JP7246926B2 - Multifunctional structured glycidic/non-glycidic matrix - Google Patents

Description

The present invention provides, in certain embodiments, skin and hair health benefits including improved skin and hair protection from environmental stress, increased moisturization, improved skin barrier function and/or hair conditioning. topical and hair care products, including stable, multifunctional skin cosmetic and conditioning ingredients as well as externally applied products (ie, final formulations).

Human skin is constantly under constant attack by environmental stressors--heat, cold, atmospheric and wind-borne pollutants, and ultraviolet radiation, among others--to repair and restore damage and maintain homeostasis, thereby rejuvenating the body. are protecting. It also does so through a series of inflammatory reactions that can have adverse effects on skin health. By destroying the skin's extracellular matrix proteins (collagen and elastin), inflammation can result in thinner, less elastic, wrinkled skin.

To combat environmental stress, formulators of personal care and skin products rely on safe and effective proven emollients and barrier protection ingredients - petroleum jelly and triglyceride fats, especially shea butter.

The use of petrolatum as an emollient to relieve dry skin conditions, including flaky skin, chapped skin, windburn and sunburn, has a long history of use in personal care and medical technology. See, for example, 43 Fed. Reg. 34628, 34639.

If petrolatum is the only moisturizing ingredient, moisturizing benefits typically require petroleum jelly to be included in the final formulation at a concentration of at least about 3% by weight of the formulation (3% plus petroleum jelly). do.

At certain use levels (30 percent or more), petrolatum has been documented in studies by the U.S. Food and Drug Administration to provide temporary protection against minor cuts, scrapes, and burns, as well as the effects of wind and cold dryness. Endorsed as a useful, over-the-counter (OTC) skin protectant. Additionally, when used in over-the-counter concentrations, petrolatum can help temporarily protect and relieve chapped or chapped skin and lips.

Various grades (ie, types) of petroleum jelly suitable for use in topical formulations are commercially available, including those manufactured by Sonneborn LLC (Parsippany, NJ). In cosmetic applications, petrolatum can be found at any use level up to 100% in skin care, body care and hair care for moisturizing, TEWL function, emollient and texturizing effects. Although petrolatum is an effective, economical, versatile, safe and inert emollient that is widely used in mass market products, it is not used as an anti-aging or natural/botanical based active skin care product in the market. Use for requests is limited. At the high use levels (30%) necessary for skin protectant claims described in the literature, petrolatum is less aesthetically appealing.

Plant-derived "fats" are triglyceride-based emollients used in topical products and typically have melting points in the range of 20-40.5°C. Fats are generally described as the fatty acid composition of the constituent triglycerides. A longer fatty acid chain length means a higher melting point and a higher degree of unsaturation means a lower melting point.

Vegetable fats have long been recognized and used for emollients and moisturizing in cosmetic and personal care applications. However, the use levels of vegetable fats in emulsions and anhydrous systems are often limited by their complex mixture of various fatty acids and their unique polymorphic crystallization behavior. Incorporating minimally refined, bleached and deodorized vegetable fat (i.e., "RBD" (refined, bleached and deodorized) fat) in the final formulation at higher concentrations (at least 2%) results in a granular emulsion. Structures or grayish formations - so-called "bloom" may occur. Further, when RBD vegetable fats are used in the final product at a concentration that provides meaningful functionality, although this concentration is at least 2%, the product may lose 1% in viscosity, color and/or gloss over time. May indicate changes in one or more. In many cases, emulsion products containing high levels of RBD vegetable fat, greater than 2%, are observed to segregate.

Mixtures of petrolatum and RBD plant-derived fats are similarly subject to additional formulation limitations, including instability and undesirable sensory properties. Prior to this invention, suitable petrolatum-based topical products could not be formulated with more than about 2 percent RBD vegetable fat; At concentrations of RBD shea butter exceeding Additionally, adding more than 2% wt/wt RBD vegetable fat to a 3%+ petrolatum formulation is known to cause gloss and/or discoloration.

Shea butter, like petrolatum, provides emollient and moisturizing properties and is used in a wide variety of personal care applications. See, for example, J. Alander "Shea butter with improved moisturisation properties" Personal Care (September 2009).

The unsaponifiable content of shea butter (as high as 7%-10%) has been shown to have anti-inflammatory, collagen protective/stimulatory, and fibroblast proliferation properties in both in vitro and ex vivo skin models. ing. See also Id.; A-C Anderson, "Protection against stress by natural triterpene esters" Personal Care (June 2011).

Triterpene esters account for 2% to 5% of RBD shea butter. Triterpene Esters in Shea Butter Reduce Skin Extracellular Matrix Proteins (Collagen and Elastin) from Stress-Related Damage, Reduce Expression of Matrix Metalloproteinases or PGE2, TNF-α and IL in 3%+Vaseline Formulations To have clinically meaningful effects, such as protection by inhibiting the release of pro-inflammatory mediators such as -1β, shea butter must be present in concentrations of at least about 2%. , which is generally the level that causes bloom, graininess, discoloration, or other organoleptic defects.

Transesterified unfractionated vegetable fats, especially shea butter, are known to be superior to their RBD counterparts in several respects. First, transesterification raises the melting point of shea butter by almost 20° C. (from 33° C. (for RBD) to 51° C. (for transesterified unfractionated). The unfractionated shea butter crystallizes more rapidly (in less than 24 hours) than its RBD counterpart, which takes 5-7 days.Third, at higher temperatures, the transesterified unfractionated shea butter retains more of its solids content than RBD shea butter.

WO 2006/037341 discloses a low lauric acid, low trans fat cocoa butter substitute that is useful in food and other applications. The composition in WO2006/037341 is a particular type of transesterified fractionated fat with a low melting fat fraction with a final melting point approximately below body temperature and a steep SFC-melting profile. (As used in this application, the term "body temperature" is understood to be about 37°C.) Comparative Example 7 in WO2006/037341 lists two lip balm formulations. there is Both formulations of Example 7 contain 55% white petrolatum and are identical except for the triglyceride component. The first formulation of Example 7, "Test Composition," is made from the low-melting, transesterified, fractionated 6% triglycerides just described. A second formulation, the "reference composition", is made from 6% Illexao 30-61, palm glycerides with a melting point of 34°C.

In marked contrast to the formulation of Example 7 of WO2006/037341, the compositions of certain embodiments of the present invention have a final melting point above or significantly above body temperature (e.g., 51°C), in addition to Made from transesterified unfractionated triglyceride components with a very slow (ie flat) SFC-melting profile. By "significantly above body temperature" is meant a temperature that is at least 10%, at least 20%, or at least 25% above body temperature. The physical properties of a melting point above or significantly above body temperature and a very slow (i.e. flat) SFC-melting profile provide excellent skin barrier protection and moisturization as measured by TEWL (i.e. reduce transepidermal water loss). It is central to achieving inventive properties of certain embodiments of the present invention, such as achieving a long-lasting protective coating on the hair.

The Illexao 30-61 palm triglycerides used in Example 7 of WO 2006/037341 and the transesterified unfractionated shea butter used in certain embodiments of the invention are additional features to the claims of the invention. Differs in terms of importance. Ilexao 30-61 contains less than about 1% unsaponifiables and therefore a very low content of functional triterpene esters. The transesterified unfractionated shea butter used in certain embodiments of the present invention has an unsaponifiable content of about 7% to about 10%. This level of unsaponifiables, triterpene esters, is present in amounts that provide anti-inflammatory, collagen protection/stimulation, and fibroblast proliferation and other skin health benefits.

Together, the above properties make the transesterified unfractionated shea butter, a component of certain embodiments of the present invention, more crystalline and thermally stable than its RBD counterpart. For example, when a final formulation containing certain transesterified unfractionated shea butter of the present invention is exposed to temperatures high enough to melt its crystals (e.g., during storage), the product , the crystals should reach a stable form (converted to the β-polymorph) within 24 hours when subjected to colder conditions where they should recrystallize. In contrast, RBD shea butter crystals begin to melt not only at a lower temperature but more rapidly than crystals of transesterified unfractionated shea butter. Furthermore, if the crystals of RBD shea butter begin to recrystallize, a fairly long period of time (5-7 days) is required to stabilize as the β-polymorph.

In summary, a functional critical concentration, e.g. There is a long-existing and unmet commercial need for stable, cosmetically elegant (i.e., non-greasy), 3%+ petroleum jelly-based products that can incorporate triglyceride-based fats of exists within the care industry. This need clearly exists for petrolatum-based products containing 30% or more petrolatum (meeting over-the-counter literature requirements for "skin protectants"); at least 2% functional Demonstrated by the lack of commercially available formulations made according to over-the-counter "skin protectants" (with more than 30% petroleum jelly) that also contain triglyceride-based plant-derived fats at upper limit concentrations. . The multifunctional structured glycidic/non-glycidic matrix of certain embodiments of the present invention overcomes physical instability and a functional threshold concentration of at least 2% triglyceride-based plant-derived It meets these needs by removing the TEWL performance degradation expected to be present in fat-incorporated, 3%+Vaseline-based products.

In one aspect, the present invention provides a topical product comprising (i) at least one triglyceride and (ii) at least one petrolatum, wherein at least 2% triglyceride and at least 6% petrolatum on a weight/weight basis. A topical application product containing

In other embodiments, the topical product does not exhibit graininess, bloom, discoloration, or separation, or change in viscosity over time.

In still other embodiments, the triglycerides are transesterified and non-fractionated.

In other embodiments, the triglycerides are transesterified and have a final melting point at or significantly above body temperature. In this embodiment, the transesterified triglyceride having a final melting point above or significantly above body temperature may be fractionated or unfractionated.

In certain embodiments, at least one triglyceride may be a combination of two (or more) transesterified fractions from one (or more) triglycerides, wherein said fractions Some or all of the minutes can be recombined.

In other embodiments, the triglycerides are transesterified, non-fractionated, and have a final melting point above or significantly above body temperature.

In still other embodiments, the triglycerides are transesterified, unfractionated, and include Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed Butter, Shorea Stenoptera Seed Butter. (Shorea Stenoptera (Illipe) Seed Butter), Astrocaryum Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Mangnifera Indica (Mango) Seed Butter selected from the group consisting of

In still other embodiments, the at least one transesterified unfractionated triglyceride is Butyrospermum Parkii (Shea) Butter.

Still other embodiments comprise at least 30% petrolatum and at least one transesterified unfractionated triglyceride, wherein the ratio of at least one transesterified unfractionated triglyceride to at least one petrolatum is 1: 39-7:13.

Still other embodiments comprise at least 30% petroleum jelly and at least one transesterified triglyceride having a final melting point above or significantly above body temperature, at least one having a final melting point above or significantly above body temperature. of transesterified triglycerides to at least one petrolatum is from 1:39 to 7:13.

Still other embodiments comprise at least 30% petrolatum and at least one transesterified unfractionated triglyceride, wherein the ratio of at least one transesterified unfractionated triglyceride to at least one petrolatum is 1: 19-1:3.

Still other embodiments comprise at least 30% petroleum jelly and at least one transesterified triglyceride having a final melting point above or significantly above body temperature, at least one having a final melting point above or significantly above body temperature. of the transesterified triglyceride to the at least one petrolatum is from 1:19 to 1:3.

Another aspect of the present invention is used in the manufacture of cosmetic, personal care and/or dermatological products comprising (i) at least one transesterified unfractionated triglyceride and (ii) at least one petrolatum. related to multifunctional chemical components.

Another aspect of the present invention is a cosmetic, personal care product, and comprising (i) at least one transesterified triglyceride having a final melting point above or significantly above body temperature and (ii) at least one petrolatum. / Or to multifunctional chemical ingredients used in the manufacture of dermatological products.

In other embodiments, the cosmetic, personal care, and/or dermatological product has a ratio of at least one transesterified unfractionated triglyceride to at least one petrolatum of 1:39 to 7:13. Consists of multifunctional chemical components.

In other embodiments, the cosmetic, personal care, and/or dermatological product has a ratio of at least one transesterified triglyceride having a final melting point above or significantly above body temperature to at least one petrolatum of 1. :39-7:13.

In still other embodiments, the cosmetic, personal care, and/or dermatological product has a ratio of at least one transesterified unfractionated triglyceride to at least one petroleum jelly from 1:19 to 1:3. , consisting of multifunctional chemical components.

In still other embodiments, the cosmetic, personal care, and/or dermatological product has a ratio of at least one transesterified triglyceride to at least one petroleum jelly that has a final melting point above body temperature or significantly above body temperature. It consists of multifunctional chemical components with a ratio of 1:19 to 1:3.

In still other embodiments, the cosmetic, personal care, and/or dermatological product is characterized in that the transesterified unfractionated triglycerides include Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed. Butter), Shorea Stenoptera (Illipe) Seed Butter, Astrocaryum Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Mango Seed Butter ( Mangnifera Indica (Mango) Seed Butter).

In other embodiments, the source of the transesterified, unfractionated triglyceride component of the cosmetic, personal care, and/or dermatological product is Shea butter (Butyrospermum Parkii (Shea) Butter).

Another aspect of the present invention is a skin beauty product comprising (i) at least one triglyceride and (ii) at least one petrolatum, wherein (a) at least 2% triglyceride and at least 6% triglyceride on a weight/weight basis. % petroleum jelly and (b) does not exhibit graininess, bloom, discoloration, separation, or change in viscosity over time. In certain such embodiments, at least one triglyceride is non-fractionated and/or has a final melting point above or significantly above body temperature.

Another aspect of the invention comprises, consists essentially of (i) at least one transesterified unfractionated triglyceride and (ii) at least one petrolatum and (iii) an optional active ingredient, or It relates to topical products consisting of them.

Another aspect of the invention comprises (i) at least one transesterified triglyceride having a final melting point above or significantly above body temperature and (ii) at least one petrolatum and (iii) an optional active ingredient. , to topical products consisting essentially of or consisting of them.

Accordingly, the present invention provides one (or more) transesterified unfractionated triglycerides and a moisturizing effective amount of one (or more) petroleum jelly, more preferably in the range of about 7:13 to about 1:39. used in the manufacture of cosmetic, personal care, and dermatological products, as well as topical formulations containing matrices, consisting of or consisting essentially of a ratio of transesterified, unfractionated triglycerides to petrolatum of It further relates to a multifunctional chemical entity that Other embodiments comprise one (or more) transesterified triglycerides having a final melting point above body temperature or significantly above body temperature and a moisturizing effective amount of one (or more) petroleum jelly, more preferably about Cosmetics, personal care products consisting of or consisting essentially of a ratio of transesterified triglycerides to petrolatum having a final melting point above or significantly above body temperature ranging from 7:13 to about 1:39, and dermatological products, as well as multifunctional chemical ingredients used in the manufacture of matrix-containing topical formulations. In topical formulations, the moisturizing effective amount of one (or more) petrolatum is at least about 3%, preferably at least about 5%, and more preferably at least about 30%, by weight of the formulation. In a preferred embodiment, the multifunctional chemical component is present in the final formulation in an amount such that transesterified unfractionated triglycerides or triglycerides with a final melting point above or significantly above body temperature are at least 2% by weight of the formulation. exist within. In a particularly preferred embodiment, the transesterified unfractionated triglycerides are Shea butter (Butyrospermum Parkii (Shea) Butter), Cocoa butter (Theobroma Cacao (Cocoa) Seed Butter) and Shorea Stenoptera (Illipe) Seed butter. Butter).

1 is a melting profile curve of a topical application product according to the present invention which is a mixture of 25% transesterified unfractionated shea butter and 75% petrolatum. Fig. 3 is a melting profile curve of a topical application product according to the present invention, which is a mixture of 25% RBD shea butter and 75% petrolatum; Fig. 4 is a melting profile curve of petrolatum; FIG. 4 is a combination of melting profile curves from FIGS. 1-3. FIG.

DEFINITIONS "Cosmetic for skin" refers to mammalian skin (epidermis, dermis, subcutaneous tissue) or other keratinous tissue [i.e. hair (including hair follicles, roots and bulbs) and nails (i.e. ventral epithelial layer of the body)], as well as suitable for inclusion in cosmetic, personal care or dermatological products for topical application on the sebaceous and sweat glands (eccrine and apocrine glands), Skin cosmetics are intended to improve the condition and/or appearance of the skin, keratinous tissue, or sebaceous/sweat glands, or to provide skin health benefits.

"Topical" means the surface of skin, other keratinous tissue, or sebaceous and sweat glands.

"Skin health benefit" means regulating and/or improving the condition of the skin, non-limiting examples of which include improving the hydration status or moisturizing of the skin; improving the barrier function of the skin improving skin appearance by reducing the appearance of one or more of fine lines and/or wrinkles, discoloration, redness or blemishes; imparting a more even skin tone; increasing skin elasticity, elasticity or firmness; Improving skin feel and texture by increasing smoothness or softness; reducing levels of inflammation; reducing degradation of extracellular skin matrix proteins; increasing quantity and quality of extracellular skin matrix proteins; Or include increasing the thickness of multiple layers.

"Skin beauty products" (also referred to herein as "finished products") include, but are not limited to, creams, moisturizers, lotions, ointments, gels, serums, tinted cosmetics ( foundations, blushes, lipsticks/lip glosses, eye shadows, concealers), masks, and cleansers and toners, including prescription and non-prescription drugs, which contain one or more active ingredients. It's okay.

“Interesterified non-fractionated triglycerides” are converted by “interesterification,” a process involving the exchange of acyl groups between (i) a triacylglycerol ester and an acid or (ii) a triacylglycerol ester and an alcohol. It means an ester formed from glycerin and three fatty acid radicals, both unfractionated and unfractionated. The exchange may be within the same triacylglycerol ester or between a triacylglycerol ester and a second ester, including another triacylglycerol ester. Transesterification is performed by techniques well known in the art to change the physical properties (molecular packing and melting point) of triglycerides, resulting in more stable crystalline forms.

"Vaseline" means a refined mixture of semi-solid hydrocarbons obtained from petroleum. In certain embodiments, petrolatum contains mineral oil, microcrystalline and paraffin wax components and is further defined with reference to the following properties: 0.815 to 0.815 according to United States Pharmacopeia (“USP”) Physical Test 841 specific gravity of 0.880 (at 60° C.); dropping melting point of 38.0-75.0° C. according to ASTM International Standard D127; consistency between 10-300 dmm (1/10 of 1 mm=1 dmm) according to ASTM International Standard D937.

The term "petroleum jelly", in certain embodiments, also includes petroleum oils (oily liquids or tar-like hydrocarbon materials from solid mineral sources), petroleum waxes (microcrystalline or paraffinic), or petroleum oils produced from non-petroleum sources. Petrolatum is understood to have the following properties: specific gravity of 0.815 to 0.880 (at 60° C.) according to United States Pharmacopeia (“USP”) Physical Test 841; ASTM International Standard Drop melting point of 38.0-75.0° C. according to D127; Consistency between 10-300 dmm (1/10 of 1 mm=1 dmm) according to ASTM International Standard D937.

The multifunctional chemical entity of the present invention is also described in this application as a "multifunctional structured glycidic/non-glycidic matrix" (referred to by the acronym "MFSG/NGM"), (i a) petroleum jelly and (ii) a transesterified triglyceride that is unfractionated and/or has a final melting point above or significantly above body temperature. . In certain embodiments, the component is described as a "structured glycidic/non-glycidic matrix." This is because the crystalline component of the transesterified unfractionated triglycerides is oriented in a lower energy, more stable configuration relative to petrolatum than the system composed of non-interesterified triglycerides and petroleum jelly ( ie, "filled"). The properties of the structured glycidic/non-glycidic matrix are one or more known in the art, including but not limited to X-ray diffraction, differential scanning calorimetry (DSC), and scanning electron microscopy. can be described in more detail based on the analytical method of

In certain embodiments, petrolatum in MFSG/NGM meets all current USP and FDA requirements (21 CFR Section 172.880).

In certain embodiments of the invention, the petrolatum portion comprises USP grade white petrolatum, a refined mixture of semi-solid hydrocarbons obtained from petroleum that has been completely or substantially decoloured and may contain stabilizers. .

In a preferred embodiment, the petrolatum portion has the following physical properties: specific gravity at 60° C. according to USP 841 of 0.815-0.880; drop melting point according to ASTM D127 between 51.6-60.0° C.; Consistency by ASTM D937 between 170-200 dmm; viscosity by ASTM D445/D2161 between 40.0-50.0 SUS at 210°F; and less than 1.0 yellow, measured according to British Petroleum Institute standard method IP 17 Lovibond® colors.

In certain preferred embodiments, the multifunctional structured glycidic/non-glycidic matrix is present in the final product at a concentration such that the total petrolatum content is at least 30% on a weight/weight basis of the final product. .

In a preferred embodiment, the transesterified unfractionated triglycerides are Shea butter (Butyrospermum Parkii (Shea) Butter), Cocoa butter (Theobroma Cacao (Cocoa) Seed Butter), Shorea Stenoptera (Illipe) Seed Butter ), Astrocaryum Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Mangnifera Indica (Mango) Seed Butter. (Interesterified shea butter, cocoa butter and illipe butter are available from AAK Sweeden AB and AAK USA Inc. as LIPEX® Sheasoft, LIPEX® Cocoasoft, and LIPEX® Illipesoft. ) The melting point of Lipex Sheasoft® is about 51°C. The slope of the solid fat content (SFC)-melting profile of LIPEX® Sheasoft from 20° C. to 35° C. is less than 1, where the percent change in SFC is plotted on the y-axis and temperature is plotted on the x-axis. are doing.

In a more preferred embodiment, the transesterified unfractionated triglycerides are Shea Butter (Butyrospermum Parkii (Shea) Butter), Cocoa Butter (Theobroma Cacao (Cocoa) Seed Butter), and Shorea Stenoptera (Illipe) Seed Butter. Seed Butter).

In one particularly preferred embodiment, the transesterified unfractionated triglyceride is shea butter having about 7% to about 10% unsaponifiables.

The unsaponifiable fraction of transesterified unfractionated shea butter consists of hydrocarbons of triterpene esters and highly unsaturated isoprenoids. Among the triterpene esters are the cinnamic acid and acetate esters of α- and β-amyrin, butyrospermol, lupeol, and parqueol.

In particularly preferred embodiments, the transesterified unfractionated shea butter contains at least about 2% triterpene esters; % triterpene esters; in even more preferred embodiments contain greater than about 5% triterpene esters.

In a first non-limiting aspect of the present invention, a petrolatum component and an transesterified non-fractionated ester component are combined to produce a multifunctional structured glycid/non-glycid that is heat stable compared to petrolatum. form a matrix. "Heat stable" means that the solid fat content (SFC) of the MFSG/NGM of the present invention is within about 3% of the SFC of petrolatum at the same temperature. Comparing the areas under the respective melting profile curves between 20° C. and 45° C. for the two materials, the MFSG/NGM embodiments of the present invention show within about 1 percent (1.3%) It is further shown to be equally thermally stable to The area under the melting profile curve for petroleum jelly (20° C.-45° C.) is 137; is 138.8. In contrast, the area under the melting profile curve for a blend of 25% non-interesterified (i.e., RBD) shea butter and 75% petroleum jelly was 101.62; 82%).

Table 1 below shows the SFC and under curve between temperatures ranging from 20°C to 45°C for a topical product according to the present invention, which is a mixture of 25% transesterified unfractionated shea butter and 75% petroleum jelly. represents area.

Table 2 below presents the SFC and area under the curve between temperatures ranging from 20°C to 45°C for a topical product according to the present invention, which is a mixture of 25% RBD shea butter and 75% petrolatum.

Table 3 below shows the melting profile curves of pure petrolatum.

The area under curve calculation above demonstrates the difference in solid fat content between two different otherwise equivalent blends of shea butter and petrolatum.

In a preferred embodiment of the first aspect of the invention, the heat-stable MFSG/NGM is one or more transesterified unfractionated triglycerides and petrolatum in the following ratios: 1:39; 1:38; 1:37; 1:36; 1:35; 1:34; 1:33; 1:1:32; 1:31; 1:25; 1:24; 1:23; 1:22; 1:21; 1:20; 1:19; 1:18; 1:10; 1:9; 1:8; 1:7; 1:6; 1:5; 1:4; 1:3; is a homogeneous mixture of the two components of

In a preferred embodiment of the first aspect of the invention, the transesterified unfractionated triglycerides are from about 2% to about 50% by weight of heat stable MFSG/NGM, about 2% by weight of heat stable MFSG/NGM. present at a concentration of from about 5% to about 35% by weight, from about 5% to about 25% by weight of the thermally stable MFSG/NGM, or from about 10% to about 20% by weight of the thermally stable MFSG/NGM; do.

In a more preferred embodiment of the first aspect of the invention, the transesterified non-fractionated triglycerides are at least 10% by weight of the heat stable MFSG/NGM, but not more than 35% by weight of the heat stable MFSG/NGM. be.

In one highly preferred embodiment of the first aspect of the present invention, the transesterified unfractionated triglyceride is shea butter, the shea butter being greater than 2% by weight of heat stable MFSG/NGM, more preferably 2% present in concentrations greater than .5% by weight but less than 35% by weight.

Thermally stable MFSG/NGM embodiments are "multifunctional" and provide multiple skin health benefits (as defined above).

In certain embodiments of the invention, the MFSG/NGM of the invention exhibits physical and organoleptic properties substantially equivalent to "pure" petrolatum (i.e., petrolatum without the addition of transesterified, unfractionated shea butter). However, it is surprising that 4 hours after application to the skin, the MFSG/NGM of the present invention provides a reduction in transepidermal water loss and a significant improvement in skin barrier function over pure petrolatum. is unexpectedly found in

The phrase "physical organoleptic properties substantially equivalent to 'pure' petrolatum" means that when pure petrolatum is assigned a score of 3 in a sensory panel test measuring seven parameters on a scale of 0-5: Meaning less than 5% difference from pure petrolatum. The seven parameters are spreadability; greasiness; softness; stickiness; absorbency; gloss; and graininess.

A second non-limiting aspect of the present invention is directed to a multifunctional skin barrier protective skin beauty product comprising MFSG/NGM as described in the first aspect of the present invention, wherein the product comprises: Separation or bloom, graininess (sometimes referred to as "graininess") or product set as perceived by a trained observer/technician or by analytical techniques using instruments well known to those skilled in the art It shows no perceptible change in viscosity during shelf life.

"Bloom" occurs when two crystalline materials are mixed to form an unstable crystal. Bloom is visible to the naked eye and can appear as a coating on the surface of the product.

"Graininess" is the tactile quality that can be perceived when a product is applied (eg, rubbed) on the skin.

Changes in viscosity are measured instrumentally. The viscosity of the product is measured with the same type of viscometer (e.g. Brookfield RVT) consisting of the same type of spindle (spindle number 4) with the same rotational speed (RPM) as specified in the certificate of analysis for the product. Measured in

For skin beauty products that are emulsions containing the MFSG/NGM of the present invention, stability (ie, not separating into oil and water phases) can be assessed as follows. Fill the product into glass jars, preferably the final package (ie, the package in which the product is intended to be sold to consumers). The filled containers (glass jars and final packages) are stored at various temperatures under various light conditions for various lengths of time. Temperatures include 50°C, 45°C, 37°C, 25°C (often described in the art as "room temperature") and 4°C. Various lighting conditions may include fluorescent light and light emitted from a solar simulator, a device that provides illumination close to that of natural sunlight. Preferably, the solar simulator is calibrated and operated according to the standards set forth in the following standards: ASTM E927-10 (2015) published by ASTM International (West Conshohocken, Pennsylvania); Standard IEC 60904-9, 2nd Edition, published by IEC, Inc., Switzerland. If the product is a sunscreen, the solar simulator complies with the latest standards promulgated by the applicable governmental or industrial body: for the United States, the Food and Drug Administration; for Europe, the European Cosmetics Association (COLIPA); , Japan Cosmetic Industry Association (JCIA). Samples can preferably be evaluated at the following time intervals: 2 weeks, 4 weeks, 8 weeks, 12 weeks. Additionally, samples stored at 25°C, 37°C and 4°C evaluations are evaluated after one year. The highest temperature and illuminated samples are preferably evaluated in the first three test intervals. Prior to testing, samples are preferably kept at room temperature for about 8 hours to equilibrate.

The emulsion separation embodiment of the present invention can occur over a period of days or weeks. The appearance of bloom or color change (discoloration) or the development of a sandy or grainy texture can likewise occur over a period of days or weeks.

A third non-limiting aspect of the present invention is the bloom, graininess or perceptible viscosity perceived by a trained observer/technician or instrumentally using analytical techniques well known to those skilled in the art. A multifunctional skin barrier protective skin beauty product that does not show a change in the product during the set shelf life of the product, comprising a moisturizing amount of petroleum jelly, e.g. at least 3% by weight of the product; preferably at least 5% by weight of the product even more preferably at least 10% by weight of the product; even more preferably at least 30% by weight of the product, and a concentration of one (or combination of) triglyceride fats of at least 2%. In preferred embodiments, the triglyceride fat is transesterified and unfractionated.

In one preferred embodiment of the third aspect of the present invention, the skin beauty product comprises (i) at least 2%, preferably at least 5%, and even more preferably at least 10% of transesterified unfractionated triglycerides and (ii) consists of at least 5%, preferably at least 10%, and even more preferably at least 30% petrolatum; A particularly preferred transesterified unfractionated triglyceride is shea butter.

The topical products or formulations containing MFSG/NGM of the present invention may also be used in a wide variety of applications, including prescription active and non-prescription pharmaceuticals for the skin, for the purpose of delivering skin health benefits as well as systemically through the skin. It may contain additional ingredients and function as a "topical delivery system" to deposit various cosmetic and dermatological ingredients. The International Cosmetic Ingredient Dictionary and Handbook published by the Personal Care Products Council and the United States Pharmacopoeia lists a large number of ingredients that can be delivered (i.e. formulated) from the topical delivery system of the present invention. An extensive list of ingredients is described, non-limiting examples of which are listed below.

In certain embodiments, the topical delivery system itself is understood to be the final product.

The term "non-prescription" includes ingredients that are generally recognized as safe and active under applicable over-the-counter drug dossiers issued by the U.S. Food and Drug Administration ("FDA") is understood. "Prescription" drugs include drugs that require approval from the FDA or a comparable agency outside the United States responsible for regulating drug activity.

Both steroidal and non-steroidal anti-inflammatory agents may be incorporated and provided in the compositions of the invention. Non-limiting examples of anti-inflammatory agents are listed below with the corresponding doses indicated in brackets: alclomethasone dipropionate (0.05%); amcinonide (0.1%); betamethasone dipropione. acid ester (0.05%); betamethasone valerate (0.01%); clobetasol propionate (0.05%); crocortolone pivalate (0.1%); desoxymethasone (0.05%) ); desonide (0.05%); diflorazone diacetate (0.05%); diflorazone diacetate (0.25%); fluocinonide (0.05%); Fluoranenolide (0.05%); Fluticasone (0.05%); Fluticasone Propionate (0.005%); Halbetasol Propionate (0.05%); hydrocortisone valerate (0.1%); hydrocortisone butyrate (0.1%); hydrocortisone valerate (0.2%); mometasone furoate (0.1%); %); mometasone furoate (0.1%); predonicarbate (0.025%); triamcinolone acetonide (0.5%).

Antipruritics known to those of skill in the art, including those listed below, may be delivered to the skin in topical products comprising the topical delivery system of the present invention. Non-limiting examples of antipruritic agents include doxepin and pramoxine.

The compositions of the present invention may be used alone (ie, blends of transesterified triglycerides and petroleum jelly without additional active ingredients) to treat diaper dermatitis. In certain embodiments of the invention, these compositions include, but are not limited to, antifungal agents (preferably nystatin cream; clotrimazole; econazole nitrate; miconazole; or amphotericin) or anti-inflammatory agents ( It can serve as a delivery system for one or more active ingredients useful in treating diaper dermatitis, including preferably hydrocortisone).

Compositions of the present invention may be used alone or to treat hemorrhoids, including one or more topical analgesics, anti-inflammatory agents and/or antipruritic agents (each of which is described in more detail elsewhere in this application). can serve as a delivery system for one or more active ingredients useful in the treatment of

alpha-hydroxy acids (AHA as defined below); azelaic acid; benzoyl peroxide; cimetidine; clindamycin; can be used to provide dermatological ingredients useful in the treatment of acne, including tretinoin.

Suitable active agents, hydrophilic hydroxycarboxylic acids, for use in the compositions of the present invention include alpha-hydroxy acids (AHA) and polyhydroxy acids (PHA). AHA has 1 to 29 carbon atoms and has the structure (R1)(R2)C(OH)COOH, wherein R1 and R2 are selected from the group consisting of hydrogen, alkyl, aralkyl and aryl groups, wherein , the alkyl, aralkyl and aryl groups may be saturated or unsaturated, isomeric or non-isomeric, straight or branched chain or cyclic, and the alkyl, aralkyl and aryl groups may be substituted with the substituents OH, CHO, COOH and an alkoxy group having 1 to 9 carbon atoms).

The term "AHA" includes not only the free acid, but also the corresponding ester (formed by the reaction of AHA with an alcohol), its corresponding lactone (formed by the reaction of the carboxylic acid group of AHA with the hydroxyl group). ), as well as its corresponding salts (formed by reaction of AHA with an organic base or inorganic alkali). R1 and R2 may be the same or different. In the latter case, AHA may be the D, L, and DL stereoisomers. AHAs suitable for use in the present invention can be classified as (i) alkyl AHAs, (ii) aralkyl and aryl AHAs, (iii) polyhydroxy AHAs, and (iv) polycarboxylic acid AHAs.

Among the preferred hydrophilic hydroxycarboxylic acids are (a) 2-hydroxyethanoic acid (glycolic acid, hydroxyacetic acid) and 2-hydroxypropanoic acid (lactic acid); and 2-hydroxybutane-1,4-dioic acid (malic acid 2-phenyl 2-hydroxyethanoic acid (mandelic acid); 2,3-hydroxybutane-1,4-dioic acid (tartaric acid); and 2-hydroxy-2-carboxypentane-1,5-dioic acid (citric acid). acid). Other preferred polyhydroxy acids include gluconolactone and lactobionic acid.

Hydrophilic hydroxycarboxylic acids are added to the present invention at concentrations ranging from about 0.1% to about 6%, preferably from about 0.2% to about 4%, and more preferably from about 0.5% to about 3%. may be used for the delivery system of

Hydrophobic hydroxycarboxylic acids, including o-hydroxybenzoic acid (salicylic acid), may also be delivered to the skin in the topical delivery systems of the present invention, preferably at concentrations of at least about 0.5%.

The topical delivery system of the present invention can include one or more active ingredients that are useful for treating warts, including but not limited to salicylic acid.

The topical delivery systems of the present invention are useful in treating various types of rosacea, including erythematotelangiectatic rosacea, papulopustular rosacea, nematode rosacea, and ocular rosacea. It can contain one or more active ingredients. Non-limiting examples of such ingredients include: azelaic acid; benzoyl peroxide; clindamycin; doxycycline or minocycline; erythromycin; tacrolimus; tetracycline; tretinoin.

Other skin conditions, including psoriasis, eczema, contact dermatitis, atopic dermatitis and seborrheic dermatitis, can be treated with topical products containing the delivery system of the present invention and at least one anti-inflammatory or antipruritic ingredient. may be treated by applying to itchy/irritated skin.

Another aspect of the present invention is directed to topical delivery of active ingredients useful for treating erythema multiforme. Active ingredients include the steroidal and non-steroidal anti-inflammatory drugs listed above.

One or more sunscreen agents, active ingredients that absorb, block or attenuate ultraviolet radiation may be included in the delivery system of the present invention.

Benign photodamage manifesting as hyperpigmentation is treated by using the topical delivery system of the present invention to deposit one or more of the following lightening (also known as bleaching) ingredients on the skin: May also be: hydroquinone, kojic acid, glycolic acid and other alpha-hydroxy acids, ascorbic acid, magnesium ascorbyl phosphate, ascorbyl glucosamine and altocarpine.

The compositions of the present invention are useful in the treatment of alopecia areata and androgenic alopecia and otherwise provide scalp components that reduce hair loss, stop hair loss or promote hair growth stimulation. may be used for Scalp ingredients include, but are not limited to: 5-α-reductase inhibitors and flutamide, cyproterone and spironolactone; cimetidine; finasteride; and other antiandrogenic compounds such as minoxidil.

The delivery system of the present invention may also include one or more depilatory ingredients including, but not limited to, thioglycollate.

The compositions of the invention are also used to treat cancerous and precancerous conditions associated with exposure to ultraviolet radiation, including actinic keratosis; basal cell carcinoma; squamous cell carcinoma; melanoma. may be used to deliver therapeutically effective amounts of pharmaceutical ingredients. Non-limiting examples of pharmaceutical ingredients useful for treating actinic keratosis that may be included in the topical delivery systems of the present invention include: Acitretin; Adapalene; In combination with hyaluronic acid. Fluorouracil; and imiquimod.

The present application is also directed to the topical delivery of active ingredients known to those skilled in the art to promote wound healing, non-limiting examples of which include a combination with one or more topical antioxidants. One or more topical antiseptics or antibiotics are included. Non-limiting examples of such ingredients include vitamin K and silver particles.

Compositions of the present invention may also include, but are not limited to, corticosteroids, lidocaine, benzocaine, prilocaine, dibucaine, tetracaine, butamben, pramoxine, benzyl alcohol, menthol, oil of wintergreen, eucalyptus oil, capsaicin, trolamine saliva. It may also be used to deliver topical analgesics, including chillates, and mixtures thereof.

Another aspect of the present invention is directed to topical antifungal and antibacterial agents known to those of ordinary skill in the art, including those listed below, which are used in topical products containing the compositions of the present invention. may be delivered to the skin with Non-limiting examples of antibacterial and antifungal agents suitable for use in the present invention include: beta-lactams, quinolones, ciprofloxacin, norfloxacin, tetracyclines, erythromycin, amikacin, 2,4,4'-trichloro-2'-hydroxydiphenyl ether, 3,4,4'-trichlorovanillide, phenoxyethanol, phenoxypropanol, phenoxyisopropanol, doxycycline, capreomycin, chlorhexidine, chlortetracycline, oxytetracycline, lindamycin, ethambutol, hexamidine isethionate, metronidazole, pentamidine, gentamicin, kanamycin, lincomycin, metacycline, methenamine, minocycline, neomycin, netilmicin, paromomycin, streptomycin, tobramycin, miconazole, tetracycline hydrochloride, erythromycin, zinc erythromycin, Erythromycin Estolate, Erythromycin Sterate, Amikacin Sulfate, Doxycycline Hydrochloride, Capreomycin Sulfate, Chlorhexidine Gluconate, Chlorhexidine Hydrochloride, Chlortetracycline Hydrochloride, Oxytetracycline Hydrochloride, Clindamycin Hydrochloride, Ethambutol Hydrochloride, Metronidazole Hydrochloride, Pentamidine Hydrochloride, Gentamicin Sulfate, Kanamycin Sulfate, Lineomycin Hydrochloride, Methacycline Hydrochloride, Methenamine Hippurate, Methenamine Mandelate, Minocycline Hydrochloride, Neomycin Sulfate, Netilmicin Sulfate, Paromomycin Sulfate salts, streptomycin sulfate, tobramycin sulfate, miconazole hydrochloride, ketaconazole, amantadine hydrochloride, amantadine sulfate, octopirox, parachlorometaxylenol, nystatin, tolnaftate, zinc pyrithione and clotrimazole.

The compositions of the present invention may also be used to deliver drugs that control cellulitis, including xanthine compounds such as caffeine, theophylline, theobromine, and aminophylline.

Non-limiting examples of antioxidants/radical scavengers that may be topically delivered in the present invention include retinol, retinal, _C2 - _C22 alkyl esters of retinol (e.g., retinyl palmitate, retinyl acetate, retinyl propionate) and/or retinoic acid; ascorbic acid (vitamin C) and its salts; ascorbyl esters of fatty acids, ascorbyl acid derivatives (e.g. magnesium ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl sorbate) tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other esters of tocopherol; butylated hydroxybenzoic acid and its salts; 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid gallic acid and its alkyl esters, especially propyl gallate; uric acid and its salts and alkyl esters; sorbic acid and its salts; lipoic acid; amines (e.g. N,N-diethylhydroxylamine, amino-guanidine); glutathione); coenzyme Q10 and its analogues, including without limitation idebenone; dihydroxyfumaric acid and its salts; lysinepidolate; silymarin; tea extract; grape skin/seed extract; melanin; and rosemary extract. Included are retinol-like compounds that have the biological activity of A, as well as geometric and stereoisomers of these compounds.

Non-limiting examples of skin soothing and/or healing agents suitable for use in the present invention include: panthenol and derivatives, synlocai and its derivatives, pantothenic acid and its derivatives, Allantoin, bisabolol, and dipotassium glycyrrhizinate.

Steroidal reproductive agents can also be provided in the compositions of the present invention, non-limiting examples of reproductive agents include: androstenediol and androisoxazole ( for anabolic disorders), testosterone (hypogonadism, muscle wasting, impotence in males, postmenopausal symptoms in females), dihydrotestosterone (hypogonadism, muscle wasting), dehydroepiandrosterone (muscle wasting, fat loss, strength) ) androgens such as; Estrogens (postmenopausal symptoms, birth control) such as , ethinylestradiol, estrone; e.g. progesterone (pregna-4-ene-3,20-dione), norethindrone, norgestrieone, norgestadienone , norgestrel, norgestimate, progestogenic acid, dihydroprogesterol, nomagesterol (prevention of endometriosis, prevention of endometrial cancer, prevention of recurrent miscarriage, prevention of ovulation) inhibition or synchronization, promotion of hair growth).

In other embodiments, a muscle relaxant (non-limiting examples of which include cinnamedrine, cyclobenzaprine, flavoxate, orphenadrine, papaverine and mebeverine pharmaceutically acceptable salts) is used in the present invention. It may be delivered using a composition. Additionally, other non-limiting aspects of the present invention include, but are not limited to: (a) protecting or relieving chapped or chapped skin and lips from the dry effects of wind and cold; (c) reducing the level of expression of one or more genes encoding IL-6 or IL-8; (d) PGE2. (e) increasing expression of one or more genes encoding extracellular matrix proteins (elastin, fibronectin); (f) is directed to methods of providing skin health benefits, including reducing expression of one or more genes encoding matrix metalloproteinases.

Raw material example Raw material example 1
Vaseline 75%
25% transesterified unfractionated shea butter (Butyrospermum Parkii (Shea) Butter)

Raw material example 2
Vaseline 80%
20% transesterified unfractionated shea butter (Butyrospermum Parkii (Shea) Butter)

Raw material example 3
Vaseline 90%
10% transesterified unfractionated cocoa butter (Theobroma Cacao (Cocoa) Seed Butter)

Any of the three raw material examples above can also be used as a final product that will meet the over-the-counter skin protectant dossier.

Final Product Examples Final Product Example 1 - Hand Cream

相ＡおよびＢそれぞれの成分を個別に７５℃に加熱する。相Ｃを相Ａに添加し；撹拌しながらＡ／Ｃを相Ｂに添加する。ホモジナイズする。撹拌しながら３０℃まで冷却する。ｐＨをクエン酸で５．５に調整する。撹拌しながら相Ｄを添加して、均質な生成物を形成する。

Heat each component of Phases A and B separately to 75°C. Add Phase C to Phase A; Add A/C to Phase B with stirring. Homogenize. Cool to 30° C. with stirring. Adjust the pH to 5.5 with citric acid. Add Phase D with stirring to form a homogeneous product.

In other embodiments, shea butter ethyl esters can be added to the MFSG/NGM of the present invention to form a three part system, transesterified unfractionated shea butter, shea butter ethyl esters and petrolatum. In these embodiments, shea butter ethyl esters comprise about 1%-25% of the MFSG/NGM.

Final Product Example 2 - Anhydrous Face and Body Treatment Cream At 70°C, blend and melt the following ingredients until a clear liquid is formed: (i) 20 parts Lipex® SheaLight (INCI: (ii) 78 parts of the structured glycidic/non-glycidic matrix of the present invention (INCI: Petrolatum (and) Butyrospermum Parkii (Shea) Butter) and (iii) 2 parts Lipex® PreAct (INCI: Canola Oil) Cool to 22°C.

Final Product Example 3 - Lip Balm

１８の成分すべてを７５℃において混ぜ合わせる。撹拌しながら混合物を３０℃まで冷却する。管に充填する。

Combine all 18 ingredients at 75°C. Cool the mixture to 30° C. while stirring. Fill the tube.

Test Example Improvement of Skin Barrier Function (TEWL)
Ten female subjects aged 36-58 years were enrolled to evaluate the effectiveness of topical products containing the skin cosmetic structured glycidic/non-glycidic matrix of the present invention in improving skin barrier function. and conducted clinical trials.

Transepidermal water loss (TEWL), a measure of skin barrier function, was measured using a DermaLab Evaporator (Cortex Technology, Hadsund, Denmark). No change in TEWL in the post-treatment interval compared to before initiation indicates that the treatment is not interfering with barrier function. A decrease in TEWL indicates improved skin barrier function (ie, less water is lost across the skin barrier).

During a "washout" period of at least 3 days prior to the start of the study, subjects used a mild bar soap to cleanse (ie, bathe) the test site, ie, the palmar surface of the subject's forearm. Subjects were instructed not to use any personal care products (eg, lotions, creams, cleansers) other than those provided by the study facility.

Subjects returned to the study site following the washout period. As instructed, subjects wore clothing that did not cover the forearms. The palmar surface of the forearm was gently wiped with a damp disposable washcloth and patted dry with a paper towel by trained staff. Staff then marked four test sites on the palmar surface of the forearm, two on one forearm and two on the other. Each test site was 4 cm x 4 cm, with adjacent test sites separated by at least 3 cm. Test sites were located at least 2 cm from the wrist joint and at least 2 cm from the elbow joint and were designated test sites 1-4. Assignment of test sites versus untreated (control) sites was randomized.

Subjects then underwent a first equilibration for a minimum of 30 minutes in a room maintained at about 22±2° C. and about 40±10% relative humidity. (Temperature and humidity were verified throughout the test and recorded before and after equilibration and before each TEWL measurement.)

Following equilibration, pre-start TEWL was read at each test site using an Evaporimer by trained staff. About 2 mg/cm ² of the test product (skin beauty product according to Formulation Example 1) was then pipetted directly onto the site and gently rubbed in using a finger cot. (Finger sacks were inspected after application to ensure that most of the test material had not adhered to the finger sacks.)

Subjects were quarantined at the study site for the remainder of their visit. During this time, subjects were instructed not to cover/expose their palmar forearm and not to cover, wet or wipe the test site.

After 3 hours and 30 minutes (±10 minutes) of treatment, subjects underwent a second equilibration under the conditions described above. Following equilibration (4 hours ± 10 minutes post-treatment), TEWL was read as above. After 7 hours and 30 minutes (±10 minutes) of treatment, subjects underwent a third and final equilibration. Following equilibration (8 hours ± 10 minutes post-treatment) TWEL measurements were taken. Subjects were released after the 8 hour measurement was completed.

After 4 hours, the test product applied sites demonstrated statistically significantly superior skin barrier function than the control untreated sites when compared to pre-start.

Sensory Panel A panel of 8 tested the MFSG/NGM of the present invention (25% transesterified unfractionated shea butter + 75% petrolatum) with (i) a blend of 25% RBD shea butter and 75% petrolatum; and (ii) compared to "pure" petrolatum. All three products used the same grade of petrolatum, namely White Protoline® Petrolatum available from Sonneborn, LLC (Parsippany, NJ). A sensory evaluation was conducted based on spreadability, greasiness, softness, stickiness, absorbency, gloss, and graininess. The score for each parameter was evaluated on a 5-point scale, with pure Protoline® being assigned a score of "3".

Additional Skin Benefit Testing Skin tightness is measured using a Cutometer®. After using the skin beauty product according to Example 1, an increase in the Cutometer® measurements was observed, indicating an improvement (increase) in skin firmness.

Skin flaking is measured by using D-Squame® Skin Surface Sampling Discs (CuDerm Corporation, Dallas, Tex.). Prior to step 2, apply a clean adhesive disc to clean, dry skin. The disc is pressed firmly against the skin for a few seconds and then peeled off the skin. Before and after, D-Squame® scores are assigned based on the following scale: 1 = very slight flaking; 2 = mild flaking; 3 = moderate flaking; 5 = severe flaking. A decrease in the D-Squame® score indicates an improvement (reduction) in dry skin. An increase in the D-Squame® score indicates worse flaking.

Skin tension is measured using a Cutometer®. After using the product according to Example 1, an increase in the Cutometer® measurements was observed, which is indicative.

Subjects exhibiting signs of skin aging, uneven skin tone/texture (browning, erythema) and visible facial fine lines and wrinkles were evaluated in improving the appearance of these signs of skin aging. , to participate in clinical trials to evaluate the efficacy of skin beauty products according to the present invention. Digital images of the face are taken before and after performing the method of the present invention. Images are captured, processed, and analyzed using the VISIA® CR Imaging System (Canfield Scientific, Inc. Fairfield, NJ). Each image is scanned horizontally and vertically; a proprietary VISIA® CR mathematical algorithm is used to determine the intensity of red, green, and blue pixels and assign a texture score. The same algorithm calculates the number and depth of fine lines and wrinkles.

A reduction in texture scores and wrinkle/fine line number and depth is observed to indicate an improvement in these skin aging parameters.

Skin Barrier Function Test TEWL was measured using a TEWL probe, DermaLab® Evaporimer (Cortex Technology, Hadsund, Denmark). A decrease in TEWL indicates an improvement in skin barrier function, thereby reducing water loss across the skin barrier.

Subjects arrived at the study site 3 days prior to the scheduled start date and were enrolled for inclusion and exclusion criteria. Subjects received a "neutral" bar soap (Neutrogena) used to wash (ie, bathe) the palmar forearm (serving the test site) for a washout period of 3 days. Subjects are prohibited from using any personal care products (e.g., lotions, creams, cleansers) on the test site (palm forearm) during the entire study, other than those provided by the study facility. given specific instructions.

Following the washout period, subjects returned to the study site. Subjects were instructed to wear clothing that did not cover the palmar forearm on the day of evaluation. The surface of the palmar forearm was gently wiped with a damp disposable washcloth and patted dry with a paper towel by trained staff. Staff then marked 6 test sites (3 sites on each forearm) on the palmar surface of the forearm. Each test site was 4 cm x 4 cm. The test sites were centered on the palmar side of the forearm (at least 2 cm from the wrist and at least 2 cm from the elbow) and identified as test sites AF. Treated and control sites (untreated) were assigned randomly using a computer-generated randomization code. Measurements were made with the TEWL Probe at these test sites throughout the study period.

Prior to measurements, subjects underwent an equilibration process in which they sat quietly for a minimum of 20 minutes in a room maintained at 20-24°C and 30-50% relative humidity. During this time, the subject was instructed to keep the palmar forearm uncovered/exposed by resting the hand on the palm with the palm facing up.

Packaging tape was applied to the treated and control (untreated) sites from which the tape was removed. TEWL was read (by Evaporimer) and repeated tape stripping was performed on the test site until a TEWL measurement of greater than 20 g/m ² /hr was reached.

Following the pre-start measurements (after tape stripping), the test products, MFSG/NGM of the invention (identified as "SHEA XP" in the table below) and "pure petrolatum" each at a concentration of 2 mg/ ^cm2 . It was applied (pipetted) to the designated test site and rubbed into the skin using a finger cot until fully absorbed. (Finger cots were inspected after application to ensure no test material adhered to the finger cots. One site serves as a control (untreated).

During the 12-hour test period, subjects were isolated in a temperature- and humidity-controlled room in the test. Subjects were instructed to keep their palmar forearms uncovered/exposed. Subjects are not allowed to cover, wet or wipe their palmar forearms until released from testing. No food or drink is allowed for 30 minutes before taking measurements.

After 3 hours and 30 minutes (±10 minutes) of treatment, subjects were allowed to equilibrate by sitting quietly for a minimum of 20 minutes in a room maintained at approximately 20-24° C. and 30-50% relative humidity. . TEWL measurements are taken 4 hours (±10 minutes) after treatment.

After 7 hours and 30 minutes (±10 minutes) of treatment, subjects were re-equilibrated by remaining seated quietly in a room maintained at approximately 20-24° C. and 30-50% relative humidity for a minimum of 20 minutes. was done. TEWL measurements were taken 8 hours (±10 minutes) after treatment.

After 11 hours and 30 minutes (±10 minutes) of treatment, subjects were equilibrated by remaining seated quietly in a room maintained at approximately 20-24° C. and 30-50% relative humidity for a minimum of 20 minutes. rice field. TEWL measurements were taken 11 hours (±10 minutes) after treatment.

Following the first 12 hours of measurements, subjects were released from the study facility and instructed to return approximately 23 hours and 30 minutes (±30 minutes) after application. Subjects were instructed not to wet their palmar forearms (ie, shower, bathe, or swim) or apply product until the 24-hour measurement. After 23 hours and 30 minutes (±30 minutes) of treatment, subjects were equilibrated by remaining seated quietly in a room maintained at approximately 20-24° C. and 30-50% relative humidity for a minimum of 20 minutes. rice field. TEWL measurements were taken 24 hours (±30 minutes) after treatment. Subjects were released after 24 hour post-treatment measurements were obtained.

Relative to pure petrolatum, TEWL with Shea XP showed a directional improvement in the range of 2.25% to 2.69%, with a directional improvement in the range of approximately 3% after 12 hours of application. rice field.

The results of this test are shown in the table below.

Analysis of skin barrier function in terms of differences between treated and pre-treatment versus control (untreated) and pre-treatment

Analysis of skin barrier function for Shea XP versus 'pure' petroleum jelly

The present invention includes the following aspects.
<1> A topical application product comprising (i) at least one transesterified unfractionated triglyceride and (ii) at least one petroleum jelly, comprising at least 2% triglyceride and at least 6% on a weight/weight basis A product for topical application, containing petrolatum.
<2> The topical product of 1 above, which does not exhibit graininess, bloom, discoloration, or separation, or change in viscosity over time.
<3> The topical product according to 1 or 2 above, wherein the triglyceride has a slope of less than 1 in solid fat content melting profile from 20°C to 35°C.
<4> The transesterified unfractionated triglycerides are Shea butter (Butyrospermum Parkii (Shea) Butter), Cocoa butter (Theobroma Cacao (Cocoa) Seed Butter), Shorea Stenoptera (Illipe) Seed Butter , Astrocaryum Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Mangnifera Indica (Mango) Seed Butter, 4. A topical product according to any one of 1-3.
<5> containing at least 30% petrolatum and at least one transesterified unfractionated triglyceride, wherein the ratio of said at least one transesterified unfractionated triglyceride to said at least one petroleum jelly is 1:39 to 5. The topical product according to any one of 1 to 4 above, which is 7:13.
<6> The topical product of any one of 1 to 5, wherein the ratio of said at least one transesterified unfractionated triglyceride to said at least one petroleum jelly is from 1:19 to 1:3.
<7> A multifunctional chemical ingredient used in the manufacture of cosmetics, personal care products and dermatological products comprising (i) at least one transesterified unfractionated triglyceride and (ii) at least one petrolatum.
<8> The multifunctional chemical ingredient of item 7, wherein the ratio of the at least one transesterified unfractionated triglyceride to the at least one petroleum jelly is from 1:39 to 7:13.
<9> The multifunctional chemical ingredient according to item 7 or 8, wherein the ratio of the at least one transesterified unfractionated triglyceride to the at least one petroleum jelly is from 1:19 to 1:3.
<10> The transesterified unfractionated triglyceride is Shea butter (Butyrospermum Parkii (Shea) Butter), Cocoa butter (Theobroma Cacao (Cocoa) Seed Butter), Shorea Stenoptera (Illipe) Seed Butter , Astrocaryum Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Mangnifera Indica (Mango) Seed Butter, 10. The multifunctional chemical entity according to any one of 7-9.
<11> The multifunctional chemical ingredient according to any one of 7 to 10 above, wherein the transesterified unfractionated triglyceride is Butyrospermum Parkii (Shea) Butter.
<12> Multifunctional used in the manufacture of cosmetics, personal care products and dermatological products consisting essentially of (i) at least one transesterified unfractionated triglyceride and (ii) at least one petrolatum Chemical composition.
<13> A skin beauty product comprising (i) at least one triglyceride and (ii) at least one petrolatum, comprising (a) at least 2% triglyceride and at least 6% petrolatum on a weight/weight basis , (b) skin beauty products that do not exhibit graininess, bloom, discoloration, separation, or changes in viscosity.
<14> A topical product comprising (i) at least one transesterified unfractionated triglyceride and (ii) at least one petrolatum and (iii) an optional active ingredient.
<15> After application to the skin of at least 10 test subjects, it causes an improvement in skin barrier function as measured by a decrease in transepidermal water loss (TEWL) after 8 hours in at least 70% of said subjects. 15. A product or ingredient according to any one of 1 to 14.
<16> Any of the above 1 to 14, which after application to the skin of at least 10 test subjects causes an improvement in skin barrier function as measured by a decrease in TEWL in at least 80% of said subjects after 8 hours. Product or ingredient stated.
<17> Any of the above 1 to 14, which after application to the skin of at least 10 test subjects causes an improvement in skin barrier function as measured by a decrease in TEWL in at least 90% of said subjects after 8 hours. Product or ingredient stated.
<18> The product or ingredient of any one of 1 to 14 above, having a sheatriterpene concentration of at least about 10 ppm.
<19> The product or ingredient of any one of 1 to 14 above, having a ciatriterpene concentration of about 100 ppm to about 10,000 ppm.
<20> The product or ingredient of any one of 1 to 14 above, having a ciatriterpene concentration of about 300 ppm to about 3,000 ppm.
<21> The product or ingredient of any one of 1 to 14 above, having a ciatriterpene concentration of about 5,000 ppm to about 10,000 ppm.
<22> The product or ingredient according to any one of 1 to 14 above, having a ciatriterpene concentration of about 6,000 ppm to about 9,000 ppm.
<23> The product or ingredient according to any one of 1 to 14 above, which causes an increase in epidermal thickness of at least 10% in an ex vivo test.
<24> The product or ingredient according to any one of 1 to 14 above, which causes an increase in epidermal thickness of at least 20% in an ex vivo test.
<25> The product or ingredient according to any one of 1 to 14 above, which causes an increase in epidermal thickness of at least 25% in an ex vivo test.
<26> The product or ingredient according to any one of 1 to 14 above, which causes an increase in skin collagen of at least 3% in an ex vivo test.
<27> The product or ingredient according to any one of 1 to 14 above, which produces an increase in skin collagen of at least 5% in an ex vivo test.
<28> The product or ingredient according to any one of 1 to 14 above, which causes an increase in skin collagen of at least 6% in an ex vivo test.
<29> The product of any one of 1 to 6 or 13 to 28 above, comprising about 8% to about 80% triglycerides and petroleum jelly.
<30> The product of 29 above in the form of baby lotion, diaper rash cream, body balm, face cream, lip gloss or lip butter.
<31> The product of 30 above, which is a baby lotion and contains about 8% to about 15% triglycerides and petroleum jelly.
<32> The product of 30 above, which is a diaper rash cream and contains about 40% to about 60% triglycerides and petroleum jelly.
<33> The product of 30 above, which is a body balm and contains about 60% to about 80% triglycerides and petroleum jelly.
<34> The product of 30 above, which is a face cream and contains about 8% to about 15% triglycerides and petroleum jelly.
<35> The product of 30 above, which is a lip gloss and contains about 20% to about 40% triglycerides and petroleum jelly.
<36> A topical application product comprising (i) at least one transesterified triglyceride having a final melting point above or significantly above body temperature and (ii) at least one petrolatum, wherein on a weight/weight basis at least A topical product containing 2% triglycerides and at least 6% petrolatum.

Claims (22)

A topical skin beauty product comprising a matrix containing (i) at least one transesterified unfractionated triglyceride and (ii) at least one petrolatum,
the petroleum jelly is present in an amount of at least 30% by weight;
said unfractionated triglycerides in an amount of 5-50% by weight of the total weight of said matrix;
said unfractionated triglycerides comprising unfractionated shea butter with an unsaponifiable fraction of 7% to 10% by weight;
said topical skin beauty product contains at least 5% by weight of triglycerides and at least 6% by weight of petroleum jelly on a weight/weight basis;
The topically applied skin beauty product is selected from the group consisting of creams, moisturizers, lotions, ointments, gels, serums, foundations, lip glosses, concealers, masks, cleansers and toners. skin beauty products. 2. The topical skin beauty product of Claim 1, which does not exhibit graininess, bloom, discoloration, or separation, or change in viscosity over time. 3. The topical skin cosmetic product according to claim 1 or 2, wherein the triglyceride has a slope of less than 1 in solid fat content melting profile from 20°C to 35°C. 4. A topical skin beauty product according to any preceding claim, wherein the ratio of said at least one transesterified unfractionated triglyceride to said at least one petroleum jelly is from 7:13 to 1:39. . 5. A topical skin cosmetic product according to any preceding claim, wherein the ratio of said at least one transesterified unfractionated triglyceride to said at least one petroleum jelly is from 1:3 to 1:19. 1. A topical skin cosmetic product comprising at least one transesterified unfractionated triglyceride and at least one petrolatum and a matrix containing an active ingredient,
the petroleum jelly is present in an amount of at least 30% by weight;
said unfractionated triglycerides in an amount of 5-50% by weight of the total weight of said matrix;
said unfractionated triglycerides comprising unfractionated shea butter with an unsaponifiable fraction of 7% to 10% by weight;
wherein said topical skin beauty product is selected from the group consisting of creams, moisturizers, lotions, ointments, gels, serums, foundations, lip glosses, concealers, masks, cleansers and toners; skin beauty products. 7. A skin beauty product according to any one of claims 1 to 6 in the form of baby lotion, diaper rash cream, body balm, face cream, lip gloss or lip butter. A skin beauty product according to claim 7 , which is a baby lotion and contains 8% to 15% by weight of triglycerides and petroleum jelly. A skin beauty product according to claim 7 , which is a diaper rash cream and contains 40% to 60% by weight of triglycerides and petroleum jelly. A skin beauty product according to claim 7 , which is a body balm and contains 60% to 80% by weight of triglycerides and petrolatum. A skin beauty product according to claim 7 , which is a face cream and contains 8% to 15% by weight of triglycerides and petroleum jelly. A skin beauty product according to claim 7 , which is a lip gloss and contains 20% to 40% by weight of triglycerides and petroleum jelly. 1. A multifunctional chemical ingredient used in the manufacture of skin beauty products comprising a matrix containing (i) at least one transesterified unfractionated triglyceride and (ii) at least one petroleum jelly, comprising:
said petrolatum is present in an amount of at least 30% by weight and said unfractionated triglycerides are present in an amount of 5-50% by weight of the total weight of said matrix;
said unfractionated triglycerides comprising unfractionated shea butter with an unsaponifiable fraction of 7% to 10% by weight;
Said multifunctional chemistry, wherein said skin beauty product is selected from the group consisting of creams, moisturizers, lotions, ointments, gels, serums, foundations, lip glosses, concealers, masks, cleansers and lotions. component. 14. The multifunctional chemical ingredient of claim 13 , wherein the ratio of said at least one transesterified unfractionated triglyceride to said at least one petroleum jelly is from 7:13 to 1:39. 15. The multifunctional chemical ingredient of claim 13 or 14 , wherein the ratio of said at least one transesterified unfractionated triglyceride to said at least one petroleum jelly is from 1:3 to 1:19. 1. A multifunctional chemical ingredient used in the manufacture of skin beauty products comprising a matrix containing (i) at least one transesterified unfractionated triglyceride and (ii) at least one petroleum jelly, comprising:
the petroleum jelly is present in an amount of at least 30% by weight;
said unfractionated triglycerides in an amount of 5-35% by weight of the total weight of said matrix;
said unfractionated triglycerides comprising unfractionated shea butter with an unsaponifiable fraction of 7% to 10% by weight;
Said multifunctional chemistry, wherein said skin beauty product is selected from the group consisting of creams, moisturizers, lotions, ointments, gels, serums, foundations, lip glosses, concealers, masks, cleansers and lotions. component. 2. The topical skin beauty product of claim 1, wherein said unsaponifiable fraction comprises triterpene esters. 18. The topical skin beauty product of claim 17 , wherein said triterpene ester comprises at least one of cinnamate or acetate. 18. The topical skin beauty product of Claim 17 , wherein said triterpene ester comprises at least one of α-amyrin, β-amyrin, butyrospermol, lupeol or parqueol. 2. The topical skin beauty product of Claim 1, wherein said at least one transesterified unfractionated triglyceride comprises at least 2% by weight of triterpene esters. 2. The topical skin cosmetic product of claim 1, wherein said at least one transesterified unfractionated triglyceride comprises from 2% to 5% by weight of triterpene esters. 2. The topical skin cosmetic product of claim 1, wherein said at least one transesterified unfractionated triglyceride is present in an amount of 5% to 35% by weight of the total weight of said matrix.

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