HRK Oseltamivir Raw Materials Powder on sale

CAS:196618-13-0

MF:C16H28N2O4

MW:312.4

EINECS:1308068-626-2

Specification​: 99% min Oseltamivir Powder

Sample:Oseltamivir Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:white

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Oseltamivir Usage and Function.

Oseltamivir was the first neuraminidase inhibitor to be made into an oral formulation for the prevention and treatment of influenza (mainly influenza A and B). It can be converted into an active metabolite in human body that has an inhibitory effect on influenza virus neuraminidase. The replication cycle of influenza viruses is known to repeat in the following stages: Hydrolytic activation of the glycoprotein kinin (HA) on the surface of the virus →HA binding to the specific neuraminidase receptor on the cell surface → host cell granulation, virus fusion with the endosome membrane → nuclear shell removal → proliferation (synthesis of viral RNA and mRNA)→ Newly generated virus is released from the host cell surface under the action of neuraminidase. The active metabolites of oseltamivir can inhibit the release and transmission of influenza A and B virus particles. After oral administration, the active metabolites of this product can enter the trachea, alveoli, nasal mucosa and other parts where influenza virus is located. It has a half-life of 6 to 10 hours and is excreted mainly by the kidneys. In addition to treating influenza, this product also has a preventive effect on influenza.

Drug interaction of Oseltamivir.

Data from pharmacological and pharmacokinetic studies indicate that there are essentially no clinically significant interactions between oseltamivir phosphate and other drugs. Cimetidine did not affect plasma concentrations of oseltamivir or its active metabolites. Combined administration of prosulfa resulted in a two-fold increase in the plasma level of the active metabolite due to reduced secretion of the active product by the renal tubules. However, there is no need to adjust the dosage of the drug when it is used with prosulfa.

It has been shown that renal excretion of active metabolites is accomplished by a combination of glomerular filtration and renal tubule excretion through anion channels. Clinically important drug interactions, including competition for renal tubule secretion, are unlikely to occur. Because the safe range of these drugs is known, the excretion of active metabolites of oseltamivir phosphate includes glomerular filtration and renal tubule excretion, and the excretion capacity of these two pathways is large. In combination with paracetamol, plasma concentrations of oseltamivir and its active metabolites or paracetamol did not change.

In Phase III clinical studies, oseltamivir phosphate has been used in combination with common drugs such as ACE inhibitors (enalapril, Pacemaker), thiazide diuretics (benzofluthiazide), antibiotics (penicillin, cephalosporin), H2 blockers (ranitidine, cimetidine), beta blockers (propranolol), and analgesics (aspirin, propranolol). Ibuprofen and paracetamol). The combination of these drugs did not lead to adverse reactions or changes in their incidence. Oseltamivir phosphate is rapidly converted into active metabolites by esterases mainly distributed in the liver and intestine. Drug interactions related to competitive esterases have not been extensively reported in the literature.

The low protein binding rates of oseltamivir and its active metabolites suggest that drug displacement interactions are unlikely. In vitro studies have shown that neither oseltamivir phosphate nor its active metabolites are good substrates for P450 mixed-function oxidase or glucuronidase, and drug interactions with P450 isoenzymes are not possible.

Pharmacological action of Oseltamivir.

Oseltamivir phosphate is a drug precursor of its active metabolite, which (oseltamivir carboxylate) is a selective influenza virus neuraminidase inhibitor. Neuraminidase is a glycoprotease on the surface of viruses whose activity is critical for the release of newly formed viral particles from infected cells and for the further dissemination of infectious viruses in the human body. The active metabolite of oseltamivir phosphate inhibits neuraminidase activity of influenza A and B viruses. The concentration of half inhibition of viral neuraminidase activity in vitro was as low as nanograms. The active metabolites were observed to inhibit the growth of influenza virus in vitro, and to inhibit the replication and pathogenicity of influenza virus in vivo. This product reduces the spread of influenza A or B viruses by inhibiting the release of the virus from infected cells. Studies of naturally acquired and laboratory influenza have shown that the administration of oseltamivir phosphate does not affect the normal humoral immune response to infection. Antibody response to inactivated vaccine was not affected by oseltamivir phosphate treatment.

Product Method of Bulk Oseltamivir Powder.