Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
  • A61K31/365—Lactones
  • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/676—Ascorbic acid, i.e. vitamin C
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
  • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/08—Anti-ageing preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
  • A61K2800/82—Preparation or application process involves sonication or ultrasonication

Definitions

• the present invention relates to the field of antioxidant compositions comprising vitamin C. More particularly, it relates to a process for improving the activity of vitamin C in aqueous solution, as well as various compositions comprising superactivated vitamin C and their preparation process. These compositions can be used in particular in the cosmetic, nutraceutical, pharmaceutical or food-processing fields.
• Vitamin C is a molecule known and used for a long time for its antioxidant properties, in particular for its ability to inhibit free radicals, and therefore oxidative stress. It is more generally found in dry form, pure or mixed with other compounds. In recent years, the dry liposomal form (vitamin C coated with liposome) has been particularly developed to improve its assimilation by the body. Assimilation occurs mainly at the level of the duodenum and the proximal jejunum and is saturable, the percentage absorbed decreasing even with the dose ingested. It is also sodium-dependent and can be inhibited by structural analogs.
• vitamin C has also been examined at the cutaneous level. In addition to its antioxidant role, its presence in high concentrations in the skin could be associated with other functions, such as the formation of collagen, the inhibition of the formation of melanomas or even the modulation of epigenetic expressions.
• vitamin C The bioavailability of vitamin C varies greatly depending on the method of preparation and assimilation. Thus, depending on the form (dry, liposomal, liquid, emulsified, etc.) and the preparation technique used, the same amount of vitamin C absorbed can lead to:
• Dry forms are widely preferred today, to guard against possible problems of chemical stability (degradation of vitamin C over time), physical (phase separation of emulsions for example) or microbiological encountered with aqueous solutions.
• chemical stability degradation of vitamin C over time
• physical phase separation of emulsions for example
• microbiological encountered with aqueous solutions it is well known that the assimilation and bioavailability of vitamin C in dry form are not optimal.
• New products are regularly offered on the market to stand out from the competition with a formulation likely to make vitamin C more active in the broad sense. It is known to use a treatment for the preparation of stable emulsions comprising a lipid phase in an aqueous phase using piezoelectric transducers.
• patent WO2010/149668 describes a method for preparing an oil-in-water emulsion produced in a container in which is immersed a piezoelectric transducer operating at high frequencies, in particular greater than 900 kHz. It has also been proposed in patent WO2017/037372 to use a similar process, using ultrasound at comparable frequencies, to vectorize hydrophobic active principles, in the form of a dispersed phase in a hydrophilic continuous phase. It has in particular been proposed to increase the bioavailability of co-enzyme Q.10 by this process.
• the invention relates to a process for improving the antioxidant activity in solution in an aqueous medium consisting in treating said solution with ultrasound at a vibration frequency greater than or equal to 1 MHz.
• the invention also relates to a process for the preparation of an aqueous antioxidant composition comprising overactivated vitamin C, said composition being treated by application of the process of the invention, as well as the composition obtained.
• the invention also relates to a process for preparing an emulsion comprising overactivated vitamin C, as well as the composition obtained in the form of an emulsion.
• composition according to the invention in the cosmetic, nutraceutical and pharmaceutical field.
• the main advantage of the process according to the invention is that it makes it possible to increase the antioxidant activity of vitamin C in solution by at least 10%, preferably by at least 20%. This property is quite surprising and very interesting.
• the process is particularly interesting because it makes it possible to formulate vitamin C in aqueous solution, that is to say that it makes it possible to prepare a stable liquid aqueous composition of vitamin C without adding stabilizing compounds (without adding active chemical, without texturizing, without emulsifying or any other compound known to stabilize solutions). It paves the way for the preparation of new formulations of vitamin C in aqueous solution. Such formulations can be presented in the form of a glass ampoule or a plastic pod.
• the dose of vitamin C can be reduced for the same effectiveness with respect to the dose comprised in the compositions available to date.
• the antioxidant activity will be higher with an overactivated vitamin C as defined in the invention.
• compositions according to the invention give access to new antioxidant formulations which can be used in cosmetics, in nutraceuticals, in pharmaceuticals and in the food industry.
• a first object of the invention relates to a process for improving the activity of vitamin C in aqueous solution, consisting in treating said solution containing vitamin C by ultrasound at a vibration frequency greater than or equal to 1 MHz.
• the main activity of vitamin C is antioxidant activity.
• Antioxidants can be defined as "any substance which, in low concentration relative to a substrate liable to be oxidized, prevents or slows down the oxidation of this substrate".
• antioxidant activity within the meaning of the invention, is meant the action of preventing or slowing down the oxidation of a substrate. This activity can be measured in particular using the PAOT-Liquid® method, which records the modifications of an electrochemical potential in a reaction medium containing a reference molecule in its free radical state; this method is described in patent application WO2020/109736.
• aqueous solution within the meaning of the invention, is meant any type of solution composed mainly of water, including a solution of pure or quasi-pure water.
• aqueous solution is meant any type of solution composed mainly of water, including a solution of pure or quasi-pure water.
• the treatment time can vary and is dependent on the volume of preparation to be treated, the amount of vitamin C, and the type and power of the ultrasonic transmitters.
• the frequency of the ultrasounds is between 1 and 3 MHz and is applied, for volumes between lOmL and 1000L, for a period that can range from 15 min to 24 hours.
• the treatment time can also be adapted according to the volume treated in batch, or the flow rate for continuous treatments.
• This process makes it possible to formulate vitamin C, a hydrophilic molecule, in solution in an aqueous medium by process, without adding any chemical active ingredient. It is therefore a very simple formulation which may contain only vitamin C, the effect of improving antioxidant activity is obtained through ultrasonic treatment. This improvement can reach 10%, even 20% or more; the activity obtained is maintained for a period of at least 3 weeks without any special precautions (ambient temperature, without inerting).
• a second object of the invention relates to a process for the preparation of an aqueous composition comprising overactivated vitamin C comprising the steps of: dissolving the vitamin C in an aqueous medium treating said solution by ultrasound at a vibrating frequency greater than or equal to 1 MHz.
• overactivated vitamin C within the meaning of the invention, is meant a vitamin C whose antioxidant activity is increased by at least 10% compared to the same quantity of reference vitamin C (untreated, in particular not treated with ultrasound), preferably by at least 20%; the method for calculating this increase in activity is described in the experimental part.
• the superactivated vitamin C according to the invention is a vitamin C treated in solution by ultrasound at a vibrational frequency greater than or equal to 1 MHz.
• a third subject of the invention relates to an aqueous composition comprising superactivated vitamin C, characterized in that said superactivated vitamin C has an antioxidant activity that is at least 10% greater than that of the same quantity of reference vitamin C; it is obtained by treatment using the method defined above.
• This composition can be called “generic composition” in the remainder of this text.
• Formulation of the composition may be limited to the superactivated vitamin itself in water.
• the aqueous medium (or aqueous solution) in which the vitamin C is dissolved can contain other molecules, for example vitamins, amino acids, one or more texturizing molecules, etc.
• the generic composition can also be used as an ingredient for the preparation of complex compositions.
• a fourth object of the invention relates to a process for the preparation of an emulsion of the oil-in-water type comprising overactivated vitamin C comprising the steps of: dissolution of vitamin C in an aqueous medium addition of an oily solution in a proportion of between 1% and 30% relative to the quantity by mass of the aqueous solution treatment of said solution by ultrasound at a higher or equal vibration frequency at 1MHz.
• the oily solution used in the emulsion can be any type of oil or oily substance, alone or as a mixture, in particular vegetable oils, among which mention may be made, by way of example, of olive oil, sweet almond, argan oil, coconut oil... but also essential oils.
• a fifth object of the invention relates to an emulsion comprising overactivated vitamin C characterized in that it is obtained by ultrasound treatment at a vibrational frequency greater than or equal to 1 MHz and that said overactivated vitamin C has antioxidant activity at least 10% higher than that of the same reference quantity of vitamin C.
• the present invention provides access to the preparation of an ampoule or a pod containing an aqueous composition of superactivated vitamin C in stable form in aqueous solution as defined above.
• the ampoule and the pod are themselves embodiments of the invention.
• the invention can be applied to the implementation of a process for the preparation of a cosmetic composition comprising overactivated vitamin C comprising the steps of: dissolving the vitamin C in an aqueous medium optionally adding a solution oily in a proportion of between 1% and 30% relative to the mass quantity of the aqueous solution addition of at least one cosmetic ingredient chosen from: vitamins other than vitamin C, moisturizing agents, depigmenting agents, texturizers, pH correctors and coloring agents treatment of the said solution obtained by ultrasound at a vibration frequency greater than or equal to 1 MHz.
• the invention also relates to a cosmetic composition
• a cosmetic composition comprising overactivated vitamin C, characterized in that it is obtained by treatment using the method defined above and that it comprises, in addition to vitamin C, at least one ingredient chosen among vitamins other than vitamin C, moisturizing agents, depigmenting agents, texturizing agents, pH correctors and coloring agents.
• the cosmetic composition can also be used as an ingredient for the preparation of complex compositions.
• the cosmetic composition can also be formulated as a lotion, milk, cream or the like.
• a sixth object of the invention relates to the use of a composition as defined previously (generic composition or cosmetic composition) to aid in the regeneration of the skin and/or to stimulate the formation of collagen and/or to improve its radiance.
• the invention can be applied to the implementation of a process for the preparation of a nutraceutical composition
• a process for the preparation of a nutraceutical composition comprising overactivated vitamin C comprising the steps of dissolving the vitamin C in an aqueous medium optional addition of an oily solution in a proportion of between 1% and 30% relative to the quantity by mass of the aqueous solution, addition of at least one component chosen from vitamins other than vitamin C, trace elements and amino acids, treatment of said solution obtained by ultrasound at a vibration frequency greater than or equal to 1 MHz.
• the invention also relates to a nutraceutical composition
• a nutraceutical composition comprising overactivated vitamin C, characterized in that it is obtained by treatment using the method defined above and that it comprises, in addition to vitamin C, at least one component chosen among vitamins other than vitamin C, trace elements and amino acids.
• the nutraceutical composition can also be used as an ingredient for the preparation of complex compositions.
• a seventh object of the invention relates to the use of a composition as defined previously (generic composition or nutraceutical composition) in nutraceuticals to prevent the effects of oxidative stress; it allows in particular to stimulate the defenses of the body, in particular the immune system, to improve the absorption of iron, to fight against fatigue.
• a composition may include other vitamins, trace elements, amino acids.
• the invention can be applied to the implementation of a process for the preparation of a pharmaceutical composition comprising overactivated vitamin C comprising the steps of: dissolving the vitamin C in an aqueous medium adding at least one component chosen from active pharmaceutical principles, or excipients treatment of said solution obtained by ultrasound at a vibrational frequency greater than or equal to 1 MHz.
• the invention also relates to a pharmaceutical composition
• a pharmaceutical composition comprising overactivated vitamin C, characterized in that it is obtained by treatment using the method defined above and that it comprises, in addition to vitamin C, at least one component chosen among the active pharmaceutical principles, or the excipients.
• the pharmaceutical composition can also be used as an ingredient for the preparation of complex compositions.
• an eighth object of the invention relates to the use of a composition as defined above (generic composition or pharmaceutical composition) in pharmaceuticals as a medicament, in particular for preventing and/or treating diseases associated with oxidative stress.
• This pharmaceutical composition can be used for example to promote healing or prevent the formation of cancers, in particular melanomas.
• diseases associated with oxidative stress we mean cancers, ocular pathologies (cataract and macular degeneration), cardiovascular pathologies (infarction), neurodegenerative diseases (ataxia, lateral sclerosis, Alzheimer's disease), metabolic diseases ( diabetes), brain disease.
• the antioxidant compositions according to the invention can be used in drinkable, topical, ocular or injectable preparations. They can in particular be formulated from vitamin C only or in very short formulas to avoid the addition of compounds likely to induce side effects (allergic reactions, irritations, etc.).
• a ninth object of the invention relates to the use of a composition comprising overactivated vitamin C in the agrifood field as a supplement or replacement for preservatives.
• composition in the field of the food industry, a composition (generic composition) according to the invention can be added to drinks, applied to food or any other use in addition to or replacement of preservative products, for their antioxidant properties.
• a composition generic composition
• the present invention will be better understood on reading the examples which follow, provided by way of illustration and should in no way be considered as limiting the scope of the present invention.
• Table 1 Composition of the four preparations made. The values indicated are the mass percentages of the ingredients in the corresponding preparation.
• Preparations 1 and 2 were made from the same stock preparation of 2L, then separated into two. Preparations 1 and 3 were made by simply dispersing/mixing the ingredients all together. Preparations 2 and 4 underwent complementary high-frequency ultrasound treatment (USHF treatment), at 1.7 MHz. For preparation 4, the USHF treatment induced a significant drop in pH, which was compensated by an addition of 1% sodium hydroxide sufficient for the final pH of the preparation to be comparable to that of the other preparations, or by a value of about 5. This pH was chosen so as to be able to correspond to that of a potential product for topical use. For To reach it, vitamin C was provided in its conjugate acid and base forms. Xanthan gum was added to preparation 4 so that its viscosity was similar to that obtained for preparation 3 with the surfactants (Twin and Span).
• USHF treatment complementary high-frequency ultrasound treatment
• Table 2 PAOT score and standard deviations (SD) obtained for the four preparations made.
• the antioxidant potential of the active ingredient is the same when it is treated alone or when it is treated within an emulsion.
• the lowest score is obtained for the conventional emulsion, produced using surfactants, which is quite significant of what is generally observed, that is to say that the antioxidants present in complex formulations lose part of their activity due to their interactions with the other ingredients.
• surfactants or other stabilizers present in conventional emulsion formulations can lead to a form of encapsulation of vitamin C, also reducing its activity.
• the PAOT-Liquid® method is also used to reproducibly quantify vitamin C in water or blood.
• the relationship is linear and a PAOT score of 100 corresponds to a concentration of approximately 1g/L.
• the PI sample respects this rule perfectly since the concentration of vitamin C (conjugate acid and base) is in fact about 6.3% in the preparation, deducting the contribution of Na + ions from the sodium ascorbate .
• the expected score is therefore approximately 630, for a measured score of 665.67.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Epidemiology (AREA)
• Chemical & Material Sciences (AREA)
• Dermatology (AREA)
• Birds (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Gerontology & Geriatric Medicine (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Cosmetics (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Coloring Foods And Improving Nutritive Qualities (AREA)

Applications Claiming Priority (2)

Publications (1)

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ID=76730594

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Family Cites Families (5)

• 2021
  • 2021-01-20 FR FR2100528A patent/FR3118869A1/fr active Pending
• 2022
  • 2022-01-20 WO PCT/FR2022/050114 patent/WO2022157460A1/fr unknown
  • 2022-01-20 EP EP22704931.9A patent/EP4281067A1/de active Pending

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