Controlled Release

An appropriately designed controlled release drug delivery system can be a major advance towards solving problems concerning the targeting of a drug to a specific organ or tissue and controlling the rate of drug delivery to the target site.


The precise control of drug release from finished oral dosage forms is highly desirable in many important therapeutic areas. At Kuecept, we have spent many years researching animal and human gastro-intestinal physiology and use this information to develop tailored solutions for controlled and targeted drug release from single-unit and multi-particulate oral dosage formulations.

In addition to conventional approaches, Kuecept has developed additional controlled release technologies to allow for the development of new and improved performance formulations that are capable of addressing unmet medical needs across a broad range of important therapeutic areas.

These technologies can be used to achieve a wide range of in vivo release profiles and are manufactured using conventional methodologies / processing equipment and approved excipients. When used alone, or in combination, they can help to improve efficacy, enhance safety and increase patient compliance

Please click on the relevant tab below for more information.

Kuecept Ltd has developed one of the world’s first erosion-based multiparticulate amorphous drug delivery technologies which enables the controlled release of drugs in the GI tract  with high precision and reproducibility. In the matrix microsphere system, the drug is homogeneously distributed throughout a GRAS cellulosic polymer matrix (HPMC-AS) in a stabilised amorphous state to afford improved kinetic solubility, whilst providing precise dissolution control and drug release, something that is difficult  to achieve with other methods of amorphous dispersion manufacture (e.g. spray drying).

Once administered, these solid microspheres rapidly disperse in the stomach and are eroded by the gastro-intestinal fluids in a controlled manner as they pass through the GI tract; each matrix is designed to erode when in contact with biological fluid at a defined pH, but at the same time, does not allow fluid to diffuse into the matrix until the point of release, thus avoiding uncontrolled drug diffusion out of the microparticles and reducing the effects of luminal enzymatic / pH activity.

By altering the composition of the matrix, three systems have been created, namely modified, prolonged and targeted release.

Key benefits:

  • Ability to manufacture at small scale (batch sizes of < 100 mg) with high product yields (> 80 %), thereby reducing API requirements during early development stages
  • Microparticles exhibit exceptional flow propeties and powder density (~ 1g/cm3), ideal for manufacture of high dose suspensions e.g. to support preclinical tox programs
  • Does not require the use of high processing temperatures or fast solvent removal processes; dispersions are therefore physically stable and do not change during storage
  • Does not require the use of expensive processing equipment, meaning formulation feasibility assessment programs are quick and cost effective
  • Ability to administer actives in controlled release dosage forms to preclinical models (e.g. rodents etc)
  • Options for immediate, modified / delayed and sustained / extended release
  • Microparticles form stable suspensions which are ideal for short / medium term preclinical dosing studies or for manufacture of niche products (e.g. paediatric / geriatric dosage forms)

The matrix microsphere technology is offered to clients on a fee-for-service basis. Options are available under license for technology transfer or for development and patent protection of specific drugs or drug classes. Please contact us directly for more information.

Conventional enteric coatings designed to release drug in the proximal small intestine normally require up to 2 hours post-gastric emptying to disintegrate. This invariably causes a significant delay in drug absorption and can compromise the bioavailability of drugs which have a narrow absorption window in the upper GI tract.

In addition, drug delivery to the ileo-colonic regions using common enteric coated systems has often proved unsuccessful because of the failure of these polymers to disintegrate and release drug prior to dosage form elimination. This technology is a proprietary technology (“solid dosage forms comprising an enteric coating with accelerated drug release” WO/2008/135090) that is clinically proven to accelerate the dissolution rate of enteric coatings and can be applied to almost all conventional dosage forms for all of your GI targeting needs.

Key benefits of Double Coating:

  • Clinically proven technology protected by a strong patent portfolio
  • Cost effective - uses standard EU and FDA approved coating materials
  • Can be applied to a variety of conventional dosage forms, inc. tablets, capsules, granules, pellets and mini-tablets
  • Provides rapid drug release in the small intestine to afford faster onset of action compared to current commercial enteric coatings. Ideal for Proton-Pump Inhibitors (PPIs) or drugs to treat acute pain
  • Enhanced bioavailability of drugs with narrow absorption windows in the proximal small intestine
  • Enhanced bioavailability of poorly soluble basic compounds (allows local delivery in a pre-solubilised form to avoid drug precipitation post gastric emptying)
  • Improved targeting of drugs to the ileo-colonic region for local or systemic action

Double Coating can be accessed either as a fee-for-service program or through technology license. Please contact us directly for more information.

 

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