Claims for Patent: 11,654,124

Summary for Patent: 11,654,124

Title:	Stabilized formulations of 4-amino-3-substituted butanoic acid derivatives
Abstract:	Pharmaceutical compositions including an active ingredient and a stabilizer, as well as methods of manufacture of the compositions, and methods of their use. The composition may include the active ingredient dispersed throughout a matrix of the stabilizer. In some embodiments, the active ingredient and the stabilizer are intimately mixed in a matrix formulation. In some embodiments, the active ingredient is selected from 4 amino-3-(4-chlorophenyl)butanoic acid) (“baclofen”) and its pharmaceutically acceptable salts.
Inventor(s):	David Penake, Sharon Hamm, Leonard O'MAHONY, John Devane, Wolfgang Mohr, Manuel Weinheimer
Assignee:	Saol International Research Ltd , Amneal Pharmaceuticals LLC
Application Number:	US17/630,297
Patent Claims:	1. An immediate release pharmaceutical composition, comprising an active ingredient selected from 4-amino-3-(4-chlorophenyl) butanoic acid) (“baclofen”) and a pharmaceutically acceptable salt thereof; and a stabilizer, wherein the stabilizer is a copolymer of poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate). 2. The immediate release composition of claim 1, wherein the active ingredient is dispersed throughout a matrix of the stabilizer. 3. The immediate release composition of claim 1, wherein the active ingredient and the stabilizer are intimately mixed in a-granular matrix composition. 4. The immediate release composition of claim 1, wherein a weight ratio of the stabilizer to the active ingredient is from about 1.5:1 to about 20:1. 5. The immediate release pharmaceutical composition of claim 1, further comprising one or more excipients selected from a group consisting of xylitol, calcium stearate, colloidal silicon dioxide, crospovidone, hypromellose, mannitol, saccharin sodium, talc, flavoring agent, and mixtures thereof. 6. An immediate release pharmaceutical composition, comprising an active ingredient selected from 4-amino-3-(4-chlorophenyl) butanoic acid) (“baclofen”) and a pharmaceutically acceptable salt thereof and a stabilizer; wherein a weight ratio of the stabilizer to the active ingredient is from about 1.5:1 to about 20:1, and wherein the stabilizer is a copolymer of poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate). 7. The immediate release composition of claim 6, wherein the active ingredient is dispersed throughout a matrix of the stabilizer. 8. The immediate release composition of claim 6, wherein the active ingredient and the stabilizer are intimately mixed in a granular matrix composition. 9. The immediate release pharmaceutical composition of claim 6, further comprising one or more excipients selected from a group consisting of xylitol, calcium stearate, colloidal silicon dioxide, crospovidone, hypromellose, mannitol, saccharin sodium, talc, flavoring agent, and mixtures thereof. 10. A method of making an immediate release pharmaceutical formulation comprising an active ingredient comprising 4-amino-3-(4-chlorophenyl) butanoic acid) (“baclofen”) or a pharmaceutically acceptable salt thereof and a stabilizer; the method comprising intimately mixing the active ingredient and the stabilizer into a granular matrix blend; wherein a weight ratio of the stabilizer to the active ingredient is from about 1.5:1 to about 20:1, and wherein the stabilizer is a copolymer of poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate); and wherein the pharmaceutical formulation exhibits immediate release characteristics. 11. The method of claim 10, wherein the intimately mixing comprises at least one of wet granulation or dry granulation. 12. The method of claim 10, wherein the intimately mixing comprises dry blending of the active ingredient and the stabilizer to obtain a dry blend, followed by wet granulation of the dry blend. 13. The method of claim 12, wherein the wet granulation comprises wetting the dry blend with ethanol and wet mixing, drying, and cooling to obtain granules comprising the active ingredient and the stabilizer.