Treatment of erectile dysfunction and other indications
Inventors
Assignees
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Publication Number
US-12138268-B2
Publication Date
2024-11-12
Expiration Date
Abstract
The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising a phosphodiesterase type 5 inhibitor and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.
Core Innovation
The invention describes topical delivery compositions for treating erectile dysfunction in a subject, in which sildenafil and/or a salt thereof is delivered to the skin in a formulation that includes a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride. The formulation is designed to function in a hostile biophysical environment characterized by high chloride and high ionic strength, together with pH optimization to promote ionization of relevant components.
The invention further emphasizes stabilization of the high-ionic-strength topical formulation. The composition includes xanthan gum as a stabilization polymer, propylene glycol, and a polysorbate surfactant, with an ionic salt that provides an ionic strength of about 0.25 M to about 15 M. Magnesium chloride is described as stabilizing higher-pKa compounds, and emulsion-based delivery vehicles, including creams and patches, are described.
A key aspect of the invention is combining the nitric oxide donor with the PDE5 inhibitor under high ionic strength topical delivery conditions to support local blood flow. The description reports unexpected temperature stability at or below 40°C and long-term retention of rapid transdermal delivery, and it includes example formulations and a clinical-use example involving a 5% sildenafil cream with a stated salt/pH composition.
Claims Coverage
The partial content includes one independent claim. It covers a topical skin-delivery composition containing an L-arginine nitric oxide donor and sildenafil or a salt thereof in a high-ionic-strength formulation, with specific excipient components and an ionic strength range.
High-ionic-strength topical L-arginine/sildenafil composition for skin delivery
A composition for topical delivery to the skin of a subject, comprising a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride; xanthan gum; propylene glycol; a polysorbate surfactant; sildenafil and/or a salt thereof; and an ionic salt, wherein the composition has an ionic strength of about 0.25 M to about 15 M.
The claim set refines the independent concept by specifying ionic-salt constituents and sildenafil salt forms, adding packaging options for the nitric oxide donor, introducing timing and rapidity for an erection after application, and imposing additional quantitative constraints related to ionic strength and formulation stability.
Stated Advantages
Unexpected temperature stability at or below 40°C.
Long-term retention of rapid transdermal delivery.
Rapid onset, including an erection produced in less than 10 minutes after application.
Documented Applications
Topical delivery to the skin for treating erectile dysfunction in a subject, including a clinical-use example using a 5% sildenafil cream producing a functional erection following topical application with a stated salt/pH composition.
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