WO2024252433A1 - Composition synergique pour améliorer la solubilité, la stabilité, la biodisponibilité et la libération immédiate de composés actifs - Google Patents

Composition synergique pour améliorer la solubilité, la stabilité, la biodisponibilité et la libération immédiate de composés actifs Download PDF

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WO2024252433A1
WO2024252433A1 PCT/IN2024/050717 IN2024050717W WO2024252433A1 WO 2024252433 A1 WO2024252433 A1 WO 2024252433A1 IN 2024050717 W IN2024050717 W IN 2024050717W WO 2024252433 A1 WO2024252433 A1 WO 2024252433A1
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extract
composition
soluble
mixture
protein
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Somashekara NIRVANASHETTY
Vivek Anand PARACHUR
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Olene Life Sciences Pvt Ltd
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Olene Life Sciences Pvt Ltd
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    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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Definitions

  • the present invention relates to a stable, synergistic composition for enhancing the solubility/dispersibility, bioavailability and immediate release of active compounds.
  • the present invention also relates to a process for preparation of said synergistic composition.
  • Natural products and extracts of natural products have a wide range of applications in food, nutraceutical and pharmaceutical industries. Most of the crude natural extracts are in viscous liquid form compared to the highly purified extracts and are very difficult to handle while formulating or manufacturing. It also cost a lot to the manufacturer in terms of product loss and other cleaning and processing expenses. However, these crude liquid extracts contain several synergistic active compounds as compared to their purified versions and may have higher safety and synergistic efficacy. On the other hand, the purified extracts are hydrophobic in nature and not soluble/dispersible in aqueous phase. Hence, formulating them into beverages and ready to drink beverages is difficult.
  • the dry extracts are not dispersible or soluble in the aqueous media and hence will have poor absorption in the gastro intestinal system, which will lead to lower efficacy.
  • Excipients such as maltodextrin has higher glycemic index and hence not suitable for people with diabetes as it may spike blood glucose levels.
  • Certain ingredients of high oil absorption capacity such as silicon dioxides are limited in the products.
  • the gums and mucilage when used individually are low in oil absorption capacity and often leads to the unstable, poorly soluble, bioavailable and oily products with low actives. They are oily and hygroscopic which hampers their use in manufacturing the finished products or filling into the capsules etc.
  • gums and mucilage will have limited application in enhancing the solubility/dispersion of the dry extracts with unacceptable solution/suspension stability.
  • Mucilage’s when used along with the active compounds will give high viscosity products which are difficult to dissolve in aqueous solutions making it unsuitable for supplement, food and beverage applications. This will lead very poor release of actives, poor bioavailability and reduced efficacy.
  • the extract loading capacity is the efficiency of the composition or an ingredient to convert liquid or oil or dry extract in to free flowing powder with high physico chemical properties such as free flowing, non-hygroscopic products with high actives and complete water solubility/dispersion.
  • ingredients or excipients are having high oil absorption or loading capacity, they always lead to hygroscopic, oily, water insoluble, products with low suspension stability and poorly bioavailable products.
  • both the concentration of actives and its aqueous solubility/suspension with good stability are essential.
  • Many of the products with low actives have to be dosed in higher quantities which is not acceptable to the general population and also may have side effects due to higher levels of excipients.
  • US20110081330 discloses a composition
  • a composition comprising gum ghatti and one or more fatsoluble active ingredients, wherein the composition comprises less than 40 weight % oil, based on the total composition in dry matter.
  • the said composition additionally comprises one or more oligosaccharides such as maltodextrin and said composition is used for the enrichment, fortification and/or coloration of food beverages, animal feed, cosmetics or pharmaceutical compositions.
  • US20080102131 disclose a particulate composition wherein an oil component (A) comprising a water-insoluble bioactive substance is poly-dispersed while forming a domain in a matrix comprising of a water-soluble excipient based on a water-soluble polymer, and wherein the sphericity of the particulate composition is not less than 0.9 micron and a method of producing the same.
  • the present invention therefore aims to provide a solution that overcomes the problem of low actives content in the product, hygroscopicity, stability, water solubility/dispersibility, quick release, enhanced absorption of active from the product which are not recognized in the art. This remains the objective of the invention.
  • the present invention provides a highly potent/high active, free flowing, non-hygroscopic, stable, water soluble/dispersible, quick release and highly bioavailable synergistic composition
  • a highly potent/high active, free flowing, non-hygroscopic, stable, water soluble/dispersible, quick release and highly bioavailable synergistic composition comprising soluble fiber, soluble protein and mucilage; wherein, said composition comprises high actives due to high active loading capacity, complete water solubility/dispersibility, quick release and high bioavailability of active ingredient/compounds.
  • the present invention provides a stable, synergistic composition for enhancing the solubility/dispersibility, stability, bioavailability and quick release of active ingredient comprising; i. Soluble fiber in an amount ranging from 0. 1% to 80% of the total composition; ii. Soluble protein in an amount ranging from 0. 1% to 80% of the total composition; and iii. Mucilage in an amount ranging from 0.1% to 55% of the total composition; wherein said active ingredient is present in an amount of 5% to 98% of the total composition; and wherein said composition is free of emulsifier, glidant and organic solvents.
  • the active compounds/ingredient of the present synergistic composition is selected from extracts, oleoresins, essential oils and purified phytochemicals selected from Ginger root extract, Turmeric extract, Marigold extract, Rosemary extract, Ashwagandha extract, Cannabis extract, Hemp oil, Garlic extracts, Beetroot extract, clove extract, cinnamon extract, cardamom extract, Black seed (Nigella sativa) extract, Lycopene extract, Vitamin D/D3 from animal or lichen source, Vitamin A, Vitamin E, Vitamin C, Vitamin K2, DL- Alpha tocopherol, sea buckthorn oil, Omega fatty acids (3,6,7 &9) sourced from fish, Algae, Krill and Buglossoides arvensis, Boswellia serrata extract, Capsicum extract, Palmitoylethanolamide (PEA), Piper nigrum extract, Fenugreek saponins, Co-enzyme Q10, plant sterols, vitamin K7, Citrus bioflavonoids,
  • the soluble fiber of the present synergistic composition is selected from galactomannans, fructooligosaccharides, inlulin, xyloglucan, beta-glucan from Albizia zygia, tamarind, Cochlospermum religiosum, Chondrus cryspus, Cassia tora Linn, Cyamompsis tetraganolobus, Acacia Arabica, Acacia Senegal, Anogeissus latifolia, Astragalus gummifer, Sterculia urens, Khaya grandifolia, Xanthomonas lempestris, Pseudomonas elodea, guar gum, xanthan gum, Tapioca, Aloe vera and the like.
  • the soluble protein of the present synergistic composition is selected from rhizomes of Curcuma longa (turmeric), seeds of Oryza sativa L. (Brown rice), stems of Bambusa vulgaris (Bamboo), aerial part of Pisum sativum (pea protein), fruit of Tamarindus indica (Tamarind), tubers of Dioscorea villosa (Wild Yam), Macroalgae (Seaweed), kernels of Triticum (wheat protein), seeds of Helianthus annuus (Sunflower seeds), seeds of Chenopodium quinoa (Quinoa) and the like.
  • the mucilages of the present synergistic composition are selected from arabinogalactans such as rhamno-galacturonan, arabinoxylan, galactoglucomannan, glucogalactomannan, galacto-glucoarabinomannan, from psyllium, Flax seed, chia seeds, Basil seeds, Chan seeds, Abelmoschus esculentus (okra), Phoenix, Cassia tora, gum spinach, Cordia obliqua, Ocimum americanum, Aloe species, Lepidum sativum, Ocimum canum, Trigonella foenum graecum, Hibiscus esculentus Linn, Plantago psyllium, Plantago ovata, Leucaena leucocephata, Ocimum gratissimum Linn, Asparagus racemosus, Tamarindus indica and the like.
  • arabinogalactans such as rhamno-galacturonan, arabinoxylan
  • the present invention discloses a synergistic composition
  • a synergistic composition comprising (a) Active ingredient standardized to contain 1 to 99% actives, in an amount ranging from 5% to 98%; (b) soluble fibers, standardized to contain >80% soluble and indigestible fiber and >1- 10% protein, in an amount ranging from 0.1% to 80% (c) soluble protein, standardized to contain >80% protein and ⁇ 15 % of polysaccharides, in an amount ranging from 0.1% to 80% and (d) mucilage, standardized to contain >80% soluble polysaccharides and >5% protein, in an amount ranging from 0.1% to 55%.
  • the present invention describes a highly potent, high active, free flowing, stable, non-hygroscopic, completely water soluble, quick release, and highly bioavailable synergistic composition
  • a highly potent, high active, free flowing, stable, non-hygroscopic, completely water soluble, quick release, and highly bioavailable synergistic composition comprise high actives (oil/liquid/dry extracts) and combination of soluble fiber, soluble protein and mucilage; wherein, said synergistic composition is free of emulsifier, glidant and any processing solvents.
  • the present invention describes a process for preparation of said synergistic composition
  • a process for preparation of said synergistic composition comprising; a) Adding mixture of soluble fiber(s) to water; b) Homogenizing the mixture of step (a) at temperature 40°C to 80°C, followed by addition of soluble protein and mucilage; c) Homogenizing the mixture of step (b) at temperature 40°C to 80°C, followed by addition of active ingredient; d) Homogenizing the mixture of step (c) at temperature 40°C to 80°C and RPM of >1400; e) Drying the mixture of step (d) in vacuum oven having temperature at 40°C to 80°C and pressure at 1-20 mBar or tray dryer with temperature at 40°C to 80°C to obtain dry flakes; and f) Milling the dried flakes of step (e) to obtain free-flowing powder.
  • Figure 1 (a) depicts the product composition of Example 1 and the product composition of Example 2 to 4
  • Figure 1 (b) depicts the Comparative solubility profde of Example 1 to 4
  • Figure 2 (a) depicts the product composition of Example 7 and the product composition of Example 8
  • Figure 2 (b) depicts the Comparative solubility profde of Example 7 and example 8
  • Figure 3 (a) depicts the product composition of Example 10 and the product composition of Example 11
  • Figure 3 (b) depicts the Comparative solubility profde of Example 10 and 11
  • Figure 4 (a) depicts the product composition of Example 12 and the product composition of Example 13
  • Figure 4 (b) depicts the Comparative solubility profde of Example 12 and 13
  • Figure 5 (a) depicts the product composition of Example 14 and the product composition of Example 15
  • Figure 5 (b) depicts the Comparative solubility profde of Example 14 and example 15
  • Figure 6 (a) depicts the product composition of Example 16 and the product composition of Example 17
  • Figure 6 (b) depicts the Comparative solubility profde of Example 16 and 17
  • Figure 7 (a) depicts the product composition of Example 19 and the product composition of Example 20
  • Figure 7 (b) depicts the Comparative solubility profde of Example 19 and 20
  • Figure 8 (a) depicts the product composition of Example 22 and the product composition of Example 23
  • Figure 8 (b) depicts the Comparative solubility profde of Example 22 and 23
  • Figure 9 (a) depicts the product composition of Example 25 and the product composition of Example 26
  • Figure 9 (b) depicts the Comparative solubility profde of Example 25 and 26
  • Figure 10 (a) depicts the product composition of Example 28 and the product composition of Example 29
  • Figure 10 (b) depicts the Comparative solubility profde of Example 28 and 29
  • Figure 11 (a) depicts the product composition of Example 31 and the product composition of Example 32
  • Figure 11 (b) depicts the Comparative solubility profde of Example 31 and 32
  • Figure 12 (a) depicts the product composition of Example 34 and the product composition of Example 35
  • Figure 12 (b) depicts the Comparative solubility profde of Example 34 and 35
  • Figure 13 (a to d) depicts the product composition of Example 37 to 40
  • Figure 14 (a) depicts the product composition of Example 41 and the product composition of Example 42
  • Figure 14 (b) depicts the Comparative solubility profde of Example 41 and 42
  • the biological materials used in the demonstration of the invention are sourced as samples from the vendors. The details of which are provided as follows:
  • Mucilage (Fenugreek) - Sourced from Mahesh Agro Food Industries RIICO Industrial Area, RICCO Housing Colony, Barmer, Bengal 344001, India.
  • Vitamin D oil Sourced from Vitashine Creation House, 50-72 Gauntley Street, Nottingham, United Kingdom.
  • high potency or “high actives” herein refers to the higher concentration of biologically active compounds present in the synergistic composition which is in the range of 5 to 98% w/w of the total composition.
  • soluble fiber herein refers to hydrolysed/unhydrolysed fiber from natural or synthetic origin which is standardized to contain >80% soluble and indigestible fiber and >1-10% protein of the total composition.
  • soluble protein herein refers to hydrolysed/unhydrolysed protein from natural or synthetic origin which is standardized to contain >80% protein and ⁇ 15% of polysaccharides of the total composition.
  • Mucilage herein refers to hydrolysed/unhydrolysed mucilage standardized to contain >5% protein and >80% polysaccharides.
  • the present invention discloses a synergistic composition comprising soluble fiber, soluble protein and mucilage that provides high efficiency in terms of actives loading capacity beside providing a high potency, high actives, free flowing, complete water solubility/dispersibility, stability, non-hygroscopic, quick release and high bioavailability of active ingredient.
  • the present invention provides a synergistic composition for enhancing the solubility, stability, bioavailability and quick release of active ingredient comprising; i. Soluble fiber in an amount ranging from 0. 1% to 80% of the total composition; ii. Soluble protein in an amount ranging from 0. 1% to 80% of the total composition; and iii. Mucilage in an amount ranging from 0.1% to 55% of the total composition; wherein said active ingredient is present in an amount of 5% to 98% of the total composition; and wherein said composition is free of emulsifier, glidant and organic solvents.
  • the active ingredient of synergistic composition is obtained from plant and animal source.
  • the active compounds/ingredient includes extracts, oleoresins, essential oils and purified phytochemicals selected from Ginger root extract, Turmeric Oleoresin, Turmeric essential oil, Marigold extract, Rosemary extract, Ashwagandha extract, Cannabis extract (Cannabinoids), Hemp oil, Garlic extracts, Beetroot extract, clove extract, cinnamon extract, cardamom extract, , Black seed (Nigella saliva) extract, Vitamin D/D3, Vitamin A, Vitamin E, Vitamin C, Vitamin K2, DL- Alpha tocopherol, sea buckthorn oil, Omega fatty acids (3, 6, 7 & 9) sourced from fish, krill, Algae, Buglossoides arvensis , Boswellia serrata extract, Capsicum extract, DHA (Docosahexaenoic acid), EPA (Eicosapentaenoic acid), Palmitoylethanolamide (PEA), Piper
  • the hydrolysed/unhydrolysed soluble fiber of present synergistic composition are selected from arabinogalactans such as rhamno-galacturonan, arabinoxylan, galactoglucomannan, glucogalactomannan, galactoglucoarabinomannan, fructooligosaccharides, inlulin, xyloglucan, beta-glucan from Albizia zygia, tamarind, Cochlospermum religiosum, Chondrus cryspus, Cassia tora Linn, Cyamompsis tetraganolobus, Acacia Arabica, Acacia Senegal, Anogeissus latifolia, Astragalus gummifer, Sterculia urens, Khaya grandifolia, Xanthomonas lempestris, Pseudomonas elodea xanthan gum Tapioca , Aloe vera and guar gum.
  • the hydrolysed/unhydrolysed mucilages of present synergistic composition are selected from arabinogalactans such as rhamno-galacturonan, arabinoxylan, galactoglucomannan, glucogalactomannan, galacto-glucoarabinomannan, galactomannans from psyllium, Flax seed, chia seeds, Basil seeds, Chan seeds, Abelmoschus esculentus (okra), , Phoenix, Cassia tora , gum spinach, Cordia obliqua , Ocimum americanum, Aloe species, Lepidum sativum, Ocimum canum, Trigonella foenum graecum, Hibiscus esculentus Linn, Plantago psyllium, Plantago ovata, Leucaena leucocephata, Ocimum graft ssimum Linn, , Asparagus racemosus and Tamarindus indica.
  • the soluble protein of the present synergistic composition is selected from rhizomes of, leaf of Aloe barbadensis (aloe vera), seeds of Oryza sativa L. (Brown rice), stems of Bambusa vulgaris (Bamboo), aerial part of Pisum sativum (pea protein), fruit of Tamarindus indica (Tamarind), Macroalgae ( Seaweed), kernels of Triticum ( wheat protein) , seeds of Helianthus annuus (Sunflower seeds) , seeds of Chenopodium quinoa (Quinoa) and the like.
  • the present invention discloses a synergistic combination of standardized soluble fibers, soluble protein and mucilage to overcome the problem of active loading, low concentration/low active loadings, poor flow properties, very oily powders, water insolubility, poor actives release and poor bioavailability.
  • the present synergistic composition has high efficiency in terms of actives loading besides being quick release, highly bioavailable, completely water soluble, and forms stable solution/suspension in aqueous media for up to two years.
  • the said hydrolysed/ unhydrolysed soluble fiber of natural origin used in the synergistic composition is standardized to contain glycoprotein and arabinogalacto protein equivalent tol to 10% protein and, >80% soluble fiber and indigestible fiber which is very important for enhancing the solubility.
  • the said soluble protein used in the synergistic composition is standardized to contain >80% protein and, ⁇ 15% polysaccharide.
  • the said mucilage used in the present synergistic composition is standardized to contain >5% protein and >80% polysaccharides.
  • the soluble fiber, soluble protein and mucilage lead to the high active composition in powder form without hampering the solubility and suspension stability of the composition in water for more than 2 years.
  • the final composition is free flowing powder with higher solubility, bioavailability and stability.
  • the present invention discloses a synergistic combination of Soluble fiber, soluble protein and mucilages; wherein, said composition is free of emulsifier, glidant and any organic solvents.
  • the active ingredient in combination of mucilage, protein and soluble fiber gives a soluble free-flowing powder; however, in the absence of these ingredients, the process results in a non free-flowing/moist product that is unable to be used further.
  • the present invention discloses a synergistic composition which forms stable solution/suspension in water without any sedimentation or precipitation and is stable for more than 2 years and at high temperature up to 90°C.
  • the present invention discloses synergistic composition which is physically and chemically stable in solid powder form and in aqueous solution for more than 2 years.
  • the present invention discloses a synergistic composition is formulated using suitable carriers into various dosage forms such as tablets, capsules, syrups, strips, gummies, beverages, ready to drink beverages, milk based products/beverage/fortified products such as curd, yogurt, energy drinks, for applications as nutraceuticals, pharmaceuticals, food or food supplements/additives.
  • the present invention discloses a synergistic composition which is useful in the treatment of inflammatory diseases, respiratory diseases, heart diseases, cognitive diseases, eye diseases, skin diseases, digestive diseases/discomfort and stress.
  • the present invention discloses a process for preparation of stable water soluble synergistic composition
  • a process for preparation of stable water soluble synergistic composition comprising; a) Adding mixture of soluble fiber(s) to water; b) Homogenizing the mixture of step (a) at temperature 40°C to 80°C, followed by addition of soluble protein and mucilage; c) Homogenizing the mixture of step (b) at temperature 40°C to 80°C, followed by addition of active ingredient; d) Homogenizing the mixture of step (c) at temperature 40°C to 80°C and RPM of >1400; e) Drying the mixture of step (d) in vacuum oven having temperature at 40°C to 80°C and pressure at 1-20 mBar or tray dryer with temperature at 40°C to 80°C to obtain dry flakes; and f) Milling the dried flakes of step (e) to obtain free-flowing powder.
  • the above process for preparation of a synergistic composition is a solvent free process.
  • the obtained free flowing powder has good flow property, complete water solubility /dispersibility, quick release of actives and high bioavailability of active ingredient.
  • the solution prepared from the said free-flowing powder is stable for up to 2 years at high temperature (25 to 80°) as well as at low temperature (4 to 8°C).
  • composition and process of the high oil loading actives are Composition and process of the high oil loading actives:
  • composition comprising Ginger Oleoresin
  • Example 1 Process for preparation of Example 1: a) Adding mixture of Soluble fiber to water in the ratio of 1 :3 respectively; b) homogenizing the mixture of step (a) for 10 minutes, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes, followed by addition of ginger oleoresin; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Process for preparation of the composition of Examples 2 to 4 a) Adding mixture of Mucilage/Soluble fiber/Soluble protein to water in the ratio of 1:2.5 respectively; b) Homogenizing the mixture of step (a) for 10 minutes, followed by addition of ginger oleoresin; c) homogenizing the mixture of step (b) for another 20 to 30 minutes at RPM of >1400; d) drying the mixture of step (c) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and e) milling the dried flakes of step (d).
  • the obtained free flowing powder from Example 1 is represented in the figure 1(a) in comparison with the compositions represented from Example 2 to 4 (Reference samples).
  • Example 5 Comparative solubility data profile of ‘Ginger Oleoresin composition of Example 1 vis-a-vis ‘Example 2 to 4
  • Example 1 The final product of Example 1 is free flowing, stable, non-hygroscopic with very good flow property, shows actives loading capacity, better solubility and quick release over the products represented in Examples 2 to 4 and highly potent product and show the synergistic effect of the mucilage and soluble fiber.
  • the composition demonstrated in Examples 2 to 4 forms a sticky paste, forms lumps which is not water-soluble product (as illustrated in Figure 1).
  • Example 1 the product prepared from of example 1 was stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C and at low temperature of 4 °C to 8 °C.
  • the stability data of Example 1 is further explained below and represented as Example 6.
  • the reduction in active content was 1.23 % with the formulation of present invention (Example 1), whereas, the reduction in active content was 19.22% with the liquid ginger oleoresin which was not formulated.
  • the results described in Table 1 show the percentage of total gingerols in each product over the entire 6 months period. However, the stability study was continued for the formulated product and the product was found to be stable till 24 months at room temperature (25 to 28 °C),
  • Table 1 Comparative stability study data of total Gingerols in Ginger Oleoresin unformulated liquid with formulated powder of example 1.
  • Example 7 and 8 Composition comprising Beetroot extract
  • Example 7 Process for Preparation of Example 7: a) Adding mixture of Soluble fiber to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 60°C, followed by addition of soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes at temperature 60°C, followed by addition of fresh beet root extract; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 60°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 8 The process for preparation of Example 8 is same as Example 7 except the step of addition of soluble protein and soluble fiber and the mucilage to water ratio is 1: 1.5.
  • Example 7 The product of Example 7 is free -flowing, non-sticky, non-hygroscopic and soluble and releases actives very quickly when provided as solution whereas the composition obtained from example 8 shows a sticky paste of the final product (as illustrated in figure 2).
  • example 7 is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 9 Composition comprising Ashwagandha Extract
  • Example 9 Process for Preparation of Example 9: a) Adding mixture of Soluble fiber to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 50°C, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes at temperature 50°C, followed by addition of ashwaganda root and leaf water extract; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 50°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • the obtained free flowing powder had complete water solubility /dispersibility, nonhygroscopicity, flow property, quick release of withanolides. Also, this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C .
  • Example 10 and 11 Composition comprising Vitamin D oil
  • Example 10 Process for Preparation of Example 10: a) Adding mixture of Soluble fiber to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 40°C, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes at temperature 40°C, followed by addition of vitamin D oil; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 40°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 11 The process for preparation of Example 11 is same as Example 10 except the step of addition of mucilage and soluble fiber and the protein to water ratio is 1: 1.5 Results:
  • Example 10 The product of Example 10 is free -flowing, non-sticky, non-hygroscopic and soluble and releases actives very quickly when provided as solution whereas the composition obtained from example 11 has shown a sticky paste of the final product (as illustrated in Figure 3).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 12 and 13 Composition comprising Asthaxanthin extract a) Adding mixture of Soluble fiber to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 40°C, followed by addition of soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes at temperature 40°C, followed by addition of Asthaxanthin extract; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 40°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 11 The process for preparation of Example 11 is same as Example 12 except the step of addition of soluble protein and mucilage and the soluble fiber to water is 1: 1.5
  • Example 12 The product of Example 12 is free -flowing, non-sticky, non-hygroscopic and soluble and releases actives very quickly when provided as solution whereas the composition obtained from example 13 has shown a sticky paste of the final product (as illustrated in Figure 4). Also, this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 14 and 15 Composition comprising Lycopene extract a) Adding mixture of Soluble fiber to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 40°C, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes at temperature 40°C, followed by addition of Lycopene extract; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 40°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 15 The process for preparation of Example 15 is same as Example 14 except the step (a) of addition of soluble protein and soluble fiber and the mucilage to water ratio is 1:4.5.
  • Example 14 The product of Example 14 is free -flowing, non-sticky, non-hygroscopic and soluble and releases actives very quickly when provided as solution whereas the composition obtained from example 15 has shown a sticky and paste nature of the final product (as illustrated in Figure 5).
  • Example 16 and 17 Composition using Turmeric Extract
  • Process for preparation of composition of Example 16 a) Adding mixture of Soluble fiber to water in the ratio of 1 :2 respectively; b) homogenizing the mixture of step (a) for 10 minutes, followed by addition of guar gum, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes, followed by addition of turmeric oleoresin; d) homogenizing the mixture of step (c) for another 20 to 30 minutes and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 17 The process for preparation of Example 17 is same as Example 16 except the step of addition of soluble protein and mucilage and the soluble fiber to water ratio is 1:2.5.
  • Example 16 results in free -flowing soluble and non-sticky, non- hygroscopic and facilitates quick release of curcuminoids whereas the product of example 17 results in a sticky paste form as a final product(as illustrated in Figure 6).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 18 Comparative solubility data profile of Turmeric extract composition of Example 16 vis-a-vis Example 17
  • the final product of Example 16 is free flowing, water soluble, stable, and highly potent product, which shows the synergistic effect of the soluble fiber and mucilage in the composition of the invention.
  • the absence of soluble fiber and mucilage in the composition as demonstrated in Example 17 results in sticky paste, which is not water soluble and forms lumps ( Figure 6 (b)).
  • Example 16 shows better oil loading capacity and better solubility over the product represented in Example 17.
  • Example 19 and 20 Composition comprising Melatonin Powder
  • Example 19 Process for Preparation of Example 19: a) Adding mixture of Soluble fiber (from Acacia Senegal) to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 60°C, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes at temperature 60°C, followed by addition of Melatonin powder; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 60°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Soluble fiber from Acacia Senegal
  • Example 20 The process for preparation of Example 20 is same as Example 19 except the step of addition of soluble protein and soluble fiber and the mucilage to water ratio is 1: 1.5.
  • the product of Example 19 is free -flowing soluble and non-sticky, non-hygroscopic and releases actives very quickly when provided as solution whereas the composition obtained from example 20 has shown a sticky and paste nature of the final product (as illustrated in Figure 15).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 21 Comparative solubility data profile of ‘Melatonin composition of Example 19 vis-a-vis Example 20
  • Example 19 The final product of Example 19 is free flowing, water soluble, stable, and highly potent. However, in the absence of these ingredients as mentioned in Example 20, the composition forms a sticky paste product which is not water soluble.
  • Process for preparation of Example 22 a) Adding mixture of Soluble fiber to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes, followed by addition of soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes, followed by addition of marigold oleoresin; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 40°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • the process for preparation of Example 23 is same as Example 22 except the step of addition of soluble protein and mucilage and the soluble fiber to water ratio is 1:2.5.
  • the product from Example 22 is free -flowing and non-sticky, non-hygroscopic and results in quick release of lutein whereas the product of example 23 has shown a sticky paste of the product, as shown in figure 8a.
  • the texture of the composition shows that active ingredient in combination of mucilage and soluble fiber gives a free flowing powder; however, in the absence of these ingredients viz., mucilage and soluble fiber, the product formed is of sticky paste in nature and thus unable to be used further.
  • this product is stable for 12 Months at room temperature (25 to 28 °C).
  • Example 24 Comparative solubility data profile of ‘Marigold extract composition of Example 22 vis-a-vis Example 23
  • Example 22 The final product of Example 22 is free flowing, water soluble, stable, and highly potent product, which demonstrates the synergistic effect of soluble fiber and mucilage in the composition. However, in the absence of these ingredients as stated in Example 23 results in a sticky paste and moreover, the product is not water soluble and forms lumps (as illustrated in Figure 8(b)).
  • Example 25 Process for preparation of Example 25: a) Adding mixture of Soluble fiber (from Acacia senega! to water in the ratio of 1: 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes, followed by addition of tragacanth gum soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes, followed by addition of rosemary oleoresin; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Soluble fiber from Acacia senega!
  • Example 26 The process for preparation of Example 26 is same as Example 25 except the step of addition of soluble protein and soluble fiber and the mucilage to water ratio is 1 :2.5
  • Example 25 The product from Example 25 is free -flowing and non-sticky, nom-hygroscopic and results in quick release of active whereas the product of example 26 has shown a sticky paste nature (as illustrated in Figure 9(a)).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 27 Comparative solubility data profile of ‘Rosemary extract composition of Example 25 vis-a-vis Example 26
  • Example 25 The final product of Example 25 is free flowing, water soluble, stable, and highly potent product, hows better oil loading capacity and better solubility which shows the synergistic effect of the soluble fiber and mucilage in the composition.
  • Example 26 forms a sticky paste, which is a not water-soluble product and forms lump (as illustrated in Figure 9(b)).
  • Example 28 and 29 Composition using Buglossoides oil a) Adding mixture of soluble fiber to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes, followed by addition of buglossoides oil; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 29 The process for preparation of Example 29 is same as Example 28 except the step of addition of soluble protein and mucilage and the soluble fiber to water ratio is 1:2.5.
  • Example 28 The product from Example 28 is free -flowing, soluble and non-sticky, non-hygroscopic and further facilitates quick release of active whereas the product of example 29 was in the form of sticky and paste form (as illustrated in Figure 10(a)).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 30 Comparative solubility data profile of ‘Buglossoides oil composition of Example 28 vis-a-vis Example 29
  • Example 28 The final product of Example 28 is free flowing, water soluble, stable, and highly potent product due to the synergy of the combination of soluble fiber and mucilage present in the composition. Although mucilage is present, however, in the absence of soluble fiber, the product of example 29 forms a sticky paste which is not water soluble and forms lumps (as illustrated in Figure 10(b)).
  • Example 31 and 32 Composition using DL- Alpha tocopherol
  • Example 31 Process for preparation of Example 31: a) Adding mixture of Soluble fiber to water in the ratio of 1 : 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes, followed by addition of DL- Alpha tocopherol; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 32 The process for preparation of Example 32 is same as Example 31 except the step of addition of soluble protein and mucilage and the soluble fiber to water ratio is 1:2.5.
  • Example 31 is non-hygroscopic, is free -flowing soluble and non-sticky and facilitates a quick release of active whereas the product of example 32 is a sticky paste in nature (as illustrated in Figure 11(a)).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 33 Comparative solubility data profile of ‘DL- Alpha tocopherol composition of Example 31 vis-a-vis Example 32
  • Example 31 The final product of Example 31 is free flowing, water soluble, stable, and highly potent product due to the synergistic effect of mucilage and soluble fiber present in the composition. However, due to the absence of combination of mucilage and soluble fiber; the product of Example 32 is sticky paste, which is not water soluble and forms lumps as illustrated in Figure 11(b).
  • Example 34 Product composition using Palmitoylethanolamide, soluble protein and soluble fiber
  • Example 34 Process for preparation of Example 34: a) Adding mixture of Soluble fiber to water in the ratio of 1 : 1.5 respectively; b) Homogenizing the mixture of step (a) for 10 minutes, followed by addition of, soluble protein and mucilage; c) Homogenizing the mixture of step (b) for 10 minutes, followed by addition of Palmitoylethanolamide d) Homogenizing the mixture of step (c) for another 20 to 30 minutes at RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 35 The process for preparation of Example 35 is same as Example 34 except the step of addition of soluble protein and mucilage and the soluble fiber to water ratio is 1: 1.5.
  • Example 34 is free -flowing soluble and non-sticky, non-hygroscopic and facilitates a quick release of active whereas the product of example 35 is a non-free flowing / moist in nature (as illustrated in Figure 12 (a)).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 36 Comparative solubility data profile of ‘Palmitoylethanolamide’ composition of Example 34 vis-a-vis Example 35
  • the final product of Example 34 is free flowing, water soluble/dispersible, stable, and highly potent product due to the synergy of the combination of soluble fiber and soluble protein present in the composition.
  • soluble fiber is present, in the absence of soluble protein, the product of example 35 forms a non-free flowing / moist which is not water soluble and forms lumps (as illustrated in Figure 12(b)).
  • Example 34 shows better active loading capacity and better solubility over the composition represented in Example 35.
  • Example 37 to 40 Composition comprising Palmitoylethanolamide Powder (PEA)
  • Process for Preparation of Example 37 a) Adding mixture of Soluble fiber to water in the ratio of 1: 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 60°C, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes at temperature 60°C, followed by addition of PEA powder; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 60°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 38 to 40 Process for Preparation of Example 38 to 40: a) Adding mixture of Soluble protein /mucilage/ Rice protein to water in the ratio of 1:2.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 60°C, followed by addition of PEA powder; c) homogenizing the mixture of step (b) for another 20 to 30 minutes at temperature 60°C and RPM of >1400; d) drying the mixture of step (c) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and e) milling the dried flakes of step (d) to obtain non free-flowing/moist powder.
  • Example 37 The obtained free flowing powder from Example 37 is represented in figure 13 (a to d) in comparison with the composition represented as Example 38-40.
  • Example 37 is non-hygroscopic , is free -flowing soluble, non-sticky and releases actives very quickly when provided as solution whereas the composition obtained from example 38-40 has shown a sticky paste nature of the final product and not soluble(as illustrated in Figure 13 (a to d)).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.
  • Example 41 and 42 Composition comprising Murraya koenigii
  • Example 41 Process for Preparation of Example 41: a) Adding mixture of Soluble fiber to water in the ratio of 1: 1.5 respectively; b) homogenizing the mixture of step (a) for 10 minutes at temperature 60°C, followed by addition of, soluble protein and mucilage; c) homogenizing the mixture of step (b) for 10 minutes at temperature 60°C, followed by addition of Curry leaf extract; d) homogenizing the mixture of step (c) for another 20 to 30 minutes at temperature 60°C and RPM of >1400; e) drying the mixture of step (d) in vacuum oven having temperature at 60°C and pressure at ImBar for 8 hours to obtain dry flakes; and f) milling the dried flakes of step (e) to obtain free-flowing powder.
  • Example 42 The process for preparation of Example 42 is same as Example 41 except the step of addition of soluble fiber and mucilage and the soluble protein to water ratio is 1: 1.5.
  • Example 41 is non-hygroscopic, is free -flowing soluble and non-sticky and releases actives very quickly when provided as solution whereas the composition obtained from example 42 has shown a sticky and paste nature of the final product(as illustrated in Figure 14).
  • this product is stable for 24 Months at room temperature (25 to 28 °C), at higher temperature of 40 °C ⁇ 2 °C.

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Abstract

La présente invention concerne une composition synergique stable pour améliorer la solubilité/dispersibilité, la biodisponibilité et la libération immédiate de composés actifs. La présente invention concerne également un procédé de préparation de ladite composition synergique.
PCT/IN2024/050717 2023-06-09 2024-06-10 Composition synergique pour améliorer la solubilité, la stabilité, la biodisponibilité et la libération immédiate de composés actifs Pending WO2024252433A1 (fr)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119792224A (zh) * 2025-01-21 2025-04-11 江苏安必生制药有限公司 一种乙酰半胱氨酸泡腾片及其制备工艺

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110177175A1 (en) * 2008-09-23 2011-07-21 Rubicon Research Private Limited Dietary fiber compositions
US20120195868A1 (en) * 2009-07-27 2012-08-02 Nestec S.A. Nutritional compositions comprising fiber and probiotics
CN112385851A (zh) * 2020-11-16 2021-02-23 东北农业大学 一种利用豆渣制备可溶性膳食纤维粉的方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110177175A1 (en) * 2008-09-23 2011-07-21 Rubicon Research Private Limited Dietary fiber compositions
US20120195868A1 (en) * 2009-07-27 2012-08-02 Nestec S.A. Nutritional compositions comprising fiber and probiotics
CN112385851A (zh) * 2020-11-16 2021-02-23 东北农业大学 一种利用豆渣制备可溶性膳食纤维粉的方法

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119792224A (zh) * 2025-01-21 2025-04-11 江苏安必生制药有限公司 一种乙酰半胱氨酸泡腾片及其制备工艺

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