Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-10-08
2001-09-18
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S725000, C514S912000
Reexamination Certificate
active
06291519
ABSTRACT:
The present invention relates to the use of a vitamin cocktail comprising both vitamin A and vitamin E in the preparation of an eye medicament for the protection of the eye against both UV-irradiation and ozone.
Eye medicaments comprising both vitamin A and vitamin E are known in the art. These are for example marketed by CIBA-Vision under the trade name Oculotecto®-Gel. Oculotect is typically prescribed for the treatment of dry eye or keratoconjunctivitis.
It has now surprisingly been found that an ophthalmic composition comprising both vitamin A and vitamin E is highly useful for protecting an eye, in particular the human eye, both against UV-irradiation and ozone exposure, both being typically permanently present as so called environmental toxins.
The ophthalmic compositions useful for the above identified protective treatment of the eye are administered either as a gel, a thermogel, a liquid eye drop or an ointment. Preferred is a gel, thermogel and a liquid composition. More preferred is a gel and a thermogel.
An ophthalmic composition comprises typically the components disclosed infra.
The present invention relates to the use of an ophthalmic composition, which contains mandatorily the two active ingredients vitamin E and vitamin A.
Within the terms of the present invention, vitamin A shall denote a compound such as Vitamin A per se (retinol), esters of retinol such as vitamin A acetate, vitamin A palmitate and the like, retinoic acid and retinoic ester such as retinoic acid methyl ester and the like. Preferred are vitamin A acetate and vitamin A palmitate.
Analogously, vitamin E shall denote within the terms of the present invention vitamin E per se, namely (+)-&agr;-tocopherol, isomers and racemates of &agr;-tocopherol such as racemic DL-&agr;-tocopherol, esters of optically pure and/or racemic &agr;-tocopherol such as DL-&agr;-tocopherol acetate, succinate and/or nicotinate, specific derivatives of &agr;-tocopherol such as D-&agr;-tocopheryl polyethylene glycol 1000 succinate (tocophersolan), tocoretinate (retinoic acid esterified with &agr;-tocopherol, see Merck Index 12th edition, No. 9639) and the like. Preferred are DL-&agr;-tocopherol acetate, tocophersolan and tocoretinate.
Optionally, a vitamin efficacy enhancing agent is present in an above concerned ophthalmic composition, such as aesculin and/or a derivative thereof. Aesculin is a natural product and exhibits an excellent topical tolerability as well.
If present, aesculin is typically present in an amount of 0.001 to approximately 10% by weight, preferably of from 0.05 to 5% by weight and in particular from 0.01-1% by weight.
An ophthalmic composition in accordance to the present invention is advantageously applied topically to the eye, especially in the form of a gel, a thermogel, a solution, a suspension, or an ointment. Such compositions comprise the above vitamins typically in a range of from approximately 0.0005 to approximately 15.0% by weight, preferably from approximately 0.001 to approximately 10.0% by weight, or more preferably in the range of from approximately 0.05 to approximately 7% by weight and most preferably in the range of from 0.01 to 1.1% by weight.
The ratio of a vitamin A to a vitamin E used in an above gel, thermogel or liquid composition is typically from 1:10, more preferably from 1:5 and in particular of from 1:1.
For ointments the ratio of a vitamin A to a vitamin E used is typically from 50:1, more preferably from 35:1 and in particular of from 20:1.
A thermogel denotes a gel which typically exhibits a thermoreversability. A thermogel in accordance to the invention exhibits a viscosity maximum at a temperature in the range of the body temperature and more precisely at a temperature in the range of about 30-60° C. It comprises preferably a polyethylen-polypropylen block copolymer. A representative example of such a block copolymer is Poloxamer 407 (Lutrol® F 127 from BASF, Germany).
Other customary ophthalmically acceptable excipients and additives known to the person skilled in the art may be comprised in an above composition, for example those of the type mentioned below, especially carriers, stabilizers, solubilizers, tonicity enhancing agents, buffer substances, preservatives, thickeners, complexing agents and other excipients. Such compositions are prepared in a manner known per se, for example by mixing the active ingredients with the corresponding excipients and/or additives to form corresponding ophthalmic compositions.
Carriers used in accordance to the present invention are preferably suitable for topical administration, and are for example water, mixtures of water and water-miscible solvents, such as C
1
- to C
7
-alkanols, vegetable oils or mineral oils comprising from 0.5 to 5% by weight hydroxyethylcellulose, ethyl oleate, carboxymethyl-cellulose, polyvinyl-pyrrolidone and other non-toxic water-soluble polymers for ophthalmic uses, such as. for example, cellulose derivatives, such as methylcellulose, alkali metal salts of carboxy-methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, methylhydroxypropyl-cellulose and hydroxypropylcellulose, acrylates or methacrylates, such as salts of polyacrylic acid or ethyl acrylate, polyacrylamides, natural products, such as gelatin, alginates, pectins, tragacanth, karaya gum, xanthan gum, carrageenin, agar and acacia, starch derivatives, such as starch acetate and hydroxypropyl starch, and also other synthetic products, such as polyvinyl alcohol, polyvinylpyrrolidone, polyvinyl methyl ether, polyethylene oxide, preferably cross-linked polyacrylic acid, such as neutral Carbopol, or mixtures of those polymers. Preferred carriers are water, cellulose derivatives, such as methylcellulose, alkali metal salts of carboxymethylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, methylhydroxypropylcellulose and hydroxypropylcellulose, neutral Carbopol, or mixtures thereof. The concentration of the carrier is, for example, from 1 to 10000 times the concentration of the active ingredient.
Carriers and further ingredients used for ointments are known in the art and are typically those described in example 6 infra.
The solubilizers used for an ophthalmic composition of the present invention are, for example, tyloxapol, fatty acid glycerol polyethylene glycol esters, fatty acid polyethylene glycol esters, polyethylene glycols, glycerol ethers or mixtures of those compounds. A specific example of an especially preferred solubilizer is a reaction product of castor oil and ethylene oxide, for example the commercial products Cremophor EL® or Cremophor RH 40®. Reaction products of castor oil and ethylene oxide have proved to be particularly good solubilizers that are tolerated extremely well by the eye. Another preferred solubilizer is tyloxapol. The concentration used depends especially on the concentration of the active ingredient. The amount added is typically sufficient to solubilize the active ingredient. For example, the concentration of the solubilizer is from 0.1 to 5000 times the concentration of the active ingredient.
Buffers, tonicity enhancing agents and preservatives different from quaternary ammonium salts may be used in an ophthalmic composition of the present invention as well.
Examples of buffer substances are acetate, ascorbate, borate, hydrogen carbonate/carbonate, citrate, gluconate, lactate, phosphate, propionate and TRIS (tromethamine) buffers. Tromethamine and borate buffer are preferred buffers. The amount of buffer substance added is, for example, that necessary to ensure and maintain a physiologically tolerable pH range. The pH range is typically in the range of from 5 to 9, preferably from 5.2 to 8.5 and more preferably from 5.5 to 8.2.
Tonicity enhancing agents are, for example, ionic compounds, such as alkali metal or alkaline earth metal halides, such as, for example, CaCl
2
, KBr, KCl, LiCl, Nal, NaBr or NaCl, or boric acid. Non-ionic tonicity enhancing agents are, for example, urea, glycerol, sorbitol, mannitol, propylene glycol, or dextrose. For example, sufficient tonicity enhancing agent is a
Fay Zohreh
Novartis AG
Wildman David E.
LandOfFree
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