Classifications

• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
  • A23L5/00—Preparation or treatment of foods or foodstuffs, in general; Food or foodstuffs obtained thereby; Materials therefor
  • A23L5/30—Physical treatment, e.g. electrical or magnetic means, wave energy or irradiation
  • A23L5/32—Physical treatment, e.g. electrical or magnetic means, wave energy or irradiation using phonon wave energy, e.g. sound or ultrasonic waves
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K41/00—Medicinal preparations obtained by treating materials with wave energy or particle radiation ; Therapies using these preparations
  • A61K41/0004—Homeopathy; Vitalisation; Resonance; Dynamisation, e.g. esoteric applications; Oxygenation of blood

Definitions

• the present invention relates to the field of improving the bioavailability of active compounds. More particularly, it relates to a process for improving the bioavailability of hydrophilic active compounds in solution in an aqueous medium.
• the hydrophilic active compounds, the bioavailability of which is improved can be used, for example, in the cosmetics, food, nutraceutical or pharmaceutical fields.
• document WO2010 / 149668 describes a process 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.
• document WO2011 / 057340 describes a process for producing edible products derived from plants and / or fungi which does not use an organic solvent to extract the active biological compounds during the first step of the process.
• This method comprises the steps of i) obtaining an aqueous medium comprising the material obtained from the plant and / or the fungus, ii) heat treating the medium and then iii) treating it with ultrasound at a frequency of between 20 and 24 KHz.
• This extraction process aims to improve the activity of the extracts obtained by improving the extraction process itself, that is to say by increasing the quantity of active ingredient extracted and thus available in the product obtained. It is not intended to improve the bioavailability of the active ingredients, so as to obtain increased efficiency for the same amount of active ingredient. Disclosure of the invention
• the invention relates to a process for improving the bioavailability of hydrophilic active compounds in solution in an aqueous medium, consisting in treating said solution containing said hydrophilic compound by ultrasound at a vibratory frequency greater than or equal to 1 MHz.
• the invention also relates to a composition comprising at least one hydrophilic active compound in an aqueous solution, said composition being treated by applying the process of the invention.
• the invention also relates to the use of a composition according to the invention in the cosmetics, agrifood, nutraceutical or pharmaceutical field.
• the main advantage of the process according to the invention is that it makes it possible to vectorize and thus increase the bioavailability of hydrophilic molecules while they are in solution in an aqueous medium. This property is quite surprising and very interesting.
• the process is particularly advantageous because it makes it possible to formulate hydrophilic compounds while increasing their bioavailability without adding chemical active agent. It opens the way to the preparation of compositions of short formula and whose effectiveness is increased.
• a first subject of the invention relates to a process for improving the bioavailability of a hydrophilic active compound in solution in an aqueous medium, consisting in treating said solution containing said compound by ultrasound at a vibratory frequency greater than or equal to 1 MHz.
• active compound within the meaning of the invention, is meant a functional compound. It is in particular any compound which can have a physiological effect on a biological matrix.
• aqueous medium means a water-based medium, in particular a hydrosol.
• the frequency of the ultrasound is between 1 and 3 MHz.
• This process makes it possible to formulate hydrophilic compounds in solution in an aqueous medium by process, without adding chemical active. It is therefore a very simple formulation which may contain only the hydrophilic active compound, the vectorization effect being obtained by means of the ultrasound treatment.
• the inventors consider that the ultrasound induces a “capsule-free vectorization” (without vectorizing agent), probably due to ionic rearrangements around the hydrophilic compounds present in the solution.
• This concept is quite new and differs from the concept of vectorization as used until now which is based on an active envelopment, based on the formation of a capsule containing the active compound, thanks to the addition of a or several other compounds in aqueous medium.
• This is particularly the case in oil-in-water emulsions, where each dispersed oil droplet forms a capsule containing one or more hydrophobic active ingredients dispersed in an oil.
• the formation of the capsule thus requires the addition of at least one oil and, very generally, also of surfactant, surfactant and / or stabilizer in order to keep the dispersion stable over time.
• a second subject of the invention relates to a composition comprising at least one hydrophilic active compound in solution in an aqueous medium, characterized in that said composition is treated by applying the process according to the invention.
• Such a hydrophilic compound can be for example a sugar, a polar amino acid, a flavor or a pigment, a trace element, an antioxidant, a salicylated analgesic, an antifungal, an antibiotic (such as glycopeptide) or any other water-soluble active principle.
• a hydrophilic compound can be for example caffeine, glucose, vitamin C, vitamin B9 (folic acid), hyaluronic acid, urea, acetylsalicylic acid or vanillin.
• the formulation of the composition can be limited to the hydrophilic active compound itself in an aqueous medium.
• the composition can also be used as an ingredient for the preparation of complex compositions.
• a third subject of the invention relates to the use of a composition according to the invention in the cosmetics or agrifood field.
• a cosmetic composition can be a lotion, a cream or any other formulation comprising an aqueous solution.
• compositions according to the invention can be, for example, drinks comprising natural hydrophilic active agents chosen for their beneficial properties or for their aromas.
• a fourth subject of the invention relates to the use of a composition according to the invention in the pharmaceutical or nutraceutical field.
• compositions for pharmaceutical use can in particular be ocular or injectable preparations for which the reduction or elimination of the excipients is very advantageous, in particular for limiting the side effects.
• An injectable composition can for example be a vaccine composition or a vaccine composition carrier, in which the antigen or the adjuvants are more bioavailable, and therefore more effective at an equivalent dose, thus making it possible to reduce the dose.
• a fifth subject of the invention relates to a process for preparing a composition according to the invention consisting of:
• the treatment time can vary and is dependent on the volume of preparation to be treated, on the molecule or molecules to be vectorized as well as on the number, type and power of the ultrasonic emitters.
• Figure 1 Illustration of the reconstructed skin model used in Example 2
• Figure 2 Caffeine diffusion kinetics through the reconstituted samples.
• Reference caffeine dispersed in water without further addition;
• HF same as reference and application of an ultrasonic treatment with a frequency of 1.7 MHz;
• TA same as reference with addition of two surfactants (Tween 80 and Span) during dispersion;
• TA&HF same as TA and application of an ultrasonic treatment at a frequency of 1.7 MHz.
• Glucose syrup (78% glucose in water) was diluted in water so as to obtain 3L of a preparation containing 10% glucose, optionally adjusted to a pH equal to 7 by adding of soda. The preparation was then separated into three lots of IL each:
• Table 1 Difference between absorbance after 24 h and initial absorbance, measured at 600nm.
• Plates of 12 wells each containing a sample of EPISKIN reconstructed skin are used.
• the system as used is shown in Figure 1.
• the formulas to be evaluated are deposited on the surface.
• the receiving medium, bathing the skin samples, is recovered and replaced every 30 min until 3 h then every hour until 12 h.
• the fraction recovered is analyzed by HPLC (High Performance Liquid Chromatography) to quantify the caffeine present therein.
• HPLC High Performance Liquid Chromatography
• the HPLC is performed on a Dionex Ultimate 3000 system, using an Interchim Vintage Sériés KRC18 separator column.
• the analyzes are carried out on an injected volume of 10 ⁇ l in a mobile phase consisting of a 50/50 (w / w) mixture of methanol and ultrapure water circulating at a flow rate of lmL / min.
• compositions comprising caffeine in solution in water are all prepared so as to contain 2% of caffeine in the end and their pH is optionally adjusted to a pH equal to 7 by adding soda.
• the preparations evaluated during this experiment are as follows:
• composition prepared without surfactant and without treatment
• hydrofeeling Composition prepared without surfactant, with ultrasound treatment at a vibratory frequency of 1.7 MHz for 30 min;
• TA Composition prepared with surfactants (3% Tween80 and 2% span in the final preparation), without ultrasound treatment;
• TA&HF Composition prepared with surfactants (3% Tween80 and 2% span in the final preparation), with ultrasound treatment at a vibratory frequency of 1.7 MHz for 30min.
• J c is calculated as the slope of the line observed on the second part of the curve.
• the ti ag is defined as the time, on the abscissa, separating the “straight” part of the curve, corresponding to the constant flow, and the “curved” part of the curve, corresponding to the acceleration of the flow at the start of diffusion.
• the shift is very different between the kinetics obtained thanks to the product prepared according to the invention on the one hand and all the others on the other hand.
• This difference confirms that the treatment according to the invention induces an ease of the active principle, hydrophilic, to diffuse through the various layers of the skin. An increased bioavailability can be deduced from this, as its ability to reach the target cells (located in the hypodermis in the case of caffeine) is improved.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Nutrition Science (AREA)
• Engineering & Computer Science (AREA)
• Food Science & Technology (AREA)
• Polymers & Plastics (AREA)
• Hematology (AREA)
• Alternative & Traditional Medicine (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Cosmetics (AREA)

Applications Claiming Priority (2)

Publications (1)

Family

ID=68654657

Family Applications (1)

Country Status (5)

Families Citing this family (1)

Family Cites Families (5)

• 2019
  • 2019-07-15 FR FR1907938A patent/FR3098732B1/fr active Active
• 2020
  • 2020-07-09 CA CA3147114A patent/CA3147114A1/fr active Pending
  • 2020-07-09 WO PCT/FR2020/051242 patent/WO2021009450A1/fr unknown
  • 2020-07-09 EP EP20750347.5A patent/EP3998870A1/de active Pending
  • 2020-07-09 US US17/627,598 patent/US20220312804A1/en active Pending

Also Published As

Similar Documents

Legal Events