Salt Selection
The process of choosing an optimal acid or base counterion to form a salt of a drug candidate, aimed at improving physicochemical properties such as solubility, dissolution rate, crystallinity, stability, and hygroscopicity. Salt form can dramatically influence bioavailability and manufacturability. Hydrochloride, sodium, mesylate, and fumarate are among the most commonly used pharmaceutical salt forms.
ตัวอย่าง
- Sertraline hydrochloride: HCl salt chosen for crystallinity and stability over free base
- Diclofenac sodium vs. diclofenac potassium: sodium salt for sustained release, potassium for rapid onset
- Amlodipine besylate: besylate salt chosen for superior stability and non-hygroscopic properties
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The process of choosing an optimal acid or base counterion to form a salt of a drug candidate, aimed at improving physicochemical properties such as solubility, dissolution rate, crystallinity, stability, …