A preliminary study on urinary excretion patterns of methylprednisolone after oral and intra-articular administration and effect on endogenous glucocorticosteroids profile.

INTRODUCTION: The use of glucocorticosteroids (GCs) through oral, intravenous, intramuscular, or rectal routes is prohibited in sports. Its use is permitted through inhalation, topical and intra-articular route of administration. Methylprednisolone (MP) is available for use by different routes for anti-inflammatory and immunosuppressive purposes. To discriminate its intake by permitted & forbidden routes, a reporting level of 30 ng/ml is set by World Anti-Doping Agency. The aim of this study was to compare MP's excretion profile following oral & intra-articular administration & to evaluate its effect on endogenous GCs profile. MATERIALS & METHODS: The MP was administered through oral and intra-articular route to different patients & urine samples were collected up to 100 h. The urine samples were hydrolyzed, extracted, and analyzed on Liquid chromatography-mass spectrometry/MS. RESULTS: MP levels in urine exceeded the reporting limit of 30 ng/ml after oral (8 mg) and intra-articular administration (80 mg) routes. After oral intake (8 mg), MP levels exceeded the reporting level up to 24 h. However, after intra-articular injection (80 mg), the MP could be detected above the reporting level up to 80 h. CONCLUSION: The findings reveal that the MP can exceed the reporting level in urine even after administration by permitted route (i.a.). Further analysis of four endogenous GCs (Cortisol, Cortisone, TH Cortisone, and 11-deoxycortisol) showed a decreased excretion following administration of MP by oral & intra-articular routes.

Simultaneous identification of prednisolone and its ten metabolites in human urine by high performance liquid chromatography-tandem mass spectrometry.

The use of prednisolone and prednisone is prohibited by the World Anti-Doping Agency (WADA) due to their performance-enhancing effect. The purpose of the present work was to explore the possibility of identification and detection of various metabolites of prednisolone by liquid chromatography-tandem mass spectrometry (LC-MS/MS) in excretion study samples. Ten metabolites of prednisolone could be identified namely prednisone (11-oxo metabolite) [M-1], 6-ß-OH-prednisolone [M-2], 20-ß-OH-prednisolone [M-3], 20-α-OH-prednisolone [M-4], 20-α-OH-prednisone [M-5], 20-ß-OH-prednisone [M-6], 2 tetrahydro epimers of 20-ß-OH-prednisolone [M-7], 2 tetrahydro epimers of 20-α-OH-prednisolone [M-8], 2 tetrahydro epimers of 20-ß-OH-prednisone [M-9], and 2 tetrahydro epimers of 20-α-OH-prednisone [M-10]. Prednisolone was administered in 10-, 20-, and 40-mg dosage to healthy volunteers to study detection of various metabolites. The parent, M-1, M-2, and M-3 could be detected up to 72 h while rest of the metabolites were detectable up to 24 h after drug administration. The detection of newer metabolites of the drug can further be used for confirmatory purposes.