Treatment of erectile dysfunction and other indications
Inventors
Assignees
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Publication Number
US-11684624-B2
Publication Date
2023-06-27
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 relates to transdermal/topical delivery for erectile dysfunction using phosphodiesterase type 5 (PDE5) inhibitors, including sildenafil and/or a salt thereof. A topical cream, gel, or lotion composition is described for delivery to the skin of a subject, and includes a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, xanthan gum, propylene glycol, and a polysorbate surfactant.
A key aspect is that the composition has an ionic strength of at least 0.25 M, described as a hostile biophysical environment characterized by high ionic strength and chloride salts. The formulation uses water and chloride salts to achieve the ionic strength, and the hostile biophysical environment is associated with stabilization and delivery performance of the sildenafil-containing topical formulation.
The invention further includes the combination of a stabilization polymer, propylene glycol, and a polysorbate surfactant that unexpectedly improves temperature stability. The topical delivery is described as producing rapid onset, and the partial content includes formulation examples and excipient lists.
Claims Coverage
The partial content provides one independent claim, with multiple dependent claims refining component identities, quantitative amounts, and performance-related conditions. The independent claim is centered on a topical skin delivery composition with an L-arginine-based nitric oxide donor, xanthan gum, propylene glycol, a polysorbate surfactant, sildenafil, and a high ionic strength threshold.
Topical skin cream, gel, or lotion with nitric oxide donor plus sildenafil
A cream, gel, or lotion composition for delivery to the skin comprising a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, xanthan gum, propylene glycol, a polysorbate surfactant, and sildenafil and/or a salt thereof, wherein the nitric oxide donor is at a concentration of at least 2.5 wt %.
High ionic strength for the topical composition
The composition has an ionic strength of at least 0.25 M.
Nitric oxide donor wt% range
The nitric oxide donor is present at a concentration between 2.5 wt % and 15 wt %.
Upper limit on xanthan gum
The composition includes xanthan gum at no more than 1 wt %.
Sildenafil minimum concentration
The composition includes sildenafil and/or a salt thereof at a concentration of at least 0.1 wt %.
Ionic strength driving through stratum corneum
The ionic strength from an ionic salt drives sildenafil and/or its salt through the stratum corneum.
Temperature stability condition
The composition is stable when exposed to 40 °C for at least 4 weeks.
Across the independent claim and dependents shown in the partial content, the inventive focus is a topical cream, gel, or lotion containing an L-arginine nitric oxide donor, sildenafil, xanthan gum, propylene glycol, and a polysorbate surfactant, with an ionic strength of at least 0.25 M, and with refinements including component wt% limits, ranges, and stability or delivery-related conditions.
Stated Advantages
Unexpected improvement in temperature stability.
Topical delivery produces rapid onset (about 1–5 minutes).
Composition is stable at 40 °C for at least 4 weeks.
Documented Applications
Topical/transdermal delivery for erectile dysfunction using PDE5 inhibitors including sildenafil.
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