Topical medicament comprising phenolic biocide and choline

Details Topical medicament comprising phenolic biocide and choline Topical medicament comprising phenolic biocide and choline

1999-08-11

2002-10-22

Jarvis, William R. A. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

C-o-group doai

C514S728000, C514S731000

Reexamination Certificate

active

06469070

ABSTRACT:

This application is 371 of PCT/GB97/01306 filed May 14, 1997 which claims priority benefit to United Kingdom 9610122.5 filed May 15, 1996.
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to the preparation of topical medicaments for the treatment of warts and related conditions. In particular it relates to the use of phenolic biocidal compounds to prepare such medicaments.
2. Description of the Related Art
A wide range of generally non-life threatening but highly irritating conditions affect both the human and animal skin. These include warts, corns and verrucae.
A range of compounds has been suggested for use in the treatment of such conditions, however they all suffer from one or more drawbacks, including lack of efficacy or excessive irritancy. Thus there is a continuing need for a treatment of warts, corns and verrucae which is both effective and non-irritant.
We have now found that a range of phenolic biocidal compounds are particularly effective at treating such conditions and that their irritancy can be sufficiently reduced by combination with choline or derivatives thereof.
SUMMARY OF THE INVENTION
According to the invention there is provided the use of phenolic biocide, which is preferably a compound of formula I
in which n is from 0 to 19,
in combination with choline or a derivative or a salt thereof,
for the preparation of a topical medicament for the treatment of warts, corns or verrucae.
There is further provided a topical medicament comprising a phenolic biocide, which is preferably a compound of formula I in which n is from 0 to 19, and choline or a derivative or a salt thereof.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
Preferably in the topical medicaments of the invention the phenolic biocide and the choline or derivative or salt thereof are in intimate admixture.
Preferably in the compound of formula I n is 3 to 13.
Most preferably the compound of formula I is 4-hexylresorcinol.
The compound of formula I is preferably used at a concentration of from 0.01 to 20% by weight, more preferably 0.1 to 5% w/w, most preferably 0.2 to 3.0% w/w
Preferred derivatives of choline include lecithin, glycerophosphocholine and acetylcholine. Preferred salts of choline include choline chloride, choline phosphate, choline iodide and choline bromide, most preferably choline chloride.
The concentration of choline, or a derivative, other than lecithin, or a salt thereof, in the topical medicaments of the invention is preferably from 0.01 to 20% w/w, more preferably 0.1 to 5% w/w, most preferably 0.2 to 3.0% w/w. When lecithin is used in the topical medicaments of the invention the concentration is preferably 0.2 to 30% w/w, most preferably 1 to 10% w/w.
We have also found that the inclusion of a surfactant in the topical medicaments of the invention may lead to improved activity versus warts, corns and verrucae.
Therefore the topical medicaments of the invention preferably further comprise a surfactant. The surfactant is preferably an anionic surfactant, most preferably N-lauroylsarcosine or a salt thereof. The concentration of surfactant in the topical medicaments of the invention is preferably from 0.1 to 5% w/w, most preferably from 0.2 to 3% w/w.
The topical medicaments of the invention may also comprise further biocidal agents in addition to the compounds of formula I. Preferably these further biocides are quaternary ammonium compounds or phenolic compounds. More preferably the further biocide is trimethyltetradecylammonium bromide (cetrimide).
The concentration of the further biocide in the topical medicaments of the invention is preferably from 0.1 to 5% w/w, most preferably from 0.2 to 3% w/w.
The topical medicaments of the invention may also comprise inositol. The concentration of inositol is preferably from 0.05 to 20% w/w; most preferably from 0.2 to 5% w/w.
The topical medicaments of the invention may be applied to any part of the body surface, including mucous membranes. The topical medicaments of the invention may be applied in conventional cream or ointment form; may be applied predispersed onto a dressing or plaster; or in conventional topical sustained release devices.
The topical medicaments of the invention may be formulated using any suitable aqueous or non-aqueous vehicles, the preferred vehicles are paraffin, Vaseline (a trademark), Lanette N (a mixture of cetearyl alcohol and sodium cetearyl alcohol sulphate), and non aqueous polymer compositions including nitrocellulose, Collodion and Carboset (available from B. F. Goodrich) and ethylcellulose. Preferably the vehicle is non-aqueous.
The topical medicaments of the invention may be manufactured using any conventional manufacturing processes, however it is preferred that the phenolic biocide and the choline or derivative or salt thereof are in intimate admixture. This may be ensured either by homogenous premixing of the phenolic biocide and the choline or derivative or salt thereof before dispersion in the vehicle, or by thorough dispersion of both ingredients directly into the vehicle.
Further according to the invention, there is provided a topical medicament comprising
i) 0.01 to 20% w/w of a compound of formula I in which n is from 0 to 19,
ii) 0.01 to 20% w/w choline, or a derivative or a salt thereof, and
iii) 0.1 to 5% w/w of a surfactant.


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Abstract, Database EPODOC. EPO XP002036477. CN 1 095 587, 1994.

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