Preservative-free ophthalmic in-situ gelling agent and preparation method thereof

A technology of gelling agent and preservative, applied in the field of pharmaceutical preparations, can solve the problems of difficulty in putting in and taking out, reducing patient compliance, poor patient compliance, etc., achieve good bioadhesion, increase absorption and bioavailability degree, prolong the effect of staying in the eye

Inactive Publication Date: 2011-09-28
SOUTH CHINA UNIV OF TECH
View PDF3 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] As a new type of ophthalmic drug carrier, liposome has the advantages of increasing corneal permeability, slow release and reducing toxicity, but due to the limitation of drug encapsulation efficiency and preparation stability, there is still no commercialization trend; Drug-loaded microspheres or nanoparticles are less affected by tear elimination and can stay at the drug site for a longer period of time, especially nanoparticles can selectively adhere to the surface of corneal tissue with inflammation and show a certain targeting effect; Ophthalmic insertion refers to placing a drug-embedded polymer film in the conjunctival sac to control drug release by diffusion or erosion, thereby maintaining a near constant drug release rate for several days. During the medication process, while improving the local bioavailability, it will cause a foreign body sen

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] In a 100-level environment, dissolve 3.00 g of chitosan with deionized water and 2.10 g of acetic acid to obtain a chitosan solution, add 0.30 g of carbomer 407 to the chitosan solution, and heat until dissolved to obtain a mixed solution; Add 0.50g sodium hyaluronate, 0.02g sorbitol, 3.80g glycerol and 0.01g vitamin E to the solution, mix well; add 0.50g sodium bicarbonate to adjust the pH value, add 0.80g glucose to adjust the osmotic pressure, and add The ophthalmic in-situ gelling agent of the present invention is obtained by adding deionized water to 1000 mL, sterilizing with a microporous membrane, and then sub-packing in small doses.

Embodiment 2

[0042] In a 100-grade environment, dissolve 6.00 g of chitosan with deionized water and 3.15 g of acetic acid to obtain a chitosan solution, add 0.90 g of carbomer 407 to the chitosan solution, and heat until dissolved to obtain a mixed solution; Add 0.80g sodium hyaluronate, 0.03g mannitol, 6.32g glycerol and 0.01g vitamin E to the solution, mix well; add 0.75g sodium bicarbonate to adjust the pH value, add 1.00g glucose to adjust the osmotic pressure, and add The ophthalmic in-situ gelling agent of the present invention is obtained by adding deionized water to 1000 mL, sterilizing with a microporous membrane, and then sub-packing in small doses.

Embodiment 3

[0044] In a 100-level environment, dissolve 10.00 g of chitosan with deionized water and 2.68 g of acetic acid to obtain a chitosan solution, add 1.20 g of carbomer 940 to the chitosan solution, and heat until dissolved to obtain a mixed solution; Add 1.00g sodium hyaluronate, 0.03g sorbitol, 6.32g glycerol and 0.02g vitamin E to the solution, mix well; add 0.50g sodium bicarbonate to adjust the pH value, add 0.90g glucose to adjust the osmotic pressure, and add The ophthalmic in-situ gelling agent of the present invention is obtained by adding deionized water to 1000 mL, sterilizing with a microporous membrane, and then sub-packing in small doses.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention discloses a preservative-free ophthalmic in-situ gelling agent and a preparation method thereof. The preservative-free ophthalmic in-situ gelling agent comprises Carbomer, chitosan, lubricant, stabilizer, thickener, antioxidant, acetic acid, pH regulator, osmoregulator and de-ionized water. By using the Carbomer and chitosan as base materials for the preparation of the in-situ gelling agent, the in-situ gelling agent increases the solubility of the medicament, improves the absorption and bioavailability of the medicament, reduces the frequency of use and enhances the safety and efficiency; by containing the chitosan, the in-situ gelling agent has biological adhesive action, so that the adhesion of medicament particles onto the cornea is enhanced; and the in-situ gelling agent is free of preservative, thereby having no stimulus or damage to the corneal epithelium. The preservative-free ophthalmic in-situ gelling agent can be used as artificial tear for treating xerophthalmia, and can be also used as an administration and transmission system of ophthalmic medicaments.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to external ophthalmic preparations. Specifically, it relates to an ophthalmic in-situ gelling agent without preservatives and a preparation method thereof. The product of the present invention can be used as an artificial tear substitute drug for the treatment of dry eye, and can also be used as a drug delivery system for ophthalmic drugs. Background technique [0002] Improving the bioavailability of external ophthalmic preparations has always been one of the main research purposes of ophthalmic preparations. The initial forms of ophthalmic preparations are eye drops, ointments and films of solution or suspension, and then with the development and utilization of pharmaceutical excipients, new technologies for ophthalmic administration have been studied, and new dosage forms have emerged. Pharmaceutical systems, including in situ gel delivery systems, colloid delivery sys...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/00A61K47/32A61K47/36A61K31/722A61P27/02A61P27/04
Inventor 魏坤张捷
Owner SOUTH CHINA UNIV OF TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products