Gel useful for the delivery of ophthalmic drugs

A gel and drug technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problem of becoming gel, and achieve the effect of prolonging residence time and improving bioavailability

Inactive Publication Date: 2009-09-16
SIGMA TAU IND FARMACEUTICHE RIUNITE SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the gelling vehicle of Rozier et al. has the disadvantage of becoming a gel in the presence of monovalent and divalent cations

Method used

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  • Gel useful for the delivery of ophthalmic drugs
  • Gel useful for the delivery of ophthalmic drugs
  • Gel useful for the delivery of ophthalmic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] 3 g of Carbopol 974P NF (Noveon) was slowly added to 190 mL of water containing 20 mg of benzalkonium chloride, and the solution was kept stirring at room temperature for 18 hours. Then, 500 mg of L-tartaric acid was added, followed by 6 g of mannitol, and finally 1 g of cysteamine, and the solution was kept stirring until the cysteamine was completely dissolved.

[0111] The gel-like system thus obtained was divided into 3 mL portions in 10 mL vials. The vial was lyophilized for 24 hours to give a white solid.

[0112] Addition of 3 mL of water to the lyophilized vial readily yielded a gel-like system with the following characteristics: pH = 4.0-4.3; Osmolality = 229 mOsm / kg.

Embodiment 2

[0114] 10 mg of benzalkonium chloride and 500 mg of L-tartaric acid were added to 95 g of 1.5% Carbopol 974P NF in water. A very free-flowing milky white solution was obtained. To the milky solution was added 3 g sorbitol and 1 g cysteamine. The mixture thus obtained was kept stirring until the cysteamine was completely dissolved.

[0115] The gel-like system thus obtained was divided into 3 mL portions in 10 mL vials. The vial was lyophilized for 24 hours to give a white solid.

[0116] Addition of 3 mL of water to the lyophilized vial readily yielded a gel-like system with the following characteristics: osmotic pressure = 267 mOsm / kg; pH = 4.5-5.0.

Embodiment 3

[0118] 1 g of L-tartaric acid was added to 95 g of 1.5% Carbopol 974P NF in water to give a very free flowing milky white solution. To this solution were added 3 g of sorbitol and 1 g of cysteamine, and the mixture thus obtained was kept stirring until the cysteamine had completely dissolved.

[0119] The gel-like system thus obtained was divided into 3 mL portions in 10 mL vials. The vial was lyophilized for 24 hours to give a white solid.

[0120] Addition of 3 mL of water to the lyophilized vial readily yielded a gel-like system with the following characteristics: pH = 4.0-4.3; Osmolality = 297 mOsm / kg.

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Abstract

It is described a gel composed of a mixture of a polymer which forms a gel, a buffer; a saccharide and one or more active ingredients useful for treating diseases of the eyes.

Description

field of invention [0001] The present invention relates to a physiological supplement or medicament in the form of a solid powder comprising a mixture of: a gel-forming polymer; a buffer; a sugar and one or more active ingredients for the treatment of eye diseases, wherein said powder When reconstituted with an appropriate amount of water or a liquid solution provides a gel useful for the prophylaxis or treatment of said eye disease. [0002] Non-limiting examples of such eye diseases are cystinosis, dry eye syndrome, corneal edema, and eye diseases due to ultraviolet radiation. Background technique [0003] Cystinosis is an inherited metabolic disorder that causes cystine to accumulate in various organs of the body. Cystine crystals accumulate in the kidneys, eyes, liver, muscles, pancreas, brain, and white blood cells. Without specific treatment, children with cystinosis develop end-stage kidney failure by about nine years of age. [0004] Cystinosis can also cause comp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/26A61K47/32
CPCA61K31/7036A61K31/205A61K47/26A61K47/32A61K45/06A61K9/0048A61K47/12A61K9/06A61K9/19A61P27/02A61K2300/00A61K9/14
Inventor A·隆戈M·圣阿尼罗N·派斯科索利多A·科沃里奇
Owner SIGMA TAU IND FARMACEUTICHE RIUNITE SPA
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