Ibudilast oral formulations and methods of using same
Inventors
Matsuda, Kazuko • Gaeta, Federico Carlos Aréjola
Assignees
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Publication Number
US-11865214-B2
Publication Date
2024-01-09
Expiration Date
Abstract
This disclosure is directed to ibudilast higher dosage oral formulations, such as tablet or capsule formulations, and the corresponding methods of treatment.
Core Innovation
The patent describes high-dose oral ibudilast pharmaceutical compositions formulated as tablets or capsules. The compositions include ibudilast in about 3% w/w to about 15% w/w along with excipients such as lactose, microcrystalline cellulose, hypromellose, magnesium stearate, and colloidal silicon dioxide, with dissolution performance defined by USP Apparatus Type II testing conditions.
A central aspect of the invention is the dissolution behavior achieved when the tablet or capsule is tested in USP Apparatus Type II at 50 rpm in 900 mL of simulated gastric fluid medium at 37°C. The composition is defined by a requirement that at least about 12% of the ibudilast has been released at about 2 hours, with extended-time release performance also described, including sequential media dissolution using simulated gastric fluid followed by phosphate buffer containing 0.3% sodium lauryl sulfate at pH 6.8.
The compositions may be provided with optional tablet coatings. The patent specifies coating compositions such as polyvinyl alcohol with a plasticizer and pigment, or methacrylic acid/ethyl acrylate copolymer dispersion with triethyl citrate and talc, and it also describes exclusions including compositions being devoid of hydroxypropyl methylcellulose-phthalate and/or devoid of hydrogenated castor oil.
Claims Coverage
The independent claim defines one core inventive composition and dosage form, with the main inventive requirements driven by the specified ibudilast/excipient composition and a dissolution profile measured in USP Apparatus Type II. Dependent claims refine the dosage form and add additional constraints and specific material choices.
Ibudilast excipient tablet or capsule composition with specified dissolution at 2 hours
A pharmaceutical composition consisting of about 3% w/w to about 15% w/w ibudilast, about 30% w/w to about 40% w/w lactose, about 30% w/w to about 40% w/w microcrystalline cellulose, about 15% w/w to about 25% w/w hypromellose, about 0.2% w/w to about 0.8% w/w magnesium stearate, and about 0.5% w/w to about 5% w/w colloidal silicon dioxide, in the form of a tablet or a capsule, wherein at least about 12% of said ibudilast has been released at about 2 hours when tested in USP Apparatus Type II at 50 rpm in 900 mL of simulated gastric fluid medium at 37°C.
Tablet with coating comprising polyvinyl alcohol, plasticizer, and pigment
The tablet or capsule wherein the tablet has a coating comprising polyvinyl alcohol, a plasticizer, and a pigment.
Lactose as lactose monohydrate
The composition wherein the lactose component is lactose monohydrate.
Ibudilast dose amount in the dosage unit
The tablet or capsule contains ibudilast in an amount from about 10 mg to about 100 mg.
Specific example weight-percent formulation
The composition comprises about 10% w/w ibudilast, about 35% w/w lactose monohydrate, about 33.5% w/w microcrystalline cellulose, about 20% w/w hypromellose, about 0.5% w/w magnesium stearate, and about 1% w/w colloidal silicon dioxide.
Overall claim coverage centers on a tablet or capsule composition comprising specified weight ranges of ibudilast and excipients, combined with an experimentally defined dissolution requirement at about 2 hours in USP Apparatus Type II. Dependent features further specify optional tablet coating components, identify the lactose as lactose monohydrate, constrain ibudilast mass per dosage unit, and provide a narrower illustrative formulation.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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