FR2513121A1 - Medicaments contg. brown or red seaweed - for treatment of capillary fragility and permeability, and anti:aggregation agents - Google Patents

Abstract

Medicaments containing a cream or protoexoplasma of brown or red seaweed, are new. Specifically the seaweed which is pref. one of the following: Bifurcaria rotunda, Fucus vesiculosus, Ascophyllum nodosum, Pelvetia canaliculata, or Delessaria sanguinea, is washed and frozen at -10 to -30 deg.C. This frozen material is ground to a particle size of 6-20 microns to give the algal cream. This may be decanted to give two products, a solid and a liq., the liq. being the protoexoplasma. Used for treatment of capillary fragility and capillary permeability, and platelet antiaggregation agents.

Description

 New drugs, cosmetics and dietary products based on seaweed extracts, and corresponding formulations.

 The present invention relates to the therapeutic, cosmetic and dietary use of extracts of certain seaweeds prepared in a special manner.

 We know that there are several families of algae.

 The algae that are used according to the present invention belong to the family of brown algae or phéophycees and red algae or rodophycées.

The invention aims more particularly at the discovery of surprising properties of the following algae
- brown algae
Bifurcaria Rotunda
.Fucus Vesiculosus
.Ascophyllum Nodosum
.Pelvetia Canaliculata
- Delesseria Sanguinea red algae
The properties discovered according to the invention are closely related to the special treatment of these algae which leads to a product exhibiting particular physicochemical characteristics.
The algae are treated as follows.

 We harvest the seaweed, and we wash them in the pool to rid them of the animals and sand.

 They are then subjected to freezing, in particular in a plate freezer, at -10 / -30 C, to allow the conservation of useful elements.

 Cold storage is usually done because the crops are seasonal.

 The algae are then subjected to cryogrinding (two cascading crushers can be used under liquid nitrogen) followed by rolling (a roll machine can be used) and finally homogenization. There is thus obtained a "mud-slurry" whose constitutive particles have a size of 6 to 20 P approximately. This mother liquor is also called "seaweed cream".

 This mother slurry can be passed on a high-speed decanter which gives two products, on the one hand the cake which is called "seaweed base" and on the other hand the decanting juice which is called protoexoplasma of algae ".

 Alternatively, as an indication, this mother-slurry can also be packaged as is.

 Also as an indication, it is possible to lyophilize both the algae cream and protoexoplasma algae to give a dry form that can give rise for example to the manufacture of tablets, etc.

 This sequence of operations is of course valid for each variety of algae.

 In the field of the preparation of these various extracts, reference may be made to French Patent No. 74/35162 filed October 18, 1974 in the name of HERVE and ROULLIER.

 The algae cake for example makes soap and the like, since it contains about 4-6% cellulose, 38-40% insoluble alginates, and fat-soluble vitamins.

 However, the present invention relates to the use for the aforementioned purposes of the cream of algae, and especially, quite preferably, the protoexoplasma of algae.

The tests carried out have in fact highlighted for these products 4 types of activities which are as follows
- venotonic activity
- activity on capillary fragility,
antiplatelet activity of platelets,
- activity at the level of capillary permeability.

 These products can therefore be used in cosmetics, pharmacy, and possibly dietary, in the aforementioned fields, in particular for treating varicose disorders, leg edemas, the phenomenon known as "heavy legs", and generally the conditions requiring an action on the central and / or peripheral circulation.

 In cosmetics, it will be mainly used topical forms, including creams.

 In the pharmaceutical field, it will of course also be possible to use topical routes of administration but also surprisingly oral routes of administration (the formulations then consisting of syrups, drinkable ampoules and the like). Injectable forms are conceivable.

 In dietetics, we can use similar forms.

Among the algae mentioned above it was found that the variety leading to the most active product was laDelesseria
Sanguinea or Pelvetia Canaliculata.

 It can be seen that the properties indicated above are within the range of activity of a known product, heparin.

 However, this known product, which must be subjected to an excessive purification that alone prevents anaphylactic rejects and shocks, is excessively expensive since the current price of the gram of Heparin is about 1.000 F. more heparin or a derivative thereof can be administered only by injection or cutaneous route.

 On the contrary, according to the invention, it is possible for the first time to obtain a Heparin-like effect thanks to a natural product which is much less expensive and which can be administered orally.

 The algae belonging to the abovementioned families, and in particular the 5 varieties indicated, may contain up to 20 g / kg of sulfuryl polysaccharides having heparinomimetic effects.

 This type of molecule has already been isolated to a certain extent, but there has been very little if any effectiveness.

 On the contrary, according to the invention, it has been possible to obtain a very active product thanks to the special process of treatment described above which leads to a product also special (seaweed cream or especially protoexoplasma algae).

 This surprising effect is thought to be due to the fact that the special process of algae treatment allows to keep around the active molecule an enzymatic system (which can also contain certain vitamins) whereas the known processes (dehydration, drying, extraction, etc.) necessarily destroy this system (this system consists in particular of amino acids, phytohormones, vitamins, etc.).

 Without this being of course any limitation, the Applicant believes that the activity that it has been possible to conserve in a surprising way is due to the conservation of this enzymatic system and to a certain interaction between this system and the basic molecule. .

 We will not return here to the basic molecule itself, which consists of a sulfuryl polysaccharide which designates a set of neighboring molecules which can be grouped into two families, the fucoidans and the xylo-galacto-urono-fucans.

With regard in particular to the variety Delesseria
Sanguinea * note the following pharmacological properties
anticoagulant properties,
anti-aggregation properties of platelets,
- antibiotic properties.

 The following is a blood test result taken before and after taking oral protoexoplasma.

HEPARIN TOLERANCE TEST
WITNESS
PATIENT X
Before taking protoexoplasma of algae
PATIENT X
After taking protoexoplasma of algae - Time tl

<tb><SEP> TIME <SEP> O <SEP> S <SEP> U <SEP> 1 <SEP> U <SEP> INDEX <SEP> FROM
<tb> DE <SEP> HOWELL <SEP>, <SEP> U. <SEP>. <SEP> U. <SEP> COAGUBILITE
<tb><SEP> FROM <SEP> BLOOD
<tb><SEP> 2 '<SEP>7'<SEP> 12 '
<tb><SEP> 2 '<SEP>7'30<SEP>13'<SEP> 1
<tb><SEP> 2 '<SEP>7'<SEP> 14 '<SEP> 0.92
<tb> (continued from table next page)
PATIENT X
After taking protoexoplasma of algae - Time t2
PATIENT X
After stopping the intake of protoexoplasma of algae
Time t3

<tb><SEP> TIME <SEP> 0.5 <SE> U. <SEP> 1U. <SEP> INDEX <SEP> OF
<tb> DE <SEP> HOWELL <SEP> 0.5 <SEP> U. <SEP> u <SEP> U. <SEP> COAGUBILITY <SEP>
<tb><SEP> FROM <SEP> BLOOD
<tb><SEP> 2 '<SEP>8'10<SEP>15'<SEP> 0.84
<tb><SEP> 2 '<SEP>7'<SEP>12'30<SEP> 1
<Tb>
This test was conducted in the following manner.

 The seaweed used is the variety Ascophyllum Nodosum.

 As described above, a protoexoplasm of this alga was prepared which was administered orally at 5cc morning and evening to an adult patient.

 The time t1 corresponds to a measurement made after one month of this treatment.

 The time t2 corresponds to the measurement made after two months of this treatment.

 Time t corresponds to a measurement made one month after t2, without administration of prctoexplasma between t2 and t3.

 There is a return of normal to t3.

The algal toxicity was determined by the method of
Litchfield and Wilcoxon in the mouse. This test did not reveal any significant toxicity.

 Those skilled in the art, given the composition and the physical presentation of the seaweed cream and the protoexoplasma of algae, will be able to prepare the formulations that can be applied in cosmetics or therapeutically administered creams, syrups, drinkable ampoules, without any difficulty.

Claims (13)

1. Novel venotonic action drugs, on capillary fragility, antiagregation of blood platelets, and on capillary permeability, characterized in that they consist of "cream" or protoexoplasma of brown or red algae. 2. New medicaments according to claim 1, characterized in that they consist of a protoexoplasma of brown or red algae, the particle size of protoexoplasma being about 6 to 20. 3. New drugs according to claim 1 or 2, characterized in that the algae used are chosen from the following:  - brown algae:  . Bifurcaria Rotunda  . Fucus Vesiculpsus  . Ascophyllum Nodosum  . Pelvetia Canaliculata  - red algae:  . Delesseria sanguinea 4. New drugs according to any one of claims 1 to 3, characterized in that the alga used is the Delesseria Sanguinea. 5. New drugs according to any one of claims 1 3, characterized in that the alga used is Pelvetia Canaliculata. 6. New medicaments according to any one of claims 1 to 3, characterized in that the alga used is Asco phyllum Nodosum. 7. Pharmaceutical form of oral administration of new drugs according to any one of claims 1 to 6, in unit oral form of 5 cc. 8. Pharmaceutical form of administration of new drugs according to any one of claims 1 to 6 in topical or injectable form. 9. Cosmetic or dietary composition characterized in that it consists of a protoexoplasma or cream of brown or red algae. 10. Composition according to claim 9, characterized in that it consists of a protoexoplasma of brown or red algae, the particle size of the protoexoplasma being from 6 to 201u. 11. Composition according to claim 9 or 10, characterized in that the algae are selected from brown algae  Bifurcaria Rotunda  - Fucus Vesiculosus  - Ascophyllum Nodosum  - Pelvetia Canaliculata and red algae  - Delesseria Sanguinea. 12. New product characterized in that it consists of a "cream" or "protoexoplasma" of red algae or rodophycec. 13. New product according to claim 12, characterized in that the red algae is Delesseria Sanguinea.