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Understanding pharmaceutical polymorphic transformations II: crystallization variables and influence on dosage forms.
Jatin Sood1, Bharti Sapra1, Sameer Bhandari1
1Department of Pharmaceutical Sciences & Drug Research, Punjabi University, Patiala, Punjab, India.
Therapeutic Delivery
|July 8, 2015
Summary
Excipients significantly impact drug formulation by influencing crystal structure and growth. This affects drug properties like color, stability, and bioavailability, crucial for effective drug delivery.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Physical Chemistry
Background:
- Excipients and formulation variables are critical for enhancing drug stability, modifying release profiles, and improving physicochemical properties of dosage forms.
- In pharmaceuticals, excipients are expected to interact at a macromolecular level, potentially altering the crystal structure of solid active pharmaceutical ingredients.
- Polymers and colloidal particles can influence the rate and direction of crystal growth, impacting solid-state properties.
Purpose of the Study:
- To investigate the influence of excipients on the crystal habit and physicochemical properties of pharmaceutical solids.
- To explore how formulation variables affect drug crystal growth and solid-state characteristics.
- To understand the relationship between crystal habit, surface properties, and pharmacokinetic parameters.
Main Methods:
- Analysis of crystal growth modification by polymers and colloidal particles.
- Investigation of color variations in different polymorphic crystals upon exposure to colorants.
- Correlation of crystal habit and lattice energy with bioavailability and release rates.
Main Results:
- Excipients can modify the rate and direction of crystal growth.
- Different polymorphic crystals show distinct color responses to colorants due to surface pH variations.
- Smaller crystal size and lower lattice energy are associated with enhanced bioavailability and faster drug release.
Conclusions:
- Excipients play a crucial role in modulating the solid-state properties of pharmaceuticals through their influence on crystal habit.
- Understanding these interactions is vital for optimizing drug formulation for desired stability, release, and pharmacokinetic profiles.
- Crystal habit directly impacts pharmacokinetic parameters, highlighting the importance of controlling crystal morphology in drug development.
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