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

A gel preparation, curcumin technology, applied in the field of new curcumin ophthalmic multi-core vesicle gel preparation and its preparation, can solve reproductive vitreoretinopathy, pterygium, vernal catarrhal conjunctivitis, age Related cataracts, difficulty in achieving effective drug concentration, low water solubility of curcumin, etc., to achieve the effects of reducing eye irritation and side effects, avoiding drug oxidation, and improving stability and drug loading

Inactive Publication Date: 2013-04-17
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] 1) Precisely weigh 1mg of curcumin, 5-10mg of polyethylene glycol monooleate PEG400MO, 5-10mg of polyethylene glycol monolaurate PEG200ML, 20mg of poloxamer F68, put in a 50ml beaker, 90℃ Heated in a water bath for 10 minutes, and immediately placed in an ice-water bath for 10 minutes, the phase transition process of the raw material from solid to liquid and then to solid, to obtain drug-loaded curcumin nonionic surfactant vesicles;

[0038] 2) Precisely weigh 100mg of soybean lecithin, and make it into an aqueous solution with a concentration of 0.25g / ml by ultrasonic dispersion method;

[0039] 3) Mix the drug-loaded curcumin non-ionic surfactant vesicles obtained in step 1) with the soybean phospholipid aqueous solution obtained in step 2) at a volume ratio of 1:6, and sonicate for 20 minutes to obtain curcumin multi-core vesicles;

[0040] 4) At room temperature and under magnetic stirring, add the glycerol phosphate solution with a concentration of 0.56 mg / L dropwi...

Embodiment 2

[0061] 1) Precisely weigh 1 mg of curcumin, 5-10 mg of polyethylene glycol dioleate (PEG400DO), 5-10 mg of polyethylene glycol dilaurate (PEG200DL), 20 mg of poloxamer F68, and place them in a 50ml beaker. Heated in a water bath at 90°C for 10 minutes, and immediately placed in an ice-water bath for 10 minutes. The phase transition process of the raw material from solid to liquid and then to solid obtained drug-loaded curcumin nonionic surfactant vesicles;

[0062] 2) Precisely weigh 100mg of lecithin, and make it into an aqueous solution with a concentration of 0.25g / ml by ultrasonic dispersion;

[0063] 3) Mix the drug-loaded curcumin non-ionic surfactant vesicles obtained in step 1) with the soybean phospholipid aqueous solution obtained in step 2) at a volume ratio of 1:6, and sonicate for 20 minutes to obtain curcumin multi-core vesicles;

[0064] 4) At room temperature and under magnetic stirring, add the glycerol phosphate solution with a concentration of 0.56 mg / L drop...

experiment example 1

[0067] Experimental example 1 investigates curcumin vesicle encapsulation efficiency

[0068] Precisely pipette 0.1 mL of the vesicle suspension prepared in Example 1 and Example 2 into a 10 mL volumetric flask, break the emulsification with methanol and dilute to the mark with ethanol, and measure the absorbance as A 2 . Similarly, after passing the vesicles through a 0.22 μm microporous membrane, pipette 0.1 mL into a 10 mL volumetric flask, break the emulsion with methanol and dilute to the mark with ethanol, and measure the absorbance as A 1 .

[0069] Encapsulation efficiency of vesicles: EE%=(A1 after passing through the membrane / A2 without passing through the membrane)×100%

[0070] Table 1 Curcumin Vesicle Encapsulation Efficiency Results

[0071] Test No.

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/50A61K31/12A61K47/36A61P27/02A61P27/06A61P27/12A61P9/10
Inventor 陈大全
Owner YANTAI UNIV
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