Related Experiment Video
Updated: May 16, 2026
05:08
Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
Melt extrusion with poorly soluble drugs
Sejal Shah1, Sindhuri Maddineni, Jiannan Lu
1Department of Pharmaceutics, Pii Center for Pharmaceutical Technology, School of Pharmacy, The University of Mississippi, University, MS 38677-1848, United States.
International Journal of Pharmaceutics
|November 27, 2012
Summary
Melt extrusion (ME) is a valuable technique for improving drug solubility and delivery. This review explores ME
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Melt extrusion (ME) is increasingly utilized in pharmaceutical development.
- Key applications include taste masking, stability enhancement, sustained release, and solubility enhancement.
- Amorphous solid dispersions generated via ME are crucial for improving solubility due to free energy benefits.
Purpose of the Study:
- To review the efficacy of melt extrusion (ME) for enhancing the solubility of poorly soluble drugs.
- To provide a comprehensive understanding of ME technology for formulation design.
- To assess the strengths and weaknesses of ME for poorly soluble drug formulations.
Main Methods:
- Review of melt extrusion processing aspects.
- Analysis of the amorphous state definition and understanding.
- Evaluation of manufacturability, analytical characterization, and biopharmaceutical performance testing.
- Exploration of combined techniques like co-crystals and spray drying.
Main Results:
- Melt extrusion effectively generates amorphous solid dispersions for solubility enhancement.
- Understanding processing parameters, amorphous state properties, and characterization methods are key.
- Fusion with other techniques can optimize formulations for specific physicochemical characteristics.
- Successful commercialized ME-based products demonstrate its practical utility.
Conclusions:
- Melt extrusion is a powerful tool for developing advanced drug delivery systems, particularly for poorly soluble compounds.
- A thorough understanding of ME technology and formulation strategies is essential for successful drug product development.
- The review highlights ME's potential and provides insights from commercialized products.
Related Concept Videos
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
01:16Bioavailability Enhancement: Drug Solubility Enhancement
Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are employed to...
01:17In Vitro Drug Dissolution: Alternative Methods
Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...