Some of the main challenges that the pharmaceutical industry
has to face is to overcome the physicochemical problems that many drugs present
due to polymorphism, low solubility, and low bioavailability. Recently, it has
been shown that the combination of solid, poorly water-soluble Active
Pharmaceutical Ingredients (APIs) with suitable counter-ions to give liquid
forms (API-ILs) can resolve these limitations. The purpose of this study was to
explore the transformation of Indomethacin and Mebendazole, two solid, poorly
water-soluble APIs into new API-ILs. Their structures were selected by their
pharmaceutical interest, their susceptibility of being transformed into API-ILs
(either to form the cation or the anion), and their limited bioavailability,
mainly due to its low solubility. The counterions were carefully chosen aiming
for high biocompatibility, low toxicity and high water solubility such as those
derived from DMEA, TMG, DBU, TED, p-toluensulfonic acid, glycolic acid,
methanesulfonic acid and saccharine. The synthesis was carried out by direct
treatment of the API with the corresponding selected acid or base. Solubility
tests showed a high increase of water solubility for all the salts synthesised,
especially for the API-ILs derived from indomethacin which showed a water
solubility in the range of 185 and 218 mg/mL, around 75000-hold higher than
free drug indomethacin.
Author(s) Details:
Emilia Tojo,
Faculty of Chemistry, University of Vigo, Marcosende, As Lagoas,
36210-Vigo, Spain.
Verónica
Fernandez-Stefanuto,
Faculty
of Chemistry, University of Vigo, Marcosende, As Lagoas, 36210-Vigo, Spain.
Please see the link here: https://stm.bookpi.org/CICMS-V6/article/view/13529
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