Treatment of erectile dysfunction and other indications
Inventors
Assignees
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Publication Number
US-10172865-B2
Publication Date
2019-01-08
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 compositions and methods for treating sexual dysfunction in a female. The compositions are applied to the genital region and are provided as a cream, gel, or lotion. The composition comprises a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride together with sildenafil and/or a salt thereof.
A key aspect is that the composition has an ionic strength of at least about 1 M. The formulations are described as being formulated for a hostile biophysical environment characterized notably by high ionic strength/high chloride. The compositions further include xanthan gum at no more than about 1 wt %, propylene glycol at least about 6% by weight, and a polysorbate at no more than about 3 wt %.
The document further describes that adding a stabilization polymer such as xanthan gum or KELTROL BT/RD, propylene glycol, and a polysorbate can improve temperature stability, including at least 40°C, compared with compositions missing one component. The composition is also described as achieving rapid onset after topical application, promoting transdermal migration under high-salt conditions, and reducing systemic exposure compared with oral dosing.
Claims Coverage
The partial content provides two independent claims covering a topical method for treating sexual dysfunction in a female using a cream, gel, or lotion containing an L-arginine or L-arginine hydrochloride nitric oxide donor and sildenafil in a high-ionic-strength formulation with specified excipient constraints. Across both independent claims, the main inventive features are the same as recited in the claim text, with dependent claims adding stability and optional salt/package options.
Topical treatment composition for female sexual dysfunction
Applying, to the genital region of a female, a cream, gel, or lotion composition comprising sildenafil and/or a salt thereof together with a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride.
High-ionic-strength hostile environment formulation
The composition has an ionic strength of at least about 1 M.
Specified excipient concentration constraints with nitric oxide donor and sildenafil
The composition includes xanthan gum at no more than about 1 wt %; propylene glycol at least about 6% by weight; and polysorbate at no more than about 3 wt %.
Both independent claims are directed to topical application to the genital region of a female using a cream, gel, or lotion that combines an L-arginine or L-arginine hydrochloride nitric oxide donor with sildenafil in an ionic-strength-at-least-about-1 M formulation, while constraining xanthan gum, propylene glycol, and polysorbate to specified weight-percentage ranges.
Stated Advantages
Improves temperature stability, including temperature stability at ≥40°C, compared with compositions missing one component.
Described as achieving rapid onset after topical application.
Promotes transdermal migration under high-salt environments.
Described as reducing systemic exposure versus oral dosing.
Documented Applications
A user case demonstrating erection after topical sildenafil cream application to the genital region for a female.
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