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Tetrandrine liquid crystal nanoparticle ophthalmic preparation and preparation method thereof

A technology for tetrandrine and ophthalmic preparations, applied in the field of medicine, can solve problems such as difficulty in achieving long-term effect, large loss of drug dose, systemic toxicity, etc., and achieve high compliance, high long-term stability and simple preparation process. Effect

Active Publication Date: 2018-06-08
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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  • Tetrandrine liquid crystal nanoparticle ophthalmic preparation and preparation method thereof
  • Tetrandrine liquid crystal nanoparticle ophthalmic preparation and preparation method thereof
  • Tetrandrine liquid crystal nanoparticle ophthalmic preparation and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0032] A preparation method for tetrandrine liquid crystal nanoparticle ophthalmic preparation, comprising the steps of:

[0033] (1) Take 30.8mg glycerol monooleate, 3.4mg Pluronic F127, 1mg Tetrandrine, add 1mL absolute ethanol, heat to 75°C, dissolve under stirring, rotary steam under reduced pressure, remove all ethanol, and obtain a uniform oil phase;

[0034] (2) Add Gelucire 44 / 14 and 3 mg of octadecyl carboxymethyl chitosan quaternary ammonium salt to 3 mL (3 g) of distilled water and stir until completely dissolved to obtain an aqueous phase; the amount of Gelucire 44 / 14 is monooleic acid Glycerides, Pluronic F127, tetrandrine, octadecyl carboxymethyl chitosan quaternary ammonium salt and 0.2% of the total weight of distilled water;

[0035] (3) Add the water phase to the oil phase, at 10000r·min -1 Shear and disperse for 3 minutes, cool to room temperature to obtain colostrum;

[0036] (4) Ultrasound the colostrum, the ultrasonic power is 200w, the ultrasonic wave...

Embodiment 2

[0039] A preparation method for tetrandrine liquid crystal nanoparticle ophthalmic preparation, comprising the steps of:

[0040] (1) Take 15mg glycerol monolinoleate, 15mg diglycerol oleate, 3.3mg pluronic F127, 1mg tetrandrine, add 0.67mL absolute ethanol, heat to 75°C, dissolve under stirring, spin under reduced pressure Steam to remove ethanol to obtain a homogeneous oil phase;

[0041] (2) Add Labrasol and 3mg carboxymethyl chitosan into 3mL (3g) distilled water and stir until completely dissolved to obtain the water phase; the amount of Labrasol added is glycerol monolinoleate, diglyceride oleate, pluronic F127, 0.1% of the total weight of tetrandrine, carboxymethyl chitosan and distilled water;

[0042] (3) Add the water phase to the oil phase, at 5000r·min -1 Shear and disperse for 3 minutes, cool to room temperature to obtain colostrum;

[0043] (4) Ultrasound the colostrum, the ultrasonic power is 200w, the ultrasonic wave is 5s, the interval is 5s, and the ultras...

Embodiment 3

[0045] A preparation method for tetrandrine liquid crystal nanoparticle ophthalmic preparation, comprising the steps of:

[0046] (1) Take 10mg of phosphatidylethanolamine, 20mg of dilinoleoylphosphatidylethanolamine, 12mg of 1-palmitoyl-2-oleoylphosphatidylcholine, 5mg of pluronic F127, 1mg of tetrandrine and add 1.66mL of absolute ethanol, Heat to 60°C, dissolve under stirring, rotary steam under reduced pressure, remove all ethanol, and obtain a homogeneous oil phase;

[0047] (2) Add Solutol HS 15 and 5 mg carboxymethyl chitosan to 5 mL (5 g) of distilled water and stir until completely dissolved to obtain an aqueous phase; the amount of Solutol HS 15 added is phosphatidylethanolamine, dilinoleoylphosphatidylethanolamine, 0.05% by total weight of 1-palmitoyl-2-oleoylphosphatidylcholine, Pluronic F127, tetrandrine, carboxymethyl chitosan and distilled water;

[0048] (3) Add the water phase to the oil phase, at 8000r·min -1 Shear and disperse for 3 minutes, cool to room t...

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Abstract

The invention discloses a tetrandrine liquid crystal nanoparticle preparation for eyes and a preparation method thereof. The method includes the steps of firstly, adding lipid material, stabilizer and tetrandrine to solvent absolute ethyl alcohol to be heated and dissolved, and conducting decompression rotary steaming to thoroughly remove ethyl alcohol to obtain a uniform oil phase; secondly, adding penetration enhancer and positive ion material to distilled water to be stirred and completely dissolved to obtain a water phase; thirdly, adding the water phase to the oil phase to be shorn, dispersed and cooled to the room temperature to obtain an initial emulsion; fourthly, conducting ultrasound treatment on the initial emulsion to obtain the tetrandrine liquid crystal nanoparticle preparation for eyes. The preparation has huge film surface area, strong medicine carrying capacity, good biological compatibility, high biological adhesiveness and high long-term stability, the number of dosage times can be decreased, and the dependence of patients on medicine is improved. The preparation has the effects on packaging and protecting medicine, increasing dissolvability, improving stability and promoting medicine absorption.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an ophthalmic preparation of tetrandrine liquid crystal 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 tetrandrine is a natural non-selective calcium ion channel blocker, which has strong anti-inflammatory, anti-oxidation, anti-fibrosis, lower intraocu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/51A61K31/4748A61P27/12
CPCA61K9/0048A61K9/1274A61K9/5161A61K31/4748A61K47/36
Inventor 刘睿王艳王双双刘煜王佳露陈京京黄兴国
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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