WO2000010511A1 - Utilisation d'emulsions stables concentrees eau dans huile pour la liberation percutanee controlee d'un principe actif - Google Patents
Utilisation d'emulsions stables concentrees eau dans huile pour la liberation percutanee controlee d'un principe actif Download PDFInfo
- Publication number
- WO2000010511A1 WO2000010511A1 PCT/FR1999/002009 FR9902009W WO0010511A1 WO 2000010511 A1 WO2000010511 A1 WO 2000010511A1 FR 9902009 W FR9902009 W FR 9902009W WO 0010511 A1 WO0010511 A1 WO 0010511A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- active principle
- emulsion
- use according
- phase
- advantageously
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/06—Emulsions
- A61K8/064—Water-in-oil emulsions, e.g. Water-in-silicone emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/06—Emulsions
-
- 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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4953—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
-
- 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
Definitions
- the invention relates to water-in-oil stable emulsions with a high percentage in internal phase which can be used in the cosmetic and pharmaceutical fields for the controlled administration through the skin of an active principle.
- the concentrated W / O emulsions can be subjected to repeated shear stresses without degrading them, as long as the critical shear point is not reached, this being however high enough to allow completely normal pumping and treatments. ;
- FR-2 258 165 describes emulsions with a high percentage in internal phase, of the water in oil or oil in water type, having the property of forming adherent films on the surface of the skin or the hair.
- This document recommends their use in cosmetics, in particular in sun lotions, moisturizers, hair emulsions, sun creams.
- hydrocortisone creams are described in particular for treating ear infections in animals or also based on benzoyl peroxide and colloidal sulfur for the treatment of acne.
- a subject of the invention is therefore the use of a stable water-in-oil emulsion, in which the dispersed phase constitutes more than 74%, advantageously at least approximately 80%, preferably approximately 90% by volume relative to the total volume of the emulsion as a vehicle for the prolonged percutaneous release of an active principle.
- the oily phase comprises the oil proper as well as the emulsifying agent.
- the concentrated W / O emulsions of the invention are particularly useful for the release through the skin of an active ingredient soluble or sparingly soluble in the aqueous phase.
- This active ingredient can be cosmetic in nature, a particularly preferred active ingredient being caffeine.
- This active principle can also be of a pharmaceutical nature. Mention may in particular be made of estradiol and hydrocortisone.
- the emulsions according to the invention are prepared in a manner known per se by mixing the aqueous phase in the oily phase. It is possible to use any of the oily substances compatible with the skin known from the state of the art.
- the oily phase can thus consist of a mineral oil, such as a paraffin oil, a vegetable oil such as a jojoba oil, or a silicone oil.
- the emulsion is produced by slow addition of the internal phase to the external phase with continuous stirring, cold.
- Any type of suitable emulsifying agent can be used. Mention may in particular be made of nonionic surfactants such as sorbitan and fatty acid esters, in particular sorbitan sesquioleate, and silicones, in particular cetyl dimethicone copolyol.
- the amount of emulsifying agent is advantageously at least 0.5%, advantageously at least 2%, preferably at least 3%, by weight relative to the total weight of the emulsion.
- the amount of active principle contained in the aqueous phase is at least 0.001%, advantageously at least 0.01%, preferably at least 0.1% and more preferably at least 2% and up to 20% or more by weight, relative to the total weight of the emulsion.
- the concentrated W / O emulsions of the invention may contain other ingredients authorized by law, in particular preservatives, electrolytes, pH adapters, buffers, antioxidants, perfumes, humectants and others.
- the stable W / O concentrated emulsions of the invention are suitable for prolonged and continuous release through the skin of an active principle for a period of at least 12 hours, advantageously at least 24 hours.
- the active principle is caffeine they allow a constant and continuous release for a period of at least 24 hours, with kinetics of order 0, after single application.
- a subject of the invention is also a slimming composition
- a slimming composition comprising, as active principle, caffeine in a concentrated stable water-in-oil emulsion as defined above.
- Caffeine is advantageously included in a concentration of at least 1%, preferably at least 3% by weight, more particularly around 5% by weight relative to the total weight of the emulsion.
- the subject of the invention is also a method for the continuous and prolonged administration of an active principle, in particular a water-soluble active principle through the skin, in particular human skin, consisting of:
- a stable water-in-oil emulsion having a dispersed (internal) phase consisting of more than 74%, advantageously at least 80%, preferably approximately 90% by volume relative to the total volume of the emulsion;
- the amount of composition to be applied to the skin is at least 2 mg / cm 2 , advantageously 2.5 mg / cm 2 , preferably 3.0 mg / cm 2 of skin.
- the composition according to the invention is applied in a conventional manner by massaging to facilitate penetration.
- a preferred composition contains caffeine as an active ingredient and is intended for the treatment of cellulite.
- An emulsion is prepared having an aqueous internal phase of 90% (w / w), the continuous phase of which is a paraffin oil.
- the composition of the emulsion is as follows:
- the glycerin, magnesium sulfate, methylparaben, sorbic acid and water are mixed and heated to 80 ° C. until the compounds are dissolved.
- the aqueous phase is added dropwise to the oily phase with stirring.
- the emulsions of Examples 1 and 2 were tested for their stability at temperature over time. Four temperatures were used: -20 ° C, 4 ° C, 42 ° C and 50 ° C. The emulsions were allowed to return to room temperature at defined time intervals (1, 8, 15 days and 1, 2, 3 and 6 months) and their stability was analyzed by observation with the naked eye of the phase separation of the emulsion. With identical time intervals, the apparent viscosity (Brookfield, U.S.A.) was measured at room temperature. The droplet size distribution was determined by laser diffractometry using a Malvern Mastersizer ⁇ plus ® device (Malvern Instruments, England).
- a high resolution cryogenic electron microscope (VG Polaron LT7 400 SEM, XL.40 FEG) was also used to obtain images of the emulsions.
- the samples were frozen in liquid nitrogen, broken at 100 ° K, covered with 4 nm of platinum and observed at 100 ° K.
- the emulsions of Examples 1 and 2 show good stability under the various storage conditions and show no signs of instability, except at 50 ° C. for the emulsion of Example 1, after 15 days of storage. However, this emulsion remained stable after storage at 42 ° C for 3 months, which is proof of good stability under normal conditions of storage. These results make it possible to predict good stability of the emulsions for storage periods of at least 36 months. Analyzes by electron microscopy showed that the emulsions consist of polyhedral domains of water surrounded by thin envelopes of surfactant and oil. The two emulsions are highly polydispersed, the emulsion of example 2 being more polydispersed than that of example 1. Table 1 below represents the percentage distribution of the droplet size two days after their manufacture.
- Percutaneous absorption was measured on human skin obtained after a breast reduction operation. After the operation, the skin was thoroughly washed in water and the subcutaneous fat was removed. Before use, the skin was cut to a thickness of 350 ⁇ m using a dermatome. Penetration through the skin was measured using static diffusion Franz cells (donor surface 1.76 cm 2 , receptor volume 6.5 ml). The preparations were applied at doses of 2.31 ⁇ 0.19 mg / cm 2 for the emulsion of example 1, 2.06 ⁇ 0.32 mg / cm 2 for the emulsion of example 2 and 2.40 ⁇ 0.12 mg / cm 2 for a commercial preparation containing 5% by weight of caffeine, the vehicle of which is a hydroalcoholic gel.
- the receiving liquid was an isotonic phosphate buffer pH 7.4 constantly stirred (300 rpm) and maintained at 32 ° C.
- the skin segment was left to return to equilibrium with the receiving phase for 2 hours before loading each donor compartment with the formulations.
- Six time intervals following application were studied (0.25 hours, 3 hours, 6 hours, 9 hours, 12 hours and 24 hours).
- 1.2 ml of the samples from the recipient phase were removed and each example removed was replaced with an equal volume of fresh recipient phase using an automated system (Microette, Hansen Research Corporation, USA). After 24 hours, the skin surface was washed with 1 ml of a MeOH / H 2 O 50/50 mixture and the excess liquid was absorbed on cotton swabs.
- the skin was removed from the cell and the epidermis and dermis were separated by heating with a dryer. Hair for 30 seconds.
- the caffeine was extracted by washing each compartment of skin with MeOH / H 2 O 50/50 for 24 hours.
- the solutions were filtered through a 0.45 ⁇ m filter and injected into an HPLC device. The dissemination experiment was carried out in triplicate for each vehicle.
- a linear standard curve was constructed using different concentrations of caffeine in the range of 2.0 to 50 mg / liter, and the unknown concentrations were determined using the standard curve as a reference.
- the analyzes were carried out on an HPLC system equipped with a pump (Beckman 110B), a UN detector. (Jasco UV-975) at 273 nm, an integrator (Merck D-2500), an injector (Merck AS-200A), an RP-18 column and a guard column (Lichrosorb 5 column ⁇ m 250 x 4 mm, Lichrospher RP-18E guard column, Merck).
- the separation was carried out at room temperature using a 34/66 methanol / aqueous solution of 7.5 mM heptanesulfonic acid containing 1% glacial acetic acid.
- the flow rate was 0.9 ml / min and the injection volume 20 ⁇ l.
- the vehicle based on hydroalcoholic gel does not make it possible to obtain a constant release of caffeine as a function of time. On the contrary, it shows a high speed during the first six hours which then drops significantly.
Abstract
Description
Claims
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP99936753A EP1104279A1 (fr) | 1998-08-20 | 1999-08-18 | Utilisation d'emulsions stables concentrees eau dans huile pour la liberation percutanee controlee d'un principe actif |
AU51740/99A AU5174099A (en) | 1998-08-20 | 1999-08-18 | Use of stable concentrated water-in-oil emulsions for controlled transcutaneous release of an active principle |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9810588A FR2782453B1 (fr) | 1998-08-20 | 1998-08-20 | Utilisation d'emulsions stables concentrees eau dans huile pour la liberation percutanee controlee d'un principe actif |
FR98/10588 | 1998-08-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2000010511A1 true WO2000010511A1 (fr) | 2000-03-02 |
Family
ID=9529800
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/FR1999/002009 WO2000010511A1 (fr) | 1998-08-20 | 1999-08-18 | Utilisation d'emulsions stables concentrees eau dans huile pour la liberation percutanee controlee d'un principe actif |
Country Status (4)
Country | Link |
---|---|
EP (1) | EP1104279A1 (fr) |
AU (1) | AU5174099A (fr) |
FR (1) | FR2782453B1 (fr) |
WO (1) | WO2000010511A1 (fr) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2997297A1 (fr) * | 2012-10-31 | 2014-05-02 | Caseosa Cosmetics | Emulsion concentree eau dans huile et son utilisation pour le traitement de desordres cutanes cosmetiques ou dermatologiques |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0009404A2 (fr) * | 1978-09-22 | 1980-04-02 | Unilever Plc | Emulsions eau-dans-l'huile et procédé pour leur préparation |
US5523090A (en) * | 1995-02-24 | 1996-06-04 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Skin treatment composition |
FR2758724A1 (fr) * | 1997-01-24 | 1998-07-31 | Javenech | Composition topique a base de protamine pour le traitement de la cellulite et des surcharges ponderales |
-
1998
- 1998-08-20 FR FR9810588A patent/FR2782453B1/fr not_active Expired - Fee Related
-
1999
- 1999-08-18 WO PCT/FR1999/002009 patent/WO2000010511A1/fr not_active Application Discontinuation
- 1999-08-18 EP EP99936753A patent/EP1104279A1/fr not_active Withdrawn
- 1999-08-18 AU AU51740/99A patent/AU5174099A/en not_active Abandoned
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0009404A2 (fr) * | 1978-09-22 | 1980-04-02 | Unilever Plc | Emulsions eau-dans-l'huile et procédé pour leur préparation |
US5523090A (en) * | 1995-02-24 | 1996-06-04 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Skin treatment composition |
FR2758724A1 (fr) * | 1997-01-24 | 1998-07-31 | Javenech | Composition topique a base de protamine pour le traitement de la cellulite et des surcharges ponderales |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2997297A1 (fr) * | 2012-10-31 | 2014-05-02 | Caseosa Cosmetics | Emulsion concentree eau dans huile et son utilisation pour le traitement de desordres cutanes cosmetiques ou dermatologiques |
Also Published As
Publication number | Publication date |
---|---|
FR2782453B1 (fr) | 2001-12-14 |
AU5174099A (en) | 2000-03-14 |
EP1104279A1 (fr) | 2001-06-06 |
FR2782453A1 (fr) | 2000-02-25 |
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