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Ophthalmic compositions

An ophthalmic composition, polymer technology, applied in or can be combined with the existing field, can solve the problems of patient compliance, time-consuming, troublesome, etc.

Pending Publication Date: 2022-02-22
ALCON INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Not only is such a procedure cumbersome and time-consuming, it can also be very expensive, often leading to patient compliance issues

Method used

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  • Ophthalmic compositions
  • Ophthalmic compositions
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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0092] Terpolymer-Poly(PEG 200 Synthesis of MA-co-MPC-co-VPBA) Terpolymer

[0093] About 1.011 g of VPBA was dissolved in 25.0 g of PrOH to obtain a VPBA solution, which was introduced through a syringe equipped with a 5 μm nylon filter into a 2 Inlet, overhead stirrer, thermocouple, condenser and bubbler in a 500 mL reactor. About 12.278g of PEG 200 MA was dissolved in 20.0 g DI water, poured into the reactor and rinsed with an additional 15.0 g DI water. About 6.714 g of MPC was dissolved in 20.0 g DI water, poured into the reactor and rinsed with an additional 15.0 g DI water. About 00693 g of AAPH was dissolved in 5.0 g deionized water, poured into the reactor and rinsed with an additional 2 x 5.0 g deionized water, followed by 5.0 g deionized water and 65.0 g n-propanol. Approximately 3.65 mL of mercaptoethanol (βME) solution (0.274 g βME in 100 mL of DI water) was added with a micropipette.

[0094] The reaction solution was purged with nitrogen (200 mL / min) for 30 ...

example 2

[0100] Synthesis of terpolymers

[0101] Poly (MPC 0.4 -co-NVP 0.5 -co-VPBA 0.1 )

[0102] In a 20 ml vial, 1.18 g (4 mmol) of MPC, 0.556 g (5 mmol) of NVP and 0.148 g (1 mmol) of VPBA were added and 10 ml of ethanol, 1.64 mg (0.01 mmol) of vazo64 were added. Nitrogen was gently bubbled into the solution for 5 min to eliminate oxygen and the vial was then sealed. Polymerization was carried out at 60°C for 6 hours. After cooling the vial, the contents were poured into a large mixture of diethyl ether and chloroform (8 / 2 by volume) to eliminate any remaining monomer and precipitate polymer. The precipitate was filtered off using a glass filter and dried under vacuum.

[0103] Poly (MPC 0.6 -co-BMA 0.3 -co-VPBA 0.1 )

[0104] In a 20 ml vial, 1.77 g (6 mmol) of MPC, 0.426 g (3 mmol) of BMA and 0.148 g (1 mmol) of VPBA were added and 10 ml of ethanol, 1.64 mg (0.01 mmol) of vazo64 were added. Nitrogen was gently bubbled into the solution for 5 min to eliminate o...

example 3

[0114] Synthesis of terpolymers

[0115]2-methacryloyloxyethylphosphorylcholine (MPC) (Mw=295.27), 4-vinylphenylboronic acid (VPBA, Mw=147.97), and optionally a third monomer (methyl Add n-butyl acrylate (BMA, Mw = 142.20) or di(ethylene glycol) methyl ether methacrylate (DGMEMA, Mw = 188.22), ethanol and DI water to a 1L jacketed reactor in the amounts shown in Table 8. Degas the solution at a nitrogen flow rate of 250 mL / min for 30 minutes. Dissolve Vazo-56 in 20 to 30 g of DI water. Degas the initiator solution at a nitrogen flow rate of about 50 mL / min in an additional funnel Gas for 30 minutes. The solution was heated in the reactor to 49° C. The initiator solution was added and the solution temperature was maintained for 16 hours.

[0116] purification:

[0117] The post-reaction solution was diluted to about 10% solids with DI water. The solution from the synthesis step was filtered through a course-fritted filter. The solution was filtered to 7.5%-5.0% solids for p...

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Abstract

The invention is generally related to topical ophthalmic compositions comprising: from about 0.05 w / v% to about 5 w / v% of galactomannan polymer; a cis- diol and about 0.5 w / v% to about 10 w / v% of a hydrophilic copolymer which comprises (a) arylborono-containing repeating units each having a boronic acid, (b) repeating units of at least one phosphorylcholine-containing vinylic monomer, and (c) acrylic monomeric units of at least one acrylic monomer having 3 to 16 carbon atoms, the ophthalmic composition is substantially free of a borate for improving lubrication, hydration and drug delivery property.

Description

[0001] The present invention relates to topical ophthalmic compositions comprising galactomannan and a hydrophilic copolymer for improved lubrication, hydration and drug delivery properties, the hydrophilic copolymer comprising (a ) each having boronic acid-containing aryl dihydroxyboryl-containing repeat units, (b) at least one phosphorylcholine-containing vinyl-based monomer repeat unit, and (c) at least one acrylic monomer-containing acrylic acid single unit. Background technique [0002] The integrity of the tear film is essential for ocular surface homeostasis and function. Dry eye syndrome is a multifactorial condition characterized by an unstable tear film and causes ocular discomfort and visual impairment, seriously affecting the patient's quality of life. The outermost lipid layer of the tear film formed by meibum helps maintain tear film stability by reducing the rate of tear evaporation. Alterations in the tear lipid layer due to impaired meibum quality or quantit...

Claims

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Application Information

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IPC IPC(8): A61K31/59A61K31/07A61K31/355A61K31/122A61K31/015A61K45/06A61K9/00A61K47/36A61K47/10A61K47/26A61K47/34A61P27/02A61P27/04A61P27/06A61P31/00A61P37/08A61P29/00
CPCA61K31/59A61K31/07A61K31/355A61K31/122A61K31/015A61K45/06A61K9/0048A61K47/36A61K47/10A61K47/26A61K47/34A61P27/02A61P27/04A61P27/06A61P31/00A61P37/08A61P29/00A61K2300/00A61K47/24A61K31/202A61K31/593A61K31/736A61K31/80
Inventor 张昀R·C·布莱特科普夫吴大庆葛俊豪M·F·古比托希拉斯皮诺A·T·库米梁微
Owner ALCON INC
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