Improper use may not bring expected therapeutic effects, and inappropriate discontinuation may even worsen the condition.
Product Specification
|
ITEMS |
STANDARDS |
RESULTS |
|
Description |
White powder |
Complies |
|
Light Absorption |
NMT0.0015 |
0.000090 |
|
limit of Lamivudine Enantiomer |
NMT0.3% |
Not detected |
|
Water |
NMT2.0% |
0.04% |
|
Related Substances
|
Lamivudine CARBOXYLIC acid impurity ≤0.3% Lamivudine-trans Impurity ≤0.2% |
0.05% Not detected |
| Salicylic acid impurity ≤0.2% |
0.09% |
|
|
Any other impurity≤0.1% |
Not detected |
|
|
Tatal impurity ≤0.6% |
0.1% |
|
|
Assay |
98%~102% |
99.7% |
|
Residual |
Ethanol NMT0.2% |
1308PP |
How to produce lamivudine powder?
Selective 6-O-sulfonylation reaction was performed on compound (I), followed by acetylation to obtain compound (II) with a yield of 96.7%. Compound (II) was reacted with 3moL of hydrogen bromide/L acid (45%, W/V) using acetic acid as a solvent, and brominated to obtain compound (III) with a yield of 99%. Bromide (III) and 3.3 moI. Potassium salt of ethyl xanthate, refluxed in acetone, thiolated and cyclized; Then, compound (IV) was obtained by hydrolysis with ammonia water in methanol, with a two-step yield of 72%. Compound (IV) was purified by column chromatography to obtain a crystalline solid. Compound (IV) was treated with 1.4 moles of sodium periodate to open the ring of 2,3-cis-1,2-diol; Then, the aldehyde formed by reduction was used to protect the diol in the form of a ketal, resulting in compound (V) with a yield of 60%. Compound (V) was silanized to protect the remaining primary alcohol, and then the ketal was removed to obtain compound (VI) with a yield of 63%. Lead tetraacetate is used to oxidize the diol in compound (VI), followed by further oxidation with pyridine dichromate salt to obtain compound (VII). This oxidation method does not affect sulfur. Compound (VII) was further oxidized with lead tetraacetate to obtain compound (VIII) with a yield of 66% [calculated as compound (VI)].
Compounds (VIII) and (IX) were condensed in dichloroethane using TMSOTf as a Lewis acid catalyst to obtain compound (X) with a yield of 64%. In addition, there are isomers of compound (X), which account for half of the amount of compound (X), and they can be separated by silica gel chromatography. Compound (X) was deacetylated with ammonia methanol in a yield of 73%; Further desilication with tetra-n-butylammonium fluoride yields Lamivudine powder with a yield of 75%
How and where to buy Lamivudine powder wholesale?
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|
Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
|
3-7 days |
DHL, Germany DHL, Germany DPD, |
Suitable for under 50kg. |
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7-15 days |
By Air |
Suitable for more than 50kg. |
|
|
15-60 days |
By Sea |
Suitable for more than 500kg. |
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