Title:Enhancing Aqueous Solubility of Ketoprofen by Fusion Technique Using Suitable Co-formers
Volume: 9
Issue: 3
Author(s): Rudra Vaghela, Parthasarathi. K. Kulkarni, Umme Hani, Vegasna Naga Sravan Kumar Varma and Raizaday Abhay
Affiliation:
Keywords:
Co-crystals, Co-formers, Fusion technique, Ketoprofen, Solubility.
Abstract: The aim of the present work was to prepare, characterize and evaluate the solubility and dissolution behavior of
ketoprofen co-crystals. Fusion method was employed for the preparation of ketoprofen co-crystals. The co-formers
selected were cinnamic acid, glutaric acid, maleic acid, malonic acid, nicotinamide, oxalic acid, p-amino-benzoic acid, pamino
salicylic acid, saccharin and urea. The prepared ketoprofen co-crystals were characterized by FT-IR, DSC and
XRD. Ketoprofen co-crystals were evaluated for solubility and dissolution. Micromeritic properties were evaluated for cocrystal
exhibiting higher solubility. A Shift in the IR peaks was observed for all the prepared co-crystals with no presence
of additional peaks. DSC studies showed decrease in the heat of fusion from 257.74 to 50.39 J/g and melting point of drug
from 95.80 to 73.57°C in the co-crystals. XRD peaks exhibited different peak patterns than peaks shown by the pure
ketoprofen. All the preparations exhibited enhanced aqueous solubility as well as dissolution when compared with pure
ketoprofen. Amongst the co-crystals prepared, Ketoprofen-p-Amino-salicylic acid co-crystals, exhibited 14 fold increases
in aqueous solubility and in vitro release was found to be 93.41% in 60 mins. This work demonstrates the potential of cocrystallization
by fusion as screening method for particle engineering. The results demonstrate the feasibility of
pharmaceutical co-crystal design for ketoprofen.
