Treatment of erectile dysfunction and other indications
Inventors
Assignees
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Publication Number
US-9675619-B2
Publication Date
2017-06-13
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 and/or topical compositions for treating erectile dysfunction by applying a cream, gel, or lotion to the genital region. The compositions are formulated to produce an erection in less than 15 minutes after application. The compositions include a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, and a pharmaceutical agent and/or salt thereof for treating sexual dysfunction.
The pharmaceutical agent comprises one or more selected from yohimbe, alprostadil, tadalafil, apomorphine, and vardenafil. The compositions further comprise an ionic salt at a concentration of at least about 0.25 M, together with xanthan gum at no more than about 1 wt % and propylene glycol at at least about 6% by weight. The compositions also include Polysorbate 20 at no more than about 3 wt %.
The formulation is described as being delivered in a hostile biophysical environment, including high chloride and/or high ionic strength conditions and an adjusted pH compatible with skin. A further aspect of the invention addresses unexpectedly improved temperature stability, including stability at 40°C for at least about 4 weeks.
Stabilization is described as being associated with the use of a stabilization polymer selected from xanthan gum and/or KELTROL® BT/RD, together with propylene glycol and Polysorbate 20. This stability is presented alongside the topical, rapid onset objective.
Claims Coverage
The partial content provides two independent claims. Each independent claim centers on a topical method of applying a cream, gel, or lotion to the genital region using a defined nitric oxide donor formulation combined with an ionic salt and specified excipients, together with a sexual dysfunction pharmaceutical agent; one independent claim further requires rapid erection onset in a male subject.
Topical composition producing erection within 15 minutes
Applying a composition comprising a cream, gel, or lotion to the genital region of a male subject, wherein the composition produces an erection in less than 15 minutes after application.
Nitric oxide donor with specified L-arginine range
The composition comprises a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride at a concentration of about 2.5% to about 15% by weight.
High ionic strength ionic salt with xanthan gum and propylene glycol
The composition comprises an ionic salt at a concentration of at least about 0.25 M, xanthan gum at no more than about 1 wt %, and propylene glycol at at least about 6% by weight.
Polysorbate 20 excipient limit
The composition comprises Polysorbate 20 at no more than about 3 wt %.
Sexual dysfunction pharmaceutical agent at minimum concentration
The composition comprises a pharmaceutical agent and/or salt thereof for treating sexual dysfunction, comprising one or more of yohimbe, alprostadil, tadalafil, apomorphine, and vardenafil at a concentration of at least about 0.1% by weight of the composition.
Topical composition with specified L-arginine formulation for genital region treatment
Applying a composition comprising a cream, gel, or lotion to the genital region of a subject, wherein the composition comprises a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride at a concentration of about 2.5% to about 15% by weight, an ionic salt at a concentration of at least about 0.25 M, xanthan gum at no more than about 1 wt %, propylene glycol at at least about 6% by weight, and Polysorbate 20 at no more than about 3 wt %.
Sexual dysfunction pharmaceutical agent at minimum concentration
The composition comprises a pharmaceutical agent and/or salt thereof for treating sexual dysfunction, comprising one or more of yohimbe, alprostadil, tadalafil, apomorphine, and vardenafil at a concentration of at least about 0.1% by weight of the composition.
Across the independent claims, coverage is directed to topical application to the genital region using a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride at defined concentration ranges, combined with an ionic salt at at least about 0.25 M, xanthan gum at no more than about 1 wt %, propylene glycol at at least about 6% by weight, and Polysorbate 20 at no more than about 3 wt %, together with a sexual dysfunction pharmaceutical agent selected from yohimbe, alprostadil, tadalafil, apomorphine, and vardenafil at at least about 0.1% by weight. One independent claim further requires that the composition produces an erection in less than 15 minutes after application in a male subject.
Stated Advantages
Rapid onset, producing an erection in less than 15 minutes after application.
Temperature stability, including stability when exposed to 40°C for at least about 4 weeks.
Unexpectedly improved temperature stability when using a stabilization polymer together with propylene glycol and Polysorbate 20.
Reduced systemic exposure.
Documented Applications
Topical/transdermal treatment of erectile dysfunction by applying a cream, gel, or lotion to the genital region of a male subject to produce an erection in less than 15 minutes.
Topical treatment of sexual dysfunction by applying a composition to the genital region of a subject using the specified nitric oxide donor and excipient composition.
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