Note: Descriptions are shown in the official language in which they were submitted.
. WO90/09779 2028136 PCT/US9~t~1041
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¦ METHOD AND COMPOSITION FOR TREATMENT !'
OF PERIODONTAL DISEASE. _ .
BACKGROUND OF THE_INVENTION
Field of the Invention
The present invention relates to a method and composition
for treatment of periodontal disease and, more
particularly, to a composition suitahle for topical
application to prevent and treat~periodontitls.
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Descri~tion of the Prior Art ~ ~
Periodontal disease is the major cause of tooth loss in
adults~ The periodontium is subj~ect to inflammation for
many reasons, primary among them ~ei~g the accumulation of
plaque deposits~under and above the gumline These~ ~
calcareous deposits of~organic and mineral matter, which ~ ~`
! : ~ consist~of micr;obial~colonies growing~in carbohydrate~
residues (from food), attach themselves to tooth surfaces~
and can, over time,~ alci~y into tartar. This hard
~;mineraliz~ed su~stance~adheres tenaciously~to the teeth~
~and~, when~under~the gumline, causes inflammation of the
periodont~ium. ~Other causes of periodontitls~ can include ~ ~-
malocclusion, food impaction and mouth breathlng.
Periodontitis~can cause~the gumline to retract due to~
supporting bone~;loss and the~;gums~to~bleed, and
`even~ually, if not treated, can result in tooth loss~.
Until~now,~ the~only~known treatment for~periodon~it~is,
outside of taklng~preventive~measures~to keep it from ;;
devel~oping in~the~fi~rst place, was~surgery. The accepted
urglcal:procedure invol-eL removIng the Inrlamed gum ~ ~-
WO90/09779 ~ 2~2~13~ PCTfUS90/01041 `~
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` tissue, which is expensive and requires a long and painful
recovery.
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There have been Yarious attempts at treating periodontal ~--
disease without such surgical intervention~ The ~est such
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attempt to date resides in an oral rinse sold by Procter & ~ -
Gamble under the name Peridex~. The chemistry of this
product is described in the 1988 Physicans' Desk Reference
at pages 1648-49. Unfortunately, Peridex~ rinse has not
proved as efficacious ~gainst periodontal disease as might
be desired and exhibits unwanted side effects, such as
staining of tooth surfaces. -
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The following patents~also disclose oral treatment agents,
but none is believed to represent a substitute for
surgical intervention as a trea~ment for periodontal
~; disease:
~Re.31,397 ~ 4,213,961
2,684,924; ~ 4,332,7gl
:: ~ ;3 j 887 ~ 712 4 r 339, 430
3,925,543 4,454,110 ~ !~
3,937,807 4,486,404 - ~
3,g57,967 4,569,837 ~ ;
4,051~234 4,601,900
4,067,962 4,661,342
4,198,392
Of interest;with regard to the present invention are U~.S.
Patent 4,486,404 which, in Example 5, discloses a ~`~
tdothpaste;containing chlorhexid;ine gluconate `and
allantoin, U.S~. Patents 3,937,807 and 4,05~,234, which
disc~lose mouthwashes~wlth~gluc~onates and anti~stain
agents,~and U.S. Pa~ent 4,569,837, which discloses the use
of~chlorhexidine gluconate and aspirin to treat
perlodontal di~sease.~
W090~09779 PCT/U~90/0l0~1
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SUMMA*Y OF THE INVENTION
It is an object of the present invention to provide a
' composition and method for treating Periodontitis I
; without costly and painful surgical intervention.
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In accordance with one aspect of the invention, a
composition suitable for treating periodontitis comprises
an a~ueous solution of an antimicrobial agent with
bacteriacidal activity, an a~ent with therapeutic action
against skin ulcers, an analgesic, a:stain remover and, if
desired, suitable wetting agents, emulsifiers,
dispersants, buffers stabilizers, preservatives, flavoring
and coloring. -
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In accordance with another aspect of the invention, thecomposition i5 used in a treatment method which comprises
the steps of topically applying the composition to
inflamed periodonkium.
DESCRIPTION OF PREFERRED EMBODIMENTS
In a preferred embodimient of the invention the various
components of the composition of the present invention are
present in an aqueous carrier of sterile distilled water,
gl.ycerine and ethanol. The glycerine provides thie
composition with the desired feel an~ texture and the
ethanol acts as an antiseptic.
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To this water glycerine-ethanol:ca~rrier is added
(1) chlorhexidîne gluconate (0.12% solution), C34H54Cl2N10Ol4
! (Merck Index 2057j, as an antimicrobial agent with
bacteriacldal action, (2):al1antoin,:or (2,5-dioxo-4- ~-
imidazolidinyllurea (Merck Index 242) as an agent that
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~ exhibits therapeutic action against skin ulcers, (3)
.~ sodium salicylate, or 2-hydroxybenzoic acid monosodium
. salt (Merck Index 8515), as an analgesic, and (4) sodium
bicarbonate (Merck Index 8414) as a stain remover, along ~
with wetting agents, preservatives, emulsifiers,
~ dispersants, buffexs stabilizers, ~lavoring and coloring, .-
t as desired (All references herein to the Merck Index
refer to the 1~83 edition.)
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In particularly preferred embodiment, the above
ingredients are provided in the following proportions: -~
TABLE 1 ~;
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Sterile Water 70.77%
Glycerine (MI 4347) - 11.15% -
Ethanol (MI 2~2) 7.50% ~ .
Polysorbate 80 :(as an emulsifier ~.
and dispersant; MI 7455) 4.20%
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Chlorhexidine gluconate (0.12% -
sol.) (MI 2057) 3.50% -~
Sodium bicarbonate (as a stain ;
remover; MI 8414) 0.50% l~.
Sodium lauryl sulfate (as a wetting
agent; MI 8474~ 0.50% ~;
Vanilla (as flavoring; MI 9732) 0.60%
Saccharine~(as flavoring; MI~8170) 0.20~ ' ...
Sodium sali~ylate ~MI 8515) 0.15% .,
~i, Allantoin (MI 242) 0.63~% -
Sodium ~enzoate (as a preservative; '-
MI 8413) 0O10% `~:
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Xanthan gum (as a stabilizer and ~:
. emulsifier; MI 9868) 0.10% `
Sodium borate (as a buffer; MI 8421) 0.085%
F.D.& C. Blue (as coloring) 0.005%
F.D.& C. Red 40 (as coloring) 0.002%
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[Notes to Table l - (l) All proportions of the above
ingredients are v/v; (2) "MI" refers to the Merck
Index]
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The above composition is prepared by first measuring an
appropriate quantity of sterile distilled water; for :
example, l000cc of the composition~ i5 to be prepared,
707.7cc of water are used. ~The remaining ingredients are
added in the order listed in Table l, with each ingredient
being thoroughly mixed by gently stirring the composition
before the next ingredient is ad~ed. ~
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A clinical test involving 30 people was performed using a
composition similar to that set out above, except for
using 72.77% sfterile water, 8.00% ethanol, 1.50%
chlorhexidine gluconate ff0.l2% solution) and 0.138%
allantoin. The subjects were chosen because~ all exhib~ited
periodontal pockets up to 8mm or 9mm deep. Prior to
beginning the treatment regimen, all 30 subjects agreed
not to brush or floss their teeth for one week. Then, 15
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cff the subjects rinsed their mouths three times a day with
1.0 cc of the abo~e composition 30 seconds before brushing
and 15 rin~sed their mouths three ~imes a day with an equal
amount of a colored sugar-water ~lacebo 30 seconds~before
brushing. The sub~jects did not know whether they were
uslng the inv~entive composition~or the placebo.
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Once a week the teeth of each~subject were chec~ed for the
- presence of plaque using a commercfially available plaque-
'~ri'' ~ ~ disclosing solutio:n, Superdent'~ disclosing solution
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concentrate, made by Rugby Laboratories, Inc., of
~' Rockville Centre, Long Island, NY 11570. All subjects
using the inventive composition showed little or no plaque
accumulation, while there was such plaque accumulation on
the teeth of the subjects using the placebo.
The test procedures were continued for 12 weeks, and the
subjects' conditions were measured in accordance with the
Simplified Oral Hygiene Index (OHI-S) described in Orbanls
Periodontics (3rd Ed. 1968~, The C.V. Mosby Co., St.
Louis, MO, at page 134. It was found that the average
OHI-S for the subjects on the placebo went from 8mm to 9mm
periodontal pocket depth to 6mm to 8mm pocket depth during
the 12 week test, while that for the subjects using the
inventive composition improved from 8mm to 9mm periodontal
pocket depth to 2mm or 3mm pocket depth, which is
considered within normal range.~
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It is expected that~repeated use of the invPntive solution
will reduce inflammation, stop bleeding and keratenize ;-
damaged periodontal tissue. ,s
Qf course, variations of the above preferred embodiment
are possible within the scope of the present invention,
such as ~arying the proportions of the chlorhexidine
i gluconate, allantoin and sodium salicylate within ranges
! i that prov`ide efficacious results. It is intended by the
claims appended below to include all such variations ~
i within the present invention.
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