KINETICS STUDY COCRYSTALS KETOCONAZOLE-SUCCINIC ACID PREPARED WITH SLURRY METHOD BASED ON POWDER X-RAY DIFFRACTION (PXRD)
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Abstract
The compounds with low solubility drugs can
be a problem in the development of drugs for
the pharmaceutical industry. Group of drugs
that are included in the Biopharmaceutical
Classification System (BCS) class II drugs can
be a challenge for the preparations of pharmaceutical
development
because
of
low
solubility
drugs
as
well
as
the
rate
of
dissolution.
In
this
case
to
increase
the solubility of
drugs
besides
salts,
pharmaceutical
cocrystals
opened
a
new
dimension
to
search
for
solid
forms
such as
solubility,
dissolution rate, stability, and shelf
life of active pharmaceutical ingredients (APIs)
without affecting their inherent pharmacological
properties1.
Pharmaceutical
co crystals are materials or
crystalline materials consisting of at least two
different components (multicomponent crystals
or mixed crystals)2-3. Co crystal could be
prepared by several methods, such as solvent
evaporation, slurry, melt, and grinding. Co
crystals formed between ketoconazole (KTZ)
as an active pharmaceutical and succinic acid
(SA) as a co crystal former (co-former)4 was increased
dissolution
rate
of
pure
ketoconazole
in
equimolar ratio (1:1)1. Physical characterization
of
co
crystal
was
performed
by
physical
mixture
of
binary
system
with
molar
ratio
using
different
thermal
analyzer
(DTA)
data
from
KTZ
and SA. Besides that, physicochemical
characterizations of cocrystal were performed
by using PXRD and infrared spectroscopy (IR).
Active solid materials in the manufacture of
pharmaceutical preparation suffered in various
thermic or
machanical
proccessed
such
as grinding, milling, granulations (wet and dry granulations), tabletasi, and storage at
various temperature, so the materials can
occure transformation polymorph or hidrat/
solvat5. Kinetic study of cocrystal KTZ-SA prepared
with slurry
method
at
various
solvent
concentrations
a
follows
2%,
3%,
4%,
5%
and
6%
(w/w).
Therefore, the aim of the present
study was determined the kinetics of co crystals
KTZ-SA prepared with slurry method by
using Powder X-ray Diffraction (PXRD) data
such as the research of co crystalline phase
transformation of binary mixture of trimethoprim
(TMP)
and
sulfamethoxazol
(SMZ)
by
slurry
technique5
