Controlled API-polymer solidification (CAPS): a novel manufacturing process approach to produce amorphous solid...

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery

Background:

• Many new drug candidates (NCEs) exhibit poor aqueous solubility, often classified as BCS class II or IV, posing significant formulation challenges.
• Enhancing the bioavailability of poorly soluble drugs is a critical hurdle in pharmaceutical development.
• Current amorphous solid dispersion (ASD) manufacturing methods like hot-melt extrusion (HME) and spray drying face material property and processing challenges.

Purpose of the Study:

• To introduce and evaluate a novel Controlled API-Polymer Solidification (CAPS) technology for preparing ASDs.
• To assess the physical properties and manufacturing advantages of CAPS-prepared ASDs.
• To compare the performance of CAPS-prepared ASDs with conventional methods.

Main Methods:

• Development of the Controlled API-Polymer Solidification (CAPS) technology.
• Preparation of ASDs using the CAPS technology.
• Characterization of ASD physical properties (density, flowability, particle size).
• In-vitro dissolution and permeation studies.
• In-vivo pharmacokinetic (PK) evaluations.

Main Results:

• CAPS technology enables cost-effective preparation of ASDs with superior physical properties, including enhanced density, flowability, and particle size distribution.
• These improved properties facilitate streamlined drug product manufacturing, allowing direct tablet compression.
• CAPS-prepared ASDs demonstrated bioequivalence to spray-dried formulations in in-vitro and in-vivo studies.

Conclusions:

• CAPS technology offers a viable alternative for ASD manufacturing, overcoming limitations of conventional methods.
• The enhanced physical properties of CAPS-prepared ASDs simplify downstream processing and improve manufacturing efficiency.
• CAPS technology holds promise for developing bioavailable formulations of poorly soluble drugs.