Puerarin and scutellarin lipid nanoparticle ophthalmic preparation and preparation method thereof

A technology of lipid nanoparticles and scutellarin, applied in the field of medicine, can solve problems such as difficulty in achieving long-term effects, large drug dose loss, and poor visual acuity, and achieve improved compliance, high long-term stability, and drug-loading capacity strong effect

Inactive Publication Date: 2018-05-25
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] With the development of biopharmaceuticals and the continuous deepening of eye pharmacokinetics research, a large number of research results have shown that traditional ophthalmic preparations such as eye drops, eye dressings, eye washes, eye ointments, etc., have a large loss of drug dose. , poor visual acuity, low bioavailability, etc.
Especially for eye diseases that require long-term treatment, it is difficult to achieve long-term effect even if it is used repeatedly, and the use of high-concentration drugs may also cause eye irritation and systemic toxicity.

Method used

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  • Puerarin and scutellarin lipid nanoparticle ophthalmic preparation and preparation method thereof
  • Puerarin and scutellarin lipid nanoparticle ophthalmic preparation and preparation method thereof
  • Puerarin and scutellarin lipid nanoparticle ophthalmic preparation and preparation method thereof

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Effect test

Embodiment 1

[0037] The preparation method of puerarin and scutellarin lipid nanoparticle ophthalmic preparation comprises the following steps:

[0038] (1) Take 32.0 mg of glycerol monooleate, 1 mg of scutellarin, add 1 mL of absolute ethanol as a solvent, heat to 60°C, and dissolve under stirring to obtain a uniform first oil phase; distilled water is the first water phase;

[0039] (2) Take another 1mg of lecithin and 1mg of cholesterol, add 1mL of methanol-ethanol mixture with a volume ratio of 1:1 for ultrasonic dissolution, and add 1mL of Tween 80 to obtain a uniform second oil phase; then add 1mg of puerarin, 4.44mg Pluronic F127, 0.5mg Gelucire 44 / 14 and 20mg octadecyl carboxymethyl chitosan quaternary ammonium salt were added to 2mL phosphate buffer with pH 6.8 and stirred until completely dissolved to obtain the second aqueous phase;

[0040] (3) Add the first oil phase to the first water phase, stir at 400 rpm for 2 hours to obtain the first primary emulsion; then add the second...

Embodiment 2

[0045] The preparation method of puerarin and scutellarin lipid nanoparticle ophthalmic preparation comprises the following steps:

[0046] (1) Take 15mg glycerol monolinoleate, 15mg diglycerol oleate, 1mg scutellarin, add 0.67mL solvent absolute ethanol, heat to 50°C, and dissolve under stirring to obtain a uniform first oil phase; distilled water is first aqueous phase;

[0047] (2) Take another 1mg of lecithin and 1mg of cholesterol, add 1mL of methanol-ethanol mixture with a volume ratio of 1:1 for ultrasonic dissolution, and add 1mL of glycerin to obtain a uniform second oil phase; then add 1mg of puerarin, 4.44mg of Pulang Nick F127, 0.3mg Labrasol and 20mg hydroxypropyl chitosan were added to 2mL pH 7.0 phosphate buffer and stirred until completely dissolved to obtain the second aqueous phase;

[0048] (3) Add the first oil phase to the first water phase, stir at 200 rpm for 1 hour to obtain the first primary emulsion; then add the second oil phase to the second water ...

Embodiment 3

[0052] The preparation method of puerarin and scutellarin lipid nanoparticle ophthalmic preparation comprises the following steps:

[0053](1) Take 10mg of phosphatidylethanolamine, 20mg of dilinoleoylphosphatidylethanolamine, 12mg of 1-palmitoyl-2-oleoylphosphatidylcholine, 1mg of scutellarin, add 1.66mL of solvent absolute ethanol, heat to 60°C, Dissolve under stirring to obtain a uniform first oil phase; distilled water is the first water phase;

[0054] (2) Take another 1mg of lecithin and 1mg of cholesterol, add 1mL of methanol-ethanol mixture with a volume ratio of 1:1 for ultrasonic dissolution, and add 1mL of polyethylene glycol 400 to obtain a uniform second oil phase; then add 1mg of puerarin, 12mg of Pluronic F127, 0.2mg of Solutol HS 15 and 20mg of carboxymethyl chitosan were added to the phosphate buffer with a pH of 6.0 and stirred until completely dissolved to obtain the second aqueous phase;

[0055] (3) Add the first oil phase to the first water phase, stir f...

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Abstract

The invention discloses a puerarin and scutellarin lipid nanoparticle ophthalmic preparation and a preparation method thereof. The preparation method comprises the steps as follows: (1) a lipid material, namely, scutellarin, is taken and dissolved in ethanol, a first oil phase is obtained, and distilled water serves as a first water phase; (2) lecithin and cholesterol are taken, a methanol and ethanol mixed solution is added, ultrasonic dissolution is performed, a solubilizer is added, a second oil phase is obtained, puerarin, a stabilizer, a penetration enhancer and a cationic material are added to a phosphate buffer solution and stirred to be completely dissolved, and a second water phase is obtained; (3) the first oil phase is added to the first water phase, stirring is performed, a first primary emulsion is obtained, the second oil phase is added to the second water phase, stirring is performed, and a second primary emulsion is obtained; (4) the first primary emulsion is dropwise added to the second primary emulsion under the stirring condition, the mixture is uniformly stirred and cooled, and a mixed primary emulsion is obtained; (5) ultrasonic treatment is performed and the preparation is obtained. The preparation has huge membrane surface area, high drug carrying capacity, good biocompatibility and higher biological adhesiveness.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an ophthalmic preparation of puerarin and scutellarin lipid nanoparticles and a preparation method thereof. Background technique [0002] Cataract is the clouding of the lens in the eye, from transparent to opaque, which prevents light from entering the eye and affects vision. The initial turbidity has little effect on vision, and then gradually aggravates, significantly affecting vision and even blindness. Cataract is the leading cause of blindness in the world. There are about 20 million people in the world who are blind due to cataract, and another 100 million cataract patients need surgery to restore vision. In most African and Asian countries, cataract accounts for at least half of the blind. Modern pharmacological studies have shown that puerarin and scutellarin are natural non-selective calcium ion channel blockers, which have strong anti-inflammatory, anti-oxidation, anti-fibros...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/7048A61K31/352A61K47/36A61K47/24A61K47/14A61P27/12
Inventor 刘睿王佳露刘煜老蕊娟赵芳王泽
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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