Steroidal compositions and method of making and use
Inventors
Boatman, Cody • DeNeui, Daniel • Graves, Justin
Assignees
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Publication Number
US-12161751-B2
Publication Date
2024-12-10
Expiration Date
Abstract
Pharmaceutical compositions are described for the treatment of hypogonadism in humans. The compositions can include testosterone and triamcinolone along with carriers and/or adjunct ingredients. In some embodiments, the compositions can be made by mixing testosterone with triamcinolone to form an admixture, adding a binding agent to the admixture to form wet granules, drying the wet granules to form bulk granules, milling the bulk granules, and combining the milled granules with a coating agent.
Core Innovation
The invention relates to steroidal implantable pharmaceutical compositions for increased testosterone levels, including pellets comprising testosterone and triamcinolone, with stearic acid and ethylcellulose. The described pellet compositions use high-percentage testosterone with low-percentage triamcinolone and are formed into pellets.
The compositions are prepared by combining testosterone, triamcinolone, and stearic acid to form an admixture, then adding ethylcellulose dissolved in a non-aqueous volatile carrier to form wet granules. The wet granules are dried to remove the volatile carrier, milled, and combined with additional stearic acid before forming the implantable composition into pellets.
The invention further provides a method for treating a subject in need of an increased testosterone level by injecting an implantable pellet subcutaneously. The pellet formulation includes about 10 mg to about 250 mg of testosterone, about 1 μg to about 50 μg of triamcinolone, about 0.4 mg to about 12 mg of stearic acid, and about 0.9 mg to about 22.5 mg of ethylcellulose, and representative data show increases in total and free testosterone after administration.
Claims Coverage
The relevant material includes three independent claims: two process claims for preparing an implantable pharmaceutical composition and one method claim for treating a subject by subcutaneous injection of an implantable pellet. Across the independent claims, the inventive subject matter centers on specified pellet compositions and on a wet granulation-to-pellet preparation workflow using ethylcellulose and stearic acid, followed by subcutaneous pellet administration.
Wet granulation-based pellet formulation process with testosterone and triamcinolone
Combining testosterone, triamcinolone, and stearic acid to form an admixture; adding ethylcellulose dissolved in a non-aqueous volatile carrier to form wet granules; drying to remove the non-aqueous volatile carrier; milling to form milled granules; and combining the milled granules with additional stearic acid to form the implantable pharmaceutical composition.
Granulation-to-pellet process yielding specified component ranges
Forming the implantable pharmaceutical composition into pellets comprising about 10 mg to about 250 mg of testosterone, about 1 μg to about 50 μg of triamcinolone, about 0.4 mg to about 12 mg of stearic acid, and about 0.9 mg to about 22.5 mg of ethylcellulose.
Subcutaneous injection treatment using a pellet with specified component ranges
Injecting an implantable pellet subcutaneously into a subject in need of an increased testosterone level, where the pellet consists of about 10 mg to about 250 mg of testosterone, about 1 μg to about 50 μg of triamcinolone, about 0.4 mg to about 12 mg of stearic acid, and about 0.9 mg to about 22.5 mg of ethylcellulose.
Together, the independent claims cover preparation of an implantable pharmaceutical composition by wet granulation and milling with ethylcellulose and stearic acid, formation into pellets with specified component ranges, and treatment by subcutaneous injection of such a pellet.
Stated Advantages
Increases in total testosterone after administration of the pellet.
Increases in free testosterone after administration of the pellet.
Documented Applications
Treatment of a subject in need of an increased testosterone level by injecting an implantable pellet subcutaneously.
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