Merck

Poorly soluble marketed drugs display solvation limited solubility.

Journal of medicinal chemistry (2007-10-13)
Christel A S Bergström, Carola M Wassvik, Kajsa Johansson, Ina Hubatsch
ABSTRACT

We determined the intrinsic aqueous solubility of 15 poorly soluble drugs with solubilities ranging from 2.9 nM to 1.1 microM. We then analyzed the data from a physicochemical perspective, using experimentally determined solid-state properties and easily interpretable two-dimensional molecular descriptors, to better understand the factors underlying poor solubility. The analysis shows that poorly soluble drugs that have reached the market are solubility limited by solvation rather than by their solid state.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Tamoxifen, ≥99%
Sigma-Aldrich
Terfenadine
Sigma-Aldrich
Glyburide, meets USP testing specifications
Sigma-Aldrich
Tolfenamic acid, NSAID
Sigma-Aldrich
Indomethacin, meets USP testing specifications
Sigma-Aldrich
Indomethacin, 98.5-100.5% (in accordance with EP)
Supelco
Albendazole, analytical standard, ≥98%