Simultaneously Improving Mechanical, Formulation, and In Vivo Performance of Naproxen by Co-Crystallization

ABSTRACT Naproxen (NAP), an anti-inflammatory drug belonging to class II of Biopharmaceutic Classification System, has low aqueous solubility and dissolution rate which limit its oral bioavailability. The focus of this investigation was to assess the impact of co-crystallization in improving the phy...

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Bibliographic Details
Published in:AAPS PharmSciTech 2018-10, Vol.19 (7), p.3249-3257
Main Authors: Abbas, Nasir, Latif, Sumera, Afzal, Hafsa, Arshad, Muhammad Sohail, Hussain, Amjad, Sadeeqa, Saleha, Bukhari, Nadeem Irfan
Format: Article
Language:English
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Pharmacology/Toxicology
Pharmacy
Research Article
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Summary:ABSTRACT Naproxen (NAP), an anti-inflammatory drug belonging to class II of Biopharmaceutic Classification System, has low aqueous solubility and dissolution rate which limit its oral bioavailability. The focus of this investigation was to assess the impact of co-crystallization in improving the physico-mechanical and in vivo performance of NAP. NAP was co-crystallized using nicotinamide as a co-former employing liquid-assisted grinding method and characterized by intrinsic dissolution rate, DSC, and PXRD. Prepared co-crystal exhibited improved physicochemical and mechanical properties. Mechanical behavior of NAP and developed co-crystal was analyzed by drawing tabletability curves. Over the entire range of used compaction pressure, NAP showed poor tensile strength (
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-018-1152-7