Ophthalmic compositions with improved dessication protection and retention

a technology of applied in the direction of drug compositions, biocides, inorganic non-active ingredients, etc., can solve the problems of cumbersome and time-consuming treatment, high cost, and inability to meet the needs of patients, so as to improve the desiccation protection and retention characteristics, the effect of improving stability

Inactive Publication Date: 2013-11-07
ALCON RES LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]The present invention relates to ophthalmic dry eye compositions comprising guar and hyaluronic acid. A cis-diol, such as sorbitol or propylene glycol, is also present in the compositions. In certain embodiments, a borate compound is also present in the compositions. The compositions of the invention provide improved desiccation protection and retention characteristics. The compositions of the present invention are also useful as drug delivery vehicles for ophthalmic

Problems solved by technology

Though existing artificial tear compositions have met with some success, problems in the treatment of dry eye nevert

Method used

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  • Ophthalmic compositions with improved dessication protection and retention
  • Ophthalmic compositions with improved dessication protection and retention
  • Ophthalmic compositions with improved dessication protection and retention

Examples

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example 1

[0030]

Ingredient% W / VHydroxypropyl Guar0.025 to 0.8 Sodium Hyaluronate0.13 to 0.17Boric Acid0.35Sorbitol1.4PEG 4000.4EDTA Sodium0.025Propylene Glycol0.3Potassium Chloride0.12Sodium Chloride0.1Polyquaternium-10.001 + 10% excess2-Amino-2-methylpropanol0.27Sodium Hydroxide / Hydrochloric Acidq.s. pH 7.9Purified Waterq.s. 100%

example 2

[0031]Guar and hyaluronate compositions of the present invention were autoclaved under standard conditions. As shown below in Table 1, the composition comprising sorbitol has a stabilized molecular weight when compared with the composition that did not contain sorbitol.

TABLE 1[HA][HA][HA]Sodium HyaluronatePowderalonewith SorbitolInitial (Powder, 1 × 106 g / mol)1.7——(PD = 1.5)Molecular Weight Before—1.91.9autoclave (1 × 106 g / mol)(PD = 1.4)(PD = 1.5)Molecular Weight After Autoclave—0.41.4(1 × 106 g / mol)(PD = 1.6)(PD = 1.3)pH before Autoclave—7.07.0pH after Autoclave—6.56.8Viscosity at 0.1 s−1 Before—241249AutoclaveViscosity at 10 s−1 After Autoclave—2496

example 3

[0032]The ability of compositions of the present invention to protect human epithelial cells from desiccating stress was evaluated as follows. Human transformed corneal epithelial cells were plated at 0.09×106 cells / mL onto collagen-coated 48-well plates (BD Biosciences #35-4505) and grown to confluence in EpiLife media (Invitrogen #MEPI500CA) supplemented with Human Corneal Growth Supplement (HCGS Invitrogen #S0095) for 48 hours. Cells were treated with test solutions for 30 minutes at 37° C. then rinsed 1× (250 μL) with supplement free media. All solutions were gently removed and the cells were subjected to desiccation at 45% humidity, 37° C. for 30 minutes in a desiccation chamber (Caron Environmental Chamber 6010 Series). Cellular viability was determined using an MTS assay (Promega # G5421) to calculate % protection relative to media control. An assessment of solution cell surface retention was conducted by modifying the above desiccation experiment whereby five “media washes” ...

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Abstract

The present invention relates to artificial tear compositions and ophthalmic compositions suitable for drug delivery. In one embodiment of the present invention, the compositions comprise a galactomannan polymer such as guar or hydroxypropyl guar, hyaluronic acid, and a cis-diol such as sorbitol. In a preferred embodiment, the compositions also comprise a borate compound.

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 / 642,901 filed May 4, 2012, the entire contents of which are incorporated herein by reference.TECHNICAL FIELD OF THE INVENTION[0002]The present invention relates to artificial tear compositions and compositions for ophthalmic drug delivery, and more specifically to compositions comprising a galactomannan such as guar, hyaluronic acid, and a cis-diol.BACKGROUND OF THE INVENTION[0003]Ophthalmic compositions for topical application, and in particular artificial tear compositions, comprise compounds that lubricate and protect the ocular surface. In the context of dry eye disorders, artificial tear compositions can prevent symptoms such as pain and discomfort and can prevent bioadhesion and tissue damage induced by friction. A large number of potential compounds are available that are useful as lubricants and ocular surface protectants. For exampl...

Claims

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Application Information

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IPC IPC(8): A61K31/736A61K31/728
CPCA61K31/736A61K31/728A61K9/0048A61K47/02A61K47/10A61K47/26A61K47/32A61K47/36A61P27/02A61P27/04A61K9/08A61K31/047
Inventor DAVIS, JAMES W.KETELSON, HOWARD ALLENCAMPBELL, ELAINE E.MEADOWS, DAVID L.RANGARAJAN, REKHA
Owner ALCON RES LTD
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