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.

Gattefosse sustained-release from lipid matrix

Advantages of Gattefossé’s modified-release agents:

• Drug release is a function of diffusion, which enables simple product design and offers both straightforward modulation of drug release and high reproducibility.
• Tablets are biopharmaceutically robust as the lipid matrix is not sensitive to physiological variations (e.g., pH, digestive processes, alcohol level).
• Agents are suitable for a wide range of processing techniques, including direct compression, granulation, melt coating, hot melt extrusion, and capsule molding.

Range of modified release agents

Compritol® 888 ATO 

  • 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)
Gattefossé technical guidelines for sustained release tabletsWe 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.

Precirol® ATO 5 

  • 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)