Excipients for modified release
Modified- or sustained-release matrices are designed to release a drug slowly over an extended period of time. Formulations must be robust to ensure drug release over time and avoid dose-dumping. Lipid-based matrices are water-insoluble and do not swell or erode when in contact with aqueous media. When used as sustained-release agents, they form an inert matrix from which the drug diffuses slowly.
Advantages of Gattefossé’s modified-release agents:
The development of lipid sustained-release matrices is straightforward and provides the following biopharmaceutical and manufacturing advantages:
- Effective modulation of drug release profile for highly water soluble, short half-life drugs
- Reduced risk of alcohol dose dumping and misuses
- Non-hygroscopic matrix for improved stability on storage
- Solvent-free processing for cleaner and greener manufacturing
- Suitable for cold and hot manufacturing processes: direct compression, granulation, 3D printing, hot melt extrusion
Range of modified release agents
- finely atomized lipid excipient powder of well-defined, reproducible composition and particle size
- used at proportion of 10%–40%, depending on drug solubility and diluent properties
- suitable for direct compression, granulation, and hot processes (i.e., hot melt coating, granulation, and extrusion)
- crystalline material with narrow melting range (∼70 °C) and rapid recrystallization, ideal for hot melt processes
- GRAS status and precedence of use with many APIs (FDA IID)
We can provide technical guidelines that offer useful tips on SR formulation development and numerous case studies with model drug molecules, e.g., bupropion HCl, levodopa, metformin HCl, metoprolol succinate, niacin, and theophylline.
- finely atomized lipid excipient powder of well-defined, reproducible composition and particle size
- crystalline material with narrow melting range (∼55 °C) and rapid recrystallization, suitable for use in hot processes (i.e., hot melt coating, extrusion, and capsule molding)
- GRAS status and precedence of use with many APIs (FDA IID)
Geleol™ Mono and Diglycerides NF
- available in pellet form
- crystalline material with narrow melting range (∼60 °C) and rapid recrystallization, suitable for use in hot processes (i.e., hot melt coating, extrusion, and capsule molding)
- GRAS status and precedence of use with many APIs (FDA IID)
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