Drug – bio-affecting and body treating compositions – Dentifrices
Reexamination Certificate
1999-08-30
2001-06-26
Rose, Shep K. (Department: 1614)
Drug, bio-affecting and body treating compositions
Dentifrices
C514S724000, C514S726000, C514S817000, C514S818000, C514S829000, C514S830000, C514S862000, C514S886000, C514S887000, C514S969000
Reexamination Certificate
active
06251371
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to diclorobenzyl alcohol, containing preparations.
2. The Prior Art
It is known to use 2,4-dichlorobenzyl alcohol (hereinafter referred to as 2,4-DCBA) as a bactericidal and/or fungicidal agent against a variety of bacteria and fungi, including yeast, mould fungi, fungi in the skin, and a number of gram-positive and gram-negative bacteria. Thus, it has been known to use 2,4-DCBA in combination with other bactericidal agents in antiseptic lozenges for more than 30 years.
2,4-DCBA has also successfully been used as an antimicrobial agent for treatment of infections in mouth and throat, in antiseptic skin preparations for disinfection and treatment of minor cuts and abrasions, and foot creams/lotions for treatment of fungi.
U.S. Pat. No. 3,123,528 discloses a pharmaceutical preparation for oral use which includes 2,4-DCBA and a pharmaceutically acceptable diluent or carrier. The compositions inter alia include mouth washes, toothpastes, pastilles, lozenges, lotions, eardrops, which compositions are used for combating infections caused by bacteria and fungi in ear, throat and skin. If desired, the composition may also contain saligenin (o-hydroxy-benzyl alcohol) which is a local anaesthetic, incorporated in order to impart both bactericidal and anaesthetic effect to compositions for oral use.
EP patent application No. 161 898 discloses dentrifice compositions, including tooth creams and tooth gels, and which comprise a bactericidal agent for treatment of plaque (bacteria coatings), e.g. 2,4-DCBA.
Further, U.S. Pat. No. 4,167,583 discloses antimicrobial compositions for disinfection of the skin of humans and animals, which compositions inter alia may contain dichlorobenzyl alcohol, e.g. 2,4-DCBA. The compositions may also be used for disinfection of surgical instruments and equipment. The compositions are particularly suited for disinfection of hands, e.g. in case of surgery.
WO 95/26134 discloses a composition for application onto a surface, such as the surface of an apparatus or an instrument, a dressing, a glove, a condom or a skin surface, and comprising an agent for inactivating a so-called irritant and a substance which effectively prevents the irritant-inactivating agent from binding to the surface. Antimicrobial agents, including 2,4-DCBA, are mentioned as examples of irritant-inactivating agents.
WO 92/1811 discloses the use of an antimicrobial agent, such as 2,4-DCBA, for preparing a preparation for treatment of gastric disorders caused by the microorganism
Helicobacter pylori.
WO 96/32934 discloses the use of a composition comprising 2,4-DCBA and amylmetacresol for preparing a medicament for the treatment or prevention of HIV viral infections.
EP 0 733 357 discloses topical pharmaceutical formulations in the form of a thixotropic gel, which formulation besides an active component contains from 2 to 15% of colloidal silica, water and optionally one or more excipients. As examples of active components, mention is made of non-steroidal anti-inflammatory agents and anti-bacterials/antibiotics. I.a. a formulation containing 2,4-DCBA is mentioned.
Further, it is known to use 2,4-DCBA in order to prevent bacterial/fungal growth in e.g. cosmetics, toilet ware, including shampoos and antiplaque toothpastes, household articles, textiles, timber, leather goods, paper etc.
SUMMARY OF THE INVENTION
The invention is based on the discovery that dichlorobenzyl alcohol, and in particular 2,4-DCBA, has a surprisingly good effect on inflammations.
An inflammation is the result of an extraneously provoked damage to cells or tissue. Such damages can be provoked by chemical and/or physical influences on the skin of humans and animals. Examples of physical influences are strokes, heat, cold, radiation and electrical chock, and examples of chemical influences are contact with acids, bases and allergens. Inflammation may also be provoked by microorganisms acting on the skin, as opposed to infections which are the result of microorganisms invading the human or animal body.
In other words, inflammation is a defense mechanism caused by extraneously provoked influences on skin or tissue. The symptoms may be one or more of the following: pain, increased surface temperature, swelling, erythema and reduced or ceased function, e.g., masticating efficiency.
Thus, the invention relates to the use of dichlorobenzyl alcohol, and in particular 2,4-DCBA, for preparing a preparation for topical treatment of inflammation.
Use of 2,4-DCBA in low concentrations has turned out not to have an irritating (inflammatory) effect on skin and mucosa. Reactions on the skin have been studied by directly applying solutions in propylene glycol under a dressing on the stomach of guinea pigs for 4-5 hours. Concentrations of up to 1% caused no or little damage, while higher concentrations caused inflammatory conditions.
In spite of 2,4-DCBA having very limited solubility in water, the substance may effectively be incorporated into aqueous systems. The solubility in organic solvents is good.
When treating an inflammatory condition, dichlorobenzyl alcohol, preferably 2,4-DCBA, can be applied onto skin or mucosa in the form of an ointment, cream, a gel or a solution.
In order for the active compound (dichlorobenzyl alcohol, 2,4-DCBA) to have the optimum effect, it is important that it be retained at the inflammatory site for prolonged time. For this purpose bioadhesives may advantageously be used, which are substances binding to biological materials, including proteins, cells or tissue. A bioadhesive may consequently be defined as a compound capable of binding to the biological material and remain bound for a given period of time. When the biological material is mucosa, it is a matter of mucoadhesive materials. Mucoadhesive materials in the form of polymers are normally capable of forming hydrogels.
In one embodiment of the invention, the active compound is combined with one or more substances which provide a controlled release and/or a prolonged retention of dichlorobenzyl alcohol at the treatment site.
In a further embodiment of the invention, the active compound is combined with one or more bioadhesive materials.
Examples of bioadhesive materials include hydrocolloids, such as sodium carboxymethylcellulose, Carbopol, Tragacanth, Karaya gum, sodium alginate, gelatin, methylcellulose and gum arabic.
It is characteristic of bioadhesive materials that they are macromolecular organic hydrocolloids with hydrophilic, functional groups capable of forming hydrogen bonds with, e.g., the corresponding functional groups on the biological material. The strength of the bioadhesive material increases when the molecular weight is increased to more than 100 000 Dalton.
By using bioadhesives, the retention time of the active agent on the ad/absorbing surface is prolonged, as mentioned above. Many different types of bioadhesive materials, both natural and synthetic, can be used for controlling the release of the active agent.
The compound 2,4-DCBA has turned out to be effective against various skin diseases, including pruritus and psoriasis. Further, the compound has turned out to be effective for treatment of insect bite/sting (inflammatory conditions).
The invention also relates to a preparation for topical treatment of inflammation which can be applied onto skin and/or mucosa, and which as active component contains dichlorobenzyl alcohol.
In an embodiment of the preparation it includes, besides the active component, a bioadhesive thickening agent and water.
In a preferred embodiment of the preparation it is formed of 0.05-2 weight-%, preferably about 1 weight-%, of dichlorobenzyl alcohol, 0.1-10 weight-%, preferably about 2 weight-%, of bioadhesive material, and 90-99 weight-%, preferably about 97 weight-%, of water.
As the new preparation is both disinfecting, anti-inflammatory and pain-relieving, and when applied for oral use in the form of a dentrifice composition, it is useful for treatment and pain-relief in a variety of conditions, e.g., paradentosis,
Holmen Hans
Pedersen Arne Martinus
Bifodan A/S
Dykema Gossett PLLC
Rose Shep K.
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