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WO 2016/105530 Al 30 June 2016 (30.06.2016) W P O P C T

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WO 2016/105530 Al 30 June 2016 (30.06.2016) W P O P C T (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2016/105530 Al 30 June 2016 (30.06.2016) W P O P C T (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, A61K 47/10 (2006.01) A61K 47/22 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, A61K 47/12 (2006.01) DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, (21) International Application Number: KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, PCT/US20 15/000302 MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, (22) International Filing Date: PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, 23 December 2015 (23. 12.2015) SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, 62/096,148 23 December 2014 (23. 12.2014) US TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (72) Inventor; and DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, (71) Applicant : HOFFMAN, Steven [US/US]; 15 Knichel LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, Road, Mahwah, NJ 07430 (US). SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). (74) Agents: LUCCI, Joseph et al; Baker & Hostetler LLP, Cira Centre, 12th Floor, 2929 Arch Street, Philadelphia, Published: PA 19104-2891 (US). — with international search report (Art. 21(3)) (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (54) Title: TRANSDERMAL FORMULATIONS (57) Abstract: The present disclosure is directed to transdermal and moisturizing compositions. TRANSDERMAL FORMULATIONS CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application claims the benefit of U.S. Provisional Application No. 62/096,148, filed December 23, 2014, the entirety of which is incorporated by reference herein. BACKGROUND [0002] Transdermal administration of therapeutic agents has many advantages, including convenience and gastrointestinal tract metabolism avoidance. But in the absence of penetration enhancing agents, many therapeutic agents are not capable of penetrating the skin in therapeutically effective concentrations. As such, compositions that facilitate the penetration of therapeutic agents through the skin are needed. [0003] Also, the loss of skin moisture results in dry skin that can be uncomfortable, painful, or unattractive. Compositions that ameliorate dry skin and increase or maintain skin hydration are also needed. SUMMARY [0004] The present disclosure is directed to compositions comprising a first component, a second component, a C 2-ioalkyl alcohol, and an organic acid having 1 to 25 carbon atoms, wherein the first and second components are further defined herein. Methods of making and using these compositions are also described. DETAILED DESCRIPTION OF ILLUSTRATIVE EMBODIMENTS [0005] The present disclosure may be understood more readily by reference to the following detailed description of desired embodiments and the examples included therein. In the following specification and the claims that follow, reference will be made to a number of terms which have the following meanings. [0006] As used in the specification and in the claims, the term "comprising" may include the embodiments "consisting of and "consisting essentially of." The terms "comprise(s)," "include(s)," "having," "has," "can," "contain(s)," and variants thereof, as used herein, are intended to be open-ended transitional phrases, terms, or words that require the presence of the named ingredients/steps and permit the presence of other ingredients/steps. However, such description should be construed as also describing compositions or processes as "consisting of and "consisting essentially of the enumerated ingredients/steps, which allows the presence of only the named ingredients/steps, along with any impurities that might result therefrom, and excludes other ingredients/steps. [0007] Unless indicated to the contrary, the numerical values should be understood to include numerical values which are the same when reduced to the same number of significant figures and numerical values which differ from the stated value by less than the experimental error of conventional measurement technique of the type described in the present application to determine the value. [0008] All ranges disclosed herein are inclusive of the recited endpoint and independently combinable (for example, the range of "from 2 to 10" is inclusive of the endpoints, 2 and 10, and all the intermediate values). The endpoints of the ranges and any values disclosed herein are not limited to the precise range or value; they are sufficiently imprecise to include values approximating these ranges and/or values. [0009] As used herein, approximating language may be applied to modify any quantitative representation that may vary without resulting in a change in the basic function to which it is related. Accordingly, a value modified by a term or terms, such as "about" and "substantially," may not be limited to the precise value specified, in some cases. In at least some instances, the approximating language may correspond to the precision of an instrument for measuring the value. The modifier "about" should also be considered as disclosing the range defined by the absolute values of the two endpoints. For example, the expression "from about 2 to about 4" also discloses the range "from 2 to 4." The term "about" may refer to plus or minus 10% of the indicated number. For example, "about 10%" may indicate a range of 9% to 11 , and "about 1" may mean from 0.9-1.1. Other meanings of "about" may be apparent from the context, such as rounding off, so, for example "about 1" may also mean from 0.5 to 1.4. [0010] As used herein, "alkyl" refers to straight chain and branched chains having the indicated number of carbon atoms, usually from 1to 20 carbon atoms, for example 1 to 8 carbon atoms, such as 1to 6 or 1to 7 carbon atoms. For example Ci-6 alkyl encompasses both straight and branched chain alkyl of from 1 to 6 carbon atoms. When an alkyl residue having a specific number of carbons is named, all branched and straight chain versions having that number of carbons are intended to be encompassed; thus, for example, "butyl" is meant to include n-butyl, sec-butyl, isobutyl and t-butyl; "propyl" includes n-propyl and isopropyl. Examples of alkyl groups include methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, pentyl, 2-pentyl, isopentyl, neopentyl, hexyl, 2-hexyl, 3-hexyl, 3-methylpentyl, and the like. [0011] As used herein, "alkenyl" refers to an unsaturated branched or straight-chain alkyl group having at least one carbon-carbon double bond. The group may be in either the cis or trans configuration about the double bond(s). The group may also be an aromatic group, for example, a phenyl or phenylene moiety. Typical alkenyl groups include, but are not limited to, ethenyl; propenyls such as prop- l -en- l-yl, prop-l-en-2-yl, prop-2-en- l-yl (allyl), prop-2-en-2-yl; butenyls such as but-l -en-l -yl, but-l -en-2-yl, 2-methyl-prop-l -en-l -yl, but-2-en-l-yl, but-2-en- 1-yl, but-2-en-2-yl, buta- l ,3-dien-l-yl, buta-l ,3-dien-2-yl; phenylene, and the like. In certain embodiments, an alkenyl group has from 2 to 20 carbon atoms. [0012] As used herein, "alkynyl" refers to an unsaturated branched or straight-chain alkyl group having at least one carbon-carbon triple bond derived by the removal of two molecules of hydrogen from adjacent carbon atoms of the parent alkyl. Typical alkynyl groups include, but are not limited to, ethynyl; propynyls such as prop-l -yn- l -yl, prop-2-yn-l -yl; butynyls such as but- 1-yn- 1-yl, but-l -yn-3-yl, but-3-yn- l-yl; and the like. In certain embodiments, an alkynyl group has from 2 to 20 carbon atoms. [0013] The present disclosure is directed to compositions that moisturize the skin or that facilitate and/or enhance the transdermal permeation of therapeutic agents through the skin. As used herein, "moisturize" refers to increasing hydration or preventing further hydration loss. As used herein, the term "transdermal permeation" includes both percutaneous delivery and transmucosal delivery, that is, passage through skin or mucosal tissue and into the bloodstream. As used herein in reference to transdermal penetration, the term "enhancing" refers to increasing the rate at which a therapeutic agent penetrates the skin or mucosal tissue and enters the bloodstream. These compositions include a first component, a second component, an alcohol, an organic acid, and, optionally, water. Other compositions of the disclosure further comprise a therapeutic agent. [0014] According to the disclosure, the first component comprises a compound of formula I R-(OCH 2CH2) -OH (I) wherein R is Ci-2oalkyl, C2-2oalkenyl; or C2-2oalkynyl; and y is 1 to 25; a tetrafunctional block copolymer surfactant terminating in primary hydroxyl groups; a sorbitan derivative; a Ce-ioalkyl ammonium salt; a compound of formula II ≡ HO-(CH CH20 )m-C(CH3)(C4H9)-C C-C(CH3)(C4H )-(OCH2CH2)n-OH (II) wherein m and n are each independently 1 to 25; or a combination thereof.
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