(12) Patent Application Publication (10) Pub. No.: US 2008/0274206A1 Lekhram Et Al
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US 20080274206A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2008/0274206A1 Lekhram et al. (43) Pub. Date: Nov. 6, 2008 (54) STABILISED OXYGEN RELEASING Related U.S. Application Data COMPOSITION (60) Provisional application No. 60/616,229, filed on Oct. (75) Inventors: Changoer Lekhram, Ijsselstein 7, 2004. (NL); Willem Frederik Van Den Publication Classification Bosch, Oegstgeest (NL); Hendrik Jan Cornelis Meijerink, Brussel (51) Int. Cl. (BE) A633/40 (2006.01) (52) U.S. Cl. ........................................................ 424/613 Correspondence Address: (57) ABSTRACT FOLEY AND LARDNER LLP SUTESOO The present invention relates to stabilised liquid oxygen 3OOOK STREET NW releasing composition comprising a component (a) selected WASHINGTON, DC 20007 (US) from the salts consisting of cations A, and anions derived from halogen oxides according to the general formula (73) Assignee: Ngen Pharmaceuticals N.V. IOX wherein A is a metal selected from Groups 1 or 2 of the Periodic System of the Elements, X is a halogen atom, (21) Appl. No.: 11/576,880 m=1-4, n=1 or 2, a component (b) selected from the group of oxygen donors, a component (c) selected from the group of (22) PCT Filed: Jul. 10, 2005 oxygen donor Stabilising agents and a component (d) selected from the group of liquid binders. The stabilised liquid oxygen (86). PCT No.: PCT/NLOS/OO728 releasing composition can be used in pharmaceutical compo sitions, cosmetic compositions and food applications, e.g. S371 (c)(1), skin care products, dental care products, tooth whitening (2), (4) Date: Mar. 14, 2008 products including chewing gums. 3,5 2, 5 2 - a - 1034-01 pH=9.0 - - 1034-02 pH=7.0 - 1034-03 pH=5.0 15 1 0.5 Patent Application Publication Nov. 6, 2008 Sheet 1 of 4 US 2008/0274206A1 (uu%) ageiocled unpoS Patent Application Publication Nov. 6, 2008 Sheet 2 of 4 US 2008/0274206A1 (u?u%) eyeloqued unpos Patent Application Publication Nov. 6, 2008 Sheet 3 of 4 US 2008/0274206A1 O OO CN SFO CN 9 O C S O s CO - O > 92 CN O C CO - s CD 75 9 S CY) 9 So G) O E O O .9 G) O) E o E C) V DS is - O CO rG2 O O OO CO. v. CN O OO CO r CN O CN W- W - v- w w - , enem-TeleC Patent Application Publication Nov. 6, 2008 Sheet 4 of 4 US 2008/0274206A1 i - s | 8 - S. Ns N O LO O LO O S. S CN w V enem eled US 2008/027420.6 A1 Nov. 6, 2008 STABLISED OXYGEN RELEASING requires experienced and qualified personnel. Alternatively, COMPOSITION when the composition is intended for example in cosmetic applications, special and complex packaging of the compo SUMMARY OF THE INVENTION nent is required to enable safe use of the composition by the customer. It is therefore apparent to the person skilled in the 0001. The present invention relates to a stabilised liquid art that it is desired to have a composition comprising com oxygen releasing composition, said stabilised liquid oxygen ponents (a) and (b) which releases the active component in a releasing composition being in particular Suitable for phar controlled manner and which shows a long lasting effect. maceutical, cosmetic and food applications. Moreover, it is apparent that it is highly desirable to have such a composition comprising components (a) and (b) that is OBJECT OF THE INVENTION stable during storage and transportation under normal condi 0002 The object of the invention is to provide a stabilised tions and that is safe to use by the end user. liquid oxygen releasing composition, said composition com 0005. A solid composition consisting essentially of prising a component (a) selected from the salts consisting of Sodium perborate monohydrate, lithium hypochlorite and cations A, and anions derived from halogen oxides accord phosphate salts is disclosed in for example U.S. Pat. No. ing to the general formula OX, wherein A is a metal 3,793.211 which is incorporated by reference herein. This selected from Groups 1 or 2 of the Periodic System of the composition is only stable in the Solid state as upon contact Elements, X is a halogenatom, m=1-4, n=1 or 2, a component with water the composition rapidly decomposes. (b) selected from the group of oxygen donors, a component 0006 EP A 0.085.891, incorporated by reference herein, (c) selected from the group of oxygen donor Stabilising agents discloses a composition for the cleaning and hygiene of the and a component (d) selected from the group of liquid bind teeth which comprises a suspension of water soluble, non CS abrasive salts selected from a large range of compounds 0003. According to the invention, the liquid composition which includes potassium perchlorate and sodium perborate. may be a product having viscosity properties and flow char EPA 0.085.891 does, however, nowhere specifically disclose acteristics that are comparable with those of rather thick to the combination of components (a) and (b). highly viscous, optionally thixotropic, liquids such as gels, 0007 GBA 552.803 discloses a solution that is prepared pastes, Suspensions, dispersions or emulsions. The liquid from borax (disodium tetraborate), calcium hypochlorite and composition may have visco-elastic properties as well. other components, wherein the borax and the other compo Examples of such liquids are peanut butter, toothpaste, oint nents are added to water and Subsequently boiled. In a next ments, creams, shampoos and the like. The liquid composi step the calcium hypochlorite is added and the mixture is tion may also be of low viscosity Such as aqueous Solutions, allowed to cool while stirred. After a period of time, sus emulsions and dispersions, which are easy to pour. As a pended matter has settled and a clear liquid and a paste is consequence, the liquid composition according to the present obtained which are separated by decantation. It is therefore invention is not intended to be a composition consisting clear to the person skilled in the art that the solution only essentially or exclusively of Solid materials, e.g. a mixture of contains reaction products of the original ingredients. powders. 0008. Other pharmaceutical and/or cosmetic composi 0004 Compositions comprising component (a) and com tions containing either component (a) or component (b) are ponent (b) are for example disclosed in U.S. Pat. No. 6,017, also known in the art for a long time. Compositions contain 515 which is incorporated by reference herein. According to ing component (a) are for example disclosed in GBA 1.469. U.S. Pat. No. 6,017,515, the preferred component (a) is 398, GB A 2.289.841, GB A 2.290.233, WO 96/13245 and sodium hypochlorite and the preferred component (b) is WO 98/04235 whereas compositions containing component Sodium perborate tetrahydrate. The disadvantage of the com (b) are for example disclosed in U.S. Pat. No. 3,574,824, U.S. positions disclosed in U.S. Pat. No. 6,017,515 is that these Pat. No. 5,041,280, U.S. Pat. No. 5,264,205, U.S. Pat. No. compositions are rather unstable, i.e. that they release oxygen 5,279,816, U.S. Pat. No. 5,302,375, U.S. Pat. No. 5,616,313, at a relatively high rate and in an uncontrolled manner with U.S. Pat. No. 5,632,972, U.S. Pat. No. 5,648,064, U.S. Pat. the consequence that the activity of the compositions No. 5,858,332, U.S. Pat. No. 6,409,993 and U.S. Pat. No. decreases rapidly during use or application and when stored 6,500.408, all incorporated by reference herein. for prolonged periods. U.S. Pat. No. 6,017,515 therefore pro poses either to keep components (a) and (b) separate just SUMMARY OF THE INVENTION before use or, when already combined, to store the composi 0009. The present invention relates to a stabilised liquid tions at low temperature. It is evident to the person skilled in oxygen releasing composition, said composition comprising the art that uncontrolled release of the active component, i.e. a component (a) selected from the salts consisting of cations oxygen, by pharmaceutical or cosmetic compositions is not A, and anions derived from halogen oxides according to the desired since the composition looses its activity very rapidly general formula O, XI, wherein A is a metal selected from and does not provide a long lasting effect. In addition, the Groups 1 or 2 of the Periodic System of the Elements, X is a compositions disclosed in U.S. Pat. No. 6,017,515 are halogen atom, m=1-4, n=1 or 2, a component (b) selected unstable (unless components (a) and (b) are kept separate) from the group of oxygen donors, a component (c) selected which necessitates special conditions to preserve the activity from the group of oxygen donor stabilising agents and a of the compositions during storage and transportation up till component (d) selected from the group of liquid binders. the moment the composition is used by the customer, e.g. a physician or a patient. Finally, if components (a) and (b) are DETAILED DESCRIPTION OF THE INVENTION kept separate, they must first be combined prior to the appli cation of the composition. When the composition is intended 0010. The present invention is directed to a stabilised liq for example in pharmaceutical applications, this usually uid oxygen releasing composition wherein the release of the US 2008/027420.6 A1 Nov. 6, 2008 active agent that is believed to be oxygen is controlled by an magnesium peroxide.