Patent ID: 11865213
Assignee: MAPI PHARMA LTD
Field: Pharmaceuticals (Chemistry)
Classification: CPC A | IPC A

Claim 0:
1. A long-acting parenteral pharmaceutical composition comprising dried microparticles comprising a therapeutically effective amount of semaglutide or a pharmaceutically acceptable salt thereof and a biodegradable carrier at a ratio of about 1:10 to about 1:15 (w/w),
wherein the composition releases less than 20% of semaglutide or a pharmaceutically acceptable salt thereof over 24 hours in a phosphate buffer at pH 7.4,
wherein the composition releases less than 80% of the semaglutide or pharmaceutically acceptable salt thereof over 14 days in a phosphate buffer at pH 7.4,
wherein the composition releases more than 80% of the semaglutide or pharmaceutically acceptable salt thereof over 28 days in a phosphate buffer at pH 7.4,
wherein semaglutide is released from the composition in a continuous manner over 14 days upon dissolution in a phosphate buffer at pH 7.4,
wherein the composition releases the semiglutide active ingredient over a period of about four weeks to about two months,
wherein the long-acting parenteral pharmaceutical composition is a long-acting depot composition suitable for administration at a medically acceptable location in a subject in need thereof at a frequency of once every four weeks to once every six months, and
wherein the dried microparticles are formed by drying water-in-oil-in-water (w/o/w) double emulsion droplets comprising:
a) an internal aqueous phase comprising a therapeutically effective amount of semaglutide or a pharmaceutically acceptable salt thereof;
b) a water immiscible polymeric phase comprising a biodegradable carrier selected from the group consisting of polylactides, polyglycolides, polycaprolactones, and combinations thereof, and a first surfactant comprising a fatty acid or a derivative thereof; and
c) an external aqueous phase comprising a tonicity modifier comprising sodium chloride,
wherein the dried microparticles are devoid of any coating layer.