Claims:We Claim:
1. A water soluble powder composition of curcuminoids with enhanced solubility and bioavailability, comprising curcuminoids or its metabolites and one or more additives.
2. A water soluble powder composition comprising:
1 to 50% w/w of curcuminoids or its metabolites,
1 to 90 % w/w of solubilizers,
1 to 90 % w/w of encapsulating agent, and
0.1 % to 90% w/w of one or more other additives.
3. A water soluble powder composition comprising:
1 to 50% w/w of curcuminoids or its metabolites,
1 to 90 % w/w of solubilizers,
1 to 90 % w/w of encapsulating agent,
0.1 to 10 % w/w of emulsifier/surfactant,
0.1 to 5.0 % w/w antitacking agent,
0.001 to 2.0 % w/w flavouring agent and
0.1 % to 90% w/w of one or more other additives.
4. The composition as claimed in claims 2 and 3, wherein said solubilizers are selected from the group consisting of polyvinylpyrrolidone, copolymers of polyvinylpyrrolidone, sugar alcohols like isomalt, sorbitol, xylitol or mannitol, cellulose derivatives (especially hydroxypropylmethyl cellulose (HPMC) and/or hydroxypropyl cellulose (HPC)), cyclodextrines and its derivatives, polyethoxylated castor oil (Cremophor) and combinations thereof.
5. The composition as claimed in claims 2 and 3, wherein said encapsulating agents are selected from the group consisting of wheat, potato, maize starches and their derivatives (modified starches (Hicap-100), dextrins, maltodextrins, glucose syrups, dextrose, polyols etc.), gum arabic and combinations thereof.
6. The composition as claimed in claim 3, wherein said emulsifiers are selected from the group consisting of sodium lauryl sulfate, ethanolamine lauryl sulfate, ethylamine lauryl sulfate, alkali metal and ammonium salts of sulfonated petroleum and paraffin oils; sodium salts of hydrocarbon sulfonic acids, such as dodecane-1-sulfonic acid and octadiene-1-sulfonic acid; sodium salts of alpha-olefin sulfonates; aralkyl sulfonates, such as sodium isopropyl benzene sulfonate, sodium dodecyl benzene sulfonate, sodium isobutyl naphthalene sulfonate, and the like; alkali metal and ammonium salts of sulfonate, and the like; alkali metal and ammonium salts of sulfonate dicarboxylic acid esters, such as sodium dioctyl sulfosuccinate disodium-n-octadecyl sulfo- succinate, and the like; alkali metal and ammonium salts of free acid of complex organic mono- and di- phosphate esters and the like. Nonionic emulsifiers, such as octyl- or nonylphenyl polyethoxyethanol, may also be used. Vinyl polymer latices having excellent stability are obtained when employing the alkali metal and ammonium salts of aromatic sulfonic acid, aralkyl sulfonates and long chain sulfonates and combinations thereof.
7. The composition as claimed in claim 3, wherein said anti-tacking agent is selected from the group consisting of talc, titanium dioxide, Colloidal silicon dioxide (Aerosil) and combinations thereof.
8. The composition as claimed in claims 2 and 3, may further comprise organic or inorganic solvent or mixtures thereof selected from isopropyl alcohol (IPA), acetone, ethanol, dichloromethane, water and mixtures thereof.
9. The composition as claimed in claim 3, wherein said flavouring agent referred above include D-limonene, thymol, vanillin, carvacrol, cinnamaldehyde, octanoic acid, heptanoic acid, diallyl disulfide, camphor, l-limonene, rosmarinic acid, p- cymene, ?-terpinene, a-pinene, a~thujone and 1,8- cineole; and - at least one organic acid chosen from the group comprising lactic acid, malic acid, benzoic acid, fumaric acid and sorbic acid or an alkali or alkaline earth metal salt thereof.
10. A process for preparing curcuminoid water soluble powder, the process comprising steps of:
a. adding encapsulating agent to solvent under continuous stirring by maintaining the temperature of 40°C and keeping the dispersion with continuous stirring for the 1hr by maintaining temperature of 40 °C (Phase 1),
b. adding anti-frothing agent to avoid froths during process,
c. adding NaOH pellets to the purified water to get 0.1 N NaOH solution and adding solubilizer/surfactant and curcuminoid into it under continuous stirring,
d. filtering the above dispersion if required and adding the citric acid anhydrous into the dispersion (Phase -2),
e. filtering the Phase -2 dispersion if required,
f. adding the Phase- 2 dispersion slowly into phase-1 dispersion under continuous stirring till getting homogenous dispersion,
g. adding flavouring agent into above dispersion and pass through high speed/pressure homogenization and adding anti-frothing agent to avoid froth observed during process,
h. drying the above dispersion using spray drying and/or vacuum tray drying,
i. blending the dried powder sample with antitacking agent using double lined polybags and sifting through mesh #60 ASTM, and
j. packing the blended powder.
11. A process for preparing curcuminoid water soluble powder, the process comprising steps of:
a. adding encapsulating agent to purified water under continuous stirring by maintaining the temperature of 40°C and keeping the dispersion with continuous stirring for the 1hr by maintaining temperature of 40 °C (Phase 1),
b. adding anti-frothing agent to avoid froths during process,
c. adding NaOH pellets to the purified water to get 0.1 N NaOH solution and adding solubilizer/surfactant and Curcumin Extract into it under continuous stirring,
d. filtering the above dispersion if required and adding the citric acid anhydrous into the dispersion (Phase -2),
e. filtering the Phase -2 dispersion if required,
f. adding the Phase- 2 dispersion slowly into phase-1 dispersion under continuous stirring till getting homogenous dispersion,
g. adding flavouring agent into above dispersion and pass through high speed/pressure homogenization and adding anti-frothing agent to avoid froth observed during process,
h. drying the above dispersion using spray drying and/or vacuum tray drying,
i. blending the dried powder sample with antitacking agent using double lined polybags and sifting through mesh #60 ASTM, and
j. packing the blended powder.
12. A process for preparing curcuminoids water soluble powder, the process comprising steps of:
a. adding encapsulating agent to solvent under continuous stirring by maintaining the temperature of 40°C,
b. adding emulsifier or surfactant to the above dispersion and keeping the dispersion with continuous stirring for the 1hr by maintaining temperature of 40 °C (Phase 1),
c. mixing the organic solvents together in a container/beaker and adding curcuminoids into it under a continuous stirring at temperature of 55°C then adding solubilizer by maintaining temperature of 55°C under continuous stirring,
d. adding stevia extract to the above dispersion under continuous stirring (Phase 1),
e. filtering the Phase -2 dispersion if required,
f. adding the Phase- 2 dispersion slowly into phase-1 dispersion under continuous stirring till getting homogenous dispersion,
g. drying the above dispersion using spray drying and/or vacuum tray drying,
h. blending the dried powder sample with presifted antitacking agent using double lined polybags and sifting through mesh #60 ASTM, and
i. Packing the blended powder.
13. A process for preparing curcuminoids water soluble powder, the process comprising steps of:
a. adding encapsulating agent to purified water under continuous stirring by maintaining the temperature of 40°C,
b. adding emulsifier or surfactant to the above dispersion and keeping the dispersion with continuous stirring for the 1hr by maintaining temperature of 40 °C (Phase 1),
c. mixing the organic solvents together in a container/beaker and adding Curcumin Extract into it under a continuous stirring at temperature of 55°C then adding solubilizer by maintaining temperature of 55°C under continuous stirring,
d. adding stevia extract to the above dispersion under continuous stirring (Phase 1),
e. filtering the Phase -2 dispersion if required,
f. adding the Phase- 2 dispersion slowly into phase-1 dispersion under continuous stirring till getting homogenous dispersion,
g. drying the above dispersion using spray drying and/or vacuum tray drying,
h. blending the dried powder sample with presifted antitacking agent using double lined polybags and sifting through mesh #60 ASTM, and
i. Packing the blended powder

Date this Twentieth (20th) day of June, 2017.

__________________________________
Dr. S. Padmaja
Agent for the Applicant
IN/PA/883 , Description:FORM 2

THE PATENTS ACT 1970
(SECTION 39 OF 1970)

&
THE PATENT RULES, 2003

COMPLETE SPECIFICATION
(SECTION 10)

COMPOSITIONS OF CURCUMINOIDS AND PROCESS FOR PREPARING SAME

We, SARVOTHAM CARE LIMITED,
a company incorporated under the companies act, 1956 having address at 1-20-248, Umajay complex, 1st floor, Rasoolpura, Secunderabad- 500 003,
Telangana State, India.

The following specification particularly describes the invention and the manner in which it is to be performed.
FIELD OF INVENTION
The present invention relates to compositions of curcuminoids. The present invention specifically relates to powder compositions of curcuminoids or its metabolites and methods for preparation thereof. The present invention more specifically relates to a water soluble powder composition and process for the preparation of curcuminoids or its metabolites thereof.

BACKGROUND OF INVENTION
Turmeric is a curry spice obtained from the rhizome of Curcuma longa of the ginger family, and has a long history of use in ayurvedic medicine and in traditional Asian diets. The principle bioactive component of turmeric is curcumin. Curcumin is known as diferuloylmethane. It is chemically described as 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadien-3,5-dione and has an empirical chemical formula C21H20O6. Curcumin is an orange-yellow crystalline powder and is an oil soluble pigment, practically insoluble in water at acidic and neutral pH, soluble in alkali, insoluble in ether and soluble in alcohol, glacial acetic acid. The curcumin is used widely for food colouring, but also as a nutraceutical. The rhizomes of Curcuma longa also contain minor amounts of oils and resins.
Curcumin can exist in at least two tautomeric forms, keto and enol. It is a tautomeric compound existing in enolic form in organic solvents and as a keto form in water.

Curcumin (keto form)

Curcumin (enol form)
Commercial curcumin contains curcumin itself (77%), demethoxycurcumin (DMC, 17%) and bisdemethoxycurcumin (BDMC, 3%); the latter two differ from curcumin only by lacking one or both methoxy groups, respectively. As a group these compounds and their derivatives for pharmaceutical use are referred to as curcuminoids. Among the major cellular metabolites of these three compounds are the tetrahydrocurcuminoids, in which both vinylidene groups are reduced, i.e., THC (i.e., tetrahydrocurcumin), TDMC and TBDMC. The tetrahydrocurcuminoids retain the bioactivity but are colorless and more chemically stable than the curcuminoids; In order to have curcumin be suitable for dietary use, the sum of the curcumin and the demethoxylated derivatives thereof must be not less than 90% of the total weight.
Tetrahydrocurcumin (THC), is a product of bacterial or intestinal metabolism of curcumin (via the bacterial enzyme NADPH-dependent curcumin reductase). In E. coli curcumin is a substrate for the enzyme NADPH-dependent curcumin reductase which catalyzes the metal-independent reduction of curcumin to dihydrocurcumin (DHC) as an intermediate product, followed by further reduction to tetrahydrocurcumin (THC) as an end product. Tetrahydrocurcumin (THC) exhibits many of the same physiologic and pharmacological activities as curcumin and in some systems may exert greater antioxidant activity than curcumin.

Curcumin is a very powerful antioxidant. Its antioxidant effect has been reported to be eight times more powerful than that of vitamin E. A number of studies provide evidence for the therapeutic properties of naturally occurring curcuminoids and synthetic curcuminoid derivatives, in particular their anti-cancer activity (for example, Pisano et al., Mol Cancer. 2010, 3;9(1):137; Bisht et al., J Nanobiotechnology. 2007, 5:3). There are also reports on other pharmacological activities of curcumin including anti-microbial and anti-inflammatory effects (Begum et al., J Pharmacol Exp Ther. 2008, 326 (1):196-208).
Although curcuminoids have been suggested for a variety of therapeutic and prophylactic applications, a major impediment in this development is the very low bioavailability of orally administered curcumin. For example, it has been reported that serum levels in humans after an oral dose of 2 g curcumin alone were either undetectable or very low. Reasons contributing to this effect are the low solubility and poor absorption of curcumin in the digestive tract as well as its rapid metabolism, in particular in the liver, and rapid systemic elimination. Thus, the serum curcumin levels sufficient to provoke the desired beneficial effect of this compound cannot be achieved by the mere consumption of turmeric with the food. Concomitant administration of piperine, an inhibitor of enzymes involved in drug metabolism, has been shown to increase the curcumin absorption and thus the serum concentration of curcumin. However, it is a significant downside of this approach that the piperine induced inhibition of drug metabolism may lead to unwanted effects, in particular when other medications are taken. (Anand et al., Mol. Pharm 2007 4(6):807-18; Shoba et al., Planta Med 1998 64(4):353-6).
WO 2007/103435 A relates to a curcuminoid composition having an enhanced bioavailability and comprising a curcuminoid, an antioxidant and a water-solubilizing, pharmaceutically acceptable carrier and further optionally a glucuronidation inhibitor.
IN 1827/DEL/2008 relates to curcumin nanoparticles and curcumin bound to chitosan nanoparticles and methods of producing the same. The bioavailability of curcumin in these formulations was shown to improve by more than 10 fold.
IN 5359/CHE/2015 relates to spray dried granulate of curcuminoids and process for preparation thereof.
US 8,568,815 B2 relates to a method of producing the curcumin water-soluble complex comprising curcumin, an alkyl ether derivative of gamma-cyclodextrin with the specified molar ratio in an aqueous phase at specified pH.
US 2009/0324703 A1 relates to the curcuminoid composition with enhanced bioavailability comprising the curcuminoid, antioxidant and phosphatidylcholine as water-solubilizing carrier.
US 2015/0011525 A1 relates to the stable ternary solid dispersion composition with enhanced bioavailability comprising poorly soluble active pharmaceutical ingredient (API) belongs to BCS class II /IV, water-soluble polymers, crosslinked polyvinylpyrrolidone (copovidone) and is formed by hot-melt extrusion in the absence of a solvent, capable of inhibiting crystallization of API in the solid state.
Int. J. of Pharm. & Life Sci. (IJPLS), Vol. 3, Issue 3: March: 2012, 1490-1497-1490 discloses methods for increasing solubility of drug using solid dispersion technique. The solid binary systems were prepared using different drug: polymer ratio (1:1, 1:4 and 1:8) with polyethylene glycol 4000 and 6000 by different techniques like physical mixing, melting method and solvent evaporation method.
The above prior art references discloses different compositions and process for the preparations for of curcuminoids or its metabolites thereof. However, the inventors of the present invention have formulated novel compositions with process which will provide enhanced solubility, dissolution and bioavailability of the curcuminoids or its metabolites.
OBJECTIVE OF INVENTION
The objective of the present invention is to provide a water soluble powder compositions of curcuminoids or its metabolites and process for the preparation thereof.
Another objective of the present invention is to provide water soluble powder formulation compositions of curcuminoids or its metabolites with enhanced solubility profile and bioavailability.

SUMMARY OF INVENTION
The present invention provides water soluble powder compositions of curcuminoids or its metabolites and methods for the preparation thereof.
The present invention provides a water soluble powder composition comprising curcuminoids or its metabolites and one or more additives.
One embodiment of the present invention provides use of curcuminoid water soluble powder, for making nutraceuticals, dietary supplements, foods, cosmetics and pharmaceuticals such as tablets, capsules, solutions, suspensions, gums and chewing gums.
One embodiment of the present invention provides a process for preparation of curcumin water soluble powder, wherein the curcumin is transformed from crystalline form to amorphous form during the preparation process.
One embodiment of the present invention provides a water soluble powder composition of curcuminoids with enhanced solubility and bioavailability of curcuminoids.
Another embodiment of the present invention provides a water soluble powder composition comprising:
1 to 50% w/w of curcuminoids or its metabolites,
1 to 90 % w/w of solubilizers,
1 to 90 % w/w of encapsulating agent, and
0.1 % to 90% w/w of one or more other additives.
Another embodiment of the present invention provides a water soluble powder composition comprising:
1 to 50% w/w of curcuminoids or its metabolites,
1 to 90 % w/w of solubilizers,
1 to 90 % w/w of encapsulating agent,
0.1 to 10 % w/w of emulsifier/surfactant,
0.1 to 5.0 % w/w antitacking agent,
0.001 to 2.0 % w/w flavouring agent and
0.1 % to 90% w/w of one or more other additives.
Another embodiment of the present invention provides a water soluble powder composition comprising:
1 to 50% w/w of curcuminoids or its metabolites,
1 to 90 % w/w of Polyvinylpyrrolidone,
1 to 90 % w/w of Hicap-100,
0.2 to 5% of Sodium hydroxide,
0.1 % to 10% w/w of Citric acid anhydrous,
0.001 % to 2% D-limonene,
0.1 to 5 % w/w of Aerosil,
0.1 % to 90% w/w of one or more other additives.
Another embodiment of the present invention provides a water soluble powder composition comprising:
1 to 50% w/w of Curcumin or its metabolites,
1 to 90 % w/w of Polyvinylpyrrolidone,
1 to 90 % w/w of Hicap-100,
0.2 to 5% of Sodium hydroxide,
0.1 % to 10% w/w of Citric acid anhydrous,
0.1 to 10 % w/w of Sodium Lauryl Sulphate (SLS),
0.001 % to 2% D-limonene,
0.1 to 5 % w/w of Aerosil,
0.1 % to 90% w/w of one or more other additives.
Another embodiment of the present invention provides a water soluble powder composition comprising:
1 to 50% w/w of Curcumin or its metabolites,
1 to 90 % w/w of Polyvinylpyrrolidone,
1 to 90 % w/w of Hicap-100,
0.1 to 10 % w/w of Sodium Lauryl Sulphate (SLS),
0.1 to 5 % w/w of Aerosil,
0.1 % to 20% w/w of Stevia extract, and
0.1 % to 90% w/w of one or more other additives.
Yet another embodiment of the present invention provides a process for preparing curcuminoid water soluble powder, the process comprising steps of:
a. adding encapsulating agent to solvent under continuous stirring by maintaining the temperature of 40°C and keeping the dispersion with continuous stirring for the 1hr by maintaining temperature of 40 °C (Phase 1),
b. adding anti-frothing agent to avoid froths during process,
c. adding NaOH pellets to the purified water to get 0.1 N NaOH solution and adding solubilizer/surfactant and curcuminoid into it under continuous stirring,
d. filtering the above dispersion if required and adding the citric acid anhydrous into the dispersion (Phase -2),
e. filtering the Phase -2 dispersion if required,
f. adding the Phase- 2 dispersion slowly into phase-1 dispersion under continuous stirring till getting homogenous dispersion,
g. adding flavouring agent into above dispersion and pass through high speed/pressure homogenization and adding anti-frothing agent to avoid froth observed during process,
h. drying the above dispersion using spray drying and/or vacuum tray drying,
i. blending the dried powder sample with antitacking agent using double lined polybags and sifting through mesh #60 ASTM, and
j. packing the blended powder.
Yet another embodiment of the present invention provides a process for preparing curcuminoid water soluble powder, the process comprising steps of:
a. adding encapsulating agent to purified water under continuous stirring by maintaining the temperature of 40°C and keeping the dispersion with continuous stirring for the 1hr by maintaining temperature of 40 °C (Phase 1),
b. adding anti-frothing agent to avoid froths during process,
c. adding NaOH pellets to the purified water to get 0.1 N NaOH solution and adding solubilizer/surfactant and Curcumin Extract into it under continuous stirring,
d. filtering the above dispersion if required and adding the citric acid anhydrous into the dispersion (Phase -2),
e. filtering the Phase -2 dispersion if required,
f. adding the Phase- 2 dispersion slowly into phase-1 dispersion under continuous stirring till getting homogenous dispersion,
g. adding flavouring agent into above dispersion and pass through high speed/pressure homogenization and adding anti-frothing agent to avoid froth observed during process,
h. drying the above dispersion using spray drying and/or vacuum tray drying,
i. blending the dried powder sample with antitacking agent using double lined polybags and sifting through mesh #60 ASTM, and
j. packing the blended powder.
Yet another embodiment of the present invention provides a process for preparing curcuminoids water soluble powder, the process comprising steps of:
a. adding encapsulating agent to solvent under continuous stirring by maintaining the temperature of 40°C,
b. adding emulsifier or surfactant to the above dispersion and keeping the dispersion with continuous stirring for the 1hr by maintaining temperature of 40 °C (Phase 1),
c. mixing the organic solvents together in a container/beaker and adding curcuminoids into it under a continuous stirring at temperature of 55°C then adding solubilizer by maintaining temperature of 55°C under continuous stirring,
d. adding stevia extract to the above dispersion under continuous stirring (Phase 1),
e. filtering the Phase -2 dispersion if required,
f. adding the Phase- 2 dispersion slowly into phase-1 dispersion under continuous stirring till getting homogenous dispersion,
g. drying the above dispersion using spray drying and/or vacuum tray drying,
h. blending the dried powder sample with presifted antitacking agent using double lined polybags and sifting through mesh #60 ASTM, and
i. Packing the blended powder.
Yet another embodiment of the present invention provides a process for preparing curcuminoids water soluble powder, the process comprising steps of:
a. adding encapsulating agent to purified water under continuous stirring by maintaining the temperature of 40°C,
b. adding emulsifier or surfactant to the above dispersion and keeping the dispersion with continuous stirring for the 1hr by maintaining temperature of 40 °C (Phase 1),
c. mixing the organic solvents together in a container/beaker and adding Curcumin Extract into it under a continuous stirring at temperature of 55°C then adding solubilizer by maintaining temperature of 55°C under continuous stirring,
d. adding stevia extract to the above dispersion under continuous stirring (Phase 1),
e. filtering the Phase -2 dispersion if required,
f. adding the Phase- 2 dispersion slowly into phase-1 dispersion under continuous stirring till getting homogenous dispersion,
g. drying the above dispersion using spray drying and/or vacuum tray drying,
h. blending the dried powder sample with presifted antitacking agent using double lined polybags and sifting through mesh #60 ASTM, and
i. Packing the blended powder.

DETAILED DESCRIPTION OF THE INVENTION
The term "comprising", which is synonymous with "including", "containing", or "characterized by" here is defined as being inclusive or open-ended, and does not exclude additional, unrecited elements or method steps, unless the context clearly requires otherwise.
The terms "curcumin", "curcuminoid" and "curcuminoids" may be used interchangeably unless otherwise stated differently. The Native curcumin may comprise curcumin, demethoxycurcumin, bisdemethoxycurcumin and mixtures thereof. Generally a mixture of two or more components selected from curcumin, demethoxycurcumin, bisdemethoxycurcumin and other curcumin derivatives is referred to as "curcuminoids" whereas a single component such as curcumin is referred to as "curcuminoid".
The curcuminoid(s) as used herein selected from a group comprising curcumin, tetrahydrocurcumin, tetrahydrodemethoxycurcumin, tetrahydrobisdemethoxy curcumin, curcumin derivative and mixtures thereof.
The curcumin composition of the present invention can be used for the treatment of different conditions of humans includes pro-inflammatory diseases including cancer, cardiovascular disease, arthritis, uveitis, ulcerative proctitis, Crohn’s disease, ulcerative colitis, irritable bowel disease, tropical pancreatitis, peptic ulcer, gastric ulcer, idiopathic orbital inflammatory pseudotumor, oral lichen planus, gastric inflammation, vitiligo, psoriasis, acute coronary syndrome, atherosclerosis, diabetes, diabetic nephropathy, diabetic microangiopathy, lupus nephritis, renal conditions, acquired immunodeficiency syndrome, ß-thalassemia, biliary dyskinesia, Dejerine-Sottas disease, cholecystitis, and chronic bacterial prostatitis.
The curcuminoid composition of the present invention can be used for the preparation of nutraceuticals, dietary supplements, foods, cosmetics, skin preparations and pharmaceuticals such as tablets, capsules, solutions, suspensions, gums and chewing gums.
Preferred solubilizers referred above include polyvinylpyrrolidone, copolymers of polyvinylpyrrolidone, sugar alcohols like isomalt, sorbitol, xylitol or mannitol, cellulose derivatives (especially hydroxypropylmethyl cellulose (HPMC) and/or hydroxypropyl cellulose (HPC)), cyclodextrines and its derivatives, polyethoxylated castor oil (Cremophor) and combinations thereof. Preferably polyvinylpyrrolidone and copolymers of polyvinylpyrrolidone.
Preferred encapsulating agents referred above include wheat, potato, maize starches and their derivatives (modified starches (Hicap-100), dextrins, maltodextrins, glucose syrups, dextrose, polyols etc.), gum arabic and combinations thereof. Preferably Hicap-100.
Preferred emulsifiers or surfactants referred above include sodium lauryl sulfate, ethanolamine lauryl sulfate, ethylamine lauryl sulfate, D-limonene, alkali metal and ammonium salts of sulfonated petroleum and paraffin oils; sodium salts of hydrocarbon sulfonic acids, such as dodecane-1-sulfonic acid and octadiene-1-sulfonic acid; sodium salts of alpha-olefin sulfonates; aralkyl sulfonates, such as sodium isopropyl benzene sulfonate, sodium dodecyl benzene sulfonate, sodium isobutyl naphthalene sulfonate, and the like; alkali metal and ammonium salts of sulfonate, and the like; alkali metal and ammonium salts of sulfonate dicarboxylic acid esters, such as sodium dioctyl sulfosuccinate disodium-n-octadecyl sulfo- succinate, and the like; alkali metal and ammonium salts of free acid of complex organic mono- and di- phosphate esters and the like. Nonionic emulsifiers, such as octyl- or nonylphenyl polyethoxyethanol, may also be used. Vinyl polymer latices having excellent stability are obtained when employing the alkali metal and ammonium salts of aromatic sulfonic acid, aralkyl sulfonates and long chain sulfonates and combinations thereof. Preferably sodium lauryl sulfate.
Preferred anti-tacking agent referred above include talc, titanium dioxide, Colloidal silicon dioxide (Aerosil) and combinations thereof. Preferably Colloidal silicon dioxide (Aerosil).
Preferred flavouring agent referred above include D-limonene, thymol, vanillin, carvacrol, cinnamaldehyde, octanoic acid, heptanoic acid, diallyl disulfide, camphor, l-limonene, rosmarinic acid, p- cymene, ?-terpinene, a-pinene, a~thujone and 1,8- cineole; and - at least one organic acid chosen from the group comprising lactic acid, malic acid, benzoic acid, fumaric acid and sorbic acid or an alkali or alkaline earth metal salt thereof.
Preferred anti-frothing agent referred above include simethicone, simethicone emulsion, methyl oleate, glyceryl oleate, sorbitan laurate, sorbitan oleate, or the like.
Preferred solvents used in the compositions of the present invention organic or inorganic solvent or mixtures thereof selected from isopropyl alcohol (IPA), acetone, ethanol, dichloromethane, water and mixtures thereof.
Other additives used in the preparations to the compositions of this invention, the following can be used and there were no limitations: stabilizer, surfactant, plasticizer, lubricant, reducing agent, buffer agent, sweetening agent, base, adsorbent, corrigent, binder, suspending agent, antioxidant, polish, coating, wetting agent, wet modifier, filler, antifoaming agent, refrigerative agent, coloring matter, flavoring agent, perfume, sugar coating agent, isotonizing agent, softener, emulsifying agent, foaming agent, pH modifier, anti-frothing agents, diluent, excipient, dispersing agent, disintegrator, fragrance, desiccant, antiseptics, preservative, solubilizing agent, solubilizer, solvent, superplasticizer, antistatic agent, extender, moisturizing agent, and the like.
The following examples describes the nature of the invention and are given only for the purpose of illustrating the present invention in more detail and are not limitative and relate to solutions which have been particularly effective on a bench scale:
Example 1:
S.No. Ingredients %w/w
1. Curcumin Extract-95% 10.1
2. Polyvinylpyrrolidone (PVP-K-30) 30.0
3. Hicap-100 56.19
4. Sodium hydroxide (NaOH) 0.43
5. Citric Acid, Anhydrous 1.68
6. D-limonene 1.0
7. Anti-frothing Agent 0.10
8. Purified Water 170.0
9. Aerosil 200 or Cab-O-Sil 0.50
Theoretical Set Assay (Overages: 20%) 9.6%

Example 2:
S.No. Ingredients %w/w
1. Curcumin Extract-95% 12.6
2. Polyvinylpyrrolidone (PVP-K-30) 42.0
3. Hicap-100 41.19
4. Sodium hydroxide (NaOH) 0.67
5. Citric Acid, Anhydrous 2.04
6. D-limonene 1.0
7. Anti-frothing Agent 0.10
8. Purified Water 240.0
9. Aerosil 200 or Cab-O-Sil 0.50
Theoretical Set Assay (Overages: 20%) 12.0%

Example 3:
S.No. Ingredients %w/w
1. Curcumin Extract-95% 25.2
2. Polyvinylpyrrolidone (PVP-K-30) 45.0
3. Hicap-100 22.92
4. Sodium hydroxide (NaOH) 1.06
5. Citric Acid, Anhydrous 4.22
6. D-limonene 1.0
7. Anti-frothing Agent 0.10
8. Purified Water 320.0
9. Aerosil 200 or Cab-O-Sil 0.50
Theoretical Set Assay (Overages: 20%) 24.0%

Example 4:
S.No. Ingredients %w/w
1. Curcumin Extract-95% 10.1
2. Polyvinylpyrrolidone (PVP-K-30) 30.0
3. Hicap-100 54.69
4. Sodium hydroxide (NaOH) 0.43
5. Citric Acid, Anhydrous 1.68
6. Sodium lauryl Sulfate (SLS) 1.5
7. D-limonene 1.0
8. Anti-frothing Agent 0.10
9. Purified Water 170.0
10. Aerosil 200 or Cab-O-Sil 0.50
Theoretical Set Assay (Overages: 20%) 9.6%

Example 5:
S.No. Ingredients %w/w
1. Curcumin Extract-95% 12.6
2. Polyvinylpyrrolidone (PVP-K-30) 42.0
3. Hicap-100 39.69
4. Sodium hydroxide (NaOH) 0.67
5. Citric Acid, Anhydrous 2.04
6. Sodium lauryl Sulfate (SLS) 1.5
7. D-limonene 1.0
8. Anti-frothing Agent 0.10
9. Purified Water 240.0
10. Aerosil 200 or Cab-O-Sil 0.50
Theoretical Set Assay (Overages: 20%) 12.0%

Example 6:
S.No. Ingredients %w/w
1. Curcumin Extract-95% 25.2
2. Polyvinylpyrrolidone (PVP-K-30) 45.0
3. Hicap-100 21.42
4. Sodium hydroxide (NaOH) 1.06
5. Citric Acid, Anhydrous 4.22
6. Sodium lauryl Sulfate (SLS) 1.5
7. D-limonene 1.0
8. Anti-frothing Agent 0.10
9. Purified Water 320.0
10. Aerosil 200 or Cab-O-Sil 0.50
Theoretical Set Assay (Overages: 20%) 24.0%

Example 7:
S.No. Ingredients %w/w
1. Curcumin Extract 95% 10.1
2. Polyvinylpyrrolidone (PVP-K-30) 30.0
3. Hicap-100 53.9
4. Sodium Lauryl Sulphate (SLS) 1.5
5. Dichloromethane (DCM) q.s
6. Ethanol (Pure) q.s
7. Purified water q.s
8. Stevia Extract 4.0
9. Aerosil 200 0.5
Theoretical Set Assay (Overages: 20%) 9.6 %

Example 8:
S.No. Ingredients %w/w
1. Curcumin Extract 95% 12.6
2. Polyvinylpyrrolidone (PVP-K-30) 35.0
3. Hicap-100 45.4
4. Sodium Lauryl Sulphate (SLS) 1.5
5. Dichloromethane (DCM) q.s
6. Ethanol (Pure) q.s
7. Purified water q.s
8. Stevia Extract 5
9. Aerosil 200 0.5
Theoretical Set Assay (Overages: 20%) 12.0 %

Example 9:
S.No. Ingredients %w/w
1. Curcumin Extract 95% 25.2
2. Polyvinylpyrrolidone (PVP-K-30) 40.0
3. Hicap-100 22.8
4. Sodium Lauryl Sulphate (SLS) 1.5
5. Dichloromethane (DCM) q.s
6. Ethanol (Pure) q.s
7. Purified water q.s
8. Stevia Extract 10.0
9. Aerosil 200 0.5
Theoretical Set Assay (Overages: 20%) 24.0 %

Example 10:
S.No. Ingredients %w/w
1. Tetrahydrocurcumin 95% 12.6
2. Polyvinylpyrrolidone (PVP-K-30) 45.0
3. Hicap-100 40.4
4. Sodium Lauryl Sulphate (SLS) 1.5
5. Ethanol (Pure) 75.0
6. Purified water 50.0
7. Aerosil 200 (Cab-O-Sil) 0.5
Theoretical Set Assay (Overages: 20%) 12.0%

Example 11:
S.No. Ingredients %w/w
1. Tetrahydrocurcumin 95% 25.2
2. Polyvinylpyrrolidone (PVP-K-30) 45.0
3. Hicap-100 27.5
4. Sodium Lauryl Sulphate (SLS) 1.5
5. Ethanol (Pure) 125.0
6. Purified water 75.0
7. Aerosil 200 (Cab-O-Sil) 0.5
Theoretical Set Assay (Overages: 20%) 24.0%

Example 12:
S.No. Ingredients %w/w
1. Tetrahydrocurcumin 95% 12.6
2. Polyvinylpyrrolidone (PVP-K-30) 42.0
3. Hicap-100 41.09
4. Sodium hydroxide (NaOH) 0.67
5. Citric Acid, Anhydrous 2.04
6. D-limonene 1.0
7. Anti-frothing Agent 0.10
8. Purified water 240.0
9. Aerosil 200 (Cab-O-Sil) 0.5
Theoretical Set Assay (Overages: 20%) 12.0%

Example 13:
S.No. Ingredients %w/w
1. Tetrahydrocurcumin 95% 25.2
2. Polyvinylpyrrolidone (PVP-K-30) 45.0
3. Hicap-100 22.92
4. Sodium hydroxide (NaOH) 1.06
5. Citric Acid, Anhydrous 4.22
6. D-limonene 1.0
7. Anti-frothing Agent 0.10
8. Purified water 400
9. Aerosil 200 (Cab-O-Sil) 0.5
Theoretical Set Assay (Overages: 20%) 24.0%

Solubility Study:
The compositions of the present invention have high water solubility. The solubility data are generated and given below:
Dissolution Media Name of Product Example No Solubility (mg/mL) Solubility (ppm)
Water N-Curcumin WSP 10% Example 2 2.2666 2266.63
N-Curcumin WSP 20% Example 3 2.2489 2248.88
N-Curcumin WSP 10% Example 5 2.3718 2371.79
N-Curcumin WSP 20% Example 6 2.2033 2203.30
Curcumin API 95% 0.0002 0.20

Curcumin saturated solubility was determined and compared to Curcumin API. The water profile was determined and solubility was found to be high solubility boundary of Curcumin. Thus, at all curcumin water soluble product required less than 30 mL to dissolve the 1mg dose strength of curcumin.

Dissolution Study:
The compositions of the present invention having higher dissolution compared with API are given below:
Min Curcumin API 95% Example No 2 Example No 3 Example No 5 Example No
6
15 17.7 46.4 50.8 76.2 48.0
30 31.1 62.9 62.9 95.8 62.0
45 38.6 73.5 72.6 103.3 71.9
60 43.2 82.9 76.5 103.5 76.0
90 51.0 82.8 83.5 104.1 83.5
120 57.5 92.2 89.6 104.4 87.2

Stability Study:
3M Stability data carried out at 40 °C and 75%RH of different compositions is shown in the table given below:
Example No Initial Assay
(% Curcuminoids) Assay (% Curcuminoids)
1M 2M 3M
2 12.4 12.3 12.1 11.7
3 21.7 21.2 21.1 20.9
5 11.46 11.5 11.40 11.26

The above data shows that Curcumin of the present invention has high solubility, better dissolution and long term stability.