Advances in Taste-masking

Taste-masking of solid dosage and liquid drugs is a challenge for pharmaceutical manufacturers. Most APIs are unpleasant or harsh tasting leading to patient noncompliance. This challenge affects all age groups, but is specifically problematic for pediatric patients. The global market for pediatric drugs and vaccines is forecast to reach $85 billion by year 2017, according to data from Global Industry Analysts. The US is the largest market for pediatric drugs followed by Western Europe. Implementing taste-masking programs into the drug-manufacturing process is crucial to avoid losses due to noncompliance. Pharmaceutical manufacturers are faced with challenges in life-cycle management, cost control, global regulations, and patent protection.

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In a recent editorial webcast, Pharmaceutical Technology examined formulation-development strategies in product life-cycle management, including specialized formulations such as pediatric formulations, and the specific technical issues that may evolve in excipient selection and functionality, including taste-masking and moisture protection, to develop an orally palatable product.

Participating in the webcast were: Avinash Thombre, PhD, research fellow, pharmaceutical sciences with Pfizer Global Research and Development, who discussed life-cycle management and new dosage form options; Karen C. Thompson, PhD, distinguished senior investigator, pharmaceutical sciences at Merck & Co., who discussed insight into pediatric formulations and related dosage forms; and Nigel Langley, PhD, MBA, head of North American technical sales, Pharma Ingredients & Services, BASF, who discussed novel taste-masking excipient solutions. The webcast may be found at www.PharmTech.com/Webcasts, see Taste-masking in Formulation Development.

In 2011, BASF launched Kollicoat Smartseal 30 D, an aqueous disperson of a film-forming polymer with taste-masking and moisture-barrier applications. The excipient is highly impermeable to water vapor, which helps preserve the potency of sensitive active ingredients, according to the company. The polymer is stable in saliva and specifically soluble in gastric juice. These properties allow for effective protection from unpleasant taste in the patient's mouth and rapid release and onset of active ingredient action in the stomach.

In October 2011, BASF and Colorcon announced a collaboration for the development of future film-coating systems using BASF's Kollicoat Smartseal 30 D and a new Colorcon preformulated additive. Colorcon developed the preformulated additive system for use with Kollicoat Smartseal 30 D to enable efficient preparation and application of this polymer in taste-masking applications. The preformulated additive lowers the number of materials to be dispensed by 50% and reduces the preparation time by almost 40%, according to an Oct. 21, 2011, BASF press release.

"We have chosen Kollicoat Smartseal 30 D because it is the best-in-class reverse enteric polymer for taste masking", said Kamlesh Oza, general manager, film coating at Colorcon, in the BASF press release. "Kollicoat Smartseal 30 D is the first water-based dispersion having both taste-masking and moisture-barrier properties. It was developed to simplify and accelerate aqueous film coating operations and opens new doors for formulating tablet, pellet, and particle coatings. Our collaboration to develop the additive will bring batch-to-batch color consistency, performance, speed, and simplicity, enabling easy reconstituting of the film former in pharmaceutical coating operations while maintaining functionality," he said.

Kollicoat Smartseal 30 D is part of BASF's existing tablet coatings portfolio. Under the Kollicoat brand, BASF markets a range of coating polymers and copolymers that are used to coat tablets, capsules, and pellets and to control the release of drugs from solid-dosage forms. The Kollicoat family includes: Kollicoat IR and Kollicoat Protect instant-release coatings, Kollicoat IR Color Coating Systems, Kollicoat MAE enteric coatings, Kollicoat SR 30 D sustained-release coatings, and the new Kollicoat Smartseal 30 D protective coatings.