TOPICAL COMPOSITIONS CONTAINING A BETA-CYCLODEXTRIN AND AN AMINO POLYSACCHARIDE

COMPOSITIONS A APPLICATION TOPIQUE CONTENANT UNE BETA-CYCLODEXTRINE ET UN AMINOPOLYSACCHARIDE

English Abstract

A composition is disclosed for topical application for the relief of
inflammation and pain. The composition is in the form of an inert powder, or a
gel, cream or dispersion containing a clathrating agent which comprises a
.beta.-cyclodextrin and an amino polysaccharide.

French Abstract

L'invention concerne une composition pour une application topique, permettant d'atténuer la douleur ou une inflammation. La composition se présente sous la forme d'un gel, d'une crème, d'une dispersion ou d'une poudre inerte, comprenant un système clathrate contenant de la .beta.-cyclodextrine et un aminopolysaccharide.

Claims

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CLAIMS
1. A composition for topical application for the relief of
inflammation comprising an inert powder, or a gel, cream or
dispersion or the like inert carrier, together with a
cyclodextrin and an amino saccharide or polysaccharide.
2. A composition as claimed in claim 1 in which the amino
polysaccharide and cyclodextrin are incorporated with a
cross-linked acrylic polymer to form a dry sterile dressing for the
treatment of wounds or injuries.
3. A composition as claimed in either of claims 1 or 2 in
which the cyclodextrin is .beta.-cyclodextrin or dimethyl
.beta.-cyclodextrin.
4. A composition as claimed in any of claims 1 to 3 wherein
both a saccharide and a polysaccharide is present.
5. A composition as claimed in any of claims 1 to 4 made into
a cream with water and coconut oil by virtue of an
organo-phosphate ester emulsifier.
6. A composition as claimed in any of claims 1 to 4 made into
a gel with water and alcosorb polymers.
7. A composition as claimed in any of claims 1 to 4 in powder
form mixed with alcosorb polymers for mixing with water prior
to use.
8. A composition substantially as hereinbefore particularly
described with reference to the foregoing examples.

Description

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TOPICAL COMPOSITIONS CONTAINING A BETA-CYCLODEXTRIN AND AN AMINO POLYSACCHARIDE
t
~ This invention relates to a treatment material applicable to
wounds, injuries and a wide variety of diseases of the skin to
reduce pain, inflammation and to increase the rate of healing
of the affected area of the skin.
The chemistry of the inflammation processes of the skin has
revealed the role of the enzyme phospholipase in the hydrolysis
of lecithin and the release of free arachidonic acid.
Arachidonic acid is rapidly transformed to the leukotriene via
lipoxygenase, thereby producing pain and inflammation.
According to the present invention this train of events can be
halted by the topical application of clathrating agents in
particular a composition for topical application for the relief
of inflammation comprising an inert powder, or a gel, cream or
dispersion or the like inert carrier, together with a ~-
cyclodextrin and an amino saccharide or polysaccharide.
Combinations of amino saccharides or polysaccharides and
cyclodextrins according to the invention have been shown to be
beneficial in the treatment of skin disorders such as eczema
and psoriasis, and have unexpectedly been found to be more
effective than either component alone. By incorporating the
amino polysaccharide and cyclodextrin with a cross linked
acrylic polymer, in accordance with a preferred embodiment, a
dry sterile dressing for the treatment wounds or injuries may
be produced to which sterile water may be added immediately
1 prior to application.
B-cyclodextrin is a cyclic polymer containing seven D-glucose
units and has a doughnut-shaped molecular structure including
an interior cavity which receive other molecules and form
clathrate compounds therewith. While the efficacy of the
,

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invention does not depend on the correctness of the theory, it
is believed that the cyclodextrin clathrates the arachidonic
acid produced by the wound and thus effectively removes it and
so prevents or reduces the pain and inflammation associated
with it.
Preferably, the amino saccharides and polysaccharides employed
include chitin and products derived from chitin, for example by
hydrolysis, to produce n-acetyl glucosamine which can then be
de-acylated to give glucosamine or glucosamine hydrochloride.
Such compounds have analgesic or or anti-inflammatory
properties and the efficacy thereof has been unexpectedly found
to be enhanced when used with cyclodextrin an accordance with
the invention.
Further combinations of these ingredients have been employed to
demonstrate the broad range of applications in creams, gels and
dispersions in the treatment or prevention of a wide range of
diseases or injuries.
The following examples will serve or illustrate the novelty and
benefits of this invention.
ExamPle
50.0g of glucosamine hydrochloride
50.0g of dimethyl ~. cyclodextrin
made up to l litre with sterile water.
The solution was then added to a mixture of l kg. coconut oil
and 40g of an organo phosphate ester emulsifier maintained at
50~C. After agitation and cooling this produced a lotion t
suitable for topical application to the skin to combat
inflammation.
_

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ExamPle II
4.0g of Alcosorb polymers
lO.Og glucosamine hydrochloride and
15.0g ~. cyclodextrin iodine clathrate
The mixture was mixed thoroughly and placed within a sachet
made from bonded synthetic polymers measuring 10 x 15 cms.
The sealed sachet was maintained in a dry, sterile condition
prior to use.
Exam~le III
40g Alcosorb polymers
lOOg glucosamine hydrochloride
150g dimethyl ~. cyclodextrin
The mixture was mixed thoroughly prior to the addition of
1800ml of sterile water, added with constant agitation for a
period of five (5) minutes.
The resultant gel was then preserved in sterile containers.
Example IV
lOOg chitin Poly-(1-4) ~-D-N-acetylglucosamine
50g ~. cyclodextrin
50g Alcosorb
The ingredients were admixed and ground to a particle size of
50 microns. The resultant powder was suitable for inclusion
with synthetic polymers of incorporation with fabricated
polymers.
J
The preparations illustrated but not limited by Examples I to
V were then subjected to a series of tests as demonstrated by
the following examples.

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Exam~le VI
The lotion prepared as in Example I was applied to the affected
tissue on patients suffering from psoriasis or eczema. All
reported relief from pruritis within lO minutes after
application and regeneration of dermal tissue was observed on
the fourth day.
~xamPle VI
A sachet, produced as in Example II, was immersed in 0.5 litres
of sterile water for five (S~ minutes and applied to a second
degree burn on a patients forearm. The dressing was bandaged
in place for twenty four hours. Relief from pain occurred
within minutes and when the dressing was removed the healing
process had commenced.
ExamPle VII
Gel, produced as in Example II, was applied to insect bites,
minor scalds and burns in a variety of patients.
The response obtained in all cases was the rapid relief from
pain and promotion of healing.
Example VIII
The powder produced as in Example IV was incorporated in the
layer of fabric used to produce sanitary wear. In the case of
infants the incidence of infection caused by the micro organism
Candida albicans, known as nappy rash, was significantly
reduced. Other applications for the reduction of infection
by this organism are related to age and sex.
In each of the Examples I to IV the dimethyl ~. cyclodextrin
and ~. cyclodextrin may be exchanged without detracting from
the principle of the invention.

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Similarly the amino polysaccharides as a group display similar
characteristics from a therapeutic standpoint although the
chemical and or physical properties may differ.
-
ExamPle IX
A colloidal suspension was prepared from a combination ofchitin, chitosan and glucosamine having a particle size of less
than 5 microns in an aqueous solution of ~-cyclodextrin in the
following manner:
40g chitin (poly(1-4)~-N-acetyl-D-glucosamine)
40g chitosan (poly(1-4)-3-glucosamine)
20g glucosamine
The above ingredients were introduced with agitation into an
aqueous solution containing ~-cyclodextrin and the whole made
up to a total volume of l litre.
A non-woven polyester fabric was wetted with this suspension by
short term immersion ~1-2 seconds, nip rollers) then dried
prior to forming into lOcm squares for use in surgical
dressings as the contact surface with the perturbed tissue.
When applied to lacerated tissue, relief from pain occured
within minutes and the healing process was accelerated.
Analysis of the treated fabric showed that the level of the
combined ingredients was 1.7% w/w. It is believed that a
combination of saccharides and polysaccharides as in this
Example is particularly effective.