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Composition for eyes and having improved drying protection and retention

An ophthalmic composition and the technology of the composition are applied in the direction of medical preparations containing active ingredients, drug combinations, drug delivery, etc., which can solve problems such as lack of value and loss of lubricating eyes, and achieve the purpose of improving ocular surface health and encapsulating products. High efficiency and enhanced bioavailability

Inactive Publication Date: 2019-08-06
嘉兴市爵拓科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented inventive product contains certain components that help protect against damage from water vapor during storage and use conditions. These products have good moisture preserving characteristics while still being able to deliver drugs through their own pores into tissue layers on the inside surfaces of the lens capsule. They may contain other substances like chlorophyll A (chloroform), bromochrome pigment B1(brown iron oxide). Additionally they include nanosphericles made by combining specific materials together called particles. Overall these factors enhance the performance and efficiency of this new type of medicine.

Problems solved by technology

This patented technical problem addressed in this patent relates to improving the maintenance and effectiveness of ophthalmology treatments like dry eye because there often cannot adequately supply enough liquid during these procedures without damaging their sensitive surfaces. Additionally, current therapy options involve frequent application of artificial tears on the entire face instead of just one small area at once.

Method used

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  • Composition for eyes and having improved drying protection and retention
  • Composition for eyes and having improved drying protection and retention
  • Composition for eyes and having improved drying protection and retention

Examples

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preparation example Construction

[0049] In the preparation method of the ophthalmic composition of the present invention, the second solute provided is hyaluronic acid or a pharmaceutically acceptable salt thereof, and its concentration in the composition is 0.1-3.0 w / v%. Hyaluronic acid is a compound accepted by the ophthalmic community to protect biological tissues or cells from compressive forces. The viscoelastic properties of hyaluronic acid (i.e. hard elastic at rest but less viscous under small shear forces) allow hyaluronic acid to act essentially as a shock absorber for cells and tissues, hyaluronic acid also It has relatively large water absorption and storage capacity. If sodium hyaluronate is to be added, warm the solution to a temperature not lower than 70°C, then add sodium hyaluronate, and stir the warm solution for 20-30 minutes until the sodium hyaluronate is completely dissolved.

[0050] In the preparation method of the ophthalmic composition of the present invention, the provided second s...

Embodiment 1

[0062] Ophthalmic compositions with improved dryness protection and retention, comprising concentrations of: 0.5w / v% cyclosporin A, 1.0w / v% nanomicelle in situ gel, 0.5w / v% Hyaluronic acid, 0.05w / v% naphazoline, adding buffering agent sodium citrate to adjust the pH of the composition is 7.5, and adding an equal proportion of sodium ascorbate and sorbitol mixture, so that the composition weight osmolality is adjusted to 300mOsmol / kg.

[0063] A process for the preparation of an ophthalmic composition with improved dryness protection and retention comprising the steps of:

[0064] 1) Mix cyclosporine A, glycerin and polyethylene glycol 15-hydroxystearate at a weight ratio of 1:3.5:5, then stir in a water bath at 85°C until dissolved, and then add 2 times the amount Double-distilled water, under the condition of power 200W, pulse 5s / 10s, ultrasonically stirred for 40s, then cooled to room temperature, and adjusted the pH of the obtained micellar solution to 7, that is, nanomice...

Embodiment 2

[0069] The difference between this example and Example 1 is that: in step 1), redistilled water contains 0.05mM gulose and 0.08mM cyclohexanol; Hydrophobic groups of polyethylene glycol fatty acid esters are combined, while the hydrophilic groups of polyethylene glycol 15-hydroxystearate are exposed, and gulose and cyclohexanol are combined with hydrophilic groups during ultrasonic energy transfer , due to the addition of the two, the steric hindrance between the formed nanoparticles increases, which enhances the mutual repulsion of the nanoparticles with small particle size in the system, avoids the self-aggregation phenomenon caused by the smaller particle size, and enhances the combination Antioxidant protection and stability of the compound, on the other hand, the hydrophilic groups of the two can increase the hydrophilicity of the composition and help enhance its penetration of the eye membrane. When the composition is applied to the eye, it can Relieve the heat stress ef...

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Abstract

The invention provides a composition for eyes and having improved drying protection and retention, and belongs to the field of pharmaceutical preparations. The composition includes cyclosporin, nano micelle in-situ gel, and hyaluronic acid or a pharmaceutically acceptable salt thereof; and the composition is in a liquid form at normal temperature or low temperature, is a hydrosol form when the temperature is more than 35 DEG C, and can still maintain complete under the shear stress caused by the eyelid blinking of patients. A preparation method includes providing first solute and second solute; and mixing the solute under a condition of taking water as a substrate so that the composition including gel dispersoid can be formed. The provided composition is high in bioavailability and small in effect on eye pain and irritation, cannot cause the blurring of vision, can improve the compliance of the patients and/or reduce side-effects, can enhance ocular surface health, and has antibacterial and antiseptic effects; and the preparation method can increase adhesiveness, enhance gelation temperature, prolong retention and effective acting time, rising encapsulation yield, avoid self-agglomeration phenomenon, and enhance antioxidant protection effects and stability performance.

Description

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Claims

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Application Information

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Owner 嘉兴市爵拓科技有限公司
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