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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 difficult insertion and removal, poor patient compliance, and reduced patient compliance, so as to achieve good bioadhesion and prolong the retention time in the eye , increase the effect of absorption and bioavailability

Inactive Publication Date: 2013-01-23
SOUTH CHINA UNIV OF TECH
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  • 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 sensation and reduce the patient's compliance; although the implantable drug delivery system has products on the market, it is still difficult to put in and out, and blinking may cause the polymer Defects such as membrane movement or even falling out, constant-rate drug release disappears when the diaphragm is twisted, and drug leakage from the reservoir-type drug delivery device; bioadhesive materials mainly include sodium hyaluronate, chitosan, polyacrylic acid, hydroxyl Propyl methyl cellulose and other bioadhesive products based on such polymers can prolong the residence time of drugs by increasing the viscosity and bioadhesiveness. However, although this type of ophthalmic gel can prolong the action time of drugs, However, this type of gel also has disadvantages such as inaccurate dosage, large Hetius, inconvenient administration, and poor patient compliance.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Under the 100-level environment, 3.00g chitosan was dissolved with deionized water and 2.10g acetic acid to obtain a chitosan solution, and 0.30g carbomer 407 was added to the chitosan solution, and heated to dissolve 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, add Deionized water to 1000mL, sterilized by a microporous membrane, then subpacked in small doses to obtain the ophthalmic in-situ gelling agent of the present invention.

Embodiment 2

[0042] Under the 100-level environment, 6.00g chitosan was dissolved with deionized water and 3.15g acetic acid to obtain a chitosan solution, and 0.90g carbomer 407 was added to the chitosan solution, and heated to dissolve to obtain a mixed solution; Add 0.80g sodium hyaluronate, 0.03g mannitol, 6.32g glycerin and 0.01g vitamin E to the solution, mix well; add 0.75g sodium bicarbonate to it to adjust the pH value, add 1.00g glucose to adjust the osmotic pressure, add Deionized water to 1000mL, sterilized by a microporous membrane, then subpacked in small doses to obtain the ophthalmic in-situ gelling agent of the present invention.

Embodiment 3

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

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PUM

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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 relates to a preservative-free ophthalmic in-situ gelling agent and a preparation method thereof. The product of the invention can be used as an artificial tear substitute medicine to treat dry eye syndrome, and can also be used as a drug delivery system for ophthalmic medicine. Background technique [0002] Improving the bioavailability of topical 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 solutions or suspensions. Later, with the development and utilization of pharmaceutical excipients and the research on new technologies for ophthalmic drug delivery, new drug delivery agents have emerged. Pharmaceutical systems, including in situ gel drug delivery systems, colloid drug delivery sys...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/32A61K47/36A61K31/722A61P27/02A61P27/04
Inventor 魏坤张捷
Owner SOUTH CHINA UNIV OF TECH
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