Compositions containing non-polar compounds

#Provided are compositions and methods for preparing foods and beverages that contain additives, such as nutraceuticals, pharmaceuticals and supplements.

#Non-polar compounds are not easily dissolved in aqueous solutions, such as water or any other polar solvent. A number of non-polar compounds are used in compositions for human ingestion, for example, pharmaceuticals, nutraceuticals and/or dietary supplements. Exemplary of non-polar compounds used in such compositions are vitamins and minerals, fatty acids, and other non-polar compounds, non-polar active agents, and non-polar active ingredients.

#Because of poor water solubility, inclusion of non-polar compounds in products for human consumption, for example, supplements, foods and beverages, often is challenging. Available compositions containing non-polar compounds, particularly aqueous compositions containing non-polar compounds, and methods for formulating such compositions, are limited. Thus, there remains a need to develop compositions containing non-polar compounds and methods for making the compositions. Accordingly, it is among the objects herein to provide compositions, including aqueous compositions, containing non-polar compounds, and methods for making the compositions.

#FIG. 1 sets forth an exemplary scaled-up process 100 of the provided methods for making the liquid nanoemulsion concentrates. This process is exemplary and variations can be used. In this example, water 101 is used as the polar solvent and the water first is purified by passage through the following purifiers, sequentially, in the following order: a carbon filter 105, ion exchange equipment 106, reverse osmosis equipment 107, a 100 micron end-point filter 108, and a 50 micron point-of-use filter 109. After purification, the water is added, with the other water phase ingredients, to a water phase tank 103. In other examples, the polar solvent is another polar solvent, such as glycerin or propylene glycol. In the illustrated example, the water phase ingredient(s) then are mixed using a standard mixer 111 attached to the tank, for example, mounted on the top of the tank. A heating apparatus (typically the water jacket on the water phase tank) is used to heat the water phase ingredients during water phase generation, typically to low heat (e.g., 60° C.). To generate the oil phase, the oil phase ingredient(s) are weighed/measured and added to an oil phase tank 102. The oil phase ingredients are mixed using a standard mixer 111 attached to the oil phase tank, for example, mounted on the tank. A heating apparatus (typically the water jacket on the oil phase tank) is used to heat the oil phase ingredients during water phase generation, typically to low heat (e.g., 60° C.). Once the oil and water phases reach 60° C., and after oil phase components have dissolved, the oil and water phases are combined by transferring the oil phase to the water phase vessel, via transfer means 112. For this process, a homogenizer 110 mounted on the water phase tank, is turned on, for example, at 850-1200 rpm. The ball valves then are opened and the transfer pump turned on, thereby effecting transfer of the oil phase liquid to the water phase tank via the transfer hose(s). As the phases are combined, the mixture is homogenized by continued mixing with the homogenizer 110. The homogenizer can be adjusted, for example, by adjusting the baffle plate on the homogenizer to achieve and maintain an emulsion, for example, by moving the baffle plate further into the forming emulsion and/or further out of the forming emulsion. During the emulsifying step, the forming emulsion is cooled, typically rapidly cooled, by repeatedly passing the forming emulsion through a recirculating cooler 115 (e.g., Model No. OC-1000 RO, sold by Turmoil, West Swanzey, N.H.), which is attached to the water phase tank. The emulsion is transferred, via transfer means 112 to a holding/packaging tank 104, where additional ingredients can be added and/or the mixture can be evaluated. The additional ingredients are mixed into the concentrate using a standard mixer 111. An end-product filter 113 is used to filter the concentrate before use.

#A. DEFINITIONS . . . 31 B. COMPOSITIONS CONTAINING NON-POLAR COMPOUNDS . . . 64 1. Liquid nanoemulsion concentrates containing the non-polar compounds . . . 66 a. Formulating the liquid concentrates . . . 68 i. Common ingredients and typical concentration ranges . . . 70 ii. Evaluation of the initial concentrate . . . 72 (1) Clarity . . . 73 (2) Empirical evaluation . . . 75 (3) Particle size . . . 76 (4) Turbidity measurement . . . 77 iii. Selecting a formulation and modifying formulations . . . 78 b. Non-Polar Compounds . . . 79 i. Polyunsaturated Fatty Acid (PUFA)-containing active ingredients . . . 82 (1) Omega-3 fatty acid compounds . . . 84 (a) DHA/EPA . . . 84 (i) Fish Oils . . . 85 (ii) Algae oil . . . 87 (b) Flax Seed Oil—omega 3 (ALA) . . . 88 (2) Omega-6 compounds . . . 89 (a) Borage oil (Gamma-Linolenic Acid (GLA)) . . . 89 (3) Saw Palmetto extract . . . 90 (4) Conjugated Linoleic Acid (CLA) . . . 90 ii. Coenzyme Q Active Ingredients . . . 91 (1) Coenzyme Q10 . . . 91 iii. Phytosterol-Containing Active Ingredients . . . 92 c. Surfactants . . . 93 i. Vitamin E derived surfactants . . . 95 (1) PEG-Derivatives of Vitamin E . . . 95 (a) Tocopherols and Tocotrienols . . . 97 (b) PEG moieties . . . 97 (c) Linkers . . . 98 (d) Tocopherol polyethylene glycol and Tocotrienol polyethylene glycol diesters (dicarboxylic acid esters of Vitamin E linked to PEG) . . . 98 (e) Other Vitamin E PEG Esters . . . 100 (f) TPGS Surfactants . . . 101 ii. Concentration of the surfactant . . . 102 iii. HLB . . . 103 d. Co-surfactants (emulsifiers) . . . 104 i. Phospholipids . . . 104 e. Polar solvents . . . 105 f. Preservatives and Sterilizers . . . 108 g. Emulsion stabilizers (co-emulsifier) . . . 108 h. Non-polar solvents . . . 110 i. Flavors . . . 110 j. pH adjusters . . . 111 2. Powder forms of the compositions . . . 112 3. Liquid dilution compositions containing the diluted concentrates . . . 116 a. Clarity . . . 118 i. Clarity determined by empirical evaluation . . . 118 ii. Clarity determined by particle size or number of particles . . . 119 iii. Turbidity . . . 119 b. Stability . . . 120 c. Desirable characteristics for human consumption . . . 121 d. Safety . . . 122 e. Oral bioavailability . . . 122 C. METHODS FOR MAKING LIQUID NANOEMULSION CONCENTRATES CONTAINING NON-POLAR COMPOUNDS . . . 123 1. Equipment for making the concentrates . . . 123 2. Scales . . . 123 a. Purifiers, including filters . . . 124 b. Vessels for mixing the ingredients . . . 125 c. Mixers . . . 126 d. Heating apparatuses . . . 128 e. Cooling apparatuses . . . 128 f. Transfer means . . . 129 g. Evaluation equipment . . . 130 3. General methods for making the liquid nanoemulsion concentrates . . . 130 a. Generating the water phase . . . 132 i. Water phase ingredients . . . 133 b. Generating the oil phase . . . 134 i. Oil phase ingredients . . . 135 c. Combining and emulsifying the oil phase and the water phase . . . 136 i. Combining the oil and water phases . . . 136 ii. Emulsifying the oil and water phases . . . 137 iii. Cooling . . . 137 d. Additional steps . . . 138 i. Additional ingredients . . . 138 ii. Evaluation of the concentrate . . . 139 iii. Filtering the concentrate . . . 139 4. Bench-top process . . . 139 5. Scaled-up manufacturing processes . . . 141 a. Water purification . . . 142 b. Generation of the water phase and oil phase: . . . 142 c. Combining and emulsifying the phases . . . 143 d. Cooling . . . 144 e. Additional steps . . . 144 D. METHODS FOR MAKING THE LIQUID DILUTION COMPOSITIONS CONTAINING THE DILUTED CONCENTRATES . . . 145 1. Dilutions . . . 146 2. Analyzing the aqueous liquid dilution compositions containing the liquid concentrates . . . 147 a. Clarity/turbidity . . . 147 i. Empirical evaluation . . . 148 ii. Particle size . . . 148 iii. Turbidity measurement . . . 149 E. EXAMPLES . . . 150

#Unless defined otherwise, all technical and scientific terms used herein have the same meaning as is commonly understood by one of skill in the art to which the invention(s) belong. All patents, patent applications, published applications and publications, GENBANK sequences, websites and other published materials referred to throughout the entire disclosure herein, unless noted otherwise, are incorporated by reference in their entirety. In the event that there is a plurality of definitions for terms herein, those in this section prevail. Where reference is made to a URL or other such identifier or address, it is understood that such identifiers can change and particular information on the internet can come and go, but equivalent information is known and can be readily accessed, such as by searching the internet and/or appropriate databases. Reference thereto evidences the availability and public dissemination of such information.

#As used herein, colloid refers to a mixture containing two phases, a dispersed phase and a continuous phase, the dispersed phase containing particles (droplets) distributed throughout the continuous phase. Colloidal mixtures include aerosols, foams and dispersions, for example, emulsions, for example, nanoemulsions. A liquid colloid, for example, a nanoemulsion, can have a similar appearance, for example, clarity, to a solution, in which there is no dispersed phase.