[Formulation and stability of suspensions for preclinical study]

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Preclinical Drug Development

Background:

• Poorly soluble drugs in preclinical studies are often administered as oral suspensions.
• Predicting the stability of these drug suspensions is crucial for reliable experimental outcomes.

Purpose of the Study:

• To investigate the factors influencing the physical stability of aqueous drug suspensions.
• To provide data for predictive estimations of suspension stability in preclinical research.

Main Methods:

• Prepared aqueous suspensions of griseofulvin, ibuprofen, and indomethacin using four suspending agents: sodium carboxymethylcellulose (CMC), microcrystalline cellulose/carboxymethylcellulose (MC/CMC), hydroxypropylmethylcellulose (HPMC), and jota carrageenan (CJ).
• Evaluated physical and physicochemical drug characteristics, rheological properties of suspending media and suspensions, and physical and chemical stability.
• Assessed the impact of suspending agent type versus drug characteristics on suspension stability.

Main Results:

• The suspending agent type significantly influenced suspension physical stability.
• Formulations utilizing suspending agents with low-temperature gelation (jota carrageenan) or thixotropic flux (MC/CMC) exhibited the highest stability.
• Drug characteristics had a lesser impact on physical stability compared to the suspending agent.

Conclusions:

• Suspending agent selection is a critical factor for achieving stable drug formulations in preclinical oral suspensions.
• Agents like jota carrageenan and MC/CMC offer superior stability profiles, aiding in reliable preclinical drug administration.
• Understanding rheological properties of suspending agents can guide the development of more stable drug delivery systems.