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

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...

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.