CA2278237A1 - Mouthwash composition - Google Patents
Mouthwash composition Download PDFInfo
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- CA2278237A1 CA2278237A1 CA002278237A CA2278237A CA2278237A1 CA 2278237 A1 CA2278237 A1 CA 2278237A1 CA 002278237 A CA002278237 A CA 002278237A CA 2278237 A CA2278237 A CA 2278237A CA 2278237 A1 CA2278237 A1 CA 2278237A1
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- Prior art keywords
- phase
- chlorhexidine
- composition according
- pvp
- composition
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- 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
- A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
- A61K8/817—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen; Compositions or derivatives of such polymers, e.g. vinylimidazol, vinylcaprolactame, allylamines (Polyquaternium 6)
- A61K8/8176—Homopolymers of N-vinyl-pyrrolidones. Compositions of derivatives of such polymers
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/43—Guanidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/52—Stabilizers
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A two phase mouthwash composition is described comprising chlorhexidine and polyvinyl pyrrolidone.
Description
MGUTHWASH COMPOSITION
The present invention relates to mouthwash compositions, in particular compositions comprising the cationic antibacterial agent, chlorhexidine.
WO 93/1668:1 discloses oral hygiene compositions including mouthwashes comprising cationic antibacterial agents such as chlorhexidine and as an anti-staining agent polyvinyl pyrrolidone (PVP).
It has now been discovered that a two phase chiorhexidine/PVP mouthwash having a particular pH range exhibits enhanced chlorhexidine efficacy.
Accordingly i~n a first aspect the present invention provides a mouthwash composition comprising two phases; a first phase comprising chlorhexidine or an orally acceptable acid addition salt thereof and an orally acceptable carrier or excipient and a second phase comprising PVP and an orally acceptable carrier or excipient; the two phases being kept separate until use, whereupon on mixing they provide a single phase having a pH between 6 and 10.
It is advantageous to separate the chlorhexidine and PVP phases until use since it has been discovered that the efficacy of chlorhexidine can otherwise be reduced upon long term storage with PVP.
The pH of the chlorhexidine phase and the PVP phase are such that on mixing they result in a pH from 6.0 to 10.0) preferably 6.0 to 9.0, more preferably 6.0 to 7.0, eg 6.2.
Conveniently equal amounts) by weight) of the chlorhexidine and PVP
phases are mixed prior to use.
Suitably the initial pH of the chlorhexidine phase is no greater than 6 which has the advantage of increasing the long term storage stability of chlorhexidine.
Preferably the initial pH of the chlorhexidine phase is from 3.0 to 6.0, more preferably 5.0 to 5.9' for example 5.5 to 5.9.
Suitably the pH of the PVP phase is from 6.0 to 10.0, preferably from 6.0 to 9.0, more preferably from 6.0 to 8Ø
Preferably the PVP phase comprises an orally acceptable buffer or pH
modifier such that on mixing with the chlorhexidine phase the desired pH is obtained.
Examples of orally acceptable buffers and pH modifiers include a base such as sodium hydroxide, or an acid such as acetic, gluconic, tartaric, citric, lactic, or phosphoric acid or a soluble salt thereof. These can be used individually or as mixtures. A preferred buffer is sodium acetate.
The buffer or pH modifier should be present in sufficient quantity to provide the desired buffering effect, suitably from 0.01 to 10 % , preferably from 0.1 to 2 by weight of the composition.
The compositions of the present invention can be packaged into a container such as a bottle or tube having two chambers for separating each phase, the container having a dispensing nozzle allowing controlled dispensing and suitably concomitant mixing of said prior phases to use. Alternatively such compositions can be packaged into a sachet having two chambers separated by a frangible seal which can be ruptured prior to use allowing mixing of the two phases within the sachet.
Alternatively the two phases may also be packaged in separate containers which can dispense the required amount of each phase prior to mixing and use.
Polyvinyl pyrrolidone for use in the present invention suitably has an average molecular weight of at least 5,000 eg in the range 5,000 to 100,00(?, preferably in the range 5,000 to 50,000. Polyvinyl pyrrolidones which have average molecular weights of 10,000, 30,000 and 40,000 are available from Sigma Chemical Co., GAF Corporation and Sigma Chemical Co. respectively. Polyvinyl pyrrolidone is suitably present in at least 0.5 % , preferably between 0.5 and 30 % , more preferably between 0.5 and 25 % , and advantageously between 1 and 15 %
by weight of the composition.
Suitably, chlorhexidine or an orally acceptable acid addition salt thereof is present in from 0.005 to 10 % preferably 0.01 to 5 % , more preferably 0.01 to 2 % , by weight of the composition.
Suitable salt; of chlorhexidine include those which have a solubility at 20 ° C
of at least 0.005 % vv/v and include the digluconate, diformate) diacetate, dipropionate, dihydroiodide, dihydrochloride, dilactate, dinitrate, sulphate, and tartrate. Of these, tt;ie digluconate, diacetate and dihydrochloride are favoured.
The compositions of the present invention may also usefully contain an ionic fluorine-containing compound. Suitable ionic fluorine-containing compounds include, for instance;, fluoride salts such as amine fluorides and alkali metal fluoride salts, for example sodium fluoride, and monofluorophosphate salts such as alkali metal monofluorophosphate salts, for example sodium monofluorophosphate.
Suitably the ionic fluorine-cc>ntaining compound is incorporated into the composition to provide between 50 and 2000ppm, preferably between 100 and 500ppm of fluoride ions.
The compositions of the present invention will suitably comprise as components of the carrier a surfactant and optionally a humectant, preferably in an aqueous or an aqueous/ethanol solution.
It will be appreciated by those skilled in the art that in order to ensure that the antibacterial efficacy of chlorhexidine is not substantially diminished, compatible components will be selected for inclusion in the orally acceptable carrier or excipient. Accordingly, where necessary anionic species should be preferably avoided as such species may cause inactivation of the chlorhexidine by the formation of an inso~iuble precipitate therewith. Thus, anionic surfactants and anionic humectants should preferably be rejected in favour of non-anionic counterparts such as nonionic, cationic or amphoteric surfactants and nonionic humectants.
Suitable notvionic surfactants include, for example, polyethoxylated sorbitol esters, in particular polyethoxylated sorbitol monoesters, for instance, PEG(40) sorbitan di-isostearate, and the products marketed under the trade name ' Tween' by ICI; polycondensates of ethylene oxide and propylene oxide (poloxamers), for instance the products marketed under the trade name 'Platonic' by BASF-Wyandotte; c:ondensates of propylene glycol; polyethoxylated hydrogenated castor oil, for instance, cremophors; and sorbitan fatty esters.
The present invention relates to mouthwash compositions, in particular compositions comprising the cationic antibacterial agent, chlorhexidine.
WO 93/1668:1 discloses oral hygiene compositions including mouthwashes comprising cationic antibacterial agents such as chlorhexidine and as an anti-staining agent polyvinyl pyrrolidone (PVP).
It has now been discovered that a two phase chiorhexidine/PVP mouthwash having a particular pH range exhibits enhanced chlorhexidine efficacy.
Accordingly i~n a first aspect the present invention provides a mouthwash composition comprising two phases; a first phase comprising chlorhexidine or an orally acceptable acid addition salt thereof and an orally acceptable carrier or excipient and a second phase comprising PVP and an orally acceptable carrier or excipient; the two phases being kept separate until use, whereupon on mixing they provide a single phase having a pH between 6 and 10.
It is advantageous to separate the chlorhexidine and PVP phases until use since it has been discovered that the efficacy of chlorhexidine can otherwise be reduced upon long term storage with PVP.
The pH of the chlorhexidine phase and the PVP phase are such that on mixing they result in a pH from 6.0 to 10.0) preferably 6.0 to 9.0, more preferably 6.0 to 7.0, eg 6.2.
Conveniently equal amounts) by weight) of the chlorhexidine and PVP
phases are mixed prior to use.
Suitably the initial pH of the chlorhexidine phase is no greater than 6 which has the advantage of increasing the long term storage stability of chlorhexidine.
Preferably the initial pH of the chlorhexidine phase is from 3.0 to 6.0, more preferably 5.0 to 5.9' for example 5.5 to 5.9.
Suitably the pH of the PVP phase is from 6.0 to 10.0, preferably from 6.0 to 9.0, more preferably from 6.0 to 8Ø
Preferably the PVP phase comprises an orally acceptable buffer or pH
modifier such that on mixing with the chlorhexidine phase the desired pH is obtained.
Examples of orally acceptable buffers and pH modifiers include a base such as sodium hydroxide, or an acid such as acetic, gluconic, tartaric, citric, lactic, or phosphoric acid or a soluble salt thereof. These can be used individually or as mixtures. A preferred buffer is sodium acetate.
The buffer or pH modifier should be present in sufficient quantity to provide the desired buffering effect, suitably from 0.01 to 10 % , preferably from 0.1 to 2 by weight of the composition.
The compositions of the present invention can be packaged into a container such as a bottle or tube having two chambers for separating each phase, the container having a dispensing nozzle allowing controlled dispensing and suitably concomitant mixing of said prior phases to use. Alternatively such compositions can be packaged into a sachet having two chambers separated by a frangible seal which can be ruptured prior to use allowing mixing of the two phases within the sachet.
Alternatively the two phases may also be packaged in separate containers which can dispense the required amount of each phase prior to mixing and use.
Polyvinyl pyrrolidone for use in the present invention suitably has an average molecular weight of at least 5,000 eg in the range 5,000 to 100,00(?, preferably in the range 5,000 to 50,000. Polyvinyl pyrrolidones which have average molecular weights of 10,000, 30,000 and 40,000 are available from Sigma Chemical Co., GAF Corporation and Sigma Chemical Co. respectively. Polyvinyl pyrrolidone is suitably present in at least 0.5 % , preferably between 0.5 and 30 % , more preferably between 0.5 and 25 % , and advantageously between 1 and 15 %
by weight of the composition.
Suitably, chlorhexidine or an orally acceptable acid addition salt thereof is present in from 0.005 to 10 % preferably 0.01 to 5 % , more preferably 0.01 to 2 % , by weight of the composition.
Suitable salt; of chlorhexidine include those which have a solubility at 20 ° C
of at least 0.005 % vv/v and include the digluconate, diformate) diacetate, dipropionate, dihydroiodide, dihydrochloride, dilactate, dinitrate, sulphate, and tartrate. Of these, tt;ie digluconate, diacetate and dihydrochloride are favoured.
The compositions of the present invention may also usefully contain an ionic fluorine-containing compound. Suitable ionic fluorine-containing compounds include, for instance;, fluoride salts such as amine fluorides and alkali metal fluoride salts, for example sodium fluoride, and monofluorophosphate salts such as alkali metal monofluorophosphate salts, for example sodium monofluorophosphate.
Suitably the ionic fluorine-cc>ntaining compound is incorporated into the composition to provide between 50 and 2000ppm, preferably between 100 and 500ppm of fluoride ions.
The compositions of the present invention will suitably comprise as components of the carrier a surfactant and optionally a humectant, preferably in an aqueous or an aqueous/ethanol solution.
It will be appreciated by those skilled in the art that in order to ensure that the antibacterial efficacy of chlorhexidine is not substantially diminished, compatible components will be selected for inclusion in the orally acceptable carrier or excipient. Accordingly, where necessary anionic species should be preferably avoided as such species may cause inactivation of the chlorhexidine by the formation of an inso~iuble precipitate therewith. Thus, anionic surfactants and anionic humectants should preferably be rejected in favour of non-anionic counterparts such as nonionic, cationic or amphoteric surfactants and nonionic humectants.
Suitable notvionic surfactants include, for example, polyethoxylated sorbitol esters, in particular polyethoxylated sorbitol monoesters, for instance, PEG(40) sorbitan di-isostearate, and the products marketed under the trade name ' Tween' by ICI; polycondensates of ethylene oxide and propylene oxide (poloxamers), for instance the products marketed under the trade name 'Platonic' by BASF-Wyandotte; c:ondensates of propylene glycol; polyethoxylated hydrogenated castor oil, for instance, cremophors; and sorbitan fatty esters.
Suitable amphoteric surfactants include, for example, long chain imidazoline derivatives such as the product marketed under the trade name 'Miranol C2M' by Miranol; long chain alkyl betaines, such as the produce marketed under the tradename 'Empigen BB' by Albright + Wilson, and long chain alkyl amidoalkyl betaines, such as cocamidopropylbetaine, and mixtures thereof.
Suitable cationic surfactants include the D,L-2-pyrrolidone-S-carboxylic acid salt of ethyl-N-cocoyl-L-arginate, marketed under the trade name CAE by Ajinomoto Co. Inc.
Preferred surfactants include the nonionic poloxamers and polyethoxylated hydrogenated castor oils.
It has been discovered that the compatibility of such surfactants with chlorhexidine is further enhanced if the pH of the combined phase is between 6 to 10, preferably between 6 to 8.
Advantageously, the surfactant is present in the range 0.005 to 5 % , preferably 0.005 to 1 % , more preferably 0.01 to 0.5 % by weight of the composition.
Suitable humectants for use in compositions of the invention include for instance glycerin, sorbitol, propylene glycol or polyethylene glycol, or mixtures thereof. The humectant may be present in the range from 5 to 70 % , preferably 5 to 30 % , more preferably 5 to 20 % by weight of the composition.
Other materials may be added to the compositions if required, for instance sweetening agents, flavouring agents, colouring agents ) preservatives and emulsifiers.
Suitably the PVP phase comprises a sweetening agent such as sodium saccharin which is advantageously kept separate from the chlorhexidine phase thereby preventing unwanted precipitation of a chlorhexidinelsaccharin complex on long term storage.
The compositions according to the present invention may be prepared by mixing the ingredients thereof in the required proportions and in any order that is convenient and thereafter and if necessary adjusting the pH to the required value.
Suitable cationic surfactants include the D,L-2-pyrrolidone-S-carboxylic acid salt of ethyl-N-cocoyl-L-arginate, marketed under the trade name CAE by Ajinomoto Co. Inc.
Preferred surfactants include the nonionic poloxamers and polyethoxylated hydrogenated castor oils.
It has been discovered that the compatibility of such surfactants with chlorhexidine is further enhanced if the pH of the combined phase is between 6 to 10, preferably between 6 to 8.
Advantageously, the surfactant is present in the range 0.005 to 5 % , preferably 0.005 to 1 % , more preferably 0.01 to 0.5 % by weight of the composition.
Suitable humectants for use in compositions of the invention include for instance glycerin, sorbitol, propylene glycol or polyethylene glycol, or mixtures thereof. The humectant may be present in the range from 5 to 70 % , preferably 5 to 30 % , more preferably 5 to 20 % by weight of the composition.
Other materials may be added to the compositions if required, for instance sweetening agents, flavouring agents, colouring agents ) preservatives and emulsifiers.
Suitably the PVP phase comprises a sweetening agent such as sodium saccharin which is advantageously kept separate from the chlorhexidine phase thereby preventing unwanted precipitation of a chlorhexidinelsaccharin complex on long term storage.
The compositions according to the present invention may be prepared by mixing the ingredients thereof in the required proportions and in any order that is convenient and thereafter and if necessary adjusting the pH to the required value.
The compositions according to the present invention are of use in reducing or eliminating the st~iin normally associated with the use of chlorhexidine.
Accordingly, in a further aspect) the present invention provides a mouthwash composition as hereinbefore defined for use in therapy, in particular anti-plaque, anti-caries, anti-calculus and/or periodontal (including anti-gingivitis) therapy.
Accordingly, in a further aspect) the present invention provides a mouthwash composition as hereinbefore defined for use in therapy, in particular anti-plaque, anti-caries, anti-calculus and/or periodontal (including anti-gingivitis) therapy.
The invention will now be illustrated by reference to the following examples.
Example 1 Chlorhexidine Mouthwash Ingredients % w/w Chlorhexidine Phase PVP Phase % w/w % w/w pVp - 15.000 Sodium saccharin - 0.104 Sodium acetate - 1.400 Chlorhexidine Gluconate0.400 -Glycerine 10.000 -Dye Solution 0.100 0.100 Ethanol 5.000 8.000 Cremophor RH60* 0.200 0.250 Flavour oil 0.120 0.120 Deionised water 84.180 75.026 Totals 100.00 100.00 On mixing the pH Initial pH = 5 Initial pH = 6.30 is 6.20 .90 *Cremophor RH60 is a polyethoxylated hydrogenated castor oil containing on average 60 ethoxy units in the polyethoxylated chain.
Example 2 The Effect of pH on Chlorhexidine binding to saliva coated Hydroxyapatite discs from mouthwashes It is well known in the art that the binding of chlorhexidine to hydroxyapatite is an effective indicator of activity in the oral cavity as chlorhexidine's effectiveness is due to its ability to bind to oral surfaces.
The following test method can be used to determine the level of binding of chlorhexidine to hydroxyapatite in vitro:-a)Hydroxyapatite discs of known surface area are soaked overnight in sterile, filtered pooled human saliva at 37 C.
b)The discs are then rinsed for l5secounds in 25m1 of deionised water.
Example 1 Chlorhexidine Mouthwash Ingredients % w/w Chlorhexidine Phase PVP Phase % w/w % w/w pVp - 15.000 Sodium saccharin - 0.104 Sodium acetate - 1.400 Chlorhexidine Gluconate0.400 -Glycerine 10.000 -Dye Solution 0.100 0.100 Ethanol 5.000 8.000 Cremophor RH60* 0.200 0.250 Flavour oil 0.120 0.120 Deionised water 84.180 75.026 Totals 100.00 100.00 On mixing the pH Initial pH = 5 Initial pH = 6.30 is 6.20 .90 *Cremophor RH60 is a polyethoxylated hydrogenated castor oil containing on average 60 ethoxy units in the polyethoxylated chain.
Example 2 The Effect of pH on Chlorhexidine binding to saliva coated Hydroxyapatite discs from mouthwashes It is well known in the art that the binding of chlorhexidine to hydroxyapatite is an effective indicator of activity in the oral cavity as chlorhexidine's effectiveness is due to its ability to bind to oral surfaces.
The following test method can be used to determine the level of binding of chlorhexidine to hydroxyapatite in vitro:-a)Hydroxyapatite discs of known surface area are soaked overnight in sterile, filtered pooled human saliva at 37 C.
b)The discs are then rinsed for l5secounds in 25m1 of deionised water.
c)Each disc is then treated for 60 seconds by submerging it in 5 ml of the test solution followed by 3 washes for 60 seconds duration in 25m1 aliquots of deionised water.
d)Bound chlorhexidine is then extracted from the disc and analysed by HPIrC.
To assess the E;ffect of pH on the binding of Chlorhexidine the control solutions and mouthwashes detailed in Tables 1 and 2 were prepared. The products were then assessed for Chlorhexidine binding using the method outlined. The results obtained are shown in Table 3 ,.
- S~~.~
o,~w/w Monthrinse:- 1 2 3 4 Chlorheaddine Gluconat~e0.00 0.03 0.06 0.09 0.1 M Sodium Acetate to to to to buffer 100.00 100.00 100.00 100.00 H 7.0 7.0 7.0 ?.0 Test mouthwashes kw/w Mouthrinse:- 5 6 7 8 9 10 Chlorhe~dine 0.06 0.06 0.06 0.06 0.06 0.06 Gluconate _ Cremaphor 0.225 0.225 0.225 0.225 0.225 0.225 lZ$60 Flavour oil 0.:12 _0.12 0.12 0.12 0.12 0.12 Ethano196 6.:50 6.50 6.50 6.50 6.50 6.50 Blue d a solution0. a 0.10 0.10 0.10 0.10 0.10 GI cerin 5.110 5.00 5.00 5.00 5.00 5.00 PVP 5.110 5.00 5.00 5.00 5.00 5.00 ~
Sodium Acetate0.'70 0.70 0.70 0.70 0.70 0.70 Sodium Fluoride0.05 0.05 0.05 0.05 0.05 0.05 Sodium 0.0'52 '0.052 0.052 0.052 0.052 0.052 Saccharin _ Acetic Acid 0.625 - - - - -solution 50bw/w NaOH solution - - 0.073 0.083 0.128 0.1625 10.2 Xc w/w Deionised waterto to to to ( to ~ to 100.00 100.00 100.00 100.00 100.00 100.00 H 5.6 6.2 7.5 8.2 8.9 9.5 Product pH Number of Mean level of binding re licates /cm 1 (standard) 7.0 10 0.32 2 (standard) 7.0 10 4.67 3 (standard) 7.0 8 8.18 4 (standard) 7.0 10 9.37 (mouthwash)5.6 10 4.76 6 (mouthwash)6.2 8 6.51 7 (mouthwash)7.5 10 5.66 8 (mouthwash)8.2 10 6.23 9 (mouthwash)8.9 9 6.83 (mouthwash)9.5 10 6.25 The results show that binding significantly increases from pH 5.6 5 (mouthwash 5) to pH 6.2 (mouthwash 6). As the pH increases from 6.2 to 9.5 (mouthwashes 6-10) no further significant differences between the products are observed.
This experiment demonstrates that enhanced binding can be achieved if a mouthwash is delivered with a pH of greater than 6.
_g_
d)Bound chlorhexidine is then extracted from the disc and analysed by HPIrC.
To assess the E;ffect of pH on the binding of Chlorhexidine the control solutions and mouthwashes detailed in Tables 1 and 2 were prepared. The products were then assessed for Chlorhexidine binding using the method outlined. The results obtained are shown in Table 3 ,.
- S~~.~
o,~w/w Monthrinse:- 1 2 3 4 Chlorheaddine Gluconat~e0.00 0.03 0.06 0.09 0.1 M Sodium Acetate to to to to buffer 100.00 100.00 100.00 100.00 H 7.0 7.0 7.0 ?.0 Test mouthwashes kw/w Mouthrinse:- 5 6 7 8 9 10 Chlorhe~dine 0.06 0.06 0.06 0.06 0.06 0.06 Gluconate _ Cremaphor 0.225 0.225 0.225 0.225 0.225 0.225 lZ$60 Flavour oil 0.:12 _0.12 0.12 0.12 0.12 0.12 Ethano196 6.:50 6.50 6.50 6.50 6.50 6.50 Blue d a solution0. a 0.10 0.10 0.10 0.10 0.10 GI cerin 5.110 5.00 5.00 5.00 5.00 5.00 PVP 5.110 5.00 5.00 5.00 5.00 5.00 ~
Sodium Acetate0.'70 0.70 0.70 0.70 0.70 0.70 Sodium Fluoride0.05 0.05 0.05 0.05 0.05 0.05 Sodium 0.0'52 '0.052 0.052 0.052 0.052 0.052 Saccharin _ Acetic Acid 0.625 - - - - -solution 50bw/w NaOH solution - - 0.073 0.083 0.128 0.1625 10.2 Xc w/w Deionised waterto to to to ( to ~ to 100.00 100.00 100.00 100.00 100.00 100.00 H 5.6 6.2 7.5 8.2 8.9 9.5 Product pH Number of Mean level of binding re licates /cm 1 (standard) 7.0 10 0.32 2 (standard) 7.0 10 4.67 3 (standard) 7.0 8 8.18 4 (standard) 7.0 10 9.37 (mouthwash)5.6 10 4.76 6 (mouthwash)6.2 8 6.51 7 (mouthwash)7.5 10 5.66 8 (mouthwash)8.2 10 6.23 9 (mouthwash)8.9 9 6.83 (mouthwash)9.5 10 6.25 The results show that binding significantly increases from pH 5.6 5 (mouthwash 5) to pH 6.2 (mouthwash 6). As the pH increases from 6.2 to 9.5 (mouthwashes 6-10) no further significant differences between the products are observed.
This experiment demonstrates that enhanced binding can be achieved if a mouthwash is delivered with a pH of greater than 6.
_g_
Claims (10)
1. A mouthwash composition comprising two phases; a first phase comprising chlorhexidine or an orally acceptable acid addition salt thereof and an orally acceptable carrier or excipient and a second phase comprising PVP and an orally acceptable carrier or excipient; the two phases being kept separate until use whereupon on mixing they provide a single phase having a pH between 6 and 10.
2. A composition according to claim 1 wherein the pH of the chlorhexidine phase and the PVP phase are such that on mixing they result in a pH from 6.0 to 8Ø
3. A composition according to claims 1 or 2 wherein the pH of the chlorhexidine phase is no greater than 6.
4. A composition according to any one of claims 1 or 3 wherein pH of the PVP
phase is from 6.0 to 10.0,
phase is from 6.0 to 10.0,
5. A composition according to claim 4 wherein the PVP phase comprises an orally acceptable buffer or pH modifier such that on mixing with the chlorhexidine phase the desired pH is obtained.
6. A composition according to any one of claims 1 or 5 wherein the PVP is present in at least 0.5 % by weight of the composition.
7. A composition according to any one of claims 1 to 6 further comprising an ionic fluorine-containing compound.
8. A composition according to any one of claims 1 to 7 comprising a nonionic amphoteric or cationic surfactant.
9. A composition according to claim 8 wherein the surfactant is a nonionic poloxamer or polyethoxylated hydrogenated castor oil.
10. A composition according to claim 8 or 9 wherein the surfactant is present in the range 0.005 to 5 % by weight of the composition.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9701031.8A GB9701031D0 (en) | 1997-01-18 | 1997-01-18 | Composition |
| GB9701031.8 | 1997-01-18 | ||
| PCT/EP1998/000381 WO1998031332A1 (en) | 1997-01-18 | 1998-01-14 | Mouthwash composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2278237A1 true CA2278237A1 (en) | 1998-07-23 |
Family
ID=10806216
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002278237A Abandoned CA2278237A1 (en) | 1997-01-18 | 1998-01-14 | Mouthwash composition |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1006991A1 (en) |
| JP (1) | JP2001508785A (en) |
| CN (1) | CN1250368A (en) |
| AR (1) | AR011535A1 (en) |
| AU (1) | AU6096998A (en) |
| BR (1) | BR9806910A (en) |
| CA (1) | CA2278237A1 (en) |
| CO (1) | CO4920205A1 (en) |
| EA (1) | EA199900547A1 (en) |
| GB (1) | GB9701031D0 (en) |
| TW (1) | TW518232B (en) |
| WO (1) | WO1998031332A1 (en) |
| ZA (1) | ZA98368B (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050158349A1 (en) * | 2004-01-20 | 2005-07-21 | Jampani Hanuman B. | Two-phase compositions containing alcohol |
| EP1797860A1 (en) * | 2005-12-15 | 2007-06-20 | JOHNSON & JOHNSON CONSUMER COMPANIES, INC. | Two-phase compositions containing alcohol |
| IT1398050B1 (en) * | 2010-02-02 | 2013-02-07 | Lastri | COMPOSITION FOR ORAL HYGIENE CONTAINING CLOREXIDINE AND A SYSTEM TO PREVENT THE FORMATION OF DARK PIGMENTS ON THE SURFACE OF TEETH AND ORAL MUCOS |
| CN105611909B (en) * | 2013-03-12 | 2020-09-15 | 普莱玛疗法公司 | Dental compositions comprising chelating agents and bases |
| EP3043786A4 (en) * | 2013-09-13 | 2017-03-01 | 3M Innovative Properties Company | Cationic antiseptic compositions, method and kit |
| US10813892B2 (en) * | 2016-05-24 | 2020-10-27 | Carefusion 2200, Inc. | Antiseptic solutions and applicators |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9204410D0 (en) * | 1992-02-29 | 1992-04-15 | Smithkline Beecham Plc | Method of treatment |
| EP0681466B1 (en) * | 1993-01-19 | 2001-09-19 | The Gillette Company | Mouthrinse |
-
1997
- 1997-01-18 GB GBGB9701031.8A patent/GB9701031D0/en active Pending
-
1998
- 1998-01-14 BR BR9806910-1A patent/BR9806910A/en not_active Application Discontinuation
- 1998-01-14 CA CA002278237A patent/CA2278237A1/en not_active Abandoned
- 1998-01-14 WO PCT/EP1998/000381 patent/WO1998031332A1/en not_active Application Discontinuation
- 1998-01-14 EA EA199900547A patent/EA199900547A1/en unknown
- 1998-01-14 JP JP53330398A patent/JP2001508785A/en active Pending
- 1998-01-14 EP EP98905343A patent/EP1006991A1/en not_active Withdrawn
- 1998-01-14 CN CN98803284A patent/CN1250368A/en active Pending
- 1998-01-14 AU AU60969/98A patent/AU6096998A/en not_active Abandoned
- 1998-01-15 ZA ZA98368A patent/ZA98368B/en unknown
- 1998-01-16 AR ARP980100195A patent/AR011535A1/en unknown
- 1998-01-16 CO CO98001594A patent/CO4920205A1/en unknown
- 1998-01-26 TW TW087101101A patent/TW518232B/en active
Also Published As
| Publication number | Publication date |
|---|---|
| EP1006991A1 (en) | 2000-06-14 |
| EA199900547A1 (en) | 2000-06-26 |
| CN1250368A (en) | 2000-04-12 |
| JP2001508785A (en) | 2001-07-03 |
| WO1998031332A1 (en) | 1998-07-23 |
| CO4920205A1 (en) | 2000-05-29 |
| GB9701031D0 (en) | 1997-03-05 |
| ZA98368B (en) | 1998-10-14 |
| TW518232B (en) | 2003-01-21 |
| AR011535A1 (en) | 2000-08-30 |
| BR9806910A (en) | 2000-05-16 |
| AU6096998A (en) | 1998-08-07 |
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