Salt formation improves solubility and bioavailability for ionizable APIs, but disproportionation poses a significant stability risk. This white paper discusses key factors influencing disproportionation—such as pKₐ, pHₘₐₓ, and moisture—and presents practical strategies for risk mitigation through rational salt selection, excipient control, and formulation design. Case studies illustrate how these principles are applied in development.

In 2024, the U.S. Food and Drug Administration (FDA) approved a total of 50 new drugs, including 34 new molecular entities (NMEs). Among these, 28 are small molecule drugs. In this paper, An analysis of their administration routes and dosage forms will be discussed.

How Crystal Pharmatech, a leading CRDMO, leverages GastroPlus® to guide small molecule development and manufacturing decisions.

How can physiologically-based pharmacokinetic (PBPK) modeling maximize ADME performance and identify a path forward for GLP Tox and FIH formulations?

Amorphous solid dispersions combine the increased solubility of an amorphous material and the improved physical stability of more stable solid forms. Amorphous solid disperions can be used in early animal studies and in marketed products.

On March 14, 2024, Madrigal Pharmaceuticals announced FDA approval of Resmetirom (Redzdira). This pivotal milestone underscores the critical importance of innovative therapies in addressing longstanding medical challenges.

In 2023, the FDA's Center for Drug Evaluation and Research (CDER) approved a total of 55 new drugs, which included 38 new molecular entities, of which 30 were small molecule drugs. In this paper, the situation of polymorph patent application of 30 small molecule new drugs will be discussed.

Compare different analytical techniques (ssNMR, XPRD, DSC) for detection and characterization of crystalline phase impurities in spray-dried dispersions (SDD) using the model compound Triamcinolone.

Batch-to-batch variability during the crystallization of active pharmaceutical ingredients (API) can have a profound impact on both safety and efficacy of the final drug formulation, and direct business and cost implications for both the API manufacturer and downstream drug-formulation partners.

A pharmaceutical co-crystal is a crystalline form that can be used to change pharmaceutical properties, such as solubility, dissolution, stability, hygroscopicity, or bioavailability. Co-crystals can be used in early development for animal pharmacokinetic studies, in human clinical trials, and in marketed products.

API phase and formulation should be able to reach desired exposures and have adequate chemical and physical stability for GLP toxicology and first in human (FIH) studies. Any changes to form or formulation will incur significant time and resource penalties.

Integrating the efforts of drug-discovery scientists, material scientists and formulation specialists earlier in the discovery process can reduce drug-development timelines, risk and overall costs and provide other competitive advantages.

A pharmaceutical salt is a crystalline form that is commonly used to change pharmaceutical properties, such as solubility, dissolution, stability, or bioavailability. Salts can be used in early development for animal pharmacokinetic studies, in human clinical trials, and in marketed products.

Solid form is a general term that refers to both crystalline and amorphous materials. The solid form will impact active pharmaceutical ingredient (API) development properties such as solubility, dissolution rate, stability, hygroscopicity, and bioavailability.