Modified/Controlled Release of Solid Oral Drugs
Flamel’s Micropump® platform permits either extended, or both delayed and extended, delivery of small molecule drugs via the oral route.
Micropump consists of a multiple-particulate system containing 5,000 to 10,000 microparticles per capsule or tablet. The 200-500 microns diameter-sized microparticles are released in the stomach and pass into the small intestine, where each microparticle, operating as a miniature delivery system, releases the drug at an adjustable rate and over an extended period of time.
Various dosage forms:
The microparticles’ design can be adapted to each drug’s specific characteristics by modifying the coating composition and thickness as well as the composition of the excipients encapsulated with the drug.
Micropump® allows the achievement of extremely precise pharmacokinetic profiles [extended (and/or delayed) release] of single or combination of drugs, in a variety of formats (such as tablets, capsules, sachet, or liquids (LiquiTime®), while preserving the targeted release rate over the shelf-life of the product.
Micropump’s Key Attributes
- extended release in the Gastro-Intestinal (“GI”) tract allowing mean plasma residence times to be extended for up to 24 hours,
- Potentially improved efficacy (by extending therapeutic coverage),
- Potentially reduced toxicity and/or side effects (by reducing Cmax or peak drug concentration in the plasma, or by reducing intra- and inter-patient variability),
- Improved patient compliance (by reducing frequency of administration),
- Applicable to poorly soluble (< 0.01mg/L) as well as highly soluble (> 500g/L) and to low dose (e.g. 4 mg) or high dose (e.g. 1,000 mg) drugs,
- Excellent mouth feel,
- Taste masking properties.
Considering R&D costs for reformulating a drug are typically substantially lower than for developing NCEs, “reformulation approvals” provide an opportunity to extend the exclusivity period of already marketed drugs or create new market exclusivity for off-patent drug.
The Micropump® platform has successfully transitioned to commercial stage with Coreg CR®.
Flamel currently has one additional Micropump®-based internal product in development (Micropump®-Sodium oxybate for narcolepsy, which has been successfully tested in two Phase 1 clinical studies).