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Plasma concentrations during repeated intravenous and oral methyl-proscillaridin application in man
Abstract:
The aim of this study was to establish data on the plasma levels of the glycoside derivative methyl-proscillaridin (MP) following repeated intravenous and oral doses. The study was carried out on healthy male volunteers. Each received 0.5 mg of MP daily at 8 a.m. for 7 days. 6 volunteers received the drug i.v., 6 p.o. as tablets and 5 p.o. as elixir. Plasma glycoside concentrations were measured utilizing a 86Rb-erythrocyte assay. The mean plasma concentrations on the 6th and 7th days of application were: 752.9 (Sx = 303.5) pg/ml for the i.v. route, 432.9 (Sx = 115.5) pg/ml for the tablets and 473.1 (Sx = 321.5) pg/ml for the elixir. The mean ratio between plasma concentrations with tablets and i.v. injection averaged 63%. It is concluded that the therapeutic activity of oral MP is about 60 to 70% that of the i.v. application.
Insights
This study measured methyl-proscillaridin (MP) plasma levels in healthy volunteers after intravenous and oral doses. Oral MP showed approximately 60-70% of the therapeutic activity compared to intravenous administration.
Area of Science:
- Pharmacology
- Clinical Pharmacology
- Drug Metabolism
Background:
- Methyl-proscillaridin (MP) is a glycoside derivative with therapeutic applications.
- Understanding the pharmacokinetic profile of MP after different administration routes is crucial for optimizing dosage and efficacy.
- Previous data on plasma levels following repeated oral and intravenous dosing may be limited.
Purpose of the Study:
- To determine and compare plasma concentrations of methyl-proscillaridin (MP) after repeated intravenous and oral administration in healthy male volunteers.
- To establish the bioavailability and relative therapeutic activity of orally administered MP compared to intravenous MP.
- To provide data for potential adjustments in clinical dosing strategies.
Main Methods:
- A pharmacokinetic study involving 17 healthy male volunteers.
- Administration of 0.5 mg of methyl-proscillaridin (MP) daily for 7 days via intravenous injection, oral tablets, or oral elixir.
- Quantification of plasma glycoside concentrations using a 86Rb-erythrocyte assay on days 6 and 7.
Main Results:
- Mean plasma concentrations of MP on days 6 and 7 were 752.9 pg/ml (i.v.), 432.9 pg/ml (tablets), and 473.1 pg/ml (elixir).
- The mean ratio of plasma concentrations between oral tablets and intravenous injection was approximately 63%.
- Plasma concentrations for the elixir route were comparable to tablets, suggesting similar oral bioavailability.
Conclusions:
- Oral administration of methyl-proscillaridin (MP) results in approximately 60-70% of the therapeutic activity observed with intravenous administration.
- The bioavailability of MP from both tablet and elixir formulations appears to be comparable.
- These findings support the understanding of MP pharmacokinetics and can inform clinical practice regarding oral versus intravenous dosing.