U.S. patent application number 12/733172 was filed with the patent office on 2010-06-24 for flavored clay-based therapeutic composition.
Invention is credited to Jerome Barra, Denis Le Hazie.
Application Number | 20100159013 12/733172 |
Document ID | / |
Family ID | 39052728 |
Filed Date | 2010-06-24 |
United States Patent
Application |
20100159013 |
Kind Code |
A1 |
Barra; Jerome ; et
al. |
June 24, 2010 |
flavored clay-based therapeutic composition
Abstract
The subject of the present invention is a flavored therapeutic
composition containing a clay as well as active principle, and
characterized in that the clay is a dioctahedral smectite and the
flavor is encapsulated.
Inventors: |
Barra; Jerome; (Neydens,
FR) ; Le Hazie; Denis; (Vernouillet, FR) |
Correspondence
Address: |
HUNTON & WILLIAMS LLP;INTELLECTUAL PROPERTY DEPARTMENT
1900 K STREET, N.W., SUITE 1200
WASHINGTON
DC
20006-1109
US
|
Family ID: |
39052728 |
Appl. No.: |
12/733172 |
Filed: |
August 12, 2008 |
PCT Filed: |
August 12, 2008 |
PCT NO: |
PCT/FR2008/001185 |
371 Date: |
February 16, 2010 |
Current U.S.
Class: |
424/488 ;
424/684 |
Current CPC
Class: |
A61P 1/12 20180101; A61P
1/06 20180101; A61P 1/00 20180101; A61K 9/0056 20130101; A61K 33/12
20130101; A61K 33/06 20130101; A61P 1/04 20180101; A61K 35/02
20130101; A61K 9/4816 20130101; A61K 9/0095 20130101; A61P 29/00
20180101 |
Class at
Publication: |
424/488 ;
424/684 |
International
Class: |
A61K 9/00 20060101
A61K009/00; A61K 33/06 20060101 A61K033/06 |
Foreign Application Data
Date |
Code |
Application Number |
Aug 13, 2007 |
EP |
07291005.2 |
Claims
1. A flavored therapeutic composition comprising a clay as an
active ingredient, wherein the clay is a dioctahedral smectite; and
the flavor is encapsulated.
2. The composition according to claim 1, wherein the dioctahedral
smectite is a montmorillonite or a beidellite or an intermediate
crystallographic structure between montmorillonite and beidellite
crystal-chemical poles.
3. The composition according to claim 1, wherein the dioctahedral
smectite is a montmorillonite or an intermediate crystallographic
structure close to the montmorillonite pole.
4. The composition according to claim 1, wherein the dioctahedral
smectite is a montmorillonite or an intermediate crystallographic
structure very close to the montmorillonite pole.
5. The composition according to claim 1, wherein the dioctahedral
smectite is a diosmectite.
6. The composition according to claim 1, wherein the flavor is a
hydrophobic liquid.
7. The composition according to claim 1, wherein the flavor has a
Hildebrand solubility parameter less than 30 MPa.sup.1/2.
8. The composition according to claim 1, wherein the flavor is in
liquid form with a log P comprised within the range -2 to 7.
9. The composition according to claim 1, wherein the flavor has a
log P comprised within the range 2 to 6.
10. The composition according to claim 1, wherein the flavor is a
natural extract, an essential oil or a mixture thereof.
11. The composition according to claim 1, wherein the composition
comprises at least one encapsulated flavor different from
vanilla.
12. The composition according to claim 1, wherein the flavor is
liquorice, exotic fruits, red fruits, extracts of citrus fruits,
vanilla, caramel, chocolate, coca-cola, green tea, caramel custard,
or mixtures thereof.
13. The composition according to claim 1, wherein the flavor is
vanilla, caramel, chocolate, extracts of citrus fruits, or mixtures
thereof.
14. The composition according to claim 1, wherein the flavor is
vanilla, caramel, chocolate, orange, lemon, grapefruit, clementine,
or mixtures thereof.
15. The composition according to claim 1, wherein the flavor is a
mixture of flavors.
16. The composition according to claim 1, wherein the flavor is a
mixture of vanilla and orange flavors.
17. The composition according to claim 1, wherein the flavor is
encapsulated in a glassy matrix of carbohydrates.
18. The composition according to claim 17, wherein the matrix
comprises maltodextrin or a mixture of maltodextrin and at least
one of sucrose, glucose, lactose, levulose, maltose, fructose,
isomalt, sorbitol, mannitol, xylitol, lactitol, maltitol or
hydrogenated starch hydrolysates.
19. The composition according to claim 17, wherein the matrix
comprises maltodextrin or a mixture of maltodextrin and at least
one of sucrose, maltose, isomalt, maltitol, or hydrogenated starch
hydrolysate.
20. The composition according to claim 17, wherein ene the matrix
comprises maltodextrin and sucrose.
21. The composition according to claim 18, wherein the maltodextrin
has a dextrose equivalent greater than 5 and less than 20.
22. The composition according to claim 1, wherein the flavor is
present in a proportion of at least 10% by weight expressed as dry
matter, with respect to the total weight of the encapsulation
matrix expressed as dry matter.
23. The composition according to claim 1, wherein the flavor is
present in a proportion comprised between 15 and 35% by weight
expressed as dry matter, with respect to the total weight of the
encapsulation matrix expressed as dry matter.
24. The composition according to claim 1, wherein the composition
comprises from 70 to 90% by weight of active ingredient.
25. The composition according to claim 1, wherein the composition
comprises from 75 to 85% by weight of active ingredient.
26. The composition according to claim 1, wherein the composition
comprises from 0.1 to 3% by weight of encapsulated flavor.
27. The composition according to claim 1, wherein the composition
comprises from 0.3 to 2.5% by weight of encapsulated flavor.
28. The composition according to claim 1, wherein the composition
comprises from 0.5 to 2% by weight of encapsulated flavor.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is the U.S. National Stage filing of
International Application No. PCT/FR2008/001185, filed Aug. 12,
2008, which claims priority to EP 07291005.2, filed Aug. 13, 2007,
the disclosures of which are hereby incorporated by reference in
their entirety.
BACKGROUND OF THE INVENTION
[0002] The present Application relates to a flavored pharmaceutical
composition containing a smectite as active ingredient.
[0003] A therapeutic composition based on smectite known as
"diosmectite" exists and is sold under the trade-mark Smecta.RTM..
But due to the particular taste of the clay which certain patients
and children in particular can sometimes find unpleasant, the
problem was therefore to find a novel composition which is flavored
and the taste of which remains predominant vis-a-vis the taste of
the clay. In order to solve this problem, the Applicant proposes a
novel flavored pharmaceutical composition based on smectite and as
defined below.
DETAILED DESCRIPTION OF THE INVENTION
[0004] The subject of the present invention is therefore a flavored
therapeutic composition containing a clay as active ingredient, and
characterized in that [0005] the clay is a dioctahedral smectite;
and [0006] the flavored is encapsulated.
[0007] A composition according to the present invention can be used
for the prevention and/or treatment of certain pathologies such as
the symptomatic treatment of pain associated with
oesogastroduodenal and colic conditions, acute and chronic
diarrhoeas, coeliac disease.
[0008] Smectites represent a particular family of clay in which
dioctaedral species such as montmorillonite and beidellite, and
trioctaedral species such as hectorite and saponite are found.
[0009] The clay used according to the invention is a dioctahedral
smectite. Preferably, the dioctahedral smectite is a
montmorillonite or a beidellite or a crystallographic structure
intermediate between the two crystal-chemical poles:
montmorillonite and beidellite. This intermediate crystallographic
structure can be close to the montmorillonite pole and even very
close to the montmorillonite pole; it can also be close to the
beidellite pole and even very close to the beidellite pole.
Preferably, a smectite according to the invention is a
montmorillonite or an intermediate structure close to the
montmorillonite pole, and very preferably very close to the
montmorillonite pole.
[0010] Also preferably, the clay used is the smectite known as
"diosmectite" and sold under the trade-mark Smecta.RTM..
[0011] The therapeutic composition according to the present
invention comprises "a flavoring ingredient or composition", called
"flavor". The term "flavor" as used in the present Application
covers the flavoring ingredients or compositions usually used in
the food industry, whether of natural or synthetic origin. It
comprises single compounds or mixtures.
[0012] Specific examples of such compounds can be found in the
literature, such as for example in Fenaroli's Handbook of Flavor
Ingredients, 1975, CRC Press; Synthetic Food Adjuncts, 1947, M. B.
Jacobs, published by Van Nostrand; or Perfume and Flavor Chemicals,
1969, S. Arctander, Montclair, N.J. (USA).
[0013] These compounds are well known to a person skilled in the
art in the field of flavoring or aromatizing consumer products,
i.e. traditionally flavored consumer products to which an odour, a
flavor or a taste has been added, or consumer products the taste of
which has been modified.
[0014] Preferably, the flavor is a hydrophobic liquid, soluble in
organic solvents but only very weakly soluble in water.
[0015] Very preferably, the flavor is characterized by a Hildebrand
solubility parameter 8 less than 30 MPa.sup.1/2. The
incompatibility with water of most of the flavors and perfumes can
in fact be expressed by means of the Hildebrand solubility
parameter which is in general less than 25 MPa.sup.1/2 while the
same parameter for water is 48 MPa.sup.1/2 and for alkanes, 15-16
MPa.sup.1/2. This parameter gives a useful polarity scale
correlated with a cohesive energy density of the molecules. For
mixing to take place spontaneously, the difference in solubility of
the molecules to be mixed must be kept to a minimum. The handbook
of solubility parameters (Handbook of Solubility Parameters, A. F.
M. Barton, CRC Press, Bocca Raton, 1991) gives a list of 8 values
for a large number of chemical products but also recommended
group-contribution methods allowing the 8 values for complex
chemical structures to be calculated.
[0016] Also preferably, the flavor is in a liquid, volatile or
labile form, with a log P comprised within the range -2 to 7, and
very preferably, from 2 to 6.
[0017] Also in a preferred fashion, a composition according to the
present invention comprises, as flavor, natural extracts, essential
oils or a mixture thereof.
[0018] As a suitable flavor, traditional flavors can be mentioned
such as liquorice, exotic fruits, red fruits, extracts of citrus
fruits such as lime, lemon, orange, grapefruit, or mandarin oils or
coffee, tea, mint, cocoa, vanilla/caramel or essential oils from
herbs and spices, or also flavors known as "modern" such as
coca-cola, green tea, caramel custard.
[0019] Preferably, a composition according to the invention
comprises at least one encapsulated flavor different from
vanilla.
[0020] The flavors are preferably chosen from the traditional
flavors such as liquorice, exotic fruits, red fruits, extracts of
citrus fruits, vanilla/caramel/chocolate but also flavors known as
"modern" such coca-cola, green tea, caramel custard.
[0021] Preferably, the flavor is chosen from
vanilla/caramel/chocolate flavors and extracts of citrus fruits and
very preferably, vanilla/caramel/chocolate and orange, lemon,
grapefruit or clementine.
[0022] Also in a preferred fashion, the flavor is a mixture of
flavors, and very preferably, a mixture of vanilla and orange
flavors.
[0023] The flavor can be mixed with solvents, adjuvants, additives
and/or other substances, for example those usually used in the
flavor and/or food industry.
[0024] The flavor according to the present invention is preferably
encapsulated in a glassy matrix (encapsulation matrix) of
carbohydrate(s).
[0025] Any sugar or sugar derivative which can be processed by
extrusion techniques can be used as constituent(s) of the
encapsulation matrix, in order to form a dry extruded solid.
Particular examples of suitable constituents can be chosen from the
following products: sucrose, glucose, lactose, levulose, fructose,
maltose, ribose, dextrose, isomalt, sorbitol, mannitol, xylitol,
lactitol, maltitol, pentatol, arabinose, pentose, xylose,
galactose, hydrogenated starch hydrolysates, maltodextrin,
Stabilite (trade name; origin: SPI Polyols, USA), agar,
carrageenan, other gums, polydextrose and the derivatives and
mixtures thereof.
[0026] Preferably, maltodextrin or mixtures of maltodextrin and at
least one product chosen from: sucrose, glucose, lactose, levulose,
maltose, fructose, isomalt, sorbitol, mannitol, xylitol, lactitol,
maltitol and hydrogenated starch hydrolysates are used. Very
preferably, the matrix is constituted by maltodextrin or a mixture
of maltodextrin and at least one product chosen from: sucrose,
maltose, isomalt, maltitol and hydrogenated starch hydrolysates.
Also very preferably, the matrix is constituted by maltodextrin and
sucrose.
[0027] Preferably, the maltodextrin has a dextrose equivalent (DE)
greater than 5 and less than 20.
[0028] An emulsifier such as lecithin, and/or a plasticizer,
typically water, can be added to the mixture if necessary.
[0029] The flavored product or the flavored composition according
to the invention, which are extruded, can be prepared by any
standard method. For example, the methods described in U.S. Pat.
Nos. 4,610,890 and 4,707,367, the content of which is incorporated
by way of reference, are suitable for supplying encapsulated
flavors as used in the present invention.
[0030] Also preferably, the flavor is present in a proportion of at
least 10% by weight expressed as dry matter, with respect to the
total weight (expressed as dry matter) of the encapsulation matrix,
and preferably in a proportion comprised between 15 and 35%.
[0031] A composition according to the invention comprises
preferably 70 to 90% by weight of active ingredient, and very
preferably from 75 to 85%, with respect to the total weight of the
composition.
[0032] Also preferably, a composition according to the invention
comprises 0.1 to 3% by weight of encapsulated flavor with respect
to the total weight of the composition, and very preferably 0.3 to
2.5%. Also very preferably, a composition according to the
invention comprises 0.5 to 2% by weight of encapsulated flavour
with respect to the total weight of the composition.
[0033] A therapeutic composition according to the present invention
can be presented in different solid forms such as for example
powders, granules, tablets or capsules. Appropriate solid supports
can be, for example, talc, sugars, lactose, dextrin, gelatin,
cellulose and its esters.
[0034] In a therapeutic composition according to the present
invention, there can also be also other additives such as colouring
agents, sweetening agents, lubricants, glidants. A composition
according to the present invention can also contain minerals.
[0035] The colouring agent(s) used according to the present
invention can be any type of colouring agents usually used in the
food and/or the pharmaceutical industries. Among the sweetening
agents, the following can be mentioned: saccharin, aspartame,
maltodextrin, monosaccharides such as fructose or glucose,
disaccharides such as saccharose. Among the lubricating agents,
talc can be mentioned for example. Among the glidant agents,
saccharose can be mentioned.
[0036] The mineral contribution can for example consist of the
addition of metal salts such as aluminium or magnesium salts such
as aluminium hydroxide, magnesium carbonate.
[0037] The administration method for a composition according to the
invention is chosen, among others, according to its pharmaceutical
form and the pathology to be treated. Preferably, the composition
as defined above is administered by the oral route.
[0038] The daily administration dose is the usual recommended dose
for this product. In the particular case of the smectite known as
"diosmectite", it can be administered at a maximum daily dose of 18
g/day.
[0039] Unless defined otherwise, all the technical and scientific
terms used here have the same meaning as that usually understood by
an ordinary specialist in the field to which this invention
belongs.
EXPERIMENTAL PART
Example 1
Preparation of an Encapsulated Orange (Oil) Flavor
[0040] A syrup is prepared from maltodextrin, sucrose, water and
flavor. The mixture is then heated to 123.degree. C. in order to
reduce the moisture content of the syrup. Then, the emulsifier is
mixed with the concentrated syrup under high shear conditions in
order to form a uniform melt. The melt is then extruded under a
pressure of 2.times.10.sup.5 Pa through an extrusion die plate with
holes of 0.8 mm diameter in a cold solvent for chilling and
breaking of the extrudates.
TABLE-US-00001 Ingredients in grams (g) % dry matter Maltodextrin
18DE 1505 44.55 Sucrose 1505 44.55 Cold-pressed oil of Valencia
orange 350 10.36 Soya lecithin.sup.1) 18 0.54 Water 400 -- Total
100.00 .sup.1)origin: Central Soya, Strong Wayne, Indiana, USA
Example 2
Preparation of an Encapsulated Vanilla Flavor
[0041] Example 1 is reproduced by using a vanilla extract (ex
Firmenich) instead of the orange flavor.
Example 3
Preparation of an Encapsulated Caramel Flavor
[0042] Example 1 is reproduced by using a caramel flavor (ex
Firmenich) instead of the orange flavor.
Example 4
Preparation of a Flavored Therapeutic Composition
[0043] The compositions below are prepared by gently mixing all the
substances together in the proportions indicated, until they are
dispersed in a homogenous fashion. In the table below, all the
quantities are expressed in mg.
TABLE-US-00002 Example Example Example Ingredients 4a 4b 4c
Diosmectite 3000 3000 3000 Encapsulated orange flavor -- -- 10
(flavor prepared according to Example 1) .sup.1 Encapsulated
vanilla flavor 50 50 50 (flavor prepared according to Example 2)
.sup.2 Encapsulated caramel .RTM. flavor 10 -- -- (flavor prepared
according to Example 3) .sup.3 Soluble saccharine + hydrated 700
710 700 glucose Water 100 100 100 .sup.1 ex Firmenich, ref. 501289
TD 0990B; .sup.2 ex Firmenich, ref. 501465 TD1591; .sup.3 ex
Firmenich, ref. 501403 TD 1094
Example 5
Stability of a Composition According to the Invention
[0044] Clay being a stable product naturally, the stability of a
composition according to the invention is measured both as regards
the organoleptic characteristics of the flavor and for its inertia
vis-a-vis the clay.
[0045] The stability of the organoleptic characteristics of the
flavor is established by testers (panel of 7 experts) on the basis
of a number of criteria (sugary, fruity, acidic, bitterness, etc.)
over a period of at least 6 months.
[0046] Moreover, it is noted that the flavor shows no deterioration
in the presence of the clay over this same period.
* * * * *