Capsugel and Merck KGaA Named Winners of the Formulation and Excipients Category of the CPhI Pharma Awards

Capsugel’s intrinsically enteric capsule technology provides enteric protection and delayed release without a functional coating. Merck’s Parteck SRP 80 sustained-release excipient is well suited for direct compression.

Capsugel won the Excellence in Formulation Award in the CPhI Pharma Awards 2016 with its intrinsically enteric capsule technology, which provides enteric protection and delayed release without a functional coating.

“Capsugel’s intrinsically enteric capsule technology is the first viable alternative to enteric coating on the market,” Keith Hutchison, senior vice president of Research and Development, Capsugel, told Pharmaceutical Technology Europe. “Through novel polymer science, the capsules are made from actual enteric polymer and the standardized capsule dimensions ensure predictable delayed release performance every time, providing protection of the stomach from potentially irritant drugs.”

Composed of pharmaceutical-grade cellulosic derivatives, these two-piece capsules enable the oral delivery of sensitive macromolecules that require enteric protection but degrade under the high temperatures associated with coating application and drying.

“Finding better ways to deliver drugs to the small intestine, formulate acid-sensitive active ingredients, and protect the stomach are significant challenges for the biopharmaceutical industry,” Hutchison said. “Historically, enteric protection or delayed release targeting the upper gastrointestinal tract for optimal absorption have been achieved using enteric coatings. Intrinsically enteric capsule technologies allow formulators to avoid coating preparation, application, and validation, which greatly simplifies preclinical and clinical studies for compounds requiring enteric protection or delayed release.”

By eliminating the need for enteric coating, the new intrinsically enteric capsule technology can accelerate preclinical assessments and clinical development for compounds requiring enteric protection and/or delayed release in the upper gastro-intestinal tract. According to Hutchison, development time can potentially be reduced by up to several months. “Capsugel now offers two distinct yet complementary intrinsically enteric capsule technologies. Vcaps Enteric capsules are suited for delivery of a wide range of APIs, while the enTRinsic Drug Delivery Technology is an ideal solution for APIs with high acid or enzyme sensitivity, such as certain peptides, proteins, vaccines, and microbiomes,” he said.

The Excellence in Excipients Award went to Parteck SRP 80 polyvinyl alcohol (PVA)-based excipient for sustained-release applications from Merck KGaA's life science business (referred to MilliporeSigma in the U.S. and Canada). The excipient is functionally designed for sustained-release matrix tablets and is well suited for direct compression processes. Constant in-vitro release behavior can be achieved over a broad range of compression forces and tablet hardness. The excipient’s compression force and tablet hardness profile make it possible to incorporate poorly compressible APIs or higher amounts of the drug while still creating tablets with sufficient galenic properties (i.e., high hardness and low friability).

According to the company, Parteck SRP 80 is resistant to pH effects and alcohol-induced dose dumping. Because the excipient is fully synthetic, issues such as batch-to-batch inconsistency and raw material variations can be eliminated, thus simplifying the quality-by-design and validation processes.