Polymers to improve processability, stability and patient satisfaction

Ashland is a global consumer market-focused additives and speciality ingredients company that responsibly solves for a better world. Ashland Life Sciences advances drug delivery with an unparalleled range of excipients. Its longstanding polymer expertise and technical support enable sophisticated science-based solutions for today’s drug formulation challenges.

The global centres of excellence of Ashland are home to advanced equipment and passionate research scientists and formulators, who are ready to work from concept to commercialisation. As a company that is always solving™, Ashland is driven by its vision to make a better world by providing creative solutions through the application of speciality ingredients and materials.

Solutions for formulators, manufacturers and patients

Available locally from SK Chemtrade, Ashland’s solutions contribute to increased patient acceptability and satisfaction. They add to the ease with which a product can be manufactured, support the overall safety and effectiveness of a drug during storage or use, and enhance stability and bioavailability.

Scientists from Ashland support the pharmaceutical industry with formulation and process development in various application areas, including:

• standard granulation, such as fluid bed, high shear and hot-melt extrusion

• tabletting, ranging from direct compression, bi-layer, multi-layer and tablet in tablet to compaction simulation and 3D printing

• solid dispersion such as hot-melt extrusion and spray drying

• controlled-release, incorporating release-profile prediction and simulation, melt extrusion, particle and pellet coating, drug layering and matrix tablets

• film coating with fluid bed coating, pan coating and colour matching.

Ashland has considerable expertise in the characterisation of powder properties, including flow, particle size, surface area, morphology and more. The company offers real-time solutions based on superior binder, film coating, solubiliser, disintegrant, rheology control, stabiliser and modified-release technologies.

Products are available in various grades for oral solid, liquid and injectable dosage forms.

Multifunctional water-soluble cellulose polymers

Klucel hydroxypropylcellulose (HPC) is a non-ionic water-soluble cellulose ether with a remarkable combination of properties. It has long been the tablet binder of choice for oral solid dosage forms in pharmaceutical applications. Klucel HPC combines organic solvent solubility, thermo-plasticity and surface activity with the aqueous thickening and stabilising properties characteristic of other water-soluble cellulose polymers available from Ashland.

Benecel hypromellose products are water-soluble, non-ionic polymers. Hypromellose is the most widely used polymer in hydrophilic matrix systems with widespread use in controlled-release dosage forms. The Benecel family of pharmaceutical products provides a full portfolio to support the controlled release of a broad range of APIs and manufacturing processes. Ashland’s newest grades, Benecel XR and XRF, are HPMC products with an optimised polymer structure and particle morphology that enable the formulation of safe, effective, and robust oral solid controlled-release dose forms.

Rheology, film coating and binding systems

Natrosol 250 hydroxyethylcellulose (HEC) is a non-ionic, water-soluble cellulose ether. It is used in solutions and gels to control rheology. In emulsions it is used for its high salt tolerance and surfactant compatibility, and in modified-release matrix tablets, where high-viscosity grades provide effective diffusion-limiting release of active pharmaceutical ingredients (API) with low water solubility.

Aquarius film coating systems have a range of functions to suit almost any core. Each of Ashland’s products is fully formulated, easily dispersed and provides a range of functions to suit almost any tablet core. Aquarius film coating systems offer an optimum balance of film strength and adhesion, even for challenging cores and release profiles. Many of Ashland’s film coating systems are sprayable at high solid concentrations, so faster coating times and reduced energy usage can be realised.

Plasdone povidones are a family of water-soluble polymers based on N-vinylpyrrolidone that combine a unique set of properties for application in a wide variety of dosage forms. Plasdone povidones are commonly used as binders for the development of tablet formulations, whether manufactured by wet granulation, dry granulation or direct compression.

Each of Ashland’s products is fully formulated, easily dispersed and provides a range of functions to suit almost any tablet core

Agents for dissolution and controlled release

Polyplasdone crospovidone superdisintegrants are synthetic, insoluble, but rapidly swellable, crosslinked homopolymers of N-vinyl-2-pyrrolidone. Crospovidone provides rapid disintegration and dissolution to oral solid dosage forms.

Viatel bioresorbable polymers is a leading technology for parenteral controlled-release drug delivery. Ashland offers five families of bioresorbable polymers and is willing to provide custom produced polymers with defined chemical structures, molar masses (molecular weight or inherent viscosity), and selective terminal end-groups.

Cyclodextrins for taste-masking and enhanced solubility

The molecular structure of cyclodextrins creates a bucket-like cavity that can function to complex with molecules or functional groups on molecules. The substitution of hydroxyl groups on native cyclodextrins to make hydroxypropyl-ß- or hydroxypropyl-γ-cyclodextrins (HPBCD or HBGCD) significantly enhances their solubility and makes them more suitable for drug solubilisation. This mechanism makes the Cavitron and Cavasol HPBCDs and HPGCDs capable of masking unpleasant taste/odour and stabilising drugs that are prone to degradation and can increase solubility of poorly soluble compounds in oral drug delivery systems. Purification of the Cavitron cyclodextrins to remove endotoxins enables their use in the solubilisation of drugs for parenteral drug products.

Cavamax cyclodextrins are biocompatible and compatible with a wide range of ingredients commonly used in pharmaceutical applications.

The regulatory compliance information for all Ashland products varies by product family and grade. For specific data about a respective grade, please refer to the Excipient Information Package and the Certificate of Analysis. •

Cavamax and Cavasol are registered trademarks of Wacker Chemie. Ashland acts as a worldwide distributor for Wacker.