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Polymeric artificial tear system

a technology of artificial tear and polymer, which is applied in the field of artificial tear formulations and formulations, can solve problems such as interfering with cross-linking, and achieve the effects of strengthening the cross-linking of galactomannan and borate, enhancing the formation of a structured galactomannan-borate polymer network, and enhancing the formation of a structured network of galactomannan-bora

Inactive Publication Date: 2009-10-29
ALCON RES LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009]The formulations of the present invention are substantially free of divalent cations such as magnesium, zinc and calcium that can strengthen cross-linking of the galactomannan and borate. Once a formulation is instilled in the eye, divalent cations present in the tear film enhance formation of a structured galactomannan-borate polymer network.

Problems solved by technology

A cis-diol, such as sorbitol or propylene glycol, is present in the formulations and interferes with the cross-linking of the galactomannan and borate.

Method used

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  • Polymeric artificial tear system
  • Polymeric artificial tear system
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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0042]

Ingredient% w / vHydroxypropyl Guar0.16 to 0.19Boric Acid0.7Sorbitol1.4Polyethylene Glycol0.4Propylene Glycol0.3Potassium Chloride0.12Sodium Chloride0.1Polyquaternium-10.001 + 10% excess2-Amino-2-methylpropanol0.57Sodium Hydroxide / Hydrochloric Acidq.s. pH 7.9Purified Waterq.s. 100%

example 2

[0043]Various solutions containing hydroxypropyl guar, borate and sorbitol were characterized in vitro to explore how the use of a cis-diol such as sorbitol can modify the bulk rheology, interfacial rheology and lubrication properties of hydroxypropyl guar-borate formulations. The experiments conducted show the effect of sorbitol in pH 7.9 formulations comprising a galactomannan-borate cross-linking system, and simulate the introduction of such formulations into the eye at a lower pH (7.6). Hydroxypropyl guar (Mn=3×106 g / mol, polydispersity ratio (PD)=2-3) was used in the preparation of the artificial tear solution (ATDS) used in these experiments. The ATDS used for these experiments is the formulation of Example 1 above, pH adjusted to 7.9 or 7.6, and with varying concentrations of sorbitol.

[0044]Bulk rheology experiments were conducted using a controlled stress rheometer (AR 2000ex, TA Instruments, Inc.). The measurement system was a 40 mm acrylic 2° cone and plate with a sample v...

example 3

[0057]The ATDS formulation of Example 1 was compared in two in vivo studies against saline control solution (Unisol®) and the carboxymethylcellulose / glycerin formulation Optive®.

Retention Time Studies

[0058]An important measure of a lubricant eye drop is the assessment of ocular surface retention or swell time. The mean retention time of a galactomannan-borate solution of the present invention (the ATDS formulation of Example 1) was compared to a saline control solution (Unisol®) using a fluorophotometric technique. Briefly, a fluorescein labeled dextran tracer of approximately 70 kD (Molecular Probes, Eugene, Oregon) was added to each test formulation at a concentration of 0.1 w / v %. A scanning fluorophotometer (Ocumetrics, Mountain View, Calif.) was used to monitor signal decay corresponding to elimination of the formulations. 25 dry eye patients were studied, and measurements were taken roughly every two minutes after application of the test formulation.

[0059]The results of the st...

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Abstract

The present invention relates to artificial tear formulations and ophthalmic formulations suitable for drug delivery. The formulations comprise galactomannans such as guar or hydroxypropyl guar and a borate source such as boric acid. The formulations further comprise a cis-diol such as sorbitol that interferes with the cross-linking of galactomannan and borate. Optionally, the formulations are substantially free of divalent cations.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]This application claims priority under 35 U.S.C. §119 to U.S. Provisional Patent Application No. 61 / 048,175, filed Apr. 26, 2008, the entire contents of which are incorporated herein by reference.TECHNICAL FIELD OF THE INVENTION[0002]The present invention relates to artificial tear formulations and formulations for ophthalmic drug delivery, and more specifically to galactomannan-borate polymer systems comprising a cis-diol.BACKGROUND OF THE INVENTION[0003]Many ophthalmic formulations comprise compounds that provide lubricity and other desirable properties. When these formulations are instilled in the eye, the properties of such compounds can prevent undesirable problems such as bioadhesion and the formation of friction-induced tissue damage, as well as encourage the natural healing and restoration of previously damaged tissues.[0004]Many marketed artificial tear solution products contain polymers that display thixotropic and viscoelastic p...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/715A61P27/02
CPCA61K9/0048A61K47/02A61K47/26A61K47/36A61K31/08A61K47/10A61K31/736A61P27/02A61P27/04
Inventor KETELSON, HOWARD ALLENDAVIS, JAMES W.MEADOWS, DAVID L.
Owner ALCON RES LTD
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