Antiviral compound, dosage form including same, and uses thereof
A compound and virus technology, applied in the field of antiviral infection, can solve the problem that influenza infection does not achieve the best therapeutic effect
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Embodiment 1
[0140] Example 1. Effect of intravenous injection of peramivir on influenza A virus infection
[0141] Experimental design: i.n. the dose of LD100, which is believed to be influenza virus, infects mice. One hour before exposure to the virus, each group of mice (10 mice / group) was treated with a single intravenous injection of peramivir at doses of 20, 10, and 3 mg / kg. Parallel to the above, placebo (sterile saline) was intravenously injected into 20 infected mice. The deaths of the infected mice treated with drugs and the control mice treated with placebo were observed every day for 21 days. As a toxicity control, 3 uninfected mice were treated with the highest dose of compound in parallel with the infected animals. Observe the death of all toxicity controls within 21 days and weigh them immediately before the initial treatment and 18 hours after the final treatment. Weigh 5 normal control mice.
[0142] Table 2. Effect of a single intravenous injection of peramivir on mice inf...
Embodiment 2
[0149] Example 2. Treatment effect on human intravenous injection and intramuscular injection of peramivir
[0150] Peramivir was studied in a placebo-controlled phase I clinical study of healthy volunteers to evaluate the safety and pharmacokinetic parameters of intravenous and intramuscular administration. Blood samples were collected from subjects at different time points after administration to determine the drug concentration in plasma. figure 1 with figure 2 The time course diagrams of intravenous and intramuscular administration are shown respectively.
[0151] In the intravenous administration study, the concentration of peramivir followed linear kinetics, and its plasma half-life was unusually extended to more than 12 hours. At a dose greater than or equal to 2 mg / kg, the plasma level of peramivir is greater than the IC of all influenza virus strains tested (including H5 virus type) 48 hours after the dose 50 . For doses greater than 4mg / kg, even at 72 hours, the drug le...
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