Abstract :
Limited water solubility of drugs is a prevailing problem to efficient drug delivery as a huge proportion of available
drugs are poorly water soluble. Poorly soluble drugs suffer with low or incomplete oral absorptions leading to low
or variable bioavalibilities. Osimertinib mesylate is a novel anticancer drug for the treatment of lung cancer. It is
reported to have low absorption and exposure at therapeutic doses of 80 mg which could be due to low solubility in
gastrointestinal tract. It is important to evaluate pH solubility profile of the drug over the gastrointestinal pH range
in order to find the most suitable region of solubility and absorption. In this study, we are reporting saturated
solubility of Osimertinib mesylate in different media with specific pH conditions including different physiological
buffers such as simulated gastric fluid, simulated intestinal fluid, phosphate buffer saline. Solubility study was done
by classical shake flask method and samples were analyzed by double beam UV spectrophotometer in triplicate. It
was found to be very slightly soluble in water with an approximate value of 924 ± 6.06 µg/ml. Of all the tested buffer
media, simulated gastric fluid pH 1.2, exhibited maximum solubility, which was approximately 2.3 folds of the
solubility exhibited in distilled water. Solubility data over different pH conditions were statistically evaluated using
one way ANOVA and post hoc Tukey test for valid conclusions. All media had significant effect on the solubility of
the drug except sodium phosphate buffer, pH 3.2 and Acetate buffer pH 5.5 with respect to distilled water.
Keywords: Osimertinib mesylate, absorption, Solubility, physiological buffers.
Keyword :
Osimertinib mesylate, absorption, Solubility, physiological buffers.