Ophthalmic carrier solution

• US 6,071,958 A
• Filed: 10/27/1997
• Issued: 06/06/2000
• Est. Priority Date: 03/14/1997
• Status: Expired due to Term

• Current Assignee: Arturo Jimenez-Bayardo, Arturo Jiminez Bayardo
• Original Assignee: Arturo Jimenez-Bayardo
• Inventors: Jimenez-Bayardo, Arturo, Cuevas-Pacheco, Gregorio, Garcia-Armenta, Maria Elena, Diaz-Perez, Juan Manuel, Tornero-Montano, Jose Ruben
• Primary Examiner(s): FAY, ZOHREH A
• Application Number:
  US08/958,681
• Time in Patent Office: 953 Days
• Field of Search: 514/535, 514/772, 514/912
• US Class Current: 514/535
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears

Abstract

This invention refers to a matter composition of the type used in the treatment of ophthalmic ailments and specifically refers to an ophthalmic carrier solution based on surface-active, emulsifying, antibacterial, antioxidant, etc. Agents which form a carrier that enwraps or masks an active ingredient such as sodium dyclophenac or other antibiotic agents such as tobracin, gentamicin or timolol sulfate, with the aim of avoiding the problems caused by the topical application of the mentioned active ingredients, such as pain, a burning sensation, irritation and other annoyances for the user.

Claims

1. An ophthalmic carrier solution for use in the topical application of ophthalmic use compounds, said carrier solution comprising the following components:

10.20% by weight of polyoxyl stearate 40;

0.15% by weight of dehydrated disodium edetate;

1.03% by weight of sodium chloride;

0.14% by weight of boric acid;

0.32% by weight of sorbic acid;

0.06% by weight of sodium bisulfite, and

88.00% by weight of distilled water.

3. An ophthalmic composition for topical use, which comprises:

68.16% by weight of the carrier solution of claim 1;

0.10% by weight of an active agent which is an anti-inflammatory agent or an antibiotic; and

distilled water to 100% by weight of the solution.

4. An ophthalmic composition for topical use according to claim 3, wherein said anti-inflammatory agent is sodium dyclophenac.

5. A process for preparing an ophthalmic composition for topical use which consists of an ophthalmic carrier solution according to claim 1 and an active ingredient which is sodium dyclophenac or an antibiotic which is tobramicin or gentamicin, said process consisting of the following steps:

i) emptying a predetermined amount of distilled water into a stainless steel container;

shaking said container at an approximate speed of between 580 and 620 rpm;

adding the sodium dyclophenac slowly, maintaining the shaker turned-on for approximately 13 to 17 minutes;

the pH at the end of the shaking time being 7.25±

0.1. The conductivity after the shaking time being 0.734 mS/cm (±

1.0 mS/cm); and

the temperature after the shaking time being between 21 and 25°

C.;

ii) transferring the sodium dyclophenac solution obtained in the previous step, into a tank containing a predetermined volume of the carrier solution prepared according to the process of claim 2, maintaining a shaker speed of 800±

50 rpm for approximately 13 to 17 minutes;

iii) heating the solution of (ii) with distilled water to a temperature of 21 to 25°

C. and with an approximate pH of between 6.00 and 6.50, the conductivity of the distilled water being no greater than 0.002 mS/cm;

iv) shaking the solution for a time of 2 hours±

5 minutes; and

v) adjusting the pH at the end of the shaking time to a value between 6.83 and 6.85, the conductivity after the shaking time being 11.77 mS/cm±

0.5 mS/cm and the temperature after the shaking time being approximately 21-25°

C.

9. An ophthalmic composition according to claim 3, wherein the antibiotic is tobramicin, gentamicin or timolol sulfate.

2. A process for preparing an ophthalmic carrier solution, said carrier solution comprising the following components:

polyoxyl stearate 40, dehydrated disodium edetate, sodium chloride, boric acid, sorbic acid, sodium bisulfite and distilled water, said process comprising the following steps;

a) Heating a predetermined volume of distilled water to an approximate temperature of 69 to 71°

C.;

adjusting the pH to 6.25 (±

0.25) and maintaining a conductivity no greater than 0.002 mS/cm;

b) Emptying the heated distilled water into a stainless steel tank;

c) Adding the polyoxyl stearate 40 slowly to the heated distilled water;

maintaining the shaker operating for a time of between 27 and 33 minutes, the pH at the end of the shaking time being approximately between 6.0 and 6.2, the conductivity after the shaking time being 0.12 mS/cm (±

0.05 mS/cm), and the temperature after the shaking time being between 63 and 67°

C.;

d) Adding the disodium edetate to H₂ O slowly to the tank, maintaining the shaker operating for a time of between 13 and 17 minutes at a speed of 750-850 rpm, the pH at the end of the shaking time being within a range of 5.54 to 5.58, the conductivity after the shaking time being between 0.679 and 0.681 mS/cm, and the temperature after the shaking time being between 59 and 61°

C.;

e) Adding the sodium chloride slowly to the tank, maintaining the shaker at a speed of between 750 and 850 rpm during an approximate time of 13 to 17 minutes;

the pH at the end of the shaking time being within a range of 5.20 to 5.22, the conductivity after the shaking time being between 15.32 and 17.32 mS/cm, and the temperature after the shaking time being between 55 and 57°

C.;

f) Adding the boric acid slowly to the tank, maintaining the shaker at a speed of between 750 and 850 rpm during an approximate time of 13 to 17 minutes;

the pH at the end of the shaking time being within a range of 5.20 to 5.24, the conductivity after the shaking time being between 11.64 and 13.64 mS/cm, and the temperature after the shaking time being between 55 and 57°

C.;

g) Cooling to approximately 49-51°

C.;

h) Adding the sorbic acid slowly to the tank, maintaining the shaker at a speed of between 750 and 850 rpm during an approximate time of 13 to 17 minutes;

the pH at the end of the shaking time being within a range of 3.84 to 3.88, the conductivity after the shaking time being between 15.82 and 15.92 mS/cm, and the temperature after the shaking time being between 46 and 48°

C.;

i) Adjusting the pH with sodium hydroxide as soon as possible to a value of 7.15±

0.1, maintaining the shaker at a speed of between 750 and 850 rpm during an approximate time of 9 to 11 minutes;

the conductivity after the shaking time being between 16.06 and 18.06 mS/cm, and the temperature after the shaking time being between 44.5 and 45.5°

C.;

j) Cooling to approximately 29-31°

C.;

k) Adding the sodium bisulfite slowly to the tank, maintaining the shaker at a speed of between 750 and 850 rpm during an approximate time of 13 to 17 minutes;

the pH at the end of the shaking time being 7.0±

0.1, the conductivity after the shaking time being 16.97 mS/cm±

1.0 mS/cm), and the temperature after the shaking time being between 25 and 29°

C.

8. A process for preparing an ophthalmic carrier solution according to claim 2, which consists essentially of the enumerated steps.

6. An ophthalmic carrier solution consisting essentially of the following components in aqueous solution:

10.20% by weight of polyoxyl stearate 40;

0.15% by weight of dehydrated disodium edetate;

1.03% by weight of sodium chloride;

0.14% by weight of boric acid;

0.32% by weight of sorbic acid; and

0.06% by weight of sodium bisulfite.

7. An ophthalmic composition for topical use consisting essentially of the carrier solution of claim 6 and an active ingredient in an amount sufficient to effect treatment of an eye.