Abstract

FORMULATION OF PARACETAMOL INFUSION

*Arshi, Dr. Amresh Gupta, Dr. Satyawan Singh and Mr. Y. A. Vohra

ABSTRACT

Paracetamol (also known as Acetaminophen) is an antipyretic, non-opioids analgesic, and non-steroidal anti-inflammatory drug (NSAID), and is one of the most commonly used medications worldwide. Paracetamol was first used clinically in 1893, then avoided for more than 60 years due concerns about Paracetamol induced methaemoglobinaemia. Paracetamol is termed a simple analgesic and an antipyretic. Despite enduring assertions that it acts by inhibition of cyclooxygenase (COX)-mediated production of prostaglandins, unlike non-steroidal anti-inflammatory drugs (NSAIDs), paracetamol has been demonstrated not to reduce tissue inflammation. The enzyme responsible for the metabolism of arachidonic acid to the prostanoids (including prostaglandins and thromboxanes), commonly referred to as cyclooxygenase, is also more appropriately called prostaglandin H2 synthetase (PGHS), and possesses two active sites: the COX and the peroxidase (POX) sites. Ruggedness of the current method was determined by analyzing six assay sample solutions of Paracetamol formulation having concentration of 100μg/ml by two analysts in the same laboratory to check the reproducibility of the test result. The % recovery and standard deviation were calculated in both cases. Objective of the present study is to evaluate the oxidative potential of available intravenous formulations in Indian market through selective stress degradation, and to understand their potential for instability, if any, through presence/absence of anti-oxidant Excipient. As paracetamol is known to be unstable in the presence of oxygen, measurements and controls with respect to the minimize of oxygen in the solution with the use of inert gas (Nitrogen) by purging Nitrogen gas throughout out the manufacturing and filling process. The aqueous formulation of Paracetamol (Paracetamol Infusion) is found to be stable as per stability has been performed at 40°C ± 2°C and 75% RH for 6 months. The analytical method validation is performed to measure Paracetamol in aqueous formulation conveniently. The formulation obtained is found well within the Indian Pharmacopoeia (IP) acceptable limit.

Keywords: Paracetamol, NSAID, formulation, Infusion.