A TOPICAL OCULAR SUSPENSION OF ANTIOXIDANTS

Abstract

A topical ocular suspension for treating or preventing age related macular degeneration (ARMD) comprising of one or more antioxidants and at least one pharmaceutically acceptable excipient, wherein the antioxidant is a carotenoid selected from lutein, zeaxanthin or a combination thereof.

Claims

1. A topical ocular suspension for treating or preventing age related macular degeneration (ARMD) comprising of one or more antioxidants and at least one pharmaceutically acceptable excipient, wherein the antioxidant is a carotenoid selected from lutein, zeaxanthin or a combination thereof.

2. The topical ocular suspension of claim 1, wherein the concentration of lutein is about 0.03% to 6.0% w/v.

3. The topical ocular suspension of claim 1, wherein the concentration of zeaxanthin is about 0.03% to 6.0% w/v.

4. The topical ocular suspension of claim 1 further comprises a suspending agent.

5. The topical ocular suspension of claim 1 wherein the suspending agent is a cellulose derivative, gum, Polyvinyl Alcohol (PVA), Povidone K30, Povidone K 90, Polycarbophil, Polyethylene Glycol (PEG), Carbomer or a combination thereof.

6. The topical ocular suspension of claim 1 wherein the cellulose derivative is Hydroxypropyl methyl cellulose (HPMC), Hydroxypropyl cellulose (HPC), Methyl Cellulose, Carboxy methylcellulose sodium, Carboxyethyl cellulose sodium, Hydroxyethyl cellulose or a combination thereof.

7. The topical ocular suspension of claim 1 wherein the gum is Gaur gum, Gellan gum, Xanthan gum or a combination thereof.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0007] As described herein, the disclosure provides a topical ocular suspension that releases the drug at a predetermined rate for an extended period of time thereby maintaining a steady concentration of antioxidants in the aqueous and vitreous humor, thereby increasing the macular pigment optical density (MPOD).

[0008] The topical ocular suspension for treating or preventing age related macular degeneration (ARMD) described herein comprises one or more antioxidants and at least one pharmaceutically acceptable excipient. The antioxidant according to the disclosure herein is a carotenoid selected from lutein, zeaxanthin or a combination thereof. The concentration of lutein in the topical ocular suspension is about 0.03% to 6.0% w/v and the concentration of zeaxanthin in the topical ocular suspension is about 0.03% to 0.06%. The topical ocular suspension further comprises a suspending agent. The suspending agent is selected from the group comprising of cellulose derivatives, gums, Polyvinyl Alcohol (PVA), Povidone K30, Povidone K 90, Polycarbophil, Polyethylene Glycol (PEG), Carbomer or a combination thereof. The cellulose derivative is Hydroxypropyl methyl cellulose (HPMC), Hydroxypropyl cellulose (HPC), Methyl Cellulose, Carboxy methylcellulose sodium, Carboxyethyl cellulose sodium, Hydroxyethyl cellulose or a combination thereof. The gum is Gaur gum, Gellan gum, Xanthan gum or a combination thereof.

[0009] In one embodiment, the topical ocular suspension comprises the antioxidants lutein and zeaxanthin, a suspending agent, a preservative and pH adjusting agents.

Example: 1

[0010] Lutein+Zeaxanthin Ocular Suspension

TABLE-US-00001 S. No Ingredient mg/mL 1 Lutein 0.03-6 mg 2 Zeaxanthin 0.03-6 mg 3 Hydroxy Propyl Methyl Cellulose (HPMC) 3 mg-9 mg 4 Benzalkonium Chloride 0.001% 5 Water for Injection q.s 6 Hydrochloride acid/sodium hydroxide q.s

[0011] Process: Required quantities of lutein and zeaxanthin are mixed with HPMC and Benzalkonium Chloride was added as a preservative and mixed with water for injection in a homogenizer. The suspension so formed is made up to the volume with water for injection and aseptically filled into containers, and sealed.

[0012] In another embodiment, the topical ocular suspension comprises the antioxidants lutein, a suspending agent, a preservative and pH adjusting agents.

Example: 2

[0013] Lutein Ocular Suspension

TABLE-US-00002 S. No Ingredient mg/mL 1 Lutein 0.03-6 mg 2 Xanthan gum 0.6% 3. Disodium Edetate 0.13% 4. Phenyl Mercuric Nitrate 0.002% 5. Sodium Chloride 0.03% 6. Hydrochloric Acid/Sodium Hydroxide q.s 7. Water for Injection q.s

[0014] Process: Required quantity of Lutein is mixed with Xanthan gum and Disodium EDTA. To the mixture so obtained, Phenyl Mercuric Nitrate was added as a preservative and sodium chloride as Osmolarity adjusting agent and mixed with water for injection in a homogenizer. The suspension so formed is made up to the volume with water for injection & the pH was adjusted using hydrochloric acid/sodium hydroxide and aseptically filled into containers, and sealed.

[0015] In another embodiment of the invention, the topical ocular suspension comprises zeaxanthin and pharmaceutical excipients.

Example: 3

[0016] Zeaxanthin Ocular Suspension

TABLE-US-00003 S. No Ingredient mg/mL 1 Zeaxanthin 0.03-6 mg 2 Tyloxapol 0.3% 3 Sodium citrate 0.5-5 mg 4 Citric Acid 0.3-1.5 mg 5 Benzalkonium chloride 0.001% 6 Hydrochloric Acid/Sodium Hydroxide q.s 7 Water for Injection q.s

[0017] Process: Required quantity of Zeaxanthin is mixed with Tyloxapol, sodium citrate & citric acid. To the mixture so obtained, Benzalkonium chloride was added as a preservative and mixed with water for injection in a high shear mixer. The suspension so formed is made up to the volume with water for injection & the pH was adjusted using hydrochloric acid/sodium hydroxide and aseptically filled into containers, and sealed.

Example: 4

[0018] Lutein+Zeaxanthin Ocular Suspension

TABLE-US-00004 S. No Ingredient mg/mL 1 Lutein 0.03-6 mg 2 Zeaxanthin 0.03-6 mg 3 Polyethylene Glycol (PEG) 400 1-5% 4 Polyethylene Glycol (PEG) 4000 3-9% 5 Sodium Chloride 0.05% 6 Phenyl Mercuric Nitrate 0.002% 7 Water for Injection q.s

[0019] Process: Required quantities of Lutein & Zeaxanthin were well mixed with PEG 4000, followed by addition of Phenyl mercuric nitrate & sodium chloride. To the mixture so obtained, was added required quantity of PEG 400, followed by addition of required quantity of water for Injection along with continuous stirring in a high shear mixer/homogenizer. The suspension so formed is filled aseptically and sealed.

Example: 5

[0020] Lutein+Zeaxanthin Ocular Suspension

TABLE-US-00005 S. No Ingredient mg/mL 1 Lutein 0.03-6 mg 2 Zeaxanthin 0.03-6 mg 3 Povidone K30 0.1-0.6% 4 Povidone K90 1.0-6% 5 Sodium Sulphate 0.9 mg 6 Sodium Citrate 0.2 mg 7 Citric Acid 0.6 mg 8 Benzalkonium Chloride 0.001% 9 Hydrochloric Acid/Sodium Hydroxide q.s 10 Water for Injection q.s

[0021] Process: Required quantities of Lutein & Zeaxanthin were well mixed with Povidone K30 & Povidone K90, followed by addition of sodium citrate, citric acid & sodium sulphate. To the mixture so obtained, was added required quantity of Benzalkonium chloride, followed by addition of required quantity of water for Injection along with continuous stirring in a high shear mixer/homogenizer. The pH was adjusted using required quantities of sodium hydroxide/hydrochloric acid. The suspension so formed is filled aseptically and sealed.

Example: 6

[0022] Lutein+Zeaxanthin Ocular Suspension

TABLE-US-00006 S. No Ingredient mg/mL 1 Lutein 0.03-6 mg 2 Zeaxanthin 0.03-6 mg 3 Hydroxy Propyl Methyl 0.03-30 mg Cellulose (HPMC) 4 Hydroxypropyl Cellulose 0.15-30 mg (HPC) 5. Benzalkonium Chloride 0.001% 6. Sodium Chloride 0.01 mg 7. Hydrochloric Acid/Sodium q.s Hydroxide 8. Water for Injection q.s

[0023] Process: Required quantities of Lutein and Zeaxanthin are mixed with HPMC, HPC and Sodium Chloride and to this was added Benzalkonium Chloride and Water for Injection. The suspension so formed was mixed in a homogenizer and the pH was adjusted using hydrochloric acid or sodium hydroxide and the volume was made adjusted using water for injection and filled and sealed.

[0024] The method for preparing the topical ocular suspension according to the disclosure described herein is not limited to the above methods. The topical ocular suspension according to the disclosure described herein can be prepared by using various other techniques.