Development and Validation of an Ultra-Sensitive UPLC-MS/MS Method for the Determination of Naloxone in Human Plasma - April, 2014

Naloxone (NLX) is a µ-opioid receptor antagonist and commonly used for counteracting opiate overdose. The combination use of buprenorphine and low dose of NLX was approved by the FDA to prevent illicit intravenous use of this formulation. The low dose of NLX requires a corresponding low limit of quantitation of NLX for pharmacokinetic studies (i.e. 5 pg/mL). Naloxone-3-glucuronide (NLG) is a major metabolite of NLX. The instability of NLG can impact the accurate measurement of NLX at such a low quantitation limit. This poster abstract summarizes the development and validation of an ultra-sensitive LC-MS/MS assay to quantify NLX in human plasma without the impact from NLG. The assay is five times more sensitive than a recently published LC–MS/MS method for NLX.


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