Method for administrating preparations containing oseltamivir guanidyl carboxylate analogues and/or ethyl esters thereof

Abstract

The invention relates to a method for administrating preparations containing oseltamivir guanidyl carboxylate analogues and / or ethyl esters thereof. Administration is carried out through inhalation. The method can be used for treating cold caused by influenza viruses. By adopting the administration method provided by the invention, not only can dependence on the single variety of drugs such as oseltamivir, zanamivir and peramivir be reduced and new drug resistant virus strains generated by using the single variety in quantity be avoided but also the method which is favorable for greatly improving the bioavailability compared with oral administration or intravenous drip is provided for oseltamivir guanidyl carboxylate analogues or ethyl esters thereof; more importantly, the method which has the advantages of small drug dose, less side effects and high effect taking speed is provided.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to (3R, 4R, 5S)-4-acetylamino-5-guanidino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid ( C 15 h 26 N 4 o 4 : Oseltamivir carboxylic acid guanidine analogue) and / or its ethyl ester are used as neuraminidase inhibitors, and are used for the method for the treatment of influenza by lung target direct respiratory administration. Background technique [0002] As we all know, influenza (Influenza) is an acute respiratory infectious disease caused by influenza virus. It is highly contagious and has a high incidence rate, which can easily cause outbreaks or pandemics. [0003] According to the World Health Organization (WHO), the outbreak of H7N9 bird flu in 2013 had infected 132 people as of May 30, of which 37 died, with a mortality rate as high as 28%. The H1N1 swine flu (Swine Flu) epidemic from 2009 to 2010 has laboratory-confirmed cases of infection in more than 2...

AI Technical Summary

Problems solved by technology

Zanamivir is also problematic, with a low bioavailability of 2%, where up to 15% of the dose is absorbed and excreted in urine

More importantly, due to the variability of influenza virus genes, large-scale use of a single species will result in new drug-resistant virus strains

[0010] A 2011 study reported that new strains of swine flu emerging in Asia had developed some resistance to Roche's Tamiflu and GSK's Reganza without significantly reducing susceptibility to peramivir

However, there is a big problem with intravenous infusion, that is, it can only be carried out in a hospital, and the patient cannot take the medicine by himself, and the economic cost is high. More importantly, the dosage is large, and one infusion takes 600mg, and it takes 30 minutes.

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