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Manipulation of Pharmaceutical Polymorphic Transformation Process Using Excipients.
Beiqian Tian1, Zhiyong Ding1, Shuyi Zong1
1National Engineering Research Center of Industrial Crystallization Technology, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China.
Excipients are crucial for stabilizing active pharmaceutical ingredients (APIs) by preventing unwanted solid-state form changes. Their strategic use ensures drug product stability and effectiveness.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Solid-State Chemistry
Background:
- Ensuring a consistent solid-state form of active pharmaceutical ingredients (APIs) is critical for drug product quality.
- APIs risk polymorphic transformation during pharmaceutical processing, formulation, and storage.
Purpose of the Study:
- To review excipients that can manipulate pharmaceutical polymorphic transformations.
- To highlight the importance of excipients in controlling API solid-state forms.
Main Methods:
- Literature review of excipient categories and their effects.
- Summarization of excipient impacts on phase transformations and crystallization.
Main Results:
- Excipients significantly influence solvent-mediated phase transformations, solid-state transitions, and amorphous crystallization.
- Amino acids, surfactants, and polymers are common excipients with diverse manipulation effects.
Conclusions:
- Strategic use of excipients can control API polymorphic transformation.
- Excipients offer a promising approach to guarantee the stability and effectiveness of drug dosage forms.
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