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Absolute bioavailability of a new high dose methylprednisolone tablet formulation
G Groenewoud1, H K Hundt, H G Luus
1Department of Pharmacology, Farmovs Institute for Clinical Pharmacology and Drug Development, University of the Orange Free State, Bloemfontein, South Africa.
International Journal of Clinical Pharmacology and Therapeutics
|December 1, 1994
Summary
The high-dose Medrol (methylprednisolone) tablet demonstrated 82% absolute bioavailability, comparable to intravenous formulations. This indicates the oral tablet is a viable alternative for high-dose methylprednisolone therapy.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Drug Development
Background:
- Methylprednisolone is a potent corticosteroid used for various inflammatory and autoimmune conditions.
- High-dose methylprednisolone therapy often requires intravenous administration for rapid and consistent delivery.
- Evaluating the bioavailability of oral formulations is crucial for therapeutic equivalence and patient convenience.
Purpose of the Study:
- To determine the absolute bioavailability of a new high-dose (100 mg) methylprednisolone tablet (Medrol).
- To compare the pharmacokinetic profile of the oral Medrol tablet with an intravenous formulation (Solu-Medrol).
Main Methods:
- A single-blind, randomized crossover study involving 14 healthy male volunteers.
- Administration of 100 mg oral Medrol and 100 mg intravenous Solu-Medrol in separate treatment periods.
- Serial blood sampling over 14 hours post-administration to measure plasma methylprednisolone concentrations using high-performance liquid chromatography.
Main Results:
- The absolute bioavailability of the Medrol tablet was calculated to be 82%.
- Geometric mean AUC values were 4,049 ng.h/ml for i.v. and 3,334 ng.h/ml for the tablet.
- No clinically significant adverse effects or changes in hematology/clinical chemistry were observed.
Conclusions:
- The 100 mg Medrol tablet exhibits good absolute bioavailability, consistent with other oral methylprednisolone forms.
- The oral tablet can be considered a suitable substitute for parenteral methylprednisolone in high-dose treatment scenarios.
- This finding supports the potential for enhanced patient convenience and alternative administration routes for high-dose methylprednisolone therapy.