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口服和关节内给药后甲泼尼龙尿液排泄模式的初步研究及其对内源性糖皮质激素谱的影响。

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

机构信息

National Dope Testing Laboratory, Ministry of Youth Affairs and Sports, J. N. Stadium, New Delhi, India.

Anti-Doping Lab Qatar (ADLQ), Doha, Qatar.

出版信息

Indian J Pharmacol. 2021 Nov-Dec;53(6):480-483. doi: 10.4103/ijp.ijp_946_20.

Abstract

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.

摘要

简介

口服、静脉、肌肉或直肠途径使用糖皮质激素(GCs)在体育运动中是被禁止的。其可通过吸入、局部和关节内途径使用。甲泼尼龙(MP)可通过不同途径用于抗炎和免疫抑制目的。为了区分其通过允许和禁止途径的摄入,世界反兴奋剂机构设定了 30 纳克/毫升的报告水平。本研究的目的是比较 MP 经口服和关节内给药后的排泄情况,并评估其对内源性 GCs 谱的影响。

材料与方法

将 MP 通过口服和关节内途径给予不同患者,并在 100 小时内收集尿液样本。将尿液样本水解、提取并在液相色谱-质谱/质谱上进行分析。

结果

口服(8 毫克)和关节内(80 毫克)给药后,尿液中的 MP 水平超过了 30 纳克/毫升的报告限值。口服摄入(8 毫克)后,MP 水平在 24 小时内超过报告水平。然而,关节内注射(80 毫克)后,MP 可在 80 小时以上的时间内检测到报告水平。

结论

这些发现表明,即使通过允许的途径(例如关节内途径)给药,MP 也可以在尿液中超过报告水平。对四种内源性 GCs(皮质醇、皮质酮、TH 皮质酮和 11-脱氧皮质醇)的进一步分析显示,口服和关节内给药后,其排泄减少。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cf8/8764973/1fbe89dbef25/IJPharm-53-480-g001.jpg

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