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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
A structure dosage form approach for solubility and dissolution rate enhancement
Xianghao Zuo1, Uday Jain2, Feihuang Deng1
1Triastek, Inc., Nanjing, Jiangsu, China.
Melt extrusion deposition (MED®) 3D printing enhances poorly water-soluble drug bioavailability by creating amorphous solid dispersions. This technology enables precise control over drug release profiles, offering tailored patient-centric medications.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Drug Delivery
Background:
- Improving bioavailability of poorly water-soluble drugs is a persistent pharmaceutical challenge.
- Melt extrusion deposition (MED®) 3D printing offers advanced capabilities for creating complex pharmaceutical dosage forms.
- Patient-centric drug delivery requires tailored formulations for diverse clinical needs.
Purpose of the Study:
- To utilize MED® 3D printing for enhancing the solubility and modulating the release of a poorly water-soluble compound.
- To demonstrate the fabrication of structurally engineered tablets with tailored release profiles.
- To explore a structure-driven approach for efficient tablet development.
Main Methods:
- Formulation of a poorly water-soluble model compound into an amorphous solid dispersion (ASD).
- Fabrication of 3D-printed tablets using MED® technology with distinct internal structures.
- Design of a mesh structure for immediate release (IR) and a multi-compartment structure for extended-plus-delayed release (ER + DR).
Main Results:
- ASD formulation increased model compound solubility by up to 4-fold (from ~15 μg/mL to ~60 μg/mL).
- MED® 3D printing successfully produced tablets with designed mesh and multi-compartment structures.
- Tailored release profiles (IR and ER + DR) were achieved through structural engineering.
Conclusions:
- MED® 3D printing is effective for enhancing solubility and precisely controlling the release of poorly water-soluble drugs.
- Structure-driven design via MED® 3D printing provides a novel pathway for pharmaceutical tablet development.
- This technology supports the creation of patient-centric medications with customized release characteristics.
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Theories of Dissolution: Diffusion Layer Model
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
