Self-preserved antibacterial nasal, inhalable, and topical ophthalmic preparations and medications

• US 20050080043A1
• Filed: 09/08/2004
• Published: 04/14/2005
• Est. Priority Date: 09/20/2000
• Status: Abandoned Application

• Current Assignee: Lee Shahinian Jr
• Original Assignee: Lee Shahinian Jr
• Inventors: Shahinian, Lee Jr.
• Application Number:
  US10/936,948
• Publication Number:
  US 20050080043A1
• Time in Patent Office: Days
• US Class Current: 514/57
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears

Abstract

Self-preserved nasal, inhalable and topical ophthalmic preparations and medications which destroy, inhibit or therapeutically significantly limit microbial growth within said preparations or medications. The nasal, inhalable, and topical ophthalmic preparations and medications have been found to be stable without buffer and maintain a stable pH at pH 3.5 or lower. They are well tolerated by patients.

Claims

1. A method for preparation of a topical ophthalmic, nasal or inhalable self-preserved solution comprising steps of:

a) preparing a formulation comprising

a pharmaceutically acceptable excipient or additive selected from the group consisting of dextrose, polyethylene glycol (PEG), hydroxypropyl methylcellulose (HPMC), sodium chloride, potassium chloride, calcium chloride, magnesium chloride, phosphoric acid, disodium edetate, bicarbonate, phosphate, povidone, carboxymethylcellulose, hydroxyethylcellulose, methylcellulose, microcrystalline cellulose, other cellulose derivatives, glycerin, polyvinyl alcohol, dextran 40, dextran 70, mannitol, gelatin, polyols, polysorbate 80, propylene glycol, zinc sulfate, poloxamer 188, 282, 407, ephedrine hydrochloride, naphazoline hydrochloride, oxymetazoline hydrochloride, phenylephrine hydrochloride, tetrahydrozoline hydrochloride, xylometazoline hydrochloride, lecithin, oleic acid and sorbitan, pheniramine maleate, pyrilamine maleate, antazoline phosphate, glycine, camphor, eucalyptol, menthol, benzyl alcohol, lavender oil, tyloxapol, bornyl acetate, phenylethyl alcohol, alone or in admixture; and

a buffering agent present from 0% to 0.01%; and

b) adjusting pH of said formulation to from about pH 1.5 to pH about 2.5.

2. The method of claim 1, wherein the pH is adjusted to about 2.0 to about 2.5.

3. The method of claim 2, wherein the pH is adjusted about 2.5.

4. The method of claim 3, wherein the solution is used as a topical eye preparation for administration of a pharmaceutical agent, artificial tear, contact lens solution or eye irrigating solution.

5. The method of claim 4, wherein the pharmaceutical agent is selected from the group consisting of an analgesic, anti-inflammatory, astringent, antihistamine, mast cell stabilizer, fluorescein, miotic, mydriatic, antibiotic, antiviral, antifungal, vasoconstricting agent, antiglaucoma medication, hypertonicity agent, decongestant, bronchodilator and topical anesthetic.

6. The method of claim 5, wherein the anesthetic is proparacaine, tetracaine, lidocaine, benoxinate, and bupivicaine.

7. The method of claim 1, wherein the anesthetic is proparacaine, tetracaine, lidocaine, benoxinate, and bupivicaine.

8. The method of claim 1, wherein the additives are at least two of:

dextrose, polyethylene glycol, hydroxypropyl methylcellulose, EDTA and sodium citrate.

9. The method of claim 1 wherein the buffering agent is present at 0%.

10. A self-preserved, preservative free topical ophthalmic, inhalable or nasal formulation comprising:

(a) a pharmaceutically acceptable excipient or additive selected from the group consisting of dextrose, polyethylene glycol (PEG), hydroxypropyl methylcellulose (HPMC), sodium chloride, potassium chloride, calcium chloride, magnesium chloride, phosphoric acid, disodium edetate, bicarbonate, phosphate, povidone, carboxymethylcellulose, hydroxyethylcellulose, methylcellulose, microcrystalline cellulose, other cellulose derivatives, glycerin, polyvinyl alcohol, dextran 40, dextran 70, mannitol, gelatin, polyols, polysorbate 80, propylene glycol, zinc sulfate, poloxamer 188, 282, 407, ephedrine hydrochloride, naphazoline hydrochloride, oxymetazoline hydrochloride, phenylephrine hydrochloride, tetrahydrozoline hydrochloride, xylometazoline hydrochloride, lecithin, oleic acid and sorbitan, pheniramine maleate, pyrilamine maleate, antazoline phosphate, glycine, camphor, eucalyptol, menthol, benzyl alcohol, lavender oil, tyloxapol, bornyl acetate, phenylethyl alcohol, alone or in admixture;

(b) an acid or base to adjust pH to about 2.3 to about 2.7;

(c) said formulation being substatntially free of buffer.

11. The formulation of claim 10 wherein the excipient, additive or a pharmaceutical agent is present in amount from 0.001 to about 8%.

12. The formulation of claim 10 comprising about 1-8% of polyethylene glycol, about 0.1% to about 0.3% of hydroxypropyl methylcellulose, and purified water, wherein the pH is adjusted to about pH 2.5

13. The formulation of claim 10 comprising about 8% of polyethylene glycol, about 0.3% of hydroxypropyl methylcellulose, and purified water, wherein the pH is adjusted to about pH 2.5.

14. The formulation of claim 10 wherein the pH is adjusted with an acid or a base.

15. The formulation of claim 14 wherein the acid is hydrochloric acid or sulphuric acid and wherein the base is sodium hydroxide or ammonium hydroxide.

16. The formulation of claim 10 additionally comprising about 2% to 6% of dextrose.

17. The formulation of claim 10 comprising about 4% of dextrose, about 1% of polyethylene glycol, and about 0.3% of hydroxypropyl methylcellulose.

18. The formulation of claim 17 wherein the pH is adjusted with an acid or a base.

19. The formulation of claim 17 wherein the acid is hydrochloric acid, phosphoric acid or sulphuric acid and wherein the base is sodium hydroxide or ammonium hydroxide.