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Technology: Diffucaps®
- Technology Overview
- Technology Description
- Case Studies
Our Diffucaps technology facilitates the development and commercialization of novel, controlled-release delivery systems for once- or twice-daily dosing of single drugs or drug combinations that exhibit extreme pH-dependent solubility profiles and/or are poorly soluble in physiological fluids.
This multiparticulate system can provide dosage strength flexibility, and required PK profile and optimal release profiles for single drugs and drug combinations. The Diffucaps® drug release system can also be used in combination with our other proprietary technologies to enhance drug solubility in the GI tract.
Advantages of Diffucaps
- Ideal for drugs exhibiting poor solubility in lower intestinal pH, in environments with pH above 8.0, or in physiological fluids
- Can combine multiple drugs and/or multiple release profiles in the same dosage form
- Simple formulation of dose-proportional strengths.
- Can minimize food effect
Learn more about the Diffucaps technology.
Diffucaps is a multiparticulate bead system comprised of multiple layers of drug, excipients, and release-controlling polymers. The beads contain a layer of organic acid or alkaline buffer to control the solubility of a drug by creating an optimal pH microenvironment for drugs that exhibit poor solubility in intestinal pH, in environments with pH greater than 8.0, or in physiological fluids.. Alternatively, the beads can contain a solid-solution of drug and crystallization inhibitor to enhance bioavailability by maintaining the drug in its amorphous state.
Diffucaps technology is especially suitable for drugs that traditionally require multiple daily doses or drugs needing customized release formulations. Each Diffucaps bead has an inert core surrounded by drug and coated with a functional polymer membrane to control the rate of drug release.
Diffucaps can also be combined with our other proprietary technologies to optimize drug delivery. Diffucaps beads are 
The flexibility of the Diffucaps system allows for easy adjustment of the release profile and dosing strength to achieve targeted in vivo results. For drug development partners involved in clinical testing, this flexibility simplifies dose-ranging studies because the beads can be encapsulated separately to create separate study arms.
The Diffucaps technology is used in several currently marketed products and in novel products in clinical development.
Learn more about the Diffucaps case studies.
AMRIX® | InnoPran XL®
AMRIX® (Cyclobenzaprine Hydrochloride
Extended-Release Capsules)
Drug |
Cyclobenzaprine is the most frequently prescribed drug for muscle relaxation in the United States. AMRIX is indicated for short-term relief of muscle spasm as an adjunct to rest and physical therapy. |
Unmet Need |
Modified-release formulation of cyclobenzaprine with reduced side effects. |
Challenge(s) |
Develop a more convenient (once-daily administration) dosage form of a leading muscle relaxant drug. (Until the approval of AMRIX in 2007, cyclobenzaprine had to be administered two to three times daily.) |
Solution |
Diffucaps® multiparticulate bead system enabled the development of a formulation with an initial release of drug for quick onset-of-action, and also for sustained release to maintain consistence plasma levels throughout the day. Proprietary polymers layered onto Diffucaps beads containing the drug reduced fluctuations in drug plasma levels associated with immediate-release dosing. |
Result |
Safety and efficacy of AMRIX were demonstrated in two phase III trials, and daytime drowsiness associated with the modified-release product was less than that with immediate release cyclobenzaprine taken three times daily. |
Product Achieved |
AMRIX - marketed by Cephalon in the U.S. Bonelax - marketed by Daewoong Pharmaceuticals, Inc. in South Korea Product has also been licensed for commercialization in South Africa, Israel, and Turkey. |
AMRIX is available in two dose-proportional strengths – 15 and 30 mg capsules. This illustrates an advantage of the Diffucaps technology - multiple product strengths can be readily developed by using differing amount of drug-layered beads contained in the final capsule dosage form.
Learn more about the Diffucaps case study InnoPran XL.
AMRIX® is a registered trademark of Cephalon, Inc., or its affiliates
InnoPran XL®
Drug |
Propranolol, a beta-blocker for the treatment of hypertension |
Goals |
Develop a delayed-release formulation of propranolol |
Challenge(s) |
Develop a unique drug release profile for a chronically administered drug to provide PM dosing with AM plasma peak levels and maintenance of adequate drug plasma levels during the day |
Solution |
Diffucaps technology was used to develop a timed and sustained release dosage form of the drug. The product was developed using a combination of controlled and delayed release membrane system and the use of multiple release profile beads in a capsule system.
Plasma levels of Propranolol for the INNOPRAN XL product. |
Result |
Diffucaps technology created a delayed release capsule that achieve peak plasma levels in the AM when patient risk is highest, and continued maintenance throughout the day |
Product Achieved |
INNOPRAN XL - marketed in the U.S. by GlaxoSmithKline |
INNOPRAN XL is a registered trademark of GlaxoSmithKline
- Saini SD, Schoenfeld P, Kaulback K, et al. Effect of medication dosing frequency on adherence in chronic diseases. Am J Manag Care. 2009;15:e22-33.
- Roose SP. Tolerability and patient adherence. J Clin Psychiatry. 1999;60 Suppl 17:14-17.
Featured Paper
“Development of Orally Disintegrating Tablets Comprising Controlled-Release Multiparticulate Beads”
Diffucaps
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