WO1998019663A1 - Compositions for topical use containing polysaccharide sulphates - Google Patents
Compositions for topical use containing polysaccharide sulphates Download PDFInfo
- Publication number
- WO1998019663A1 WO1998019663A1 PCT/EP1997/006074 EP9706074W WO9819663A1 WO 1998019663 A1 WO1998019663 A1 WO 1998019663A1 EP 9706074 W EP9706074 W EP 9706074W WO 9819663 A1 WO9819663 A1 WO 9819663A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- polysaccharide
- compositions according
- sulphates
- molecular weight
- daltons
- Prior art date
Links
- 229920001282 polysaccharide Polymers 0.000 title claims abstract description 43
- 239000005017 polysaccharide Substances 0.000 title claims abstract description 43
- -1 polysaccharide sulphates Chemical class 0.000 title claims abstract description 39
- 239000000203 mixture Substances 0.000 title claims abstract description 38
- 230000000699 topical effect Effects 0.000 title claims abstract description 8
- 229920001525 carrageenan Polymers 0.000 claims abstract description 20
- 235000010418 carrageenan Nutrition 0.000 claims abstract description 20
- 239000000499 gel Substances 0.000 claims abstract description 15
- 239000002537 cosmetic Substances 0.000 claims abstract description 13
- 239000006071 cream Substances 0.000 claims abstract description 10
- 239000004480 active ingredient Substances 0.000 claims description 14
- 229910021653 sulphate ion Inorganic materials 0.000 claims description 10
- 238000002360 preparation method Methods 0.000 claims description 4
- 239000002245 particle Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 239000002671 adjuvant Substances 0.000 claims description 2
- 239000004615 ingredient Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract description 4
- 238000009472 formulation Methods 0.000 description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- 210000002615 epidermis Anatomy 0.000 description 6
- MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 description 5
- 239000008223 sterile water Substances 0.000 description 5
- 150000004676 glycans Chemical class 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 239000000725 suspension Substances 0.000 description 4
- 229920002385 Sodium hyaluronate Polymers 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 239000002304 perfume Substances 0.000 description 3
- 229940010747 sodium hyaluronate Drugs 0.000 description 3
- JNAYPSWVMNJOPQ-UHFFFAOYSA-N 2,3-bis(16-methylheptadecanoyloxy)propyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCC(C)C)COC(=O)CCCCCCCCCCCCCCC(C)C JNAYPSWVMNJOPQ-UHFFFAOYSA-N 0.000 description 2
- 241000195493 Cryptophyta Species 0.000 description 2
- 235000014121 butter Nutrition 0.000 description 2
- 239000004205 dimethyl polysiloxane Substances 0.000 description 2
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 2
- 239000006210 lotion Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- DNIAPMSPPWPWGF-UHFFFAOYSA-N monopropylene glycol Natural products CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 2
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N n-octadecyl alcohol Natural products CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 108010011485 Aspartame Proteins 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 244000146462 Centella asiatica Species 0.000 description 1
- 235000004032 Centella asiatica Nutrition 0.000 description 1
- 241000206575 Chondrus crispus Species 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- 102000011782 Keratins Human genes 0.000 description 1
- 108010076876 Keratins Proteins 0.000 description 1
- 229920000715 Mucilage Polymers 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
- 229960003438 aspartame Drugs 0.000 description 1
- 235000010357 aspartame Nutrition 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 description 1
- 210000004207 dermis Anatomy 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 229930182830 galactose Natural products 0.000 description 1
- 229940075529 glyceryl stearate Drugs 0.000 description 1
- 230000035876 healing Effects 0.000 description 1
- 229940119170 jojoba wax Drugs 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- 229940073665 octyldodecyl myristate Drugs 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 239000003973 paint Substances 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229940069338 potassium sorbate Drugs 0.000 description 1
- 235000010241 potassium sorbate Nutrition 0.000 description 1
- 239000004302 potassium sorbate Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 239000002453 shampoo Substances 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 238000002791 soaking Methods 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000002344 surface layer Substances 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
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
- A61K8/042—Gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- 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 present invention relates to a new polysaccharide sulphate having an average molecular weight of from 60 000 to 180 000 Daltons for use mainly in the field of cosmetics and pharmaceuticals.
- Polysaccharide sulphates and in particular copolymer sulphates of (l-3)-D- galactose and (l-4)-3,6-anhydro-D-galactose or (l-4)-3,6- anhydro-L- galactose generally known as carrageenins, carrageenans or carrageens (The Merck Index, 11th Edition), have already been known and used for a long time owing to their properties of increasing the viscosity of aqueous solutions and suspensions and for their role as stabilising agents in respect of such solutions and suspensions.
- polysaccharide sulphates are generally used for the preparation of gels, lotions, pastes, creams and ointments for topical use, although they are often used in other fields, such as, for example, in the food industry, especially with regard to the stabilisation of suspensions and emulsions containing milk or its derivatives, or in the paint and dyestuff industry.
- Carrageenins in particular, are polysaccharide sulphates of natural origin which are normally extracted from algae and mucilage and which are classified in accordance with their structural formula as kappa, kappa II, iota, lambda, mu, nu and theta carrageenins.
- the commercial carrageenins generally available on the market contain all the forms in variable percentages, although the kappa, iota and lambda forms generally predominate.
- viscosity values are of substantial importance because they permit optimum "spreadability" of the formulation, thus increasing the permeability, through the epidermis, of the active ingredients optionally contained therein.
- the aim of the present invention is to provide cosmetic or pharmaceutical compositions for topical use, in the form of gels or creams, which do not have the disadvantages which characterised and still characterise the formulations currently on the market containing polysaccharide sulphates having a high molecular weight.
- the customary formulations in the form of gels or creams for topical use contain polysaccharide sulphates and/or carrageenins having a molecular weight of generally from 250 000 to 500 000 Daltons.
- the aim of the present invention is therefore to provide new cosmetic and pharmaceutical compositions in the form of gels or creams containing polysaccharide sulphates and capable of carrying active ingredients, while avoiding both the formation of troublesome and excessively rigid films on the epidermis, and the difficulties of absorption and thus lesser therapeutic or cosmetic efficacy.
- polysaccharide sulphates preferably carrageenins, having an average molecular weight of from 60 000 to 180 000 Daltons, preferably from 70 000 to 160 000 Daltons.
- the carrageenins and, more generally, the polysaccharide sulphates used in the implementation of the present invention are obtained by the depolymerisation of polysaccharide sulphates, preferably commercial carrageenins, having a higher molecular weight.
- the starting polysaccharide sulphates must have an average molecular weight of from 400 000 to 1 000 000 Daltons, preferably from 500 000 to 700 000
- the preferred concentrations of the suitably depolymerised polysaccharide sulphate for the implementation of the present invention may vary from 0.2 to
- the gels and the creams according to the present invention may be prepared simply by soaking the depolymerised polysaccharide in an aqueous solution containing the active ingredients, and optionally also conventional excipients and adjuvants, at a temperature of from 40 to 60°C for a period of from 45 to
- formulations are thus obtained which have a viscosity (generally from 3000 to 9000 mPas at a temperature of 25°C when the concentration of the polysaccharide sulphate is
- the formulations thus obtained have the ability to create surface layers which penetrate completely into the epidermis, avoiding the creation of a rigid and troublesome film thereon.
- the formulations of the present invention are also colourless, clear and perfectly spreadable on the epidermis with rapid and complete penetration, leaving the skin with a pleasant soft, glowing and smooth feel.
- the polysaccharides according to the present invention can be used in association with other gelling substances, both of synthetic nature (such as carboxypolymethylcellulose or carboxymethylcellulose) and of natural origin, thus obtaining gel-form formulations that are especially continuous, uniform and consistent, without losing the characteristics mentioned above.
- the formulations according to the present invention therefore lend themselves well to various uses, both in the cosmetic field and the pharmaceutical field; they can be used as carriers for one or more active ingredients or can be used directly for their moisturising and toning power.
- microsuspensions in the form of homogeneous and uniform gels even in cases where water-insoluble active ingredients are used, such as, for example, sucralphate and non-steroidal anti- inflammatory drugs, in the case of active ingredients for pharmaceutical use, and Centella asiatica or liposoluble vitamins in the case of active ingredients for cosmetic use.
- active ingredients such as, for example, sucralphate and non-steroidal anti- inflammatory drugs, in the case of active ingredients for pharmaceutical use, and Centella asiatica or liposoluble vitamins in the case of active ingredients for cosmetic use.
- the active ingredient for introduction into the composition it is, however, necessary for the active ingredient for introduction into the composition to be in the form of micronised particles having a diameter of less than 10 ⁇ .
- the preparation of microsuspensions in the form of gels would be difficult if not impossible using carrageenins having a low molecular weight, such as, for example, those in US patent No. 4,543,250 because, in addition to the already- mentioned contra-indications, it would not be possible to obtain a density sufficient to maintain the microsuspension and therefore the active ingredient would precipitate.
- the formulations of the present invention can be subjected to lyophilisation without any contra-indications.
- the following Examples are given purely by way of non-limiting illustration of the invention (the parts are to be understood as parts by weight).
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Dermatology (AREA)
- Birds (AREA)
- Dispersion Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Cosmetics (AREA)
- Medicinal Preparation (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
Abstract
New cosmetic or pharmaceutical compositions for topical use in the form of gels or creams are described. The compositions contain polysaccharide sulphates, preferably carrageenins, having an average molecular weight of from 60 000 to 180 000 Daltons, preferably from 70 000 to 160 000 Dalton.
Description
COMPOSITIONS FOR TOPICAL USE CONTAINING POLYSACCHARIDE SULPHATES
The present invention relates to a new polysaccharide sulphate having an average molecular weight of from 60 000 to 180 000 Daltons for use mainly in the field of cosmetics and pharmaceuticals.
Polysaccharide sulphates and in particular copolymer sulphates of (l-3)-D- galactose and (l-4)-3,6-anhydro-D-galactose or (l-4)-3,6- anhydro-L- galactose, generally known as carrageenins, carrageenans or carrageens (The Merck Index, 11th Edition), have already been known and used for a long time owing to their properties of increasing the viscosity of aqueous solutions and suspensions and for their role as stabilising agents in respect of such solutions and suspensions. Therefore, polysaccharide sulphates are generally used for the preparation of gels, lotions, pastes, creams and ointments for topical use, although they are often used in other fields, such as, for example, in the food industry, especially with regard to the stabilisation of suspensions and emulsions containing milk or its derivatives, or in the paint and dyestuff industry. Carrageenins, in particular, are polysaccharide sulphates of natural origin which are normally extracted from algae and mucilage and which are classified in accordance with their structural formula as kappa, kappa II, iota, lambda, mu, nu and theta carrageenins. The commercial carrageenins generally available on the market contain all the forms in variable percentages, although the kappa, iota and lambda forms generally predominate.
The literature describes numerous methods of extracting and purifying carrageenins, and also various examples of cosmetic and pharmaceutical compositions based on polysaccharide sulphates and, in particular, carrageenins. US patent No. 3,236,833 describes a process for the extraction of carrageenin from marine algae by using hydrogen peroxide, while US patent No. 4,443,486 describes a process for the depolymerisation of commercial carrageenins based on the use of an aqueous hydrogen peroxide solution at a temperature of 75°C.
As evidenced in US patent No. 4,543,250, carrageenins which are generally used for the preparation of formulations for pharmaceutical or cosmetic use are characterised in that they have a molecular weight of generally from 250 000 to 500 000 Daltons. These formulations have typical viscosities of from 3000 to 20 000 mPas at ambient temperature, in the case of concentrations of the polysaccharide variable from 1.5 to 2 % by weight.
These viscosity values, in particular, are of substantial importance because they permit optimum "spreadability" of the formulation, thus increasing the permeability, through the epidermis, of the active ingredients optionally contained therein.
The above-mentioned US patent No. 4,543,250 of Henry J. Witt marked a turning-point of substantial importance as regards the already well established approach to the use of polysaccharide sulphates and more specifically carrageenins in the production of formulations for cosmetic use and, in particular, in the production of shampoos or lotions for hair treatment. That patent teaches the use of polysaccharides having an extremely low molecular weight which, owing to their reduced dimensions, permit a substantial increase in the speed of reaction with the proteins of the dermis and above all the hair (keratin), leading to a considerable improvement in the healing effect which confers a smooth, soft and shining appearance on the hair.
According to the teaching of Henry J. Witt, these results are achieved by using highly depolymerised polysaccharide sulphates having a molecular weight of from 15 000 to 10 000 Daltons so that a 1.5 % by weight aqueous solution thereof has a viscosity not greater than 5 mPas at 75°C. The technical problem which the present invention is to solve differs substantially from those forming the main objects of the above-mentioned US patent.
The aim of the present invention is to provide cosmetic or pharmaceutical compositions for topical use, in the form of gels or creams, which do not have
the disadvantages which characterised and still characterise the formulations currently on the market containing polysaccharide sulphates having a high molecular weight. As already mentioned, the customary formulations in the form of gels or creams for topical use contain polysaccharide sulphates and/or carrageenins having a molecular weight of generally from 250 000 to 500 000 Daltons. However, this type of formulation has the disadvantage, which has still not been resolved satisfactorily, of creating on the epidermis a more or less rigid film which, in the majority of cases, renders the application thereof unpleasant and troublesome, causing preference to be given to the use of formulations having a lower viscosity, such as, for example, those of the already mentioned US patent No. 4,543,250. These latter formulations, owing to their lower viscosity and density, are more difficult for the epidermis to absorb, to the detriment of the cosmetic or therapeutic effect of the active ingredient contained therein. The aim of the present invention is therefore to provide new cosmetic and pharmaceutical compositions in the form of gels or creams containing polysaccharide sulphates and capable of carrying active ingredients, while avoiding both the formation of troublesome and excessively rigid films on the epidermis, and the difficulties of absorption and thus lesser therapeutic or cosmetic efficacy.
This surprising result is obtained by using polysaccharide sulphates, preferably carrageenins, having an average molecular weight of from 60 000 to 180 000 Daltons, preferably from 70 000 to 160 000 Daltons. The carrageenins and, more generally, the polysaccharide sulphates used in the implementation of the present invention are obtained by the depolymerisation of polysaccharide sulphates, preferably commercial carrageenins, having a higher molecular weight. For a more advantageous implementation of the invention, the starting polysaccharide sulphates must have an average molecular weight of
from 400 000 to 1 000 000 Daltons, preferably from 500 000 to 700 000
Daltons.
Processes for depolymerising the polysaccharide sulphates are well known in the art and generally use hydrogen peroxide (see, for example, US patents No. 3,236,833 and No. 4,443,486) or alkalies.
The preferred concentrations of the suitably depolymerised polysaccharide sulphate for the implementation of the present invention may vary from 0.2 to
10 % by weight as a function of the desired final viscosity.
The gels and the creams according to the present invention may be prepared simply by soaking the depolymerised polysaccharide in an aqueous solution containing the active ingredients, and optionally also conventional excipients and adjuvants, at a temperature of from 40 to 60°C for a period of from 45 to
90 minutes.
As can be seen from the data compiled in Table 1, formulations are thus obtained which have a viscosity (generally from 3000 to 9000 mPas at a temperature of 25°C when the concentration of the polysaccharide sulphate is
1.5 % by weight) comparable to that of the formulations currently available on the market, and which are therefore also spreadable but free from the disadvantages mentioned above.
TABLE 1
As already mentioned, the formulations thus obtained have the ability to create surface layers which penetrate completely into the epidermis, avoiding the creation of a rigid and troublesome film thereon.
In contrast, the carrageenins having a low molecular weight described in US patent No. 4,543,250 could not be used for the purposes of the present invention. It has been found that formulations containing carrageenins having a molecular weight of 48 000 - 49 000 Daltons in concentrations of 1.5 and 2 % have, respectively, viscosities of 1000 and 5000 mPas, respectively, which values are too low to ensure perfectly and easily spreadable formulations and which thus preclude a priori the use of polysaccharide sulphates having a molecular weight of approximately 10 000 - 15 000 Daltons for this purpose.
The formulations of the present invention are also colourless, clear and perfectly spreadable on the epidermis with rapid and complete penetration, leaving the skin with a pleasant soft, glowing and smooth feel. The polysaccharides according to the present invention can be used in association with other gelling substances, both of synthetic nature (such as carboxypolymethylcellulose or carboxymethylcellulose) and of natural origin, thus obtaining gel-form formulations that are especially continuous, uniform and consistent, without losing the characteristics mentioned above. The formulations according to the present invention therefore lend themselves well to various uses, both in the cosmetic field and the pharmaceutical field; they can be used as carriers for one or more active ingredients or can be used directly for their moisturising and toning power. In this connection, it is important to underline that, according to the present invention, it is also possible to obtain microsuspensions in the form of homogeneous and uniform gels even in cases where water-insoluble active ingredients are used, such as, for example, sucralphate and non-steroidal anti- inflammatory drugs, in the case of active ingredients for pharmaceutical use, and Centella asiatica or liposoluble vitamins in the case of active ingredients for cosmetic use.
For this particular embodiment of the invention it is, however, necessary for the active ingredient for introduction into the composition to be in the form of micronised particles having a diameter of less than 10 μ. The preparation of microsuspensions in the form of gels would be difficult if not impossible using carrageenins having a low molecular weight, such as, for example, those in US patent No. 4,543,250 because, in addition to the already- mentioned contra-indications, it would not be possible to obtain a density sufficient to maintain the microsuspension and therefore the active ingredient would precipitate.
It is also important to note how the formulations of the present invention can be subjected to lyophilisation without any contra-indications. The following Examples are given purely by way of non-limiting illustration of the invention (the parts are to be understood as parts by weight). Example 1 - Day cream
- Stearyl alcohol (21 ) EO : 3 %
- Stearyl alcohol (2) EO : 3.5 %
- Cetylstearyl alcohol : 2.5 %
- Karit butter: 3 % - Octyldodecyl myristate: 7 %
- Transesterified glyceryl triiso stearate (6) EO: 2 %
- Dimethylpolysiloxane: 1 %
- Sterile water: q.s. 100
- Acrylates: 1 % - Low MW* polysaccharide sulphate (102 000 Da): 0.5 %
- Glycosamine glycans: 0.3 %
- Vitamin E acetate: 1 %
- Perfume: 0.25 % *MW = molecular weight Example 2 - Moisturising cream
- Glyceryl stearate: 10 %
- Cetylstearyl alcohol: 10 %
- Hydrolysed potassium palmital protein: 10 %
- Jojoba oil: 5 % - Non-hydrolysable olive oil: 4 %
- Dimethylpolysiloxane: 1 %
- Karit butter: 5 %
- Self-oxidising mixture: 0.05 %
- Sterile water: q.s. 100
- Sodium hyaluronate: 0.1 %
- Low MW polysaccharide sulphate (75 000 Da): 0.6 %
- Glycerol: 4 %
- Perfume: 0.25 %
Example 3 - Leg gel
- Glycerol: 30 %
- Propylene glycol 20 %
- Sodium hyaluronate 0.1 %
- Low MW polysaccharide sulphate (75 000 Da): 0.4 %
- Glycosamine glycans: 0.3 %
- Sterile water: q.s. 100
Example 4 - Moisturising gel
- Glycerol: 3 %
- Sodium hyaluronate: 3%
- Acrylates: 0.5 %
- Low MW polysaccharide sulphate (115 000 Da): 0.6 %
- Sterile water: q.s. 100
- Perfume: 0.25 %
Example 5 - Moisturising gel
- Low MW polysaccharide sulphate (75 000 Da): 1.5 %
- Sterile water: q.s. 100
- Optional addition of KC1
Example 6 - Suspension in the form of sucralphate gel
- Sucralphate: 20 %
- Low MW polysaccharide sulphate (162 000 Da): 0.4 %
- Sorbitol: 12 %
- Potassium sorbate: 0.2 %
- Aspartame: 0.1 %
- Pulvaroma: 1.4 %
- Demineralised water: q.s. 100
These gels by themselves or with active ingredients in suspension or in solution together with other excipients give rise to crosslinked light patches keeping the active ingredients completely distributed. These patches can be used as such with bandages or in other manners.
Claims
I . Compositions for topical use in the form of gels or creams, characterised in that they contain polysaccharide sulphates having an average molecular weight of from 60 000 to 180 000 Daltons.
2. Compositions according to Claim 1, characterised in that the polysaccharide sulphates have an average molecular weight of from 70 000 to 160 000 Daltons.
3. Compositions according to Claim 1, characterised in that the polysaccharide sulphates are carrageenins.
4. Compositions according to Claim 1, characterised in that they contain at least one cosmetic or pharmaceutical active ingredient.
5. Compositions according to Claim 1, characterised in that the polysaccharide sulphates are obtained by the depolymerisation of polysaccharide sulphates having an average molecular weight of from 400 000 to 1 000 000 Daltons.
6. Compositions according to Claim 5, characterised in that the polysaccharide sulphates are obtained by the depolymerisation of polysaccharide sulphates having an average molecular weight of from 500 000 to 700 000 Daltons.
7. Compositions according to Claim 1, characterised in that the polysaccharide sulphates are present in a variable amount of from 0.2 to 10 % by weight.
8. Compositions according to Claim 1, characterised in that they exhibit a viscosity of from 3000 to 9000 mPas at a temperature of 25°C when the concentration of the polysaccharide sulphate is 1.5 % by weight.
9. Compositions according to Claim 8, characterised in that they exhibit a viscosity of from 3500 to 4300 mPas.
10. Compositions according to Claim 1, characterised in that they contain the conventional excipients and adjuvants.
I I . Compositions according to Claim 1, characterised in that they contain water-insoluble ingredients in the form of micronised particles.
12. Compositions according to Claim 11, characterised in that the micronised particles have a diameter of less than 10 μ.
13. Compositions according to Claims 11 and 12, characterised in that they are in the form of gelled microsuspensions.
14. Compositions according to Claim 1 in lyophilised form.
15. Use of polysaccharide sulphates having an average molecular weight of from 60 000 to 180 000 Daltons for the preparation of compositions for topical use in the form of gels or creams.
16. Use according to Claim 15, characterised in that the polysaccharide sulphates have an average molecular weight of from 70 000 to 160 000 Daltons.
17. Use of polysaccharide sulphates according to Claim 15 together with cosmetic and pharmaceutical active ingredients.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP97950086A EP0955997A1 (en) | 1996-11-04 | 1997-10-29 | Compositions for topical use containing polysaccharide sulphates |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH271996A CH690814A5 (en) | 1996-11-04 | 1996-11-04 | Compositions for topical use containing sulphates polysaccharides. |
| CH2719/96 | 1996-11-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO1998019663A1 true WO1998019663A1 (en) | 1998-05-14 |
Family
ID=4240068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP1997/006074 WO1998019663A1 (en) | 1996-11-04 | 1997-10-29 | Compositions for topical use containing polysaccharide sulphates |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP0955997A1 (en) |
| CH (1) | CH690814A5 (en) |
| WO (1) | WO1998019663A1 (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1424081A4 (en) * | 2001-08-10 | 2005-09-21 | Toray Industries | Polysaccharide-containing compositions and use thereof |
| FR2876581A1 (en) * | 2004-10-20 | 2006-04-21 | Interpharm Dev | BIOADHESIVE COMPOSITION WITH PROGRAMMED RELEASE |
| FR2895907A1 (en) * | 2006-01-06 | 2007-07-13 | Anteis Sa | VISCOELASTIC GEL FOR DERMATOLOGICAL USE |
| WO2011117547A1 (en) * | 2010-03-25 | 2011-09-29 | Greentech | Oligosaccharide extracted from halymenia durvillaei, method for preparing such an oligosaccharide, and cosmetic use of said oligosaccharide |
| AU2012200105B2 (en) * | 2004-10-20 | 2014-11-20 | Care & Pharma Perspectives Sa | Bioadhesive composition with programmed release |
| WO2017129780A1 (en) * | 2016-01-29 | 2017-08-03 | Societe Industrielle Limousine D'application Biologique | Cosmetic agent consisting of galactomannans obtained from caesalpinia spinosa and cross-linked sulphated galactans obtained from kappaphycus alvarezii |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1984004039A1 (en) * | 1983-04-11 | 1984-10-25 | Fmc Corp | Toiletry formulations |
| JPS63150209A (en) * | 1986-12-15 | 1988-06-22 | Kanebo Ltd | Skin cosmetic |
| EP0495421A1 (en) * | 1991-01-15 | 1992-07-22 | Alcon Laboratories, Inc. | Use of carrageenans in topical ophthalmic compositions |
| FR2690450A1 (en) * | 1992-04-27 | 1993-10-29 | Coletica | Derivatives of undecylenic acid with hydrophilic macromolecules and uses in cosmetics or pharmacy. |
| WO1994015624A1 (en) * | 1993-01-08 | 1994-07-21 | The Population Council | Use of sulphated polysaccharides for preventing sexually transmitted diseases |
| JPH07118306A (en) * | 1993-10-26 | 1995-05-09 | Maruho Kk | Water-in-oil emulsion containing sulfated polysaccharide |
| EP0730867A2 (en) * | 1995-03-09 | 1996-09-11 | RES PHARMA S.r.l. | Non-animal polyanions for use in dermatology and cosmetics |
-
1996
- 1996-11-04 CH CH271996A patent/CH690814A5/en not_active IP Right Cessation
-
1997
- 1997-10-29 EP EP97950086A patent/EP0955997A1/en not_active Withdrawn
- 1997-10-29 WO PCT/EP1997/006074 patent/WO1998019663A1/en not_active Application Discontinuation
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1984004039A1 (en) * | 1983-04-11 | 1984-10-25 | Fmc Corp | Toiletry formulations |
| US4543250A (en) * | 1983-04-11 | 1985-09-24 | Fmc Corporation | Toiletry formulations comprising low molecular weight carrageenan |
| JPS63150209A (en) * | 1986-12-15 | 1988-06-22 | Kanebo Ltd | Skin cosmetic |
| EP0495421A1 (en) * | 1991-01-15 | 1992-07-22 | Alcon Laboratories, Inc. | Use of carrageenans in topical ophthalmic compositions |
| FR2690450A1 (en) * | 1992-04-27 | 1993-10-29 | Coletica | Derivatives of undecylenic acid with hydrophilic macromolecules and uses in cosmetics or pharmacy. |
| WO1994015624A1 (en) * | 1993-01-08 | 1994-07-21 | The Population Council | Use of sulphated polysaccharides for preventing sexually transmitted diseases |
| JPH07118306A (en) * | 1993-10-26 | 1995-05-09 | Maruho Kk | Water-in-oil emulsion containing sulfated polysaccharide |
| EP0730867A2 (en) * | 1995-03-09 | 1996-09-11 | RES PHARMA S.r.l. | Non-animal polyanions for use in dermatology and cosmetics |
Non-Patent Citations (2)
| Title |
|---|
| DATABASE WPI Section Ch Week 9527, Derwent World Patents Index; Class A11, AN 95-203841, XP002058631 * |
| PATENT ABSTRACTS OF JAPAN vol. 012, no. 410 (C - 540) 28 October 1988 (1988-10-28) * |
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1424081A4 (en) * | 2001-08-10 | 2005-09-21 | Toray Industries | Polysaccharide-containing compositions and use thereof |
| FR2876581A1 (en) * | 2004-10-20 | 2006-04-21 | Interpharm Dev | BIOADHESIVE COMPOSITION WITH PROGRAMMED RELEASE |
| WO2006043005A3 (en) * | 2004-10-20 | 2007-04-05 | Interpharm Dev Sa | Bioadhesive composition with programmed release |
| AU2012200105B2 (en) * | 2004-10-20 | 2014-11-20 | Care & Pharma Perspectives Sa | Bioadhesive composition with programmed release |
| US20160235715A1 (en) * | 2004-10-20 | 2016-08-18 | Care & Pharma Perspectives Sa | Pasty Bio-Adhesive Sustained Release Compositions |
| US10646435B2 (en) * | 2004-10-20 | 2020-05-12 | Care & Pharma Perspectives Sa | Pasty bio-adhesive sustained release compositions |
| FR2895907A1 (en) * | 2006-01-06 | 2007-07-13 | Anteis Sa | VISCOELASTIC GEL FOR DERMATOLOGICAL USE |
| WO2011117547A1 (en) * | 2010-03-25 | 2011-09-29 | Greentech | Oligosaccharide extracted from halymenia durvillaei, method for preparing such an oligosaccharide, and cosmetic use of said oligosaccharide |
| FR2957923A1 (en) * | 2010-03-25 | 2011-09-30 | Greentech | NOVEL HALYMENIA DURVILLEI EXTRACT, PROCESS FOR PREPARING SUCH EXTRACT AND COSMETIC USE THEREOF |
| WO2017129780A1 (en) * | 2016-01-29 | 2017-08-03 | Societe Industrielle Limousine D'application Biologique | Cosmetic agent consisting of galactomannans obtained from caesalpinia spinosa and cross-linked sulphated galactans obtained from kappaphycus alvarezii |
| FR3047173A1 (en) * | 2016-01-29 | 2017-08-04 | Soc Ind Limousine D'application Biologique | COSMETIC AGENT CONSISTING OF GALACTOMANNANES OBTAINED FROM CAESALPINIA SPINOSA AND SULFATE GALACTANES OBTAINED FROM KAPPAPHYCUS ALVAREZII |
| US10987297B2 (en) | 2016-01-29 | 2021-04-27 | Societe Industrielle Limousine D'application Biologique | Cosmetic agent formed by galactomannans obtained from Caesalpinia spinosa and cross-linked sulphated galactans obtained from Kappaphycus alvarezii |
Also Published As
| Publication number | Publication date |
|---|---|
| EP0955997A1 (en) | 1999-11-17 |
| CH690814A5 (en) | 2001-01-31 |
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