Diffucaps® Customized Release Technology
This technology has the flexibility to incorporate functional, release-controlling polymers or protective coatings onto drug-layered cores, granules, or crystals. This multiparticulate system provides sophisticated control of drug delivery and optimizes release profiles for single drugs and drug combinations.
Examples of customized release particles
How Diffucaps® Customized Release Technology works
A drug core (granulated or layered onto a neutral surface) is created, followed by the application of one or more rate-controlling, functional polymer membranes. The drug-layering process can be conducted from either aqueous or organic solvent–based drug solutions/suspensions and results in a small (approximately 1.5 mm or less in diameter), spherical, multilayered bead.
Advantages of Diffucaps® Customized Release Technology
- Permits easy adjustment of both dosage strength and dissolution profile to achieve the desired in vivo pharmacokinetic profile
- Beads can have different release profiles, different active ingredients, or both—all in one product
- Can be used in combination with other proprietary technologies to enhance drug solubility in certain sections of the gastrointestinal tract
- Reduces gastric mucosal irritation
- Available as a capsule, orally disintegrating tablet, rapidly disintegrating tablet, or as a sprinkle
- Can minimize food effect
Diffucaps® (Organic Acid or Alkaline Buffer) Solubility-Modulation Technology
Many weakly basic drugs exhibit pH-dependent solubility profiles. Some weakly basic drugs are extremely soluble in physiological fluids (ie, solubility >500 mg/mL over the pH range of 1-8 and practically insoluble at a pH ≥8), making it difficult to achieve a prolonged release profile. Further, other weakly basic drugs are moderately soluble at a pH ≤4 but are poorly soluble or practically insoluble at a pH ≥6. Certain other weakly basic drugs are practically insoluble at all physiological pHs. Diffucaps® technology can be used to customize the release profiles of drugs demonstrating varying solubility profiles at physiological pHs.
How Diffucaps® Solubility-Modulation Technology works
An optimal pH microenvironment is created within the coated bead. For drugs that are practically insoluble at a pH ≥6, an acidic microenvironment is created by incorporating an organic acid layer in order to solubilize and release the drug for systemic absorption. For drugs with extreme solubility at physiological pHs, a basic microenvironment is created by incorporating an alkaline buffer layer to reduce solubility, thereby prolonging its release. Furthermore, the organic acid layer is placed underneath the drug layer while the alkaline buffer is placed over the drug layer and coated with one or more functional polymers in order to ensure that the organic acid or the alkaline buffer is not depleted until release of the drug is complete.