CA2059152A1 - Topical preparation for relief of cold sores and fever blisters and method of use - Google Patents
Topical preparation for relief of cold sores and fever blisters and method of useInfo
- Publication number
- CA2059152A1 CA2059152A1 CA 2059152 CA2059152A CA2059152A1 CA 2059152 A1 CA2059152 A1 CA 2059152A1 CA 2059152 CA2059152 CA 2059152 CA 2059152 A CA2059152 A CA 2059152A CA 2059152 A1 CA2059152 A1 CA 2059152A1
- Authority
- CA
- Canada
- Prior art keywords
- composition
- group
- mixture
- preservative
- phenoxyethanol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 206010067152 Oral herpes Diseases 0.000 title claims abstract description 28
- 208000004898 Herpes Labialis Diseases 0.000 title claims abstract description 23
- 238000000034 method Methods 0.000 title claims abstract description 14
- 230000000699 topical effect Effects 0.000 title claims abstract description 12
- 238000002360 preparation method Methods 0.000 title abstract description 15
- 239000003755 preservative agent Substances 0.000 claims abstract description 23
- 230000002335 preservative effect Effects 0.000 claims abstract description 18
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 229960005323 phenoxyethanol Drugs 0.000 claims abstract description 13
- 239000000203 mixture Substances 0.000 claims description 57
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 21
- -1 alkyl p-hydroxybenzoates Chemical class 0.000 claims description 10
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical group NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 claims description 10
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 claims description 10
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 8
- 239000004615 ingredient Substances 0.000 claims description 7
- 239000000375 suspending agent Substances 0.000 claims description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
- 230000003444 anaesthetic effect Effects 0.000 claims description 6
- 230000000202 analgesic effect Effects 0.000 claims description 6
- 230000001139 anti-pruritic effect Effects 0.000 claims description 6
- 239000003908 antipruritic agent Substances 0.000 claims description 6
- 239000002736 nonionic surfactant Substances 0.000 claims description 6
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims description 5
- 239000005995 Aluminium silicate Substances 0.000 claims description 5
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 5
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical class OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 5
- 239000004166 Lanolin Substances 0.000 claims description 5
- 206010039509 Scab Diseases 0.000 claims description 5
- 239000002250 absorbent Substances 0.000 claims description 5
- 230000002745 absorbent Effects 0.000 claims description 5
- 229960000458 allantoin Drugs 0.000 claims description 5
- 235000012211 aluminium silicate Nutrition 0.000 claims description 5
- 230000001580 bacterial effect Effects 0.000 claims description 5
- 229960005274 benzocaine Drugs 0.000 claims description 5
- 239000001902 eugenia caryophyllata l. bud oil Substances 0.000 claims description 5
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 claims description 5
- 229940039717 lanolin Drugs 0.000 claims description 5
- 235000019388 lanolin Nutrition 0.000 claims description 5
- 229940041616 menthol Drugs 0.000 claims description 5
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 5
- 229920000053 polysorbate 80 Polymers 0.000 claims description 5
- 239000000454 talc Substances 0.000 claims description 5
- 229910052623 talc Inorganic materials 0.000 claims description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 claims description 4
- DHVLDKHFGIVEIP-UHFFFAOYSA-N 2-bromo-2-(bromomethyl)pentanedinitrile Chemical compound BrCC(Br)(C#N)CCC#N DHVLDKHFGIVEIP-UHFFFAOYSA-N 0.000 claims description 4
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 claims description 4
- 241000723346 Cinnamomum camphora Species 0.000 claims description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 4
- 229960000846 camphor Drugs 0.000 claims description 4
- 229930008380 camphor Natural products 0.000 claims description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 4
- 239000003974 emollient agent Substances 0.000 claims description 4
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 4
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 3
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 3
- 239000004264 Petrolatum Substances 0.000 claims description 3
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims description 3
- 235000011187 glycerol Nutrition 0.000 claims description 3
- 229940066842 petrolatum Drugs 0.000 claims description 3
- 235000019271 petrolatum Nutrition 0.000 claims description 3
- 239000000600 sorbitol Substances 0.000 claims description 3
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 4
- 239000007788 liquid Substances 0.000 claims 4
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 2
- 229960003742 phenol Drugs 0.000 claims 2
- 229920000136 polysorbate Polymers 0.000 claims 2
- 229950008882 polysorbate Drugs 0.000 claims 2
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 229920001214 Polysorbate 60 Polymers 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- BEGBSFPALGFMJI-UHFFFAOYSA-N ethene;sodium Chemical group [Na].C=C BEGBSFPALGFMJI-UHFFFAOYSA-N 0.000 claims 1
- 239000003208 petroleum Substances 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 description 10
- 244000005700 microbiome Species 0.000 description 4
- 235000014469 Bacillus subtilis Nutrition 0.000 description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 description 3
- 229960001927 cetylpyridinium chloride Drugs 0.000 description 3
- 239000002054 inoculum Substances 0.000 description 3
- 244000004005 Nypa fruticans Species 0.000 description 2
- 235000005305 Nypa fruticans Nutrition 0.000 description 2
- 241000589516 Pseudomonas Species 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- 238000011109 contamination Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000003906 humectant Substances 0.000 description 2
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 1
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-M 4-hydroxybenzoate Chemical compound OC1=CC=C(C([O-])=O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-M 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical class OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 241001139382 Allantion Species 0.000 description 1
- 241000228257 Aspergillus sp. Species 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 241000589513 Burkholderia cepacia Species 0.000 description 1
- 241000191070 Escherichia coli ATCC 8739 Species 0.000 description 1
- 208000009889 Herpes Simplex Diseases 0.000 description 1
- 241000588749 Klebsiella oxytoca Species 0.000 description 1
- 241000588747 Klebsiella pneumoniae Species 0.000 description 1
- 206010034133 Pathogen resistance Diseases 0.000 description 1
- 241000228168 Penicillium sp. Species 0.000 description 1
- 241000588768 Providencia Species 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000001668 ameliorated effect Effects 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 239000008367 deionised water Substances 0.000 description 1
- 229910021641 deionized water Inorganic materials 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 239000003605 opacifier Substances 0.000 description 1
- 125000006353 oxyethylene group Chemical group 0.000 description 1
- LKTOWUZQHJSGAK-UHFFFAOYSA-N phenol;4,7,7-trimethylbicyclo[2.2.1]heptan-3-one Chemical compound OC1=CC=CC=C1.C1CC2(C)C(=O)CC1C2(C)C LKTOWUZQHJSGAK-UHFFFAOYSA-N 0.000 description 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 1
- 229940068968 polysorbate 80 Drugs 0.000 description 1
- GCLGEJMYGQKIIW-UHFFFAOYSA-H sodium hexametaphosphate Chemical compound [Na]OP1(=O)OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])O1 GCLGEJMYGQKIIW-UHFFFAOYSA-H 0.000 description 1
- 239000001593 sorbitan monooleate Substances 0.000 description 1
- 235000011069 sorbitan monooleate Nutrition 0.000 description 1
- 229940035049 sorbitan monooleate Drugs 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000012956 testing procedure Methods 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
ABSTRACT
A topical aqueous preparation for relief of cold sores and fever blisters and method of use. The preparation contains, as per example, 2-phenoxyethanol as a preservative.
A topical aqueous preparation for relief of cold sores and fever blisters and method of use. The preparation contains, as per example, 2-phenoxyethanol as a preservative.
Description
20~9~!~2 TOPICAL PREPARATION FOR RELIEF OF COLD SORES AND FEVER BLISTERS
AND METHOD OF USE.
BACXGROUND OF THE INVENTION
o It is well recognized that cold sores and fever blisters are nuisances both from an aesthetic point of view and from the discomfort that they produce. There are numerous such products available but each falls short of the goal of easy satisfactor~
alleviation of the affliction.
It is pointed out that fever blisters and cold sores are defined as a vesicle that occurs at the junction of the mucous ~embrane and skin on the lips or nose. It is said to be caused by the virus herpes simplex, type 1.
It is contemplated with regard to the present invention to employ a variety of efficacious ingredients.
In regard thereto the topical composition includes a humectant or softener for the crusts or scabs associated with cold sores and fever blisters. Such applicable humectants are water, glycerin and sorbitol and like compounds.
The composition also contains an absorbent or opacifier such as talc or kaolin and mixtures thereof as well as other like compounds~
A suspending agent is also present in the formulation which is a cellulose-based product, for example hydroxyethyIcellulose, ox sodium carboxymethylcellulose. Another applicable suspending agent is Veegum, which is a magnesium aluminum silicate.
Included also is a nonionic surfactant such as poly-oxyethylene and poly-oxvpropylene compounds, e.y., as derivatives of sorbitan and fatty alcohol ethers and esters. Applicable is Tween 80 which is POE 20 sorbitan monooleate polysorbate 80.
An anti-suppurative compound such as allantion is also included.
7,~9~2 An emollient such as petrolatum or lanolin :is also included.
Other additives are included, i.ncluding a topical analgesic such as clove bud oil, an antipruritic such as phenol camphor and menthol and an anesthetic such as benzocaine.
S UYMA~ _ VENTION
It has been found essential to include in the rormulation a preservative to effectively maintain the preparation against contamination by microorganisms associated with the normal use by consumers of the preparation.
It has been found that a safe and effective preservative for topical preparations used for the relief of cold sores and fever blisters is a compound selec~ed from 2-phenoxyethanol, and ~5 mixtures of 2-phenoxye~hanol with o~her ingredients such as a lower alkyl p-hydroxybenzoate, 1,2-dibromo-2, 4-dicyanobutane and mixtures of a lower alkyl p-hydroxybenzoate, propylene glycol and ethylene diamine tetraacetic acid salt.
The composition of the present invention is applied directly unto cold sore or fever blisters as needed. The topical application is continued until the affliction is ameliorated.
Due to the analgesic effect of the composition there is at least an immediate ebbing of the discomfort associated with cold sores and/or fever blisters. Further~ore, the composition decreases greatly the possibilities of secondary bacterial infection commonly occurring when the blisters are ruptured.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
The preservative compounds used in the practice of the present invention are available from commercial suppliers. For example, mixtures of 2-phenoxyethanol with lower alkyl p-hydroxybenzoates are available from Nipa, Inc under the trademark Phenonip which is a 7:3 weight ratio of 2-phenoxyethanol and a mixture of lower alkyl (C1-C4) p-hydroxybenzoates. The alkyl p-hydroxybenzoate mixture is available commercially from Nipa, Inc 20~91~2 ~ er the trademark, Nipastat. Another commercially avallablecomposition suitable as a preservative in the practice of the present invention is Euxyl K-400 (trademark) a 4:1 mixture of 2-phenoxyethanol and 1,2-dibromo-2,4-dicyanobutane available from Calgon Corporation.
An additional composition effective as a preservatives in the practice of the present invention is a combination of Nipastat and propylene glycol. In the absence of propylene glycol, Nipastat is not effective as a preservative in the 0 topical preparations of the present invention.
The preparations of the present invention contain as preservatives the following antibacterial agents in the respective concentration ranges listed in Table I below:
TABLE I
Antibacterial Concentration (Wt.%) Aqent Minlmum Maximum (A) 2-phenoxyethanol0.05 1.0 (B) Phenonip 0.10 1.50 (C) Euxyl K-400 0.05 1.0 (D) Nipastat 0.25 0.5 EDTA 0.10 0.5 Propylene glycol 5.0 15.0 EDTA is ethylene diamine tetraacetic acid salt.
In formulating the cold sore preparations of the present invention, the preservative of Table I is admixed with the following ingredients in the respective concentration ranges listed in Table II below:
TABLE II
CONCENTRATION (% BY WEIGHT) INGREDIENTS MINIMUM MAXIMUM
Preservative 0.05 1.0 Suspending Agent 1.0 3.0 Non-ionic Surfactant 0.05 4.0 Topical anesthetic o.oo 25.0 Anti-Suppurative0.10 3.0
AND METHOD OF USE.
BACXGROUND OF THE INVENTION
o It is well recognized that cold sores and fever blisters are nuisances both from an aesthetic point of view and from the discomfort that they produce. There are numerous such products available but each falls short of the goal of easy satisfactor~
alleviation of the affliction.
It is pointed out that fever blisters and cold sores are defined as a vesicle that occurs at the junction of the mucous ~embrane and skin on the lips or nose. It is said to be caused by the virus herpes simplex, type 1.
It is contemplated with regard to the present invention to employ a variety of efficacious ingredients.
In regard thereto the topical composition includes a humectant or softener for the crusts or scabs associated with cold sores and fever blisters. Such applicable humectants are water, glycerin and sorbitol and like compounds.
The composition also contains an absorbent or opacifier such as talc or kaolin and mixtures thereof as well as other like compounds~
A suspending agent is also present in the formulation which is a cellulose-based product, for example hydroxyethyIcellulose, ox sodium carboxymethylcellulose. Another applicable suspending agent is Veegum, which is a magnesium aluminum silicate.
Included also is a nonionic surfactant such as poly-oxyethylene and poly-oxvpropylene compounds, e.y., as derivatives of sorbitan and fatty alcohol ethers and esters. Applicable is Tween 80 which is POE 20 sorbitan monooleate polysorbate 80.
An anti-suppurative compound such as allantion is also included.
7,~9~2 An emollient such as petrolatum or lanolin :is also included.
Other additives are included, i.ncluding a topical analgesic such as clove bud oil, an antipruritic such as phenol camphor and menthol and an anesthetic such as benzocaine.
S UYMA~ _ VENTION
It has been found essential to include in the rormulation a preservative to effectively maintain the preparation against contamination by microorganisms associated with the normal use by consumers of the preparation.
It has been found that a safe and effective preservative for topical preparations used for the relief of cold sores and fever blisters is a compound selec~ed from 2-phenoxyethanol, and ~5 mixtures of 2-phenoxye~hanol with o~her ingredients such as a lower alkyl p-hydroxybenzoate, 1,2-dibromo-2, 4-dicyanobutane and mixtures of a lower alkyl p-hydroxybenzoate, propylene glycol and ethylene diamine tetraacetic acid salt.
The composition of the present invention is applied directly unto cold sore or fever blisters as needed. The topical application is continued until the affliction is ameliorated.
Due to the analgesic effect of the composition there is at least an immediate ebbing of the discomfort associated with cold sores and/or fever blisters. Further~ore, the composition decreases greatly the possibilities of secondary bacterial infection commonly occurring when the blisters are ruptured.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
The preservative compounds used in the practice of the present invention are available from commercial suppliers. For example, mixtures of 2-phenoxyethanol with lower alkyl p-hydroxybenzoates are available from Nipa, Inc under the trademark Phenonip which is a 7:3 weight ratio of 2-phenoxyethanol and a mixture of lower alkyl (C1-C4) p-hydroxybenzoates. The alkyl p-hydroxybenzoate mixture is available commercially from Nipa, Inc 20~91~2 ~ er the trademark, Nipastat. Another commercially avallablecomposition suitable as a preservative in the practice of the present invention is Euxyl K-400 (trademark) a 4:1 mixture of 2-phenoxyethanol and 1,2-dibromo-2,4-dicyanobutane available from Calgon Corporation.
An additional composition effective as a preservatives in the practice of the present invention is a combination of Nipastat and propylene glycol. In the absence of propylene glycol, Nipastat is not effective as a preservative in the 0 topical preparations of the present invention.
The preparations of the present invention contain as preservatives the following antibacterial agents in the respective concentration ranges listed in Table I below:
TABLE I
Antibacterial Concentration (Wt.%) Aqent Minlmum Maximum (A) 2-phenoxyethanol0.05 1.0 (B) Phenonip 0.10 1.50 (C) Euxyl K-400 0.05 1.0 (D) Nipastat 0.25 0.5 EDTA 0.10 0.5 Propylene glycol 5.0 15.0 EDTA is ethylene diamine tetraacetic acid salt.
In formulating the cold sore preparations of the present invention, the preservative of Table I is admixed with the following ingredients in the respective concentration ranges listed in Table II below:
TABLE II
CONCENTRATION (% BY WEIGHT) INGREDIENTS MINIMUM MAXIMUM
Preservative 0.05 1.0 Suspending Agent 1.0 3.0 Non-ionic Surfactant 0.05 4.0 Topical anesthetic o.oo 25.0 Anti-Suppurative0.10 3.0
2 0 ~ 2 Absorbent 3.00 lO.00 Anti-pruritic 0.05 5.50 Emollient 15.00 50.0 Analge6ic 0.00 1.0 Balance Deionized Water To illustrate the invention the compounds listed below were used as preservatives:
O PRESERVA~IVE CONCENTRATION (% BY WEIGHT) (A) 2-phenoxylethanol 0.6 (B) Phenonip 0.35 (C) Euxyl K-400 0.08 (D) Nipostat 0.5 EDrA 0.2 Propylene glycol lO.0 (E) Phenonip 0.35 propylene glycol 10.00 The above identified compounds were individually a~mixed with the ingredients listed below to formulate cold sore preparations which were tested for antibacterial activity.
I~9E~E~ÇONCENrRATION_(% BY WEIGHTL
2s White pe~rolatum 25.00 Talc 6.40 Benzocaine 5.00 Lanolin, anhydrous3,oO
Veegum 2.60 Kaolin 2.00 Tween 80 1.50 Allantoin 1.50 Sodium carboxymethylcellulose 0.75 Menthol 0.50 ~5 Camphor 0.50 2~91~
Clove bud oil 0.20 Phenol 0.10 Balance deionized ~ater -The cold sore preparations were tested to determine ~hether the preservatlve would protect the formulation from outside contamination by microbial agents associated with its normal use.
The bacterial resistance of the formulatlons was demonstrated in-vitro by challanging the cold sore fo~nulations with a mixed batkery of microorganisms. The microorganismS were as follows:
MOLD INOCULUM
a) Asperqillus a~aucus PLS M 130 b) Aspergillus_ni~er PLS M 131 c) ~9E~o9~ L---erreus PLS M 132 d) Asperaillus sp. PLS M 134 e) Aspergillus sp. PLS M 139 f) Penicillium sp. PLS M 140 g) Pen~ci~lium sp. PLS M 142 B. subtilis Inoculum B. subtilis ATCC 6051 B. subtilis PLS 116 Bacterial Inc~culum a) Yeast PLSY 109 b) Yea~t PLSY 219 c) Pseudomonas cepacia PLS 122 d) Pseudomonas putidan PLS 111 e) Escherichia coli ATCC 8739 f) Klebsiella oxytoca PLS 104B
g) Klebsiella pneumoniae PLS 113 h) Providencia rettqeri PLS 200 20~9~52 i) Pseudomonas eru~nosa ATCC 15442 j) ~ PLS 201 k) Staph aureu ArrCC 6538 1) ~ PLS llOB
The inoculums were mixed with a sample of the individual cold sore preparation. Each cold sore preparation was examined for microorganism growth over a 30 day period.
No growth was observed indicat:ing that the preservatives were effective in preventing bacterial growth in the cold sore preparations.
For comparison purposes, using the above testing procedure, the following compounds were individually substituted for the preservatives of Table I and incorporated in the cold sore composition of Table II and tested ~or antibacterial efficacy.
Comparative Compound Concentration Test Wt.%
No.
1. Nipastat 0.5 2. 5-Chloro-2-(2,4~
dichlorophenoxy)phenol 0.3
O PRESERVA~IVE CONCENTRATION (% BY WEIGHT) (A) 2-phenoxylethanol 0.6 (B) Phenonip 0.35 (C) Euxyl K-400 0.08 (D) Nipostat 0.5 EDrA 0.2 Propylene glycol lO.0 (E) Phenonip 0.35 propylene glycol 10.00 The above identified compounds were individually a~mixed with the ingredients listed below to formulate cold sore preparations which were tested for antibacterial activity.
I~9E~E~ÇONCENrRATION_(% BY WEIGHTL
2s White pe~rolatum 25.00 Talc 6.40 Benzocaine 5.00 Lanolin, anhydrous3,oO
Veegum 2.60 Kaolin 2.00 Tween 80 1.50 Allantoin 1.50 Sodium carboxymethylcellulose 0.75 Menthol 0.50 ~5 Camphor 0.50 2~91~
Clove bud oil 0.20 Phenol 0.10 Balance deionized ~ater -The cold sore preparations were tested to determine ~hether the preservatlve would protect the formulation from outside contamination by microbial agents associated with its normal use.
The bacterial resistance of the formulatlons was demonstrated in-vitro by challanging the cold sore fo~nulations with a mixed batkery of microorganisms. The microorganismS were as follows:
MOLD INOCULUM
a) Asperqillus a~aucus PLS M 130 b) Aspergillus_ni~er PLS M 131 c) ~9E~o9~ L---erreus PLS M 132 d) Asperaillus sp. PLS M 134 e) Aspergillus sp. PLS M 139 f) Penicillium sp. PLS M 140 g) Pen~ci~lium sp. PLS M 142 B. subtilis Inoculum B. subtilis ATCC 6051 B. subtilis PLS 116 Bacterial Inc~culum a) Yeast PLSY 109 b) Yea~t PLSY 219 c) Pseudomonas cepacia PLS 122 d) Pseudomonas putidan PLS 111 e) Escherichia coli ATCC 8739 f) Klebsiella oxytoca PLS 104B
g) Klebsiella pneumoniae PLS 113 h) Providencia rettqeri PLS 200 20~9~52 i) Pseudomonas eru~nosa ATCC 15442 j) ~ PLS 201 k) Staph aureu ArrCC 6538 1) ~ PLS llOB
The inoculums were mixed with a sample of the individual cold sore preparation. Each cold sore preparation was examined for microorganism growth over a 30 day period.
No growth was observed indicat:ing that the preservatives were effective in preventing bacterial growth in the cold sore preparations.
For comparison purposes, using the above testing procedure, the following compounds were individually substituted for the preservatives of Table I and incorporated in the cold sore composition of Table II and tested ~or antibacterial efficacy.
Comparative Compound Concentration Test Wt.%
No.
1. Nipastat 0.5 2. 5-Chloro-2-(2,4~
dichlorophenoxy)phenol 0.3
3. Cetyl Pyridinium Chloride 0.5 30 4. Cetyl Pyridinium Chloride 0.2 5-chloro-2-(2,~-dichloro- 0.15 phenoxy)phenol 5. Cetyl Pyridinium chloride 0.5 Nipastat 0.2 6. Diazolitinylurea 0.5 7. Nipastat 0.5 ED~A 0.2 Bacterial growth was observed in all of these products within 9 days.
Claims (28)
1. A liquid composition for topical application to cold sores and fever blisters comprising a softener for crusts or scabs associated with said cold sores and fever blisters, a suspending agent, an absorbent, a nonionic surfactant, an anesthetic, an emmollient, an anti-pruritic, an anti-suppurative, an analgesic and a preservative effective to inhibit bacterial growth in the composition.
2. The composition of claim 1 wherein the preservative is selected from the group consisting of 2-phenoxyethanol, a mixture of 2-phenoxyethanol and a mixture of lower alkylp-hydroxybenzoates, a mixture of lower alkyl p-hydroxybenzoates, a glycol and a disodium ethylenediaminetetraacetic acid salt.
3. The composition of claim 2 wherein the softener is selected from the group consisting of water, glycerine and sorbitol.
4. The composition of claim 2 wherein the emollient is selected from the group consisting of petrolatum and lanolin and mixtures thereof.
5. The composition of claim 2 wherein the nonionic surfactant is a polyoxyethylene sorbitan monoleate polysorbate.
6. The composition of claim 2 wherein the suspending agent is selected from the group consisting of sodium carboxymethylcellulose and magnesium aluminum silicate and mixtures thereof.
7. The composition of claim 2 wherein the anti-suppurative is allantoin.
8. The composition of claim 2 wherein the absorbent is selected from the group consisting of talc and kaolin and mixtures thereof.
3. The composition of claim 2 wherein the anesthetic is benzocaine.
10. The composition of claim 2 wherein the antipruritic is selected from the group consisting of phenol, menthol and camphor.
11. The composition of claim 2 wherein the analgesic is clove bud oil.
12. A liquid composition for topical application to cold sores and fever blisters comprising the following ingredients in the weight by percent of:
13. A liquid composition for topical application to cold sores and fever blisters comprising the following ingredients in the amount weight by percent:
Preservative 0.05-1.0 Sodium Carboxymethycellulose 0.75 Veegum 2.60 Tween 80 1.50 Benzocaine 5.00 Allantoin 1.50 Talc 6.00 Kaolin 2.00 Menthol 0.50 Camphor 0.50 Phenol 0.10 Lanolin Anhydrous 3.00 White Petroleum 25.00 Clove Bud Oil 0.20 Balance Water
Preservative 0.05-1.0 Sodium Carboxymethycellulose 0.75 Veegum 2.60 Tween 80 1.50 Benzocaine 5.00 Allantoin 1.50 Talc 6.00 Kaolin 2.00 Menthol 0.50 Camphor 0.50 Phenol 0.10 Lanolin Anhydrous 3.00 White Petroleum 25.00 Clove Bud Oil 0.20 Balance Water
14. The composition of claim 13 wherein the preservative is p-phenoxyethanol and is present in the composition at a concentration of 0.6% by weight.
15. The composition of claim 13 wherein the preservative is a 1:4 mixture of 1,2- dibromo -2,4 dicyanobutane and 2-phenoxyethanol and is present in the composition at a concentration of 0.08% by weight.
16. The composition of claim 13 wherein the preservative is a 7:3 ratio of 2-phenoxyethanol to a mixture of lower alkyl p-hydroxybenzoates and is present in the composition at a concentration of 0.35% by weight.
17. The composition of claim 13 wherein the preservative is a mixture of propylene glycol, ethylene diamine tetraacetic acid salts and a mixture of lower alkyl p-hydroxybenzoates, the preservative being present in the composition at a concentration of 0.5% by weight.
18. A method for treating cold sores and fever blisters comprising applying thereto a liquid composition including a softener for curst or scabs associated with said cold sores and fever blisters, a suspending agent, an absorbent, a nonionic surfactant, an anesthetic, an emmollient, an anit-suppurative, an anti-pruritic, an analgesic and a preservative effective to inhibit bacterial growth in the composition.
19. The method of claim 18 wherein the preservative is selected from the group consisting of 2-phenoxyethanol, a mixture of 2-phenoxyethanol and a mixture or lower alkyl p-hydroxybenzoates, a mixture of 2-phenoxyethanol and 1, 2-dibromo-2, 4-dicyanobutane and mixture of lower alkyl p-hydroxybenzoates, a glycol and sodium ethylene diamne tetracetic acid.
20. The method of claim 18 wherein the softener is selected from the group consisting of water, glycerine and sorbitol.
21. The method of claim 18 wherein the emollient is selected from the group consisting of petrolatum and lanolin and mixtures thereof.
22. The method of claim 18 wherein the nonionic surfactant is a polyoxyethylene sorbitan monooleate polysorbate.
23. The method of claim 18 wherein the suspending agent is selected from the group consisting of sodium carboxymethylcellulose and magnesium aluminum silicate and mixtures thereof.
240 The method of claim 18 wherein the anti-suppurative is allantoin.
25. The method of claim 18 wherein the absorbant is selected from the group consisting of talc and kaolin and mixtures thereof.
26. The method of claim 18 wherein the anesthetic is benzocaine.
27. The method of claim 18 wherein the anti-pruritic is selected from the group consisting of phenol, menthol and camphor.
28. The method of claim 18 wherein the analgesic is clove bud oil.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64481991A | 1991-01-23 | 1991-01-23 | |
| US644,819 | 1991-01-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2059152A1 true CA2059152A1 (en) | 1992-07-24 |
Family
ID=24586467
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA 2059152 Abandoned CA2059152A1 (en) | 1991-01-23 | 1992-01-10 | Topical preparation for relief of cold sores and fever blisters and method of use |
Country Status (3)
| Country | Link |
|---|---|
| BR (1) | BR9200191A (en) |
| CA (1) | CA2059152A1 (en) |
| MX (1) | MX9200184A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0954312A1 (en) * | 1996-08-12 | 1999-11-10 | Bruce Miller | Topical composition for burn healing |
-
1992
- 1992-01-10 CA CA 2059152 patent/CA2059152A1/en not_active Abandoned
- 1992-01-16 MX MX9200184A patent/MX9200184A/en unknown
- 1992-01-22 BR BR929200191A patent/BR9200191A/en not_active Application Discontinuation
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0954312A1 (en) * | 1996-08-12 | 1999-11-10 | Bruce Miller | Topical composition for burn healing |
| EP0954312A4 (en) * | 1996-08-12 | 1999-12-01 |
Also Published As
| Publication number | Publication date |
|---|---|
| BR9200191A (en) | 1992-10-06 |
| MX9200184A (en) | 1992-07-01 |
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