WO2001067864A2 - Topical virucidal formulation - Google Patents

Topical virucidal formulation Download PDF

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Publication number
WO2001067864A2
WO2001067864A2 PCT/GB2001/001121 GB0101121W WO0167864A2 WO 2001067864 A2 WO2001067864 A2 WO 2001067864A2 GB 0101121 W GB0101121 W GB 0101121W WO 0167864 A2 WO0167864 A2 WO 0167864A2
Authority
WO
WIPO (PCT)
Prior art keywords
formulation
active ingredient
cream
acid
group
Prior art date
Application number
PCT/GB2001/001121
Other languages
French (fr)
Other versions
WO2001067864A3 (en
Inventor
Joshua Berkowitz
Original Assignee
Norton Healthcare Ltd.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from GB0006243A external-priority patent/GB0006243D0/en
Priority claimed from GB0007327A external-priority patent/GB0007327D0/en
Application filed by Norton Healthcare Ltd. filed Critical Norton Healthcare Ltd.
Priority to AU4083301A priority Critical patent/AU4083301A/en
Publication of WO2001067864A2 publication Critical patent/WO2001067864A2/en
Publication of WO2001067864A3 publication Critical patent/WO2001067864A3/en

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Classifications

    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N59/00—Biocides, pest repellants or attractants, or plant growth regulators containing elements or inorganic compounds
    • A01N59/08—Alkali metal chlorides; Alkaline earth metal chlorides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/42—Phosphorus; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants

Definitions

  • This invention relates to a topical virucidal formulation, particularly but not exclusively to a cream or other solid formulation for eradication or treatment of viral infections particularly on the skin or mucous membranes.
  • the formulation may be used for therapeutic or prophylactic purposes.
  • the invention also relates to ointments, pastes, emulsions, gels and rigid foam formulations.
  • a virucidal disinfectant composition for use with surgical equipment is disclosed in GB-A-2164851.
  • This comprises and oxidising agent, for example potassium persulphate, sodium chloride, sulphamic acid, a non-reducing organic acid, an acid pyrophosphate and an anionic surfactant.
  • oxidising agent for example potassium persulphate, sodium chloride, sulphamic acid, a non-reducing organic acid, an acid pyrophosphate and an anionic surfactant.
  • Such disinfectants are sold under the trade mark VIRKON. There is no disclosure that this composition may be used in a pharmaceutical formulation.
  • a topical virucidal pharmaceutical formulation comprises as active ingredients an inorganic halide and an oxidising agent capable of generating hypohalite ions in aqueous solution, a sulphamic acid, a non-reducing organic acid and an inorganic phosphate optionally with a surfactant, preferably an anionic surfactant, together with one or more pharmaceutically acceptable excipients.
  • compositions for manufacture of a topical virucidal formulation comprising as ingredients an inorganic halide and an oxidising agent capable of generating hypohalite ions in aqueous solution, a sulphamic acid, a non-reducing organic acid and an inorganic phosphate optionally with a surfactant, preferably an anionic surfactant, together with one or more pharmaceutically acceptable excipients.
  • the oxidising agent is preferably a persulphate or pyroxiphthalate, particularly potassium persulphate.
  • the inorganic halide is preferably sodium chloride.
  • the non-reducing organic acid may be selected from: malic acid, succinic acid and mixtures thereof.
  • the phosphate may be selected from disodium hydrogen pyrophosphate or potassium dihydrogen phosphate. Alternative anhydrous phosphates may be employed. Any compatible pharmaceutically acceptable surfactant may be employed, for example sodium dodecylbenzene sulphonate, lauryl ethyl sulphonate and polyethylene oxide/polypropylene oxide condensates.
  • VIRKON potassium persulphate (triple salt) 50% sodium chloride 15% sulphamic acid 5% malic acid 10% disodium pyrophosphate 5% anionic surfactant 15%
  • the amount of the ingredients containing the active moeities is preferably a minimum amount necessary to provide virucidal efficacy.
  • An amount of 0.1% to 40%, preferably 0.2% to 5%, preferably 1 to 3% by weight may be employed. Amounts and proportions in this specification are by weight unless otherwise indicated otherwise.
  • the formulation may comprise a cream wherein particles of the active-containing ingredients are uniformly dispersed. In order to ensure homogeneity of the product the particles may have a dimension less than 75 ⁇ ra to provide a smooth cream having good dermal contact.
  • the formulation may include a hydrocarbon base, for example petrolatum or white ointment.
  • An absorption base may be added, for example lanolin, lanolin isolates, cholesterol, lanosterol, acylated sterols or partial esters of polyhydric alcohols for example sorbitan monostearate or monooleate, or mixtures thereof.
  • Water removable bases are preferred to facilitate removal of the cream from the skin or clothing.
  • Creams in accordance with the present invention may incorporate one or more emulsifiers optionally together with one or more co-emulsifiers for example cetyl alcohol or glyceryl monostearate.
  • Polyvalent ions for example magnesium, calcium or aluminium may be added to stabilise the emulsion.
  • a mixed emulsifier system maybe employed.
  • a humectant, for example glycerin, propyleneglycol or sorbitol may be employed to prevent drying of the cream on storage.
  • Formulations of the present invention find particular application as a prophylactic treatment for HIV or hepatitis infections for example as a vaginal cream or as a lining for surgical, dental, other medical or veterinary gloves
  • An advantage arising from use of the present formulation is that the formulation is pink in colour. Loss of the pink colour before or during use indicates a loss of activity.
  • a formulation was prepared using the following ingredients:
  • the resultant formulation was a pink cream.
  • a formulation was prepared using: Aqueous cream BP 97.5 g
  • the resultant formulation was a pink cream. Tests were carried out to determine virucidal activity. Hepatitis A virus was used on account of its known resistance to virucides. The cream showed excellent efficacy.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

A topical virucidal pharmaceutical formulation comprising as active ingredient an inorganic halide, an oxidising agent capable of generating hypohalite ions in aqueous solution, a sulphamic acid, a non-reducing organic acid and an inorganic phosphate optionally with a surfactant, preferably an anionic surfactant, together with one or more pharmaceutically acceptable excipients.

Description

TOPICAL VIRUCIDAL FORMULATION
This invention relates to a topical virucidal formulation, particularly but not exclusively to a cream or other solid formulation for eradication or treatment of viral infections particularly on the skin or mucous membranes. The formulation may be used for therapeutic or prophylactic purposes. The invention also relates to ointments, pastes, emulsions, gels and rigid foam formulations.
A virucidal disinfectant composition for use with surgical equipment is disclosed in GB-A-2164851. This comprises and oxidising agent, for example potassium persulphate, sodium chloride, sulphamic acid, a non-reducing organic acid, an acid pyrophosphate and an anionic surfactant. Such disinfectants are sold under the trade mark VIRKON. There is no disclosure that this composition may be used in a pharmaceutical formulation.
According to a first aspect of the present invention a topical virucidal pharmaceutical formulation comprises as active ingredients an inorganic halide and an oxidising agent capable of generating hypohalite ions in aqueous solution, a sulphamic acid, a non-reducing organic acid and an inorganic phosphate optionally with a surfactant, preferably an anionic surfactant, together with one or more pharmaceutically acceptable excipients.
According to a second aspect of the present invention there is provided use of a composition for manufacture of a topical virucidal formulation, the composition comprising as ingredients an inorganic halide and an oxidising agent capable of generating hypohalite ions in aqueous solution, a sulphamic acid, a non-reducing organic acid and an inorganic phosphate optionally with a surfactant, preferably an anionic surfactant, together with one or more pharmaceutically acceptable excipients.
The oxidising agent is preferably a persulphate or pyroxiphthalate, particularly potassium persulphate. The inorganic halide is preferably sodium chloride.
The non-reducing organic acid may be selected from: malic acid, succinic acid and mixtures thereof.
The phosphate may be selected from disodium hydrogen pyrophosphate or potassium dihydrogen phosphate. Alternative anhydrous phosphates may be employed. Any compatible pharmaceutically acceptable surfactant may be employed, for example sodium dodecylbenzene sulphonate, lauryl ethyl sulphonate and polyethylene oxide/polypropylene oxide condensates.
A preferred formulation available under the trade mark VIRKON comprises potassium persulphate (triple salt) 50% sodium chloride 15% sulphamic acid 5% malic acid 10% disodium pyrophosphate 5% anionic surfactant 15%
100%
The amount of the ingredients containing the active moeities is preferably a minimum amount necessary to provide virucidal efficacy. An amount of 0.1% to 40%, preferably 0.2% to 5%, preferably 1 to 3% by weight may be employed. Amounts and proportions in this specification are by weight unless otherwise indicated otherwise.
The formulation may comprise a cream wherein particles of the active-containing ingredients are uniformly dispersed. In order to ensure homogeneity of the product the particles may have a dimension less than 75 μra to provide a smooth cream having good dermal contact.
The formulation may include a hydrocarbon base, for example petrolatum or white ointment. An absorption base may be added, for example lanolin, lanolin isolates, cholesterol, lanosterol, acylated sterols or partial esters of polyhydric alcohols for example sorbitan monostearate or monooleate, or mixtures thereof.
Water removable bases are preferred to facilitate removal of the cream from the skin or clothing.
Creams in accordance with the present invention may incorporate one or more emulsifiers optionally together with one or more co-emulsifiers for example cetyl alcohol or glyceryl monostearate. Polyvalent ions, for example magnesium, calcium or aluminium may be added to stabilise the emulsion. A mixed emulsifier system maybe employed. A humectant, for example glycerin, propyleneglycol or sorbitol may be employed to prevent drying of the cream on storage.
Formulations of the present invention find particular application as a prophylactic treatment for HIV or hepatitis infections for example as a vaginal cream or as a lining for surgical, dental, other medical or veterinary gloves
An advantage arising from use of the present formulation is that the formulation is pink in colour. Loss of the pink colour before or during use indicates a loss of activity.
The invention is further described by means of example but not in any limitative sense.
Example 1
A formulation was prepared using the following ingredients:
Aqueous cream BP 495 g
Virkon 5 g
500 g
The resultant formulation was a pink cream.
Example 2
A formulation was prepared using: Aqueous cream BP 97.5 g
Virkon 2.5 g
100 g
The resultant formulation was a pink cream. Tests were carried out to determine virucidal activity. Hepatitis A virus was used on account of its known resistance to virucides. The cream showed excellent efficacy.

Claims

1. A topical virucidal pharmaceutical formulation comprising as active ingredient an inorganic halide, an oxidising agent capable of generating hypohalite ions in aqueous solution, a sulphamic acid, a non-reducing organic acid and an inorganic phosphate optionally with a surfactant, preferably an anionic surfactant, together with one or more pharmaceutically acceptable excipients.
2. A formulation as claimed in claim 1, wherein the oxidising agent is selected from the group consisting of persulphate and pyroxiphthalate.
3. A formulation as claimed in claim 2, wherein the oxidising agent is potassium persulphate.
4. A formulation as claimed in any preceding claim, wherein the non- reducing organic acid is selected from the group consisting of: malic acid, succinic acid and mixtures thereof.
5. A formulation as claimed in any preceding claim, wherein the phosphate is selected from the group consisting of disodium hydrogen phosphate and potassium dihydrogen phosphate.
6. A formulation as claimed in any preceding claim, wherein the surfactant is selected from the group consisting of sodium dodecylbenzene sulphonate, lauryl ethyl sulphonate and polyethylene oxide/polypropylene oxide condensates.
7. A formulation as claimed in any preceding claim, wherein the active ingredient consists of: potassium persulphate (triple salt) 50% sodium chloride 15% sulphamic acid 5% malic acid 10% disodium pyrophosphate 5% anionic surfactant 15%
100%
8. A formulation as claimed in any preceding claim, comprising 0.1 to 40% of active ingredient.
9. A formulation as claimed in any preceding claim, comprising 0.2 to 5% of active ingredient.
10. A formulation as claimed in any preceding claim, comprising 1 to 3% of active ingredient.
12. A formulation as claimed in any preceding claim, comprising a cream wherein particles of active ingredient have a dimension less than 75 μm.
13. A formulation as claimed in any preceding claim, comprising a cream including a hydrocarbon base.
14. A formulation as claimed in claim 13, further comprising an absorption base selected from the group consisting of lanolin, lanolin isolates, cholesterol, lanosterol, acylated sterols and partial esters of polyhydric alcohols.
15. A formulation as claimed in claim 13 or 14, comprising a cream incorporating one or more emulsifiers optionally together with one or more co-emulsifiers.
16. A hand cream comprising a formulation as claimed in any of claims 13
17. A coating for an internal surface of a surgical, dental, veterinary or other medical glove comprising a formulation as claimed in any of claims 1 to 15.
18. A vaginal cream comprising a formulation as claimed in any of claims 1 to 15.
19. A surgical glove having a coating of a formulation as claimed in any of claims 1 to 15 on an internal surface thereof.
20. Use of a composition for manufacture of a topical virucidal formulation, the composition comprising a formulation as claimed in any of claims 1 to 15.
PCT/GB2001/001121 2000-03-15 2001-03-15 Topical virucidal formulation WO2001067864A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU4083301A AU4083301A (en) 2000-03-15 2001-03-15 Topical virucidal formulation

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0006243A GB0006243D0 (en) 2000-03-15 2000-03-15 Topical virucidal formulation
GB0006243.0 2000-03-15
GB0007327A GB0007327D0 (en) 2000-03-28 2000-03-28 Topical virucidal formulation
GB0007327.0 2000-03-28

Publications (2)

Publication Number Publication Date
WO2001067864A2 true WO2001067864A2 (en) 2001-09-20
WO2001067864A3 WO2001067864A3 (en) 2002-07-04

Family

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Application Number Title Priority Date Filing Date
PCT/GB2001/001121 WO2001067864A2 (en) 2000-03-15 2001-03-15 Topical virucidal formulation

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AU (1) AU4083301A (en)
WO (1) WO2001067864A2 (en)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1360940A1 (en) * 2002-05-02 2003-11-12 Belle L. Chou Anti-microbial elastomeric flexible article, such as a glove, and manufacturing method
WO2004000025A1 (en) * 2002-06-24 2003-12-31 Bonyf Ag Use of a composition and a cleaning tablet containing said composition for disinfecting purposes
US6692756B2 (en) 1999-04-07 2004-02-17 Shen Wei (Usa), Inc. Aloe vera glove and manufacturing method
US6953582B2 (en) 1999-04-07 2005-10-11 Sheh Wei (Usa), Inc. Skin-enhancing glove and method of manufacture
CN102265904A (en) * 2011-06-03 2011-12-07 宋海鹏 Compound potassium hydrogen persulfate disinfectant and manufacturing process thereof
IT201700109583A1 (en) * 2017-09-29 2019-03-29 Piante Acqua Natura Srl P A N NEW LYMPH-COMPATIBLE FORMULATE
EP3574759A1 (en) * 2018-06-01 2019-12-04 LANXESS Deutschland GmbH Disinfectant composition

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2164851A (en) * 1984-10-01 1986-04-03 Auchincloss Thomas R Dry, water soluble biocidal compositions
GB2187098A (en) * 1986-03-01 1987-09-03 Auchincloss Thomas R Biocidal, particularly virucidal, compositions
US5262174A (en) * 1983-07-27 1993-11-16 Efamol Limited Anti-viral compositions
US5965610A (en) * 1994-03-28 1999-10-12 The Trustees Of Columbia University In The City Of New York Composition for inactivating irritants in fluids

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5262174A (en) * 1983-07-27 1993-11-16 Efamol Limited Anti-viral compositions
GB2164851A (en) * 1984-10-01 1986-04-03 Auchincloss Thomas R Dry, water soluble biocidal compositions
GB2187098A (en) * 1986-03-01 1987-09-03 Auchincloss Thomas R Biocidal, particularly virucidal, compositions
US5965610A (en) * 1994-03-28 1999-10-12 The Trustees Of Columbia University In The City Of New York Composition for inactivating irritants in fluids

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6692756B2 (en) 1999-04-07 2004-02-17 Shen Wei (Usa), Inc. Aloe vera glove and manufacturing method
US6953582B2 (en) 1999-04-07 2005-10-11 Sheh Wei (Usa), Inc. Skin-enhancing glove and method of manufacture
EP1360940A1 (en) * 2002-05-02 2003-11-12 Belle L. Chou Anti-microbial elastomeric flexible article, such as a glove, and manufacturing method
WO2004000025A1 (en) * 2002-06-24 2003-12-31 Bonyf Ag Use of a composition and a cleaning tablet containing said composition for disinfecting purposes
CN102265904A (en) * 2011-06-03 2011-12-07 宋海鹏 Compound potassium hydrogen persulfate disinfectant and manufacturing process thereof
CN102265904B (en) * 2011-06-03 2015-01-07 宋海鹏 Compound potassium hydrogen persulfate disinfectant and manufacturing process thereof
IT201700109583A1 (en) * 2017-09-29 2019-03-29 Piante Acqua Natura Srl P A N NEW LYMPH-COMPATIBLE FORMULATE
WO2019064219A1 (en) * 2017-09-29 2019-04-04 Piante Acqua Natura S.R.L. - P.A.N. New sap-compatible formulation
EP3574759A1 (en) * 2018-06-01 2019-12-04 LANXESS Deutschland GmbH Disinfectant composition
WO2019228980A1 (en) * 2018-06-01 2019-12-05 Lanxess Deutschland Gmbh Disinfectant composition
CN112203514A (en) * 2018-06-01 2021-01-08 朗盛德国有限责任公司 Disinfectant composition
CN112203514B (en) * 2018-06-01 2021-10-15 朗盛德国有限责任公司 Disinfectant composition
US11427485B2 (en) 2018-06-01 2022-08-30 Lanxess Deutschland Gmbh Disinfectant composition

Also Published As

Publication number Publication date
WO2001067864A3 (en) 2002-07-04
AU4083301A (en) 2001-09-24

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