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Euro Pharma Chemistry & Future Pharma 2019
Volume 08
Research & Reviews: Journal ofPharmaceutical Analysis | ISSN : 2320-0812
June 27-28, 2019 | Amsterdam, Netherlands
12th World congress on
Joint Event
4
th
Pharmaceutical Chemistry Conference Future Pharma
Improving biopharmaceutical properties of diacerein using crystal engineering approach
Rajeshri D Patel, Riddhi H Shukla, Prakruti R Buch, Tejas P Sharma
and
Mihir K Raval
Saurashtra University, India
M
anipulating the biopharmaceutical properties of poorly water-soluble drug molecule seems to be
the need of the hour in pharmaceutical industry nowadays. The phenomenon of multi-component
crystalline adducts such as salts, co-crystal, eutectics, solid solutions etc., has attracted interest from majority
of crystal engineering and pharmaceutical researchers in the past decade to improve the said properties of
drug molecule. In context to this, the present research work was aimed to prepare co-crystal of diacerein
(DIA) with improved biopharmaceutical properties. Temperature-composition phase diagrams of DIA and
conformers were constructed using DSC thermograms obtained for mixtures prepared by liquid assisted
grinding. Apart from characteristic V shaped binary phase diagram, no noticeable changes in the FT-IR and
PXRD spectra further confirmed eutectic formation of DIAwith fumaric acid-FMA (1:2) and 2, 4-dihydroxy
benzoic acid-DHA (1:3). As adhesive forces established by complimentary functional groups on DIA and
conformers were unable to overcome the stress due to size shape mismatch of component molecules, explains
the formation of eutectics. Kinetic solubility in 0.1 N HCl (pH 1.2), acetate buffer (pH 4.5), and phosphate
buffer (pH 6.8) was conducted, it revealed that eutectics showed higher solubility than their physical mixtures
vis-a-vis parent drug in all three medias.
In-vitro
dissolution and bioavailability profiles of prepared eutectics
were improved as compared with pure DIA. Additionally, the study demonstrated that flow properties and
tabletability of eutectics were enhanced as compared to DIA alone. Thus, produced eutectics of DIA-FMA
and DIA-DHA systems having fast dissolving capabilities, improved tabletability and enhanced in-vivo
performance make them more favourable candidates for better dosage form development.
Pharmaceutical Analysis 2019, Volume 08