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Publication Number
US-11969416-B1
Publication Date
2024-04-30
Expiration Date
Abstract
The present disclosure relates to pharmaceutical solid forms and pharmaceutical compositions comprising ibutamoren or a pharmaceutically acceptable salt thereof, and methods for administering to a pediatric subject for treating growth hormone deficiency.
Core Innovation
The invention relates to ibutamoren or a pharmaceutically acceptable salt thereof in a pediatric solid oral dosage form. It provides a compressed tablet comprising a plurality of roller-compacted drug-containing granules and extragranular excipients, sized for pediatric use with specified tablet weight and diameter constraints.
The problem addressed is the provision of an oral solid dosage form for pediatric subjects for treating growth hormone deficiency, while maintaining tablet manufacturability and suitable physical properties at very high drug load. The disclosure frames the need for compressed tablets with low friability and adequate hardness, including when the tablet weighs less than about 20 mg and has a diameter of less than about 4 mm, and with pediatric-appropriate small diameters.
The invention further characterizes and controls the formulation by specifying excipient components such as pregelatinized starch, mannitol, croscarmellose sodium, and magnesium stearate and/or talc, together with extragranular disintegrant and lubricant. It also supports tablet performance by describing roller-compacted drug-containing granules and their physical properties, including density and particle size distribution metrics.
Claims Coverage
The document includes one independent claim covering a compressed tablet formulation with roller-compacted drug-containing granules and tightly defined excipient amounts and tablet physical properties. Dependent claims further narrow specific aspects such as drug amount, granule density metrics, coating composition constraints, and packaging.
Roller-compacted ibutamoren compressed tablet with extragranular excipients
A compressed tablet comprising a plurality of roller-compacted drug-containing granules and extragranular excipients, wherein the drug-containing granules comprise ibutamoren or a pharmaceutically acceptable salt thereof, pregelatinized starch, mannitol, croscarmellose sodium, and a magnesium stearate and/or talc, wherein the ibutamoren or a pharmaceutically acceptable salt thereof is in an amount greater than or equal to 70% by weight of the tablet, wherein the extragranular excipients comprise a disintegrant and a lubricant, wherein the tablet weighs less than about 20 mg and has a diameter of less than about 4 mm, and wherein the tablet has a hardness from about 2.5 Kp to about 6 Kp and a friability less than 1%.
Tablet with ibutamoren at 70% to 90% by weight
The tablet wherein the ibutamoren or a pharmaceutically acceptable salt thereof is in an amount from about 70% by weight to about 90% by weight of the tablet.
Drug-containing granules with constrained bulk and/or tapped density
The tablet wherein the drug-containing granules have a bulk density less than 0.6 g/cc and/or a tapped density less than 0.78 g/cc.
Tablet properties linked to hardness and friability constraints
The tablet has a hardness from about 2.5 Kp to about 6 Kp and a friability of less than 0.5%.
Coated tablet with specific coating compositions and PEG exclusion
The tablet wherein the compressed tablet has a coating comprising either a N,N-dimethylaminoethyl methacrylate/methacrylate/butylmethacrylate copolymer or a polyvinyl alcohol (PVA)-based coating that is free of polyethylene glycol.
Capsule containing multiple tablets
A pharmaceutical composition provided as a capsule that contains 2-12 pharmaceutical tablets.
Across the independent claim and its refinements, the coverage centers on a pediatric-sized compressed tablet of ibutamoren or a pharmaceutically acceptable salt thereof formulated as roller-compacted drug-containing granules with specified excipients and defined tablet physical properties. Dependent claims further constrain drug loading, granule density metrics, hardness and friability, include optional coating embodiments, and specify a capsule packaging embodiment containing multiple tablets.
Stated Advantages
Provides a compressed oral tablet with low friability and defined hardness.
Enables a high drug loading ibutamoren content at greater than or equal to 70% by weight of the tablet while maintaining specified tablet physical properties.
Provides pediatric-sized tablets, including a tablet weight less than about 20 mg and a diameter less than about 4 mm.
Documented Applications
Oral solid treatment approach for growth hormone deficiency (GHD) in pediatric subjects, using ibutamoren in a compressed tablet dosage form.
Pediatric administration using a capsule containing multiple pharmaceutical tablets (2-12).
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