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Soluble polymer eye insert with biodegradable polymer

A biodegradable polymer technology, applied in the direction of drug combinations, organic active ingredients, medical preparations of non-active ingredients, etc., can solve problems such as slow dissolution properties, irritation or congestion, blurred vision, etc.

Pending Publication Date: 2022-07-15
ALCON INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Slow dissolution properties combined with stick hardness and design may lead to side effects including blurred vision, foreign body sensation and / or discomfort, eye irritation or congestion, hypersensitivity reactions, photophobia, puffy eyelids and clumping or drying of sticky material on eyelashes

Method used

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  • Soluble polymer eye insert with biodegradable polymer
  • Soluble polymer eye insert with biodegradable polymer
  • Soluble polymer eye insert with biodegradable polymer

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0050] Example 1 - Polymeric Eye Inserts Containing Alpha-2-Adrenergic Agonists

[0051] In other inventions, alpha-2 adrenergic receptor agonists such as brimonidine were used to prepare intercalated membranes at different concentrations, namely 90 ppm, 495 ppm and 5048 ppm, respectively.

[0052] Prepare control insert membrane_brimonidine:

[0053] Transfer 300 mL of DI water from the graduated cylinder to a clean 500 mL Erlenmeyer flask. HA (0.94 g) and PVP (0.21 g) were added to a 500 ml Erlenmeyer flask. stir the mixture

[0054] After 1.5 hours, a homogeneous solution was obtained. Add HP Guar Gum (0.84g) and

[0055] The mixture was stirred for 1 hour, making the mixture homogeneous again. PEG (0.21 g) was added and the mixture was stirred for an additional 30 min. The mixture is then allowed to sit

[0056] (without stirring) for 30 min to remove air bubbles. Pour the mixture (150g) into a petri dish,

[0057] The dishes were then placed in an evaporation ove...

example 2

[0076] Example 2 - Polymer Eye Inserts Containing PLGA

[0077] The addition of PLGA (MW: 10,000 to 18,000 and 96,000) to polymer insert compositions at different concentrations (1%, 1.7%, 2% and 4%) was evaluated. The PLGA doped film exhibited a similar spectrum to the undoped film. The presence of PLGA slowed the dissolution rate without significantly changing the mechanical properties of the membrane. The concentration and molecular weight of PLGA had obvious effects on the dissolution profile.

[0078] PLGA solubility screening:

[0079] Both low or high MW PLGA were found to be insoluble in DI water, ethanol, amyl alcohol, methanol and PEG 400. Low or high MW PLGA was found to be soluble in DCM, THF, EA and acetone. Either low or high MW PLGA will be introduced into the current formulation as a solution in acetone.

[0080] Prepare control insert membrane_PLGA:

[0081] Transfer 300 mL of DI water from the graduated cylinder to a clean 500 mL Erlenmeyer flask. HA (...

example 11

[0105] Example 11 - Polymeric Eye Insert Containing TRPM8 Agonist (Mentone Glycerol Ketal)

[0106] The addition of MGA to the polymer insert composition was evaluated at 20 ppm and 40 ppm. The MGA doped films exhibited similar color and transparency to the undoped films. The presence of MGA significantly altered the folding durability results. After less than 20 folding cycles, the MGA-doped dry films exhibited cracks / breaks. In contrast, both doped and undoped hydrated films exhibited similar folding durability properties.

[0107] Prepare control insert membrane_MGA:

[0108] Transfer 800ml of DI water from the graduated cylinder to a clean 1000ml Erlenmeyer flask. HA (2.24g) and PVP (0.56g) were added to a 1000ml Erlenmeyer flask. The mixture was stirred by mechanical stirring and sonicated at the same time. After a total of 1.5 hours, the mixture was observed to appear homogeneous. HP guar gum (2.24 g) was added and the mixture was stirred again while being sonicat...

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Abstract

The present application provides a polymeric ophthalmic insert comprising: a biodegradable polymer and one or more mucoadhesive polymers that are biocompatible with the ocular surface and tear film of the eye wherein the biodegradable polymer, compared to a control polymeric ophthalmic insert, has a thickness of less than or equal to 20 [mu] m, and a thickness of less than or equal to 20 [mu] m, and a thickness of less than or equal to 20 [mu] m, and a thickness of less than or equal to 20 [mu] m. The dissolution time of the polymeric eye insert is increased by at least 15%, and the control polymeric eye insert is the same polymeric eye insert other than the absence of the biodegradable polymer.

Description

technical field [0001] The present disclosure relates generally to polymer eye insert technology, and more particularly to dissolvable polymer eye inserts having biodegradable polymers, and these polymer eye inserts are long lasting compared to topical drop dosage forms Lubricants and drugs are released into the eye (including but not limited to the anterior and posterior segments) over time. Background technique [0002] Many ophthalmic formulations include compounds that provide lubricity and other desirable properties. When these formulations are instilled into the eye, the properties of this compound can prevent undesirable problems such as bioadhesion and the formation of tissue damage caused by friction, and can promote the natural healing and recovery of previously damaged tissue. [0003] Application compliance with topical ophthalmic formulations (eg, liquids, ointments, gels, sprays) is often poor, especially for the treatment of dry eyes, allergies, infections, a...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/32A61K47/36A61K47/38A61K47/10A61K47/12A61K31/498A61K31/122A61P27/02
CPCA61K9/0051A61K47/34A61K47/32A61K47/36A61K47/38A61K47/10A61K47/12A61K31/498A61K31/122A61K31/357
Inventor H·A·凯特尔森R·兰加拉詹
Owner ALCON INC