Novel ophthalmic curcumin multi-core vesicle gel preparation and preparation method thereof

Abstract

The invention relates to a novel ophthalmic curcumin multi-core vesicle gel preparation and a preparation method thereof. The preparation consists of the following medicaments: 0.5 to 2.5 milligrams of curcumin, 5 to 25 milligrams of polyethylene glycol monooleate or polyethylene glycol dioleate, 5 to 25 milligrams of polyethylene glycol monolaurate or polyethylene glycol dilaurate, 5 to 25 milligrams of poloxamer F68, 20 to 200 milligrams of soybean phospholipid or lecithin, and mixed solution of 0.1 to 0.7 mg / L of glycerophosphate solution and 0.01 to 0.05 mg / L of chitosan hydrochloride solution in a volume ratio of 1:1-1:10. By organically combining a multi-core vesicle preparation technology with thermo-sensitive gel, the medicament loading capacity is improved, the bioavailability is also improved, meanwhile, an effect of slow release is achieved, the blank of the ophthalmic curcumin multi-core vesicle gel preparation is filled, and a novel ophthalmic preparation with good treatment effect and low price is provided for clinic.

Description

technical field [0001] The invention relates to a novel curcumin ophthalmic multi-core vesicle gel preparation and a preparation method thereof, belonging to the field of pharmacy. Background technique [0002] Eye administration means that the drug exerts a local therapeutic effect through the cornea. Most of the existing ophthalmic preparations are in a single dosage form, mainly eye drops, but eye drops have many disadvantages: such as the drug is immediately absorbed by the conjunctival sac after being instilled. Tears are diluted and quickly discharged from the lacrimal duct, so it is difficult to achieve effective drug concentration; the time of interaction with the cornea is short, and frequent administration is required; the bioavailability is low; patient compliance is also poor. Most of the drugs contained in existing ophthalmic preparations are antibacterial drugs (such as levofloxacin, etc.), with many safety and adverse reactions, and there are few reports on op...

AI Technical Summary

Problems solved by technology

[0002] Eye administration means that the drug exerts a local therapeutic effect through the cornea. Most of the existing ophthalmic preparations are in a single dosage form, mainly eye drops, but eye drops have many disadvantages: such as the drug is immediately absorbed by the conjunctival sac after being instilled. Tears are diluted and quickly discharged from the lacrimal duct, so it is difficult to achieve effective drug concentration; the time of interaction with the cornea is short, and frequent administration is required; bioavailability is low; patient compliance is also poor

Curcumin has low water solubility, but is easily soluble in glacial acetic acid and alkali, which limits its clinical use as an intravenous preparation; it is easily oxidized in vitro, unstable in nature, low in oral bioavailability, and mostly in the stomach broken down in the gut

The pharmacological effects of curcumin include lowering blood lipids, anti-oxidation, anti-inflammation, and anti-atherosclerosis, etc., but there are few reports on the application of ophthalmology, and no patents have been reported in this area. The main ophthalmic treatments include: proliferative vitreoretinal disease, pterygium, vernal catarrhal conjunctivitis, age-related cataract, post-cataract, scarring of the glaucoma filter tract, and corneal neovascularization, etc., its anti-fibrosis, anti-allergy, anti-proliferation, induction of apoptosis and inhibition New angiogenesis and other effects will surely become an excellent natural medicine for the prevention and treatment of ophthalmic diseases, and curcumin has a wide range of drug sources, low price, wide range of pharmacological effects and no obvious adverse reactions, and has broad industrialization prospects

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