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Co-Crystallization Approach to Enhance the Stability of Moisture-Sensitive Drugs
Madhukiran R Dhondale1, Pradip Thakor2, Amritha G Nambiar1
1Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (BHU), Varanasi 221005, India.
Pharmaceutics
|January 21, 2023
Summary
Co-crystals enhance the stability of moisture-sensitive pharmaceutical ingredients (APIs) by reducing water absorption. This crystal engineering approach improves drug product efficacy and safety, offering a superior alternative to salt forms.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Chemical Engineering
Background:
- Drug stability is crucial for pharmaceutical formulation quality, impacting efficacy and safety.
- Moisture content is a primary driver of degradation in nearly 50% of medicinal products, leading to impurities.
- Active pharmaceutical ingredient (API) properties like polarity and surface chemistry influence water affinity and stability.
Purpose of the Study:
- To review recent advancements in improving the hygroscopic stability of moisture-sensitive APIs.
- To explore the mechanisms behind enhanced stability in pharmaceutical formulations.
- To discuss co-former screening strategies for moisture-sensitive drugs.
Main Methods:
- Review of recent scientific literature on co-crystals and hygroscopic stability.
- Analysis of factors influencing API-water interactions.
- Discussion of co-crystal formation and screening methodologies.
Main Results:
- Co-crystals demonstrate a significant reduction in hygroscopicity compared to pure APIs.
- Crystal engineering via co-crystals offers improved stability for moisture-sensitive compounds.
- The co-crystal approach circumvents solubility issues sometimes associated with salt forms.
Conclusions:
- Co-crystals are a promising strategy for enhancing the hygroscopic stability of pharmaceutical formulations.
- Understanding API-water interactions is key to designing stable drug products.
- Co-former screening is essential for developing effective co-crystals for moisture-sensitive drugs.
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