Preliminary investigation for preparing amorphous paracetamol Balamurugan Sumalatda Devi1, Venkatesan Aravindhanathan1, Radhakrishnan Arun1, Kuppusamy Gowthamarajan1*, Singh Sachin Kumar2 1Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty, Nilgiris, Tamil Nadu, India. 2School of Pharmaceutical Sciences, Lovely Professional University, Punjab, 144411, India. *Corresponding Author E-mail: gowthmsang@jssuni.edu.in
Online published on 30 April, 2021. Abstract Drugs with poor aqueous solubility are still an ongoing challenge in the successful formulation of therapeutic products due to their low oral bioavailability. It reports that over 70% of drugs and active entities are poorly water-soluble compounds. Paracetamol is a BCS class II drug which has low solubility and high permeability. Hence there is a solubility rate limiting step for paracetamol which is less solubility and ultimately has low bioavailability which instigates formulation challenges because of limited dissolution and/or low permeability. To overcome this solubility rate limiting step the polymorphism of paracetamol can be altered to various polymorphic forms but altering the polymorphic form does not work all the time. Hence it is converted into amorphous form where it has no polymorphic structure. By converting it to an amorphous form higher dissolution, bioavailability can be achieved and hence marketed doses can be reduced. However amorphous product are not stable over a period of time, this study was focused on preparation and stabilization of amorphous product. In this study the paracetamol was PEGylated with PEG 4000 of different concentrations 1: 0.5, 1: 1, 1: 2, 1: 4 by melt method. The interactions between paracetamol and polyethylene glycol 4000 in the solid state were probed by FTIR studies and it was proved that there was no incompatibility between paracetamol and PEG 4000. Solubility of the prepared paracetamol-PEG mixture using method C were determined in Millipore Water and it was found that as the ratio increases the solubility also increases. The increase in solubility of such BCS class II drug will overcome the industrial challenges of formulation and manufacturing expenses. Top Keywords BCS class II, Paracetamol, PEG 4000, Amorphous, Solubility enhancement. Top |