Oligosaccharide formulations of kappa opioid receptor agonists
Inventors
Wilson, Bryan R. • O'Connor, Stephen J.
Assignees
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Publication Number
US-11986509-B2
Publication Date
2024-05-21
Expiration Date
Abstract
The invention provides formulations for oral delivery of a therapeutic agent wherein the formulation comprises a kappa opioid receptor agonist, an oligosaccharide stabilizing agent and an optional absorption enhancer. The kappa opioid receptor agonist may be coated with, embedded in or mixed with an oligosaccharide, such as trehalose. Also provided are capsules containing the oral formulations of the kappa opioid receptor agonists, the oligosaccharide and the absorption enhancer of the invention. The invention further provides methods of manufacture of the formulations and methods of their use for the prophylaxis, inhibition and treatment of variety of kappa opioid receptor-associated diseases and conditions such as pain, pruritus and inflammation. The methods of use include administering to the mammal the formulation of the kappa opioid receptor agonist, oligosaccharide and optional absorption enhancers.
Core Innovation
The invention relates to an oral delivery formulation for a kappa opioid receptor agonist comprising particles including the kappa opioid receptor agonist and an oligosaccharide. The kappa opioid receptor agonist is CR845 having the formula D-Phe-D-Phe-D-Leu-D-Lys-[ω(4-aminopiperidine-4-carboxylic acid)]-OH or a hydrate, salt, acid salt or acid salt hydrate thereof, and the oligosaccharide is trehalose.
The formulation includes particles wherein CR845 and trehalose are present together, with optional pharmaceutically acceptable components and optional absorption enhancers. The oral delivery formulation is associated with enteric protection using an enteric coating or an enteric capsule, including examples based on enteric polymers and capsules.
A manufacturing approach is described in which particles are formed by spray drying a mixture of CR845 and trehalose, thereby embedding or associating the CR845 within trehalose-containing particles. Additional approaches include forming particles by coating drug and oligosaccharide onto beads and producing a particulate system suitable for enteric coated dosage forms.
Claims Coverage
The provided independent claim covers an oral delivery formulation defined by four inventive features: CR845, trehalose as the oligosaccharide, a particle-based composition, and a stability requirement. No additional independent claims are provided in the partial content.
Particles comprising CR845 and trehalose with stability requirement
A formulation for oral delivery comprising particles including a kappa opioid receptor agonist and an oligosaccharide, wherein the kappa opioid receptor agonist is CR845 having the formula D-Phe-D-Phe-D-Leu-D-Lys-[ω(4-aminopiperidine-4-carboxylic acid)]-OH or a hydrate, salt, acid salt or acid salt hydrate thereof; wherein the oligosaccharide is trehalose and wherein the CR845 is stable for at least a year at 25°C.
The core inventive coverage is the CR845 oral delivery particle formulation using trehalose as the oligosaccharide with CR845 stability of at least one year at 25°C, with dependent claim coverage refining optional components and dosage and optionally spray drying to form the particles.
Stated Advantages
CR845 stability for at least a year at 25°C.
Documented Applications
Treating kappa-opioid-associated conditions including pain, pruritus, and inflammation, including prophylaxis/inhibition/treatment.
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