Development of paracetamol-caffeine co-crystals to improve compressional, formulation and in vivo performance

Paracetamol, a frequently used antipyretic and analgesic drug, has poor compression moldability owing to its low plasticity. In this study, new co-crystals of paracetamol (PCM) with caffeine (as a co-former) were prepared and delineated. Co-crystals exhibited improved compaction and mechanical behav...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 2018-07, Vol.44 (7), p.1-1108
Main Authors: Latif, Sumera, Abbas, Nasir, Hussain, Amjad, Arshad, Muhammad Sohail, Bukhari, Nadeem Irfan, Afzal, Hafsa, Riffat, Sualeha, Ahmad, Zeeshan
Format: Article
Language:English
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Summary:Paracetamol, a frequently used antipyretic and analgesic drug, has poor compression moldability owing to its low plasticity. In this study, new co-crystals of paracetamol (PCM) with caffeine (as a co-former) were prepared and delineated. Co-crystals exhibited improved compaction and mechanical behavior. A screening study was performed by utilizing a number of methods namely dry grinding, liquid assisted grinding (LAG), solvent evaporation (SE), and anti-solvent addition using various weight ratios of starting materials. LAG and SE were found successful in the screening study. Powders at 1:1 and 2:1 weight ratio of PCM/CAF by LAG and SE, respectively, resulted in the formation of co-crystals. Samples were characterized by PXRD, DSC, and ATR-FTIR techniques. Compressional properties of PCM and developed co-crystals were analyzed by in-die heckle model. Mean yield pressure (Py), an inverse measure of plasticity, obtained from the heckle plots decreased significantly (p 
ISSN:0363-9045
1520-5762
DOI:10.1080/03639045.2018.1435687