right methodology for a compound is both time-consuming and
requires a considerable amount of active pharmaceutical ingredient
(API) to be used for each test. This makes it an incredibly costly and
resource heavy option for drug developers. Furthermore, the risk of
missing the best excipient for a compound is high due to the limited
experiments and cost associated with performing manual handling.
To overcome the challenges, a HTS approach has been developed to offer a more
cost and time efficient alternative to existing
techniques. The aim was to develop a robust,
automatic platform that would use minimal
amounts of compound to provide conclusive
information about a drug’s solubility and stability in a variety of solvents and excipients.
To establish the methodology, a large number of experiments were performed to optimize the technique, using a broad screening
list of excipients, including water-soluble organic solvents, non-ionic surfactants, water-insoluble lipids, organic liquids/semi solids,
cyclodextrins, and phospholipids.
Using the approach, different excipients
are shown to be most appropriate for varying drug delivery systems. For example,
Selection of an appropriate excipient, or combination of ex-
Figure 1. Solubility of the six drug candidates in the testing excipients. 15mg/mL was set as the maximum amount.
Degradation of the drug is indicated in red.
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