Ketothiphen-containing ophthalmic composition

FIELD: medicine, ophthalmology.

SUBSTANCE: the suggested ophthalmic composition contains ketothiphen salt, nonionic agent to regulate tonicity in the quantity that total tonicity of composition should correspond to osmolarity of 210-290 mOsm, a conserving agent, not obligatory, either acid or foundation to achieve pH value being slightly acid and water, moreover, if the mentioned conserving agent is not available, the concentration of ketothiphen salt should correspond to 0.01-0.04 weight%, or if the mentioned conserving agent is available, the concentration of ketothiphen salt should correspond to 0.01-0.03 weight%. As ketothiphen salt the suggested composition contains ketothiphen fumarate; tonicity should be controlled with nonionic agent - glycerol.

EFFECT: more prolonged action of the composition suggested.

15 cl, 2 ex

 

The present invention relates to ophthalmic compositions comprising as pharmaceutical active substance ketotifen.

Ophthalmic composition containing ketotifen fumarate, already known, and it is available in the market. The advantage of the composition according to the present invention compared with the known compositions is that it includes significantly lower dose of the pharmaceutical active substance. As a result, this composition combines high efficacy with better tolerability. Another unexpected advantage is represented in this song is that this song can be sterilized without any noticeable decomposition of the pharmaceutical active substance or other components of the composition.

The composition according to the present invention includes a ketotifen salt in a concentration of from 0.01 to 0.04%, non-ionic agent for regulating toychest in such quantity that the total toychest composition corresponded osmolarity 210-290 mOsm, optional preservative, acid or base to bring the pH to slightly acidic and water.

Salt ketotifen preferably represents ketotifen fumarate. The concentration of ketotifen salt is preferably 0.03 to 0.04%, even more preferably of 0.025%. Non-ionic agent to regulate the Finance of toychest preferably represents glycerin. Non-ionic agent for regulating toychest preferably present in an amount such that the total toychest composition corresponded osmolarity 230-260 mOsm, more preferably 235-255 mOsm. If used, the glycerol, the concentration of glycerin is preferably from 1.5 to 2.5%. The preservative is present in a standard dosage forms, including several doses, but as a rule, there is no standard dosage forms, including one dose. If the preservative is present, it preferably represents benzylaniline. Typically, the amount of preservative is 0.005 to 0.02, preferably of 0.01%. To regulate the pH of the acid or base used in small quantities, such as 0.05 to 0.1%, preferably apply a small amount of 1 n sodium hydroxide solution, for example of 0.075% of such solution. The pH value of the composition is adjusted to a weakly acidic to optimize stability and portability, with a slightly acidic pH value preferably understand the value of pH from 4.4 to 5.8, more preferably a pH value of from 5 to 5.5, and most preferably a pH value of 5.3. Present in the composition of the water is usually water for injection.

A preferred composition according to the invention includes ketotifen fumarate in a concentration of 0.03 to 0.04%, glyceri is at a concentration of 2-2,5%, optional benzylaniline at a concentration of 0.005 to 0.02%, sodium hydroxide and water. Even more preferred composition comprises ketotifen fumarate in concentrations of 0.025%, glycerin at a concentration of 2,125%, not necessarily benzylaniline at a concentration of 0.01%, sodium hydroxide and water.

Ophthalmic composition according to the invention is used in the form of eye drops in the form containing the preservative standard dosage forms, including multiple doses, and containing no preservative standard dosage forms, including one dose. These eye drops should have a high therapeutic efficacy, in consequence of which they can be used for the treatment and temporary prevention of itching of the eye due to allergic conjunctivitis, in addition, they can be used to treat and prevent signs and symptoms of seasonal allergic conjunctivitis.

Despite the fact that the pharmaceutical active substance, i.e. ketotifen fumarate used in low concentration, its recommended dose is lower in comparison with known compositions based fumarata ketotifen. So, it is advisable to apply 1 drop of the composition according to the invention twice a day as opposed to the recommended dose is known from the prior art compositions 1-2 drops 4 times a day. When creating the invention of the unexpected I had ILSA the fact, the composition according to the invention can be used with extremely low levels of pharmaceutical active substance, i.e. fumarata ketotifen. In the claimed invention also unexpectedly found that a stabilizer, such as, for example, edetate sodium, can not be used.

Specified ophthalmic composition can be prepared by mixing the ingredients and filling the resulting mixture using for both operations known in the field of methods. Sterilization of the composition and primary packing can be done, for example, by using gamma irradiation, treatment with ethylene oxide, electron beam, by autoclaving or steam sterilization.

Example 1: Standard forms, including multiple doses:

fumarate ketotifen 0.25 mg(0,025%)

benzylaniline 0.10 mg (0,010%)

25 glycerin, 100%each holding 21.25 mg (2,125%)

sodium hydroxide, 1 BC to about 0.75 mg (~0,075%)

water for injection to 1.0 ml

Example 2: Standard forms, including one dose:

fumarate ketotifen 0.25 mg (0,025%)

glycerin, 100%each holding 21.25 mg (2,125%)

sodium hydroxide, 1 BC to about 0.75 mg (~0,075%)

water for injection to 1.0 ml

1. Ophthalmic composition intended for the treatment of allergic conjunctivitis, including as an active substance ketotifen salt in a concentration of from 0.01 to 0.04 wt.%, non-ionic the Gent to control toychest in such numbers, to the General toychest composition corresponded osmolarity 210-290 mOsm, and water, and the pH value of the composition is from 4.4 to 5.8.

2. The composition according to claim 1, in which the ketotifen salt is a fumarate ketotifen.

3. The composition according to claim 1, in which the salt concentration of ketotifen is from 0.03 to 0.04 wt.%.

4. The composition according to claim 1, in which the non-ionic agent for regulating toychest represents glycerin.

5. The composition according to claim 4, in which the concentration of glycerin is from 1.5 to 2.5%.

6. The composition according to claim 1, optionally containing a preservative.

7. The composition according to claim 6, in which the preservative is benzylaniline.

8. The method of treatment of allergic conjunctivitis, including introduction to a subject suffering from allergic conjunctivitis or susceptible to allergic conjunctivitis, an effective amount of the ophthalmic composition containing as active substance ketotifen salt in a concentration of from 0.01 to 0.04 wt.%, non-ionic agent for regulating toychest in such quantity that the total toychest composition corresponded osmolarity 210-290 mOsm, and water, and the pH value of the composition is from 4.4 to 5.8.

9. The method of claim 8, where the ketotifen salt is a fumarate ketotifen.

10. The method of claim 8, where the salt concentration of ketotifen comp is made from 0.03 to 0.04 wt.%.

11. The method of claim 8, where the non-ionic agent for regulating toychest represents glycerin.

12. The method according to claim 11, where the concentration of glycerin is from 1.5 to 2.5%.

13. The method of claim 8, where the ophthalmic composition further comprises a preservative.

14. The method according to item 13, where the preservative is benzylaniline.

15. The method of claim 8, where the treatment is treatment or prevention of signs and symptoms of seasonal allergic conjunctivitis.



 

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EFFECT: more prolonged action of the composition suggested.

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