Topical composition

Abstract

The present invention relates to topical compositions that provide a warming sensation when applied to the skin. Specifically, the invention pertains to compositions comprising vanillyl butyl ether, camphor, menthol, Zingiber officinale (ginger) root extract, and an emulgel base.

Description

[0001] 70260W001

[0002] TOPICAL COMPOSITION

[0003] FIELD OF THE INVENTION

[0004] The present invention relates to topical compositions that provide a warming sensation when applied to the skin. Specifically, the invention pertains to compositions comprising vanillyl butyl ether, camphor, menthol, Zingiber officinale (ginger) root extract, and an emulgel base.

[0005] BACKGROUND TO THE INVENTION

[0006] Topical warming compositions are widely used for various therapeutic and cosmetic purposes, including pain relief, muscle relaxation, and skin care. Existing formulations often suffer from limitations such as slow onset of warming effect, skin irritation, or insufficient duration of the warming sensation. Therefore, there is a need for improved topical warming compositions that provide a rapid and sustained warming effect with minimal irritation.

[0007] SUMMARY OF THE INVENTION

[0008] In a First Aspect of the Invention, there is provided a topical warming composition for application to the skin of a subject, the topical warming composition comprising: (i) vanillyl butyl ether; (ii) camphor; (iii) menthol; (iv) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising at least one pharmaceutically acceptable excipient.

[0009] Particularly the emulgel base comprises (i) an oily phase comprising at least one oil, (ii) an aqueous phase comprising water and / or pharmaceutically acceptable water-soluble components, (iii) at least one emulsifier and (iv) at least one gelling agent.

[0010] Particularly, the at least one oil in the oily phase comprises a refined mineral oil, particularly liquid paraffin.

[0011] Particularly, the aqueous phase comprises water. More particularly, the aqueous phase comprises water and propylene glycol.

[0012] Particularly the at least one emulsifier is ceteareth-20.70260W001 Particularly, the at least one gelling agent is a carbomer, particularly a carbomer homopolymer type B such as a carbomer having CAS number 9003-01-04 or 151687-96-6. Particularly, the carbomer is Carbopol® 974P NF.

[0013] The topical warming composition may further comprise at least one emollient. Preferred emollients include coco-ca pry late, coco-caprate, coco ca pry loca prate and combinations thereof, particularly coco caprylocaprate.

[0014] Topical warming compositions of the Invention may comprise at least one antioxidant, particularly at least one oil-soluble antioxidant and / or at least one preservative.

[0015] Particularly, the at least one oil-soluble antioxidant is selected from the group consisting of butylated hydroxytoluene (BHT), ascorbyl palmitate and combinations thereof. More particularly, the at least one oil-soluble antioxidant is butylated hydroxytoluene and ascorbyl palmitate. Particularly, the at least one preservative is phenoxyethanol (PE). In certain embodiments, compositions of the Invention comprise butylated hydroxytoluene, ascorbyl palmitate and phenoxyethanol.

[0016] Particularly, at least 80% (w / w) of the topical warming composition comprises emulgel base. In certain embodiments, the emulgel base comprises or consists of water, coco caprylocaprate, propylene glycol, ceteareth-20, liquid paraffin and carbomer Particularly, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract.

[0017] Particularly, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising water, coco caprylocaprate, propylene glycol, ceteareth-20, liquid paraffin and carbomer.

[0018] Compositions of the Invention may further comprise phenoxyethanol, 1,2-hexanediol, caprylyl glycol, butylated hydroxytoluene (BHT), ascorbyl palmitate and sodium hydroxide.

[0019] In some embodiments, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract and (v) an emulgel base70260W001 comprising water, coco caprylocaprate, propylene glycol, ceteareth-20, liquid paraffin and carbomer, the composition further comprising phenoxyethanol, 1,2-hexanediol, caprylyl glycol, butylated hydroxytoluene (BHT), ascorbyl palmitate and sodium hydroxide.

[0020] Particularly, compositions of the Invention may have a viscosity of from about 7,500 to about 20,000 centipoise, for example, from about 7,500 to about 10,000 centipoise or from about 10,000 to about 20,000 centipoise. More particularly a viscosity of from about 7,500 to about 20,000 centipoise measured using a Brookfield viscometer, T-B helipath spindle at 20 RPM for 1 min at room temperature. Such as a viscosity of from about 10,000 to about 20,000 centipoise measured using a Brookfield viscometer, T-B helipath spindle at 20 RPM for 1 min at room temperature or a viscosity of from about 7,500 to about 10,000 centipoise measured using a Brookfield viscometer, T-B helipath spindle at 20 RPM for 1 min at room temperature. In certain embodiments, the composition is an emulgel having a viscosity of from about 7,500 to about 10,000 centipoise. In certain embodiments, the composition is an emulgel having a viscosity of from about 10,000 to about 20,000 centipoise, particularly 13,000 centipoise. In certain embodiments, the composition is a lotion having a viscosity of from about 1,500 to about 12,000 centipoise, particularly 9,660 centipoise.

[0021] In a Second Aspect of the Invention, there is provided a skin applicator comprising the topical warming composition of the First Aspect. Particularly, the skin applicator comprises a dispenser or holder comprising the topical warming composition. Suitable skin applicators include pump spray tubes, roll-on devices, aerosol cans and adhesive patches.

[0022] In a Third Aspect of the Invention, there is provided a topical warming composition of the First Aspect or a skin applicator of the Second Aspect, for use in a non-therapeutic method for warming the skin of a subject. Particularly, the method comprises applying the topical warming composition to the skin of the subject.

[0023] In a Fourth Aspect of the Invention, there is provided a method of preparing a topical warming composition according to First Aspect. Particularly, the method comprises the steps of: (i) combining purified water and carbomer to form an aqueous phase; (ii) combining liquid paraffin, propylene glycol, coco caprylocaprate, macrogol, phenoxy ethanol, menthol, vanillyl butyl ether, camphor, butylated hydroxytoluene, Zingiber70260W001 officinale (ginger) root extract to form an oily phase and (iii) combining the oily phase with the aqueous phase.

[0024] BRIEF DESCRIPTION OF DRAWINGS

[0025] Figure 1: Figure la is a line graph showing the warming intensity (0-100 scale) measured on the shoulder over 60 minutes for Formulation 3 compared with four commercially available comparator products. Formulation 3 exhibits a gradual rise in warming sensation, reaching a moderate peak between 5 and 10 minutes and then declining steadily to a low but perceptible warmth at 60 minutes. By contrast, Puressentiel and Deep Heat show substantially higher early warming intensities, peaking at 6-8 minutes, whereas Kneipp and Physiorelax display milder warming comparable to Formulation 3. Formulation 3 avoids the high intensity peak and associated discomfort observed in some comparator products. Formulation 3 demonstrated favourable levels of "soothing warmth" in the sensory panel, being significantly more soothing than Deep Heat and Puressentiel for up to 12 minutes on the shoulder (Figure lb). Uniformity of warming was comparable to all four competitor products after the initial minute of application, indicating consistent heat distribution across the skin (Figure lc)

[0026] Figure 2: is a line chart comparing sensory panel scores (0-100 scale) for ease of spreading, smoothness, greasiness and speed of absorption for Formulation 3 and four comparator formulations. The inventive composition demonstrates significantly faster absorption than Deep Heat, Kneipp, and Puressentiel and equal or superior performance in spreading and smoothness relative to all comparators. Greasiness scores show Formulation 3 to be among the least greasy products evaluated. These results illustrate favourable textural characteristics relative to the benchmark products.

[0027] Figure 3: is a set of four warming-over-time curves generated after applying Formulation 3 in quantities of 1 g, 2 g, 4 g and as sequential applications of 1 g at 10-minute intervals (4 x 1 g). Increasing the applied quantity produces an increase in peak warming intensity, with 2 g delivering approximately one third greater peak warming than 1 g and 4 g generating higher warming than 2 g after approximately 12 minutes. Sequential 1 g applications generate a later and sustained peak, ultimately exceeding the warmth provided by the single 4 g dose. These data demonstrate that70260W001 the composition provides a controllable, dose dependent warming response without excessive warmth.

[0028] Figure 4: is a histogram showing the proportion of consumer participants reporting warming-onset at different time intervals. Approximately 44% reported perceiving warming within 2 minutes, and 77% reported warming within 5 minutes. A small minority reported onset times greater than 10 minutes. These data demonstrate rapid onset of the warming effect under typical home use conditions.

[0029] Figure 5: is a histogram illustrating the duration of warming reported in the home use test. Around one third of users experienced warming for up to 30 minutes following application, with the majority reporting warming durations aligned with expectations of a warming product. A minority indicated shorter warming duration, consistent with individual variation in sensation perception.

[0030] Figure 6: is a bar chart presenting the proportion of respondents selecting "agree slightly" or "agree strongly" with key performance statements. High levels of agreement were recorded for the product being fast absorbing (89%), moisturising (89%), non-greasy (87%), providing a pleasant warming experience (78%) and relieving muscle tension (80%). These data indicate broad consumer recognition of the formulation's functional benefits.

[0031] DETAILED DESCRIPTION OF THE INVENTION

[0032] The present invention relates to topical warming compositions for application to the skin of a subject. The Inventors have identified formulations wherein the onset of warming sensation commences within around two minutes following application to the skin. The compositions of the Invention have a texture and other attributes, such as skin absorption, greasiness and moisturizing effect, that are rated as being superior in consumer testing studies. In addition, the warming effect is of long duration with no or little skin irritation.

[0033] The topical warming compositions of the Invention generally comprise: (i) vanillyl butyl ether; (ii) camphor; (iii) menthol; (iv) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising at least one pharmaceutically acceptable excipient.

[0034] Topical application refers to the application of a composition or formulation externally to the skin of a subject. Thus, a "topical composition" (or synonymously "topical70260W001 formulation") refers to a composition that can be applied topically, i.e. to the skin of a subject.

[0035] Substances which are known to provide a sensation of warmth or warmth modulation on application are called "warming agents". The skin contains sensory receptors found in the upper layers of the epidermis. Warming agents work by activating different neuro-responsive transient receptor potential cation channels, referred to as TRP channels. Vanillyl Butyl Ether (VBE) is a warming agent known to activate the TRPV-1 channel, imparting a warming sensation and inducing vasodilation upon application. Preferably, the composition comprises vanillyl butyl ether.

[0036] The vanillyl butyl ether may be present in any suitable concentration, for example from about 0.1% (w / w) to about 2% (w / w). For instance, may comprise about 0.1% (w / w), about 0.2% (w / w), about 0.3% (w / w), about 0.4% (w / w), about 0.5% (w / w), about 0.6% (w / w), about 0.7% (w / w), about 0.8% (w / w), about 0.9% (w / w), about 1% (w / w), about 1.1% (w / w), about 1.2% (w / w), about 1.3% (w / w), about 1.4% (w / w), about 1.5% (w / w), about 1.6% (w / w), about 1.7% (w / w), about 1.8% (w / w), about 1.9% (w / w) or about 2% (w / w). In some cases, the vanillyl butyl ether may be present at no more than about 2% (w / w), no more than about 1.9% (w / w), no more than about 1.8% (w / w), no more than about 1.7% (w / w), no more than about 1.6% (w / w), no more than about 1.5% (w / w), no more than about 1.4% (w / w), no more than about 1.3% (w / w), no more than about 1.2% (w / w), no more than about 1.1% (w / w), no more than about 1% (w / w), no more than about 0.9% (w / w), no more than about 0.8% (w / w), no more than about 0.7% (w / w), no more than about 0.6% (w / w), no more than about 0.5% (w / w), no more than about 0.4% (w / w), no more than about 0.3% (w / w), no more than about 0.2% (w / w), or no more than about 0.1% (w / w). Combinations of any of these are also possible. Particularly, the composition may comprise vanillyl butyl ether at between 0.1% (w / w) and 2.0% (w / w).

[0037] Camphor is a vasodilator that has the ability to provide both warming and cooling sensations and may improve capillary blood flow circulation of the skin.

[0038] Camphor may be present in the topical composition at any suitable concentration, for example from about 0.5% (w / w) to about 2% (w / w). For instance, compositions may comprise about 0.5% (w / w), about 0.6% (w / w), about 0.7% (w / w), about 0.8% (w / w), about 0.9% (w / w), about 1% (w / w), about 1.1% (w / w), about 1.2% (w / w), about70260W001 1.3% (w / w), about 1.4% (w / w), about 1.5% (w / w), about 1.6% (w / w), about 1.7% (w / w), about 1.8% (w / w), about 1.9% (w / w) or about 2% (w / w). In some cases, the camphor may be present at no more than about 2% (w / w), no more than about 1.9% (w / w), no more than about 1.8% (w / w), no more than about 1.7% (w / w), no more than about 1.6% (w / w), no more than about 1.5% (w / w), no more than about 1.4% (w / w), no more than about 1.3% (w / w), no more than about 1.2% (w / w), no more than about 1.1% (w / w), no more than about 1% (w / w), no more than about 0.9% (w / w), no more than about 0.8% (w / w), no more than about 0.7% (w / w), no more than about 0.6% (w / w) or no more than about 0.5% (w / w). Combinations of any of these are also possible. Particularly the composition may comprise 0.5%-2% (w / w) camphor.

[0039] Menthol may be used to provide a topical cooling effect. However, unlike camphor, menthol does not appear to provide a topical warming sensation.

[0040] Menthol may be present in the topical composition at any suitable concentration, for example from about 0.1% (w / w) to about 1% (w / w). For instance, compositions may comprise about 0.1% (w / w), about 0.2% (w / w), about 0.3% (w / w), about 0.4% (w / w), about 0.5% (w / w), about 0.6% (w / w), about 0.7% (w / w), about 0.8% (w / w), about 0.9% (w / w) or about 1% (w / w). In some cases, the camphor may be present at no more than about 1% (w / w), no more than about 0.9% (w / w), no more than about 0.8% (w / w), no more than about 0.7% (w / w), no more than about 0.6% (w / w), no more than about 0.5% (w / w), no more than about 0.4% (w / w), no more than about 0.3% (w / w), no more than about 0.2% (w / w) or no more than about 0.1% (w / w). Combinations of any of these are also possible. Particularly the composition may comprise 0.1%-l% (w / w) menthol.

[0041] Compositions of the present Invention are emulgels with vanillyl butyl ether, camphor, menthol, Zingiber officinale (ginger) root extract formulated within an emulgel base. An "emulgel" is composition that has the characteristics of a gel and an emulsion, for example compositions either of the oil-in-water or water-in-oil type, that are gelled by mixing with a gelling agent. Emulgels are mixtures of two or more liquids that are normally immiscible with one liquid dispersed as globules (dispersed phase) in the other liquid (continuous phase).70260W001 Particularly the emulgel base comprises (i) an oily phase comprising at least one oil, (ii) an aqueous phase comprising water and / or pharmaceutically acceptable water-soluble components, (iii) at least one emulsifier and (iv) at least one gelling agent.

[0042] Particularly, the at least one oil in the oily phase comprises a refined mineral oil, particularly liquid paraffin.

[0043] Particularly, the aqueous phase comprises water. More particularly, the aqueous phase comprises water and propylene glycol. More particularly, emulgels of the present Invention comprise water as the main solvent.

[0044] The term "emulsifier" as used herein, refers to a substance that can stabilize an emulsion. Particularly the at least one emulsifier is ceteareth-20.

[0045] The term "gelling agent" refers to a polymer compound capable of conferring on the composition the texture of a gel. Particularly, the at least one gelling agent is a synthetic polymer derived from cross- 1 inking of poly(acrylic acid), referred to as carbomers, particularly a carbomer homopolymer type B such as a carbomer having CAS number 9003-01-04 or 151687-96-6. Particularly, the carbomer is Carbopol® 974P NF. By way of non-limiting example, other suitable gelling agents include Carbopol® 980P, and Carbopol Ulterez® 20.

[0046] The topical warming composition may further comprise at least one emollient.

[0047] Emollients are compounds that increase skin hydration, thereby softening the external layers of the skin. Preferred emollients include coco-ca pry late, coco-caprate, coco ca pry loca prate and combinations thereof.

[0048] Topical warming compositions of the Invention may comprise at least one antioxidant, particularly at least one oil-soluble antioxidant and / or at least one preservative.

[0049] Particularly, the at least one oil-soluble antioxidant is selected from the group consisting of butylated hydroxytoluene (BHT), ascorbyl palmitate and combinations thereof. More particularly, the at least one oil-soluble antioxidant is butylated hydroxytoluene and ascorbyl palmitate. Particularly, the at least one preservative is phenoxyethanol (PE). In certain embodiments, compositions of the Invention comprise butylated hydroxytoluene, ascorbyl palmitate and phenoxyethanol.70260W001 Particularly, at least 80% (w / w) of the topical warming composition comprises emulgel base. In certain embodiments, the emulgel base comprises or consists of water, coco ca pry loca prate, propylene glycol, ceteareth-20, liquid paraffin and carbomer Particularly, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract.

[0050] Particularly, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising water, coco caprylocaprate, propylene glycol, ceteareth-20, liquid paraffin and carbomer.

[0051] Particularly, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising water, coco caprylocaprate, propylene glycol, ceteareth-20, liquid paraffin and carbomer, wherein at least 80% (w / w) of the topical warming composition comprises emulgel base.

[0052] Compositions of the Invention may further comprise phenoxyethanol, 1,2-hexanediol, caprylyl glycol, butylated hydroxytoluene (BHT), ascorbyl palmitate and sodium hydroxide.

[0053] In some embodiments, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising (vi) 70%-80% (w / w) water, (vii) 6%-9% (w / w) coco caprylocaprate, (viii) 3%-6% (w / w) propylene glycol, (ix) l%-4% (w / w) ceteareth-20, (x) l%-4% (w / w) liquid paraffin and (xi) 0.1%-2% (w / w) carbomer, the composition further comprising phenoxyethanol, 1,2-hexanediol, caprylyl glycol, butylated hydroxytoluene (BHT), ascorbyl palmitate and sodium hydroxide.

[0054] In some embodiments, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract and (v) an emulgel base70260W001 comprising (vi) 70%-80% (w / w) water, (vii) 6%-9% (w / w) coco-caprylate, coco caprate or coco caprylocaprate (viii) 3%-6% (w / w) propylene glycol, (ix) l%-4% (w / w) ceteareth-20, (x) l%-4% (w / w) liquid paraffin and (xi) 0.1%-2% (w / w) carbomer, the composition further comprising (xii) 0.1%-2% (w / w) phenoxyethanol, (xiii) 0.1%-0.5% (w / w) 1,2-hexanediol, (xiv) 0.1%-0.5% (w / w) caprylyl glycol, (xv) 0.01%-0.1% (w / w) butylated hydroxytoluene (BHT), (xvi) 0.001%-0.005% (w / w) ascorbyl palmitate and (xvii) 0.001%-0.5% (w / w) sodium hydroxide.

[0055] In some embodiments, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising (vi) 70%-80% (w / w) water, (vii) 6%-9% (w / w) coco-caprylate, coco caprate or coco caprylocaprate (viii) 3%-6% (w / w) propylene glycol, (ix) l%-4% (w / w) ceteareth-20, (x) l%-4% (w / w) liquid paraffin and (xi) 0.1%-2% (w / w) carbomer, the composition further comprising (xii) 0.1%-2% (w / w) phenoxyethanol, (xiii) 0.1%-0.5% (w / w) 1,2-hexanediol, (xiv) 0.1%-0.5% (w / w) caprylyl glycol, (xv) 0.01%-0.1% (w / w) butylated hydroxytoluene (BHT), (xvi) 0.001%-0.005% (w / w) ascorbyl palmitate and (xvii) 0.001%-0.03% (w / w) sodium hydroxide.

[0056] In some embodiments, compositions of the Invention may comprise (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising (vi) 70%-80% (w / w) water, (vii) 6%-9% (w / w) coco-caprylate, coco caprate or coco caprylocaprate (viii) 3%-6% (w / w) propylene glycol, (ix) l%-4% (w / w) ceteareth-20, (x) l%-4% (w / w) liquid paraffin and (xi) 0.1%-2% (w / w) carbomer, the composition further comprising (xii) 0.1%-2% (w / w) phenoxyethanol, (xiii) 0.1%-0.5% (w / w) 1,2-hexanediol, (xiv) 0.1%-0.5% (w / w) caprylyl glycol, (xv) 0.01%-0.1% (w / w) butylated hydroxytoluene (BHT), (xvi) 0.001%-0.005% (w / w) ascorbyl palmitate and (xvii) 0.465% (w / w) sodium hydroxide.

[0057] Compositions of the Invention may be packaged in formats known in the art. Thus, there is provided a skin applicator comprising the topical warming composition of the Invention. Particularly, the skin applicator comprises a dispenser or holder comprising the topical warming composition. Suitable skin applicators include pump spray tubes, roll-on devices, aerosol cans and adhesive patches.70260W001 Topical warming compositions of the Invention may be used in therapeutic and non-therapeutic methods for warming the skin of a subject. Particularly, the methods comprise applying the topical warming composition to the skin of the subject.

[0058] Topical warming compositions of the Invention may be prepared by: (i) creating an aqueous phase, (ii) creating an oily phase, (iii) combining and emulsifying the aqueous phase and the oily phase to provide an emulsion, and optionally (iv) neutralizing the emulsion to provide a composition having a pH of from pH4 to pH7. More particularly, the process may comprise (i) dispersing the carbomer in water to create an aqueous phase, (ii) preparing an oily phase by adding the other constituents to a vessel, (iii) combining the oily phase with the aqueous phase, (iv) emulsifying the oily phase in the aqueous phase to provide an emulsion, and (v) neutralising the emulsion with sodium hydroxide. In more detail, to prepare the aqueous phase, purified water and the carbomer were added to a BecomixlO vessel and dispersed at a mixing speed of 2.5 m / s and pumping speed of 25 m / s. The liquid paraffin, propylene glycol, coco ca pry loca prate, macrogol, phenoxy ethanol, menthol, vanillyl butyl ether, camphor, butylated hydroxytoluene, Zingiber officinale (ginger) root extract were added to a Becomix 30 Melting Vessel and warmed to 50°C + / - 2°C with mixing to prepare the oily phase. The oily phase was added to the dispersed carbomer (aqueous phase) at a mixing speed of 2.5 m / s and pumping speed of 15-22 m / s. Emulsification of the oily phase into the aqueous phase took place at a mixing speed of 2.5 m / s and pumping speed of 15-22 m / for at least 10 minutes. Following this, the emulsion was neutralized with 30% sodium hydroxide solution, combining the sodium hydroxide with the emulsion and homogenizing for at least 10 minutes at 2.5 m / s mixing speed with pumping speed of 15-22 m / s set in pumping and homogenization mode.

[0059] General

[0060] The term "comprising" encompasses "including" e.g. a composition "comprising" X may include something additional e.g. X + Y. In some implementations, the term "comprising" refers to the inclusion of the indicated active agent, such as recited compounds, as well as inclusion of other active agents, and carriers, excipients, emollients, stabilizers, etc., known in the consumer health industry and generally recognized as safe (GRAS). Use of the transitional phrase "consisting essentially of" means that the scope of a claim is to be interpreted to encompass the specified materials or steps recited in the claim, and those that do not materially affect the basic70260W001 and novel characteristic(s) of the claimed invention. See, In re Herz, 537 F.2d 549, 551-52, 190 USPQ 461, 463 (CCPA 1976) (emphasis in the original); see also MPEP § 2111.03. Thus, the term "consisting essentially of" when used in a claim of this invention is not intended to be interpreted to be equivalent to "comprising". The term "consisting of" and variations thereof means including and limited to (for example, the specific recited constituents or steps). In certain territories, the term "comprising an active ingredient consisting of" may be used in place of "consisting essentially". The term "about" in relation to a numerical value x is optional and means, for example, that the numerical value may comprise some variance around the stated number to allow for routine experimental fluctuation, measurement variance or to encompass minor deviations that may achieve substantially the same results as the stated number, such as x±10%, x±5%, x±4%, x±3%, x±2% or x±l%. The word "substantially" does not exclude "completely" e.g. a composition which is "substantially free" from Y may be completely free from Y. Where necessary, the word "substantially" may be omitted from the definition of the invention. All percentages and ratios used herein are by weight of total composition, unless otherwise indicated. For the avoidance of doubt, reference to percent by weight, "X% by weight", "X% (w / w)" and the like means by weight of the total composition, the amount of each ingredient being selected so that total ingredients in the composition sum to 100 percent by weight.

[0061] All references or patent applications cited within this patent specification are incorporated by reference herein. In order that this invention may be better understood, the following examples are set forth. These examples are for purposes of illustration only and are not to be construed as limiting the scope of the invention in any manner.

[0062] EXAMPLES

[0063] Example 1:

[0064] The following three formulations were prepared (all quantities shown in % w / w):

[0065]

[0066] 70260W001

[0067]

[0068] 1: Thermolat® comprises Vanillyl Butyl Ether, 1,2-Hexanediol, Caprylyl Glycol, Ascorbyl Palmitate;

[0069] 2: Cocoyl caprylocaprate / Coco-caprylate-caprate;

[0070] 3: macrogol cetostearyl ether 20, polyoxyl 20 cetostearyl ether;

[0071] 4: Butylated hydroxytoluene.

[0072] To prepare the aqueous phase, purified water and the carbomer were added to a BecomixlO vessel and dispersed at a mixing speed of 2.5 m / s and pumping speed of 25 m / s. The liquid paraffin, propylene glycol, coco caprylocaprate, macrogol, phenoxy ethanol, menthol, vanillyl butyl ether, camphor, butylated hydroxytoluene, Zingiber officinale (ginger) root extract were added to a Becomix 30 Melting Vessel and warmed to 50°C + / - 2°C with mixing to prepare the fatty phase. The fatty phase was added to the dispersed carbomer (aqueous phase) at a mixing speed of 2.5 m / s and pumping speed of 15-22 m / s. Emulsification of the fatty phase into the aqueous phase took place at a mixing speed of 2.5 m / s and pumping speed of 15-22 m / for at least 10 minutes. Following this, the emulsion was neutralized with 30% sodium hydroxide solution, combining the sodium hydroxide with the emulsion and homogenizing for at least 1070260W001 minutes at 2.5 m / s mixing speed with pumping speed of 15-22 m / s set in pumping and homogenization mode.

[0073] In patient testing, the addition of menthol and camphor increased the warming sensation of the formulation.

[0074] Example 2: Scale up batch

[0075] Formulation 3 was selected for further evaluation and the following commercial batch was prepared as described above:

[0076]

[0077] * Quantity of water and sodium hydroxide solution was calculated based on sodium hydroxide at 10 mol / L concentration.

[0078] Example 3: Sensory Panel Evaluation of Warming Intensity and Texture The commercial batch was evaluated in a trained Quantitative Descriptive Analysis (QDA) sensory panel (n = 11). A 1 g dose of the composition was applied to the forearm, shoulder, lower back or calf and assessed over 60 minutes for warmth onset, intensity, textural attributes, aroma and after-feel.70260W001 The composition demonstrated moderate, comfortable warming, with peak warmth occurring between 5-10 minutes on the shoulder and lower back and sustained low level warmth remaining after 60 minutes. Whilst competitor products such as PURESSENTIEL and DEEP HEAT exhibited higher warming intensity, these were frequently reported as being too intense or unpleasant, with some panellists experiencing burning sensations requiring dose reduction in the case of PURESSENTIEL. By contrast, Formulation 3 delivered a controlled warming profile that avoided excessive heat whilst still producing a clearly perceptible warming effect (Figure la). Further, Formulation 3 exhibited superior textural behaviour, being significantly faster absorbing than Deep Heat, Kneipp, and Puressentiel and at parity or better across spreading, smoothness and greasiness compared with all four competitor benchmarks. The rapid absorption and smooth, non-greasy texture represent material advantages in consumer usability (Figure 2).

[0079] These findings demonstrate that the combination of ingredients confers an improved sensorial profile, balancing efficacy with consumer comfort.

[0080] Example 4: Effect of Application Quantity on Warming Profile

[0081] Further tests were performed to assess warming intensity of Formulation 3 as a function of applied quantity (1 g, 2 g, 4 g, or sequential 1 g applications at 10-minute intervals). On the lower back, warming increased proportionally with dose, with 2 g producing approximately one third greater peak warmth than 1 g and 4 g exceeding the warmth of 2 g after approximately 12 minutes (Figure 3).

[0082] Sequential dosing (4 x 1 g at 10-minute intervals) produced a progressive and extended warming curve, ultimately exceeding the warming delivered by a single 4 g application and maintaining warmth for longer into the 60-minute assessment period. This demonstrates that the formulation retains warming responsiveness even with repeated application, without triggering the intolerable sensations observed for certain competitor products such as Puressentiel (which caused burning and skin redness at 2 g application) (Figure 3).

[0083] The results show that the formulation provides dose dependent tuning of the warmth experience, allowing consumers to adjust warming intensity without risk of excessive or painful heat.70260W001 Example 5: Uniformity and Soothing Warmth Performance

[0084] Formulation 3 demonstrated favourable levels of "soothing warmth" in the sensory panel, being significantly more soothing than Deep Heat and Puressentiel for up to 12 minutes on the shoulder (Figure lb). Uniformity of warming was comparable to all four competitor products after the initial minute of application, indicating consistent heat distribution across the skin (Figure lc).

[0085] This is notable given that competitor products showing higher peak warmth also scored lower on soothing character and higher on discomfort or burning. The balanced profile of warming plus soothing effect reflects improved consumer tolerability.

[0086] Example 6: Consumer Home Use Study of Warming Satisfaction

[0087] A 2-day home use test (n = 224) was conducted in the UK to evaluate real world performance. The composition of Formulation 3 was applied twice daily to the neck / shoulder and lower back in amounts of 2 g and 3 g respectively. Across the study:

[0088] • 76-79% of respondents reported a warming sensation, with average intensity of 6.6 / 9, consistent across application sites.

[0089] • 77% reported warming within 5 minutes (Figure 4), and around one third experienced warming lasting up to 30 minutes (Figure 5).

[0090] • 78% agreed the warming sensation was pleasant, and 80% agreed the product would relieve muscle tension.

[0091] • 89% found the texture non greasy and well absorbing, aligning with sensory panel findings on rapid absorption (Figure 6).

[0092] Some participants reported the warming as milder than expected; however, this was not considered a barrier to purchase for the majority, with 67% expressing purchase intent and 68% indicating they would recommend the product. Importantly, respondents appreciated that the product did not produce the burning discomfort associated with competitor products (e.g., Deep Heat type sensations) and valued the ability to reapply due to the non-medicated nature of the formulation.

[0093] The light, moisturising texture of Formulation 3 contributed significantly to consumer acceptance. In the home use test, 89% reported that the product absorbed well, 87%70260W001 that it moisturised the skin and 90% found it easy to spread, with many respondents explicitly contrasting it with their existing warming creams, noting absence of greasiness or stickiness.

[0094] These results demonstrate that the formulation provides warming perceived as effective, pleasant and well tolerated in real world use. In addition, the sensorial profile supports the technical effect that the formulation's emulgel structure not only enables controlled, comfortable warmth but also enhances usability, contributing to consumer willingness to switch from incumbent warming products.

[0095] The purpose of the above description is to illustrate some embodiments of the present invention without implying a limitation. It will be apparent to those skilled in the art that various modifications and variations may be made in the apparatus or procedure of the invention without departing from the scope or spirit of the invention.

Claims

70260W001CLAIMS1. A topical warming composition for application to the skin of a subject, the topical warming composition comprising: (i) vanillyl butyl ether; (ii) camphor; (iii) menthol; (iv) Zingiber officinale (ginger) root extract and (v) an emulgel base comprising at least one pharmaceutically acceptable excipient.

2. The topical warming composition of claim 1, wherein the emulgel base comprises (i) an oily phase comprising at least one oil, (ii) an aqueous phase comprising water and / or pharmaceutically acceptable water-soluble components, (iii) at least one emulsifier and (iv) at least one gelling agent.

3. The topical warming composition of claim 2, wherein the oily phase comprises a refined mineral oil, particularly liquid paraffin, mineral oils, vegetable oils, waxes, and butters, for example cacao butter.

4. The topical warming composition of claim 2 or 3, wherein the aqueous phase comprises water and propylene glycol.

5. The topical warming composition of any one of claims 2, 3 or 4, wherein the at least one emulsifier is ceteareth-20.

6. The topical warming composition of claim 5, wherein the at least one gelling agent is a carbomer, particularly Carbopol® 974P NF.

7. The topical warming composition of claim 6, further comprising at least one emollient selected from the group consisting of coco caprylocaprate, coco-caprylate, cococaprate, caprylic / capric triglyceride, jojoba oil, jojoba esters, isopropyl jojobate, ethyl macadamiate, isoamyl laurate, heptyl undecylenate, methylheptyl isostearate, isostearyl isostearate, glyceryl ricinoleate, isostearyl palmitate, myristyl myristate, octyldodecyl myristate, octyldodecyl hydroxystearate, butyl myristate, ethylhexyl cocoate, ethylhexyl palmitate, ethylhexyl stearate, butyl stearate, decyl oleate, isocetyl behenate, isocetyl myristate, isocetyl palmitate, isocetyl stearate, isodecyl oleate, isopropyl isostearate, isopropyl myristate, isopropyl palmitate, oleyl oleate, propylene glycol laurate, octyldodecyl erucate, C12-C13 alkyl lactate, C12-C15 alkyl lactate, isostearyl lactate, glycereth-5-lactate, lauryl lactate, myristyl lactate, oleyl lactate, laureth-2-benzoate, C12-C15 alkyl benzoate, C12-C15 pareth-3-benzoate, dipropylene70260W001 glycol benzoate, isodecyl salicylate, C12-C15 alkyl salicylate, tridecyl salicylate, ethylhexyl isononanoate, cetyl ethylhexanoate, isononyl isononanoate, isodecyl ethylhexanoate, isodecyl isononanoate, tridecyl ethylhexanoate, isotridecyl isononanoate, isostearyl isononanoate, cetearyl isononanoate, laureth-2-ethylhexanoate, cetearyl ethylhexanoate, isodecyl neopentanoate, isostearyl neopentanoate, nyristyl neopentanoate, isostearyl behenate, octyldodecyl neopentanoate, tridecyl neopentanoate, and combinations thereof.

8. The topical warming composition of claim 7, wherein the emollient is selected from the group consisting of coco-caprylate, coco-caprate, coco caprylocaprate and combinations thereof.

9. The topical warming composition of claim 8, further comprising (a) at least one oilsoluble antioxidant selected from the group consisting of butylated hydroxytoluene (BHT), ascorbyl palmitate and combinations thereof; and / or (b) at least one preservative is selected from the group consisting of benzalkonium chloride, benzethonium chloride, benzoic acid, benzyl alcohol, butylparaben, cetrimonium bromide, cetylpyridinium chloride, chlorobutanol, chlorocresol, cresol, dehydroacetic acid, ethylparaben, methylparaben, phenoxyethanol, phenylethyl alcohol, potassium benzoate, potassium sorbate, propylparaben, sodium benzoate, sodium dehydroacetate, sodium propionate and combinations thereof.

10. The topical warming composition of any one of claims 1 to 9 wherein at least 80% (w / w) of the topical warming composition comprises emulgel base.

11. The topical warming composition of claim 10, comprising (i) 0.1%-l% (w / w) vanillyl butyl ether; (ii) 0.5%-2% (w / w) camphor; (iii) 0.1%-l% (w / w) menthol and (iv) 0.1%-2% (w / w) Zingiber officinale (ginger) root extract.

12. The topical warming composition of claim 10 or 11 comprising, water, coco-caprylate or coco caprate, propylene glycol, ceteareth-20, liquid paraffin and carbomer.

13. The topical warming composition of claim 12, further comprising: phenoxyethanol, 1,2-hexanediol, caprylyl glycol, butylated hydroxytoluene (BHT), ascorbyl palmitate and sodium hydroxide.

14. A skin applicator comprising the topical warming composition of any one of claims 1 to 13, wherein the skin applicator comprises a dispenser or holder comprising the70260W001 topical warming composition, wherein the dispenser or holder is selected from a spray tube, roll-on, aerosol can or adhesive patch.

15. A method of preparing a topical warming composition according to claims 1 to 13, the method comprising the steps of: (i) dispersing the carbomer in water to create an aqueous phase, (ii) preparing a fatty phase by adding the other constituents to a vessel, (iii) combining the fatty phase with the aqueous phase, (iv) emulsifying the fatty phase in the aqueous phase to provide an emulsion, and (v) neutralising the emulsion with sodium hydroxide.

16. The topical warming composition of any one of claims 1 to 13 or the skin applicator of claim 14, for use in a method for warming the skin of a subject, the method comprising applying the topical warming composition to the skin of the subject.

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