Compositions
Inventors
Crowe, Scott • West, Mike • Roberts, Kevin • Carlton, Tim • Maggiore, Luana • Cubitt, Marion • Whale, Gary • Wahlich, John • Frodsham, Mike
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10772839-B2
Publication Date
2020-09-15
Expiration Date
Abstract
There is provided a solid pharmaceutical composition for delivering by oral administration a pharmaceutically active binding polypeptide to a region of the intestinal tract comprising a compressed core, wherein the compressed core comprises a pharmaceutically active binding polypeptide and wherein the compressed core is coated with a pH sensitive enteric coating.
Core Innovation
The invention relates to oral solid pharmaceutical compositions comprising a compressed core that includes a pharmaceutically active binding polypeptide coated with a pH sensitive enteric coating. The pharmaceutically active binding polypeptide is an immunoglobulin or an immunoglobulin fragment, and the compressed core further comprises one or more compression aids and one or more disintegrants.
The compressed core is coated with a pH sensitive enteric coating to deliver local intestinal therapeutic effect while limiting undesired release behavior such as dose dumping and reduced systemic exposure. The approach is configured to provide delayed release and sustained release in the intestinal tract using the pH profile of the gastrointestinal environment.
The patent also describes that improved thermal stability of the pharmaceutically active binding polypeptide can be achieved in the coated compressed core. It further describes release behavior characterized using Pharmacopeial enteric coating and dissolution testing frameworks, including Pharmacopeial Enteric Coating Test and Pharmacopeial Dissolution Test, as well as a Dynamic Dissolution Test with a delayed start of release.
Claims Coverage
The independent claim defines an oral solid pharmaceutical composition with a compressed core coated with a pH sensitive enteric coating, and the key inventive elements include the composition ratios in the compressed core and the selection of the pharmaceutically active binding polypeptide as an immunoglobulin or immunoglobulin fragment. Only one independent claim (clm-00001) is identified in the received content.
Compressed core with defined component weight ranges
A solid pharmaceutical composition comprising a compressed core, wherein the pharmaceutically active binding polypeptide is present at 40-75% by weight relative to the weight of the core, one or more compression aids is present at 20-55% by weight relative to the weight of the core, and one or more disintegrants is present at 2-6% by weight relative to the weight of the core.
pH sensitive enteric coated immunoglobulin binding polypeptide
The compressed core is coated with a pH sensitive enteric coating and the pharmaceutically active binding polypeptide is an immunoglobulin or an immunoglobulin fragment.
The claim coverage is centered on the defined compressed core composition combined with a pH sensitive enteric coating and an immunoglobulin or immunoglobulin fragment binding polypeptide. Dependent claim themes in the provided excerpts further define release behavior in Pharmacopeial dissolution and Dynamic Dissolution Test timepoints and narrow the immunoglobulin fragment identity, but these are not independent claim elements in the received independent claim text.
Stated Advantages
Delayed and sustained release in the intestinal tract using a pH sensitive enteric coating.
Targeted release with reduced dose dumping and reduced systemic exposure.
Improved polypeptide thermal stability.
High luminal concentrations of ICVD in the lower GI and recovery in faeces over extended time.
Documented Applications
Local intestinal therapeutic effect in the intestinal tract, including use in intestinal tract diseases such as inflammatory bowel disease, Crohn's disease, and ulcerative colitis.
Interested in licensing this patent?