WO2006103198A2

WO2006103198A2 - Ophthalmic composition

Info

Publication number: WO2006103198A2
Application number: PCT/EP2006/061013
Authority: WO
Inventors: Günther Bellmann; Gudrun Claus-Herz
Original assignee: Dr. Gerhard Mann Chem.-Pharm. Fabrik Gmbh
Priority date: 2005-03-31
Filing date: 2006-03-23
Publication date: 2006-10-05
Also published as: RU2007139145A; DE202005005094U1; RU2397776C2; EP1863509A2; WO2006103198A3

Abstract

The invention relates to an ophthalmic composition containing, in relation to the total weight of the composition, the following elements: ≥ 0.02 wt. % to ≤ 2 wt. % of extract(s) and/or tincture(s) that can be obtained from the plant and/or plant parts of Euphrasia officinalis, and between ≥ 0.2 wt. % and ≤ 2 wt. % of sodium chloride.

Description

DR. GERHARD MAN CHEM.-PHARM. GMBH

Brunsbüttel dam 165 - 173

13581 Berlin

Ophthalmic composition

The present invention relates to an ophthalmic composition. The ophthalmic composition can be used, for example, for the treatment of diseases or conditions of the eye or the organs or tissues surrounding or related to the eye. It is well known that the eye is constantly exposed to high loads. In particular, the wearing of contact lenses or a strained visual behavior such as long-lasting work in front of the screen can lead to over-exertion and irritation of the eye.

For administration in irritated, dry or inflamed eyes, compositions in the form of eye drops are commonly used. The compositions typically comprise solutions incorporating the active ingredients, for example herbal extracts, essential oils or zinc compounds.

These solutions are often added to other ingredients, preservatives and antimicrobial substances that cause allergies, cause irritation or sensitization to the ingredients and thus are not suitable for long-term use. A disadvantage also arises from the fact that the solutions can produce incompatibilities.

From EP 1 417 970 A2 a solution is known which discloses the use of dilute seawater as a basis for avoiding incompatibilities. A disadvantage of this type of preparation, however, is that the salt composition of the sea does not correspond to that of the eye. A significant disadvantage also results from the fact that even such solutions themselves can frequently produce itching, burning or other unpleasant side effects on contact with the eye.

It is the object of the present invention to provide a composition which overcomes at least one of the aforementioned disadvantages of the prior art. In particular, it is the object of the present invention to provide a composition which is suitable for use in irritated, dry or inflamed eyes. The object is achieved by an ophthalmic composition, the composition comprising, based on the total weight of the composition, the following substances:

Extract (s) and / or tincture (s) obtainable from the plant and / or parts of plants of Euphrasia officinalis in the range of> 0.02 wt .-% to <2 wt .-%, and

- Sodium chloride in the range of> 0.2 wt .-% to <2 wt .-%.

Advantageous embodiments of the ophthalmic composition according to the invention are specified in the subclaims.

Surprisingly, it has been found that administration of the ophthalmic composition according to the invention to or into the eye causes diseases or conditions of the eye or the tissues or organs surrounding or related to the eye, such as redness, swelling, injuries, inflammations such as conjunctivitis and eyelid inflammation, overexertion or can affect dry eyes positively.

Advantageously, the ophthalmic compositions according to the invention are particularly well tolerated. A further advantage is that the ophthalmic compositions according to the invention lead to no or only a very slight irritation or discomfort when applied to the eye.

For the purposes of the present invention, the term "extract" is understood to mean extracts of liquid or dry nature of plants or parts thereof obtained, for example, using water. Preferred are dry-type extracts, which are preferably obtainable from the fresh or dried aerial parts of Euphrasia officinalis such as leaves, flowers and / or stems. Particularly preferred are extracts of the whole herb of Euphrasia officinalis, also referred to as Herba Euphrasiae.

For the purposes of the present invention, the term "Euphrasia officinalis" (eyebright) is understood to mean all the species of the genus Euphrasia usually designated by this term, for example Euphrasia stricta, Euphrasia montana and / or Euphrasia rostkoviana.

For the purposes of this invention, the term "tincture" refers to extracts of plants or parts thereof which are prepared using solvents such as water and / or alcohols such as ethanol, vegetable pressed juices or solutions of dried plants in a solvent mixture such as an alcohol-water mixture. Mixture understood.

For the purposes of this invention, the term "substance" is to be understood as meaning the substances having the composition, in particular extract (s) and / or tincture (s) obtainable from the plant and / or from plant parts of Euphrasia officinalis, sodium chloride, boric acid, sodium hydroxide solution , Polyvinyl pyrrolidone (s), polysorbate (s), preservatives such as cetrimide and / or benzododecinium chloride.

In preferred embodiments, the ophthalmic composition comprises, based on the total weight of the composition, the following substances:

Extract (s) and / or tincture (s) obtainable from the plant and / or from plant parts of Euphrasia officinalis in the range from> 0.03% by weight to <0.5% by weight, preferably> 0.04 Wt .-% to <0.2 wt .-%, preferably> 0.05 wt .-% to

<0.1 wt .-%, and / or

Sodium chloride in the range of> 0.4% by weight to <1.5% by weight, preferably> 0.5% by weight to <1% by weight, preferably> 0.7% by weight to <0.8% by weight. Unless stated otherwise, the weight contents of the respective substances are chosen so that the total weight of the respective substances does not exceed 100% by weight, based on the total composition.

In particular, the selection and weight contents of the substances contained make it possible for the ophthalmic composition to be used safely, in particular over a relatively long period of time.

In particular, the preferred concentration of sodium chloride can also contribute to improved compatibility of the composition. In preferred embodiments of the inventive composition, the sodium chloride content is adjusted to the salinity of the tear fluid in the eye. It is of particular advantage that the content of the composition according to the invention of sodium chloride is matched to the content of the composition of further salts, so that the compatibility of the composition is not reduced by a salt content exceeding the physiological salt concentrations of the eye.

The composition according to the invention may also comprise further components, for example preservatives, preferably selected from the group comprising cetrimide and / or benzododecinium chloride. "Cetrimide" is the usual name for N-cetyl-N, N, N-trimethyl-ammonium bromide, "benzododecinium chloride" the usual name for N-benzyl-N-dodecyl-N, N-dimethyl-ammonium chloride. It is preferred that the ophthalmic composition, based on the total weight of the composition, preservatives in the range of> 0 wt .-% to <0.05 wt .-%, preferably in the range of> 0 wt .-% to <0, 01 wt .-%, preferably in the range of> 0 wt .-% to <0.005 wt .-% comprises. In preferred embodiments, the composition comprises less than 0.01% by weight, based on the total weight of the Composition, cetrimide and / or benzododecinium chloride. In particularly preferred embodiments, the composition is free of preservatives.

In advantageous embodiments, the composition has a pH in the range of 6.8 to 7.6, preferably in the range of 7.0 to 7.4. Preferably, the pH of the ophthalmic composition with acids and / or bases, preferably with boric acid and / or sodium hydroxide, with 1 N sodium hydroxide solution is particularly advantageous adjusted. In preferred embodiments, the composition comprises boric acid in the range from> 0.2% by weight to <0.4% by weight, preferably in the range from> 0.3% by weight to <0.35% by weight, preferably 0.31% by weight, based on the total weight of the composition. In further preferred embodiments, the composition comprises 1 N sodium hydroxide solution in the range from> 0.1% by weight to <0.4% by weight, preferably in the range from> 0.17% by weight to <0.28% by weight. %, based on the total weight of the composition.

An advantage of the ophthalmic composition according to the invention is realized in that the composition leads to no or very little irritation during the application. Furthermore, irritations in contact with the eye can advantageously be completely or almost completely avoided. This means a very big advantage, since in the application of solutions to the eye, there is often a very unpleasant feeling of "burning" on the eye.

The ophthalmic composition may be solid, liquid and / or gel. The composition according to the invention is particularly suitable for a topical ophthalmic application, for example for application to the surface of the eye or to the areas directly surrounding the eye. Preferably, the composition is in the form of an aqueous solution. In particularly preferred embodiments, the composition is suitable to be administered in dosage forms selected from the group comprising eye drops and / or eye baths to the eye.

The ophthalmic composition expediently comprises boric acid, sodium hydroxide solution and / or auxiliaries, preferably selected from the group consisting of viscosity-increasing additives, preferably polyvinylpyrrolidone (s), preferably povidone 25, and / or solubilizer, preferably polysorbate (s), more preferably polyoxyethylene sorbitan monooleate (Polysorbate 80), on.

In preferred embodiments, the ophthalmic composition comprises extract (s) and / or tincture (s) obtainable from the plant and / or from plant parts of Euphrasia officinalis, sodium chloride, boric acid, caustic soda, polyvinylpyrrolidone, polysorbate, cetrimide and / or benzododecinium chloride.

Preferably, the composition has no further salts usually contained in ophthalmic preparations, in particular no zinc sulfate. Advantageously, this can be used to avoid, for example, hypersensitivity, which is often caused by zinc sulfate.

In preferred embodiments, the ophthalmic composition comprises, based on the total weight of the composition, the following: a. 0.05% by weight of extract obtainable from the plant and / or from plant parts of Euphrasia officinalis; b. 0.73 wt .-% sodium chloride. In particularly preferred embodiments, the ophthalmic composition comprises, based on the total weight of the composition, the following substances: a. 0.1% by weight of extract obtainable from the plant and / or from plant parts of Euphrasia officinalis; b. 0.73 wt .-% sodium chloride.

In further preferred embodiments, the ophthalmic composition comprises, based on the total weight of the composition, the following substances: a. 0.05% by weight of extract obtainable from the plant and / or from plant parts of Euphrasia officinalis; b. 0.73% by weight of sodium chloride; c. From 0.001% to 0.01% by weight of cetrimide.

In still further preferred embodiments, the ophthalmic composition comprises, based on the total weight of the composition, the following: a. 0.05% by weight of extract obtainable from the plant and / or from plant parts of Euphrasia officinalis; b. 0.73% by weight of sodium chloride; c. 0.001% to 0.01% by weight of benzododecinium chloride.

In preferred embodiments, the ophthalmic composition is free of chamomile extract (s), camomile tincture (s) and / or essential oils such as lavender oil, orange blossom oil and / or rose oil. This realizes a further advantage of the composition according to the invention over conventional preparations, since chamomile in particular can cause allergies. In addition, essential oils have a harmful potential, often lead to allergies, sensitization or irritation and can, for example, trigger photoallergic reactions. Of particular advantage is that the ophthalmic composition of the invention for the preparation of a cosmetic and / or pharmaceutical agent for the treatment of diseases or conditions of the eye or surrounding or related organs or tissues, in particular redness, swelling, injuries, inflammations such as conjunctiva - and Lidrandentzündungen, overexertion, dry eyes, and / or for the prevention of Augenkatarrh and / or Augenschleimfluß is usable.

The ophthalmic composition is preferably usable as a medical product within the meaning of Section 3 (1) of the Medical Devices Act.

The ophthalmic composition of the present invention is particularly advantageously useful in long-term use in diseases or conditions of the eye or organs or tissues surrounding or related to the eye, especially redness, swelling, injury, inflammation such as conjunctivitis, eyestrain, dry eyes, and / or for the prevention of ocular catarrh and / or eye mucus flow. Due to the beneficial substances of the ophthalmic composition, the ophthalmic composition is safe for use in the preventive prevention of reddened or irritated eyes, as well as existing redness or dry eyes.

It was surprisingly found that within a few hours, a significant improvement in the symptoms such as redness, swelling, injury or inflammation can be effected.

By the beneficial substances of the ophthalmic preparation, these may be used as agents for the treatment of diseases or conditions of the eye or of the eye surrounding or related organs or tissues, in particular in the form of eye drops and / or eye bath, are used.

Preferably, the ophthalmic preparation is administrable in the form of drops for eyes or usable in the form of an eye bath for rinsing.

For use, the composition of the invention is preferably filled into suitable containers, which are preferably designed so that the contents can be applied to the eye, for example eye drop bottles, preferably based on polyethylene, preferably LDPE (low density polyethylene, low density polyethylene), or HDPE (High density polyethylene, high density polyethylene). The filling volume of the eye-drop bottles is preferably in the range of 5 ml to 10 ml. In further preferred embodiments of the ophthalmic composition, this is for use as eye bath in containers preferably based on LDPE contained.

In preferred embodiments of the ophthalmic composition, it is in the form of eye drops in a single dose ophthalmic solution, preferably based on LDPE. In particularly preferred embodiments of the ophthalmic composition, it is free of preservatives in the form of eye drops in a single dose ophthalmic solution.

It goes without saying that the ophthalmic composition is preferably sterile for use. Preferably, sterile materials are used under sterile conditions or the composition is sterilized after incorporation of the materials or the ophthalmic composition is prepared under so-called aseptic conditions resulting in a sterile product.

The following embodiments serve only to illustrate the invention and are not limiting. example 1

Eye drops comprising 100% by weight:

- 0.05% by weight of dry extract from Euphrasia officinalis;

0.73% by weight of sodium chloride;

2.0% by weight of povidone 25.

The eye drops were sterilized and filled into single dose ophthalmos.

Example 2

Eye drops comprising 100% by weight:

0.1% w / w dry extract from Euphrasia officinalis;

0.73% by weight of sodium chloride;

2.0% by weight of povidone 25.

The eye drops were sterilized and filled into single dose ophthalmos.

Claims

Ophthalmic composition, characterized in that the composition, based on the total weight of the composition, comprises the following substances:

- Sodium chloride in the range of> 0.2 wt .-% to <2 wt .-%.

Ophthalmic composition according to claim 1, characterized in that the composition comprises, based on the total weight of the composition, the following substances:

<0.1 wt .-%, and / or

Sodium chloride in the range of> 0.4% by weight to <1.5% by weight, preferably> 0.5% by weight to <1% by weight, preferably> 0.7% by weight to <0.8% by weight.

3. Ophthalmic composition according to claim 1 or 2, characterized in that the composition preservative, preferably selected from the group comprising cetrimide and / or benzododecinium chloride comprises.

4. Ophthalmic composition according to one of the preceding claims, characterized in that the composition, based on the total weight of the composition, preservatives in the range of> 0 wt .-% to <0.05 wt .-%, preferably in the range of> 0 Wt .-% to <0.01 wt .-%, preferably in the range of> 0 wt .-% to <0.005 wt .-% comprises.

5. Ophthalmic composition according to one of the preceding claims, characterized in that the composition has a pH in the range of 6.8 to 7.6, preferably in the range of 7.0 to 7, 4.

6. Ophthalmic composition according to one of the preceding claims, characterized in that the composition is solid, liquid and / or gel.

7. Ophthalmic composition according to one of the preceding claims, characterized in that the composition is in the form of an aqueous solution.

8. Ophthalmic composition according to one of the preceding claims, characterized in that the composition boric acid, sodium hydroxide and / or auxiliaries, preferably selected from the group comprising viscosity-increasing additives, preferably polyvinylpyrrolidone (s), and / or solubilizers, preferably polysorbate (s), having.

9. Ophthalmic composition according to one of the preceding claims, characterized in that the composition extract (s) and / or tincture (s) obtainable from the plant and / or from plant parts of Euphrasia officinalis, sodium chloride, boric acid, caustic soda, polyvinylpyrrolidone (s) , Polysorbate (s), cetrimide and / or benzododecinium chloride.

10. Ophthalmic composition according to one of the preceding claims, characterized in that the composition, based on the total weight of the composition, comprises the following substances: a. 0.05% by weight of extract obtainable from the plant and / or from plant parts of Euphrasia officinalis; b. 0.73 wt .-% sodium chloride.

11. Ophthalmic composition according to one of the preceding claims, characterized in that the composition, based on the total weight of the composition, comprises the following substances: a. 0.1% by weight of extract obtainable from the plant and / or from plant parts of Euphrasia officinalis; b. 0.73 wt .-% sodium chloride.

Ophthalmic composition according to any one of the preceding claims, characterized in that the composition, based on the total weight of the composition, comprises the following substances: a. 0.05% by weight of extract obtainable from the plant and / or from plant parts of Euphrasia officinalis; b. 0.73% by weight of sodium chloride; c. From 0.001% to 0.01% by weight of cetrimide.

An ophthalmic composition according to any one of the preceding claims, characterized in that the composition, based on the total weight of the composition, comprises the following substances: a. 0.05% by weight of extract obtainable from the plant and / or from plant parts of Euphrasia officinalis; b. 0.73% by weight of sodium chloride; c. 0.001% to 0.01% by weight of benzododecinium chloride.

14. Ophthalmic composition according to one of the preceding claims, characterized in that the composition is free of chamomile extract (s), chamomile (s) and / or essential oils such as lavender oil, orange blossom oil and / or rose oil.

15. Use of an ophthalmic composition according to one of the preceding claims for the preparation of a cosmetic and / or pharmaceutical agent for the treatment of diseases or conditions of the eye or of the eye surrounding or related organs or tissues, in particular redness, swelling, injuries, inflammations such Conjunctivitis and eyelid inflammation, overexertion, dry eyes, and / or for the prevention of ocular catarrh and / or mucus.

16. A composition for the treatment of diseases or conditions of the eye or of the organs or tissue surrounding or related to the eye, in particular in the form of eye drops and / or eye bath, comprising substances according to one of the preceding claims.

17. Eindose Ophtiole containing an ophthalmic composition according to any one of the preceding claims.

18. Eindose Ophtiole according to claim 17, characterized in that the ophthalmic composition is free of preservatives.