Compositions and methods of use for modified release minoxidil
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Publication Number
US-12268688-B2
Publication Date
2025-04-08
Expiration Date
Abstract
The compositions and methods provided herein include a pharmaceutical formulation for oral administration comprising a daily dose of a modified release formulation of minoxidil or a pharmaceutically acceptable salt thereof. Also provided herein are pharmaceutical formulations for oral administration comprising a daily dose of a modified release formulation of minoxidil or a pharmaceutically acceptable salt thereof and one or more additional active agents. Also provided herein are methods of treating hair loss by administering to a subject in need thereof a daily dose of a modified release formulation of minoxidil or a pharmaceutically acceptable salt thereof. Further provided herein is a kit including a slow modified release vehicle comprising oral minoxidil or a pharmaceutically acceptable salt thereof.
Core Innovation
The disclosed invention relates to modified release pharmaceutical formulations comprising minoxidil or a pharmaceutically acceptable salt thereof, for oral administration to a subject in need thereof treatment of hair loss. The formulations are defined by the systemic exposure they provide, including a blood level of about 1 ng/ml to about 20 ng/ml, a Cmax of about 0.25 ng/ml to about 20 ng/ml, and a Tmax of about 30 to about 360 minutes. The invention specifies dosing amounts of about 3.5 mg to about 20 mg and includes daily dose embodiments within these ranges.
The modified release formulations are characterized by dosage form design intended to avoid dissolution in acidic gastric pH and to dissolve in intestinal pH, using pH-sensitive polymers and enteric-coated, modified-release oral formulations. pH-sensitive polymers listed include carboxylate polymers and polymers such as polyvinyl alcohol, methacrylic acid-ethyl acrylate copolymer, cellulose acetate phthalate, hydroxypropylmethylcellulose succinate, hydroxypropylmethylcellulose phthalate, hydroxypropyl methylcellulose, polyvinyl acetate phthalate, methacrylic acid-methyl methacrylate copolymer, and shellac. The formulations also include enteric coating compositions and optional coating compositions as described.
In addition to the pH-sensitive and enteric-coated modified-release approach, the disclosed formulations define component options for the modified release pharmaceutical formulation, including release modifier, filler, glidant, lubricant, and matrix polymers. The document describes quantitative amounts for at least some formulation components, including a release modifier present in an amount of about 50% to about 80% (w/w) of the total formulation. The invention also includes example case studies and a Phase 1 crossover PK/safety study plan comparing modified-release prototypes versus immediate-release minoxidil, including pharmacokinetics endpoints and safety monitoring.
Claims Coverage
The partial claim set includes four independent claims, each centered on oral administration of minoxidil or a pharmaceutically acceptable salt in a modified-release formulation for treating hair loss, with pharmacokinetic profile constraints on blood level, Cmax, and Tmax. Across the independent claims, inventive features focus on dose amount, specified systemic exposure targets, and, in dependent content, formulation composition and comparative AUC and cardiac-effect limitations.
Modified release formulation for hair loss with systemic exposure targets
Orally administering to a subject a modified release pharmaceutical formulation comprising from about 3.5 mg to about 20 mg of minoxidil or a pharmaceutically acceptable salt thereof, wherein the modified release pharmaceutical formulation provides a blood level of about 1 ng/ml to about 20 ng/ml, a Cmax of about 0.25 ng/ml to about 20 ng/ml, and a Tmax of about 30 to about 360 minutes.
Modified release formulation with specific minoxidil dose and systemic exposure targets
Orally administering to a subject a modified release pharmaceutical formulation comprising about 4.5 mg of minoxidil or a pharmaceutically acceptable salt thereof, wherein the modified release pharmaceutical formulation provides a blood level of about 1 ng/ml to about 20 ng/ml, a Cmax of about 0.25 ng/ml to about 20 ng/ml, and a Tmax of about 30 to about 360 minutes.
Modified release formulation with about 9 mg minoxidil and systemic exposure targets
Orally administering to a subject a modified release pharmaceutical formulation comprising about 9 mg of minoxidil or a pharmaceutically acceptable salt thereof, wherein the modified release pharmaceutical formulation provides a blood level of about 1 ng/ml to about 20 ng/ml, a Cmax of about 0.25 ng/ml to about 20 ng/ml, and a Tmax of about 30 to about 360 minutes.
Daily oral dosing with systemic exposure targets for hair loss
Orally administering to a subject a daily dose of minoxidil or a pharmaceutically acceptable salt thereof, wherein the daily dose is from about 3.5 mg to about 20 mg; and the oral administration provides a blood level of about 1 ng/ml to about 20 ng/ml, a Cmax of about 0.25 ng/ml to about 20 ng/ml, and a Tmax of about 30 to about 360 minutes.
Across the independent claims, the coverage is primarily the combination of oral modified-release or daily oral minoxidil dosing for treating hair loss with specified pharmacokinetic target ranges for blood level, Cmax, and Tmax. The dependent content further narrows by including enteric coating and pH-sensitive dissolution design, maintenance of blood levels for at least about 12 hours, comparative AUC limitations versus immediate release at an equivalent dose, and constraints on additional formulation components and dosing frequency options.
Stated Advantages
Substantially no cardiac effects when orally administering the modified release pharmaceutical formulation.
A reduced AUC compared with an immediate release formulation containing an equivalent dose.
Maintenance of blood levels for at least about 12 hours.
Documented Applications
Treating hair loss in a subject in need thereof by orally administering modified release or daily dose minoxidil (or pharmaceutically acceptable salt).
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