Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Tetrandrine lipid nanoparticle ophthalmic preparation and preparation method thereof

A technology of lipid nanoparticles and tetrandrine, which is applied in the field of medicine, can solve problems such as difficulty in exerting biological activity of drugs, limited distribution of intraocular tissues, and short residence time in the cornea, so as to improve bioavailability, promote drug absorption, prolong The effect of residence time

Inactive Publication Date: 2019-07-09
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
View PDF3 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Traditional tetrandrine ophthalmic preparations have problems such as short residence time before the cornea, poor corneal permeability, limited distribution of intraocular tissues, low absorption rate, strong eye irritation, etc., making it difficult for the drug to exert biological activity

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Tetrandrine lipid nanoparticle ophthalmic preparation and preparation method thereof
  • Tetrandrine lipid nanoparticle ophthalmic preparation and preparation method thereof
  • Tetrandrine lipid nanoparticle ophthalmic preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The preparation method of tetrandrine lipid nanoparticle ophthalmic preparation includes the following steps:

[0041] (1) Take 350mg monooleic acid glyceride, 10mg tetrandrine, add an appropriate amount of absolute ethanol, heat to 75°C, dissolve it ultrasonically at a power of 190W, rotate under reduced pressure at 45°C, and remove the ethanol to obtain the oil phase ;

[0042] (2) Take another 42 mg poloxamer 407, 0.46 mg Gelucire 44 / 14 and 60 mg N-trimethyl chitosan with a viscosity average molecular weight of 400,000 and a quaternization degree ≥ 60%, and place them in ultrapure water and stir. , Raise the temperature to 65℃ to completely dissolve, and then get the water phase;

[0043] (3) Add the water phase to the oil phase, shear and disperse at 10000 rpm for 2 minutes, and cool to room temperature to obtain colostrum; ultrasonic wave for 5 seconds at a power of 150 W and ultrasonic wave for 5 minutes at an interval of 5 seconds to obtain tetrandrine lipid nano Opht...

Embodiment 2

[0046] A preparation method of tetrandrine lipid nanoparticle ophthalmic preparation includes the following steps:

[0047] (1) Take 350 mg of glyceryl monooleate and 5 mg of tetrandrine, add an appropriate amount of absolute ethanol, heat to 65°C, dissolve it ultrasonically at a power of 150W, rotate under reduced pressure at 45°C, and remove all ethanol to obtain an oil phase;

[0048] (2) Take another 20mg poloxamer 407, 0.04mg Labrasol and 40mg carboxymethyl chitosan with a viscosity average molecular weight of 350,000 and a degree of substitution ≥90%, place them in ultrapure water, stir, and heat to 75℃ to complete Dissolve, get the water phase;

[0049] (3) Add the water phase to the oil phase, shear and disperse at 10000rpm for 2.5min, cool to room temperature to obtain colostrum; under the condition of 190W, sonicate for 5s with 5s interval for 10min to obtain tetrandrine Lipid nanoparticle ophthalmic preparation.

Embodiment 3

[0051] A preparation method of tetrandrine lipid nanoparticle ophthalmic preparation includes the following steps:

[0052] (1) Take 350mg of glyceryl monooleate and 20mg of tetrandrine, add an appropriate amount of absolute ethanol, heat to 85°C, dissolve it ultrasonically at a power of 250W, rotate under reduced pressure at 45°C, and remove the ethanol to obtain the oil phase;

[0053] (2) Take another 50 mg poloxamer 407, 1 mg Plurol Oleique CC497 and 80 mg hydroxypropyl chitosan with a viscosity average molecular weight of 370,000 and a degree of substitution ≥80%, put them in ultrapure water, stir, and heat to 85°C To completely dissolve, get the water phase;

[0054] (3) Add the water phase to the oil phase, shear and disperse at 10000rpm for 3min, and cool to room temperature to obtain colostrum; under the condition of 250W, ultrasonic wave for 5s, 5s interval, 15min for tetrandrine Nanoparticle ophthalmic preparations.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
The average particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a tetrandrine lipid nanoparticle ophthalmic preparation and a preparation method thereof, wherein the preparation method comprises the following steps of: adding glycerol monooleate and tetrandrine into absolute ethyl alcohol, heating, carrying out ultrasonic dissolving and pressure-reducing rotary evaporation, and removing all the ethyl alcohol to obtain an oil phase; (2)placing a slow-release material, a penetration enhancer and a cationic material into ultrapure water, stirring, heating and dissolving to obtain a water phase; (3) adding the water phase into the oilphase, shearing, dispersing and cooling to the room temperature to obtain colostrum; and carrying out ultrasound to obtain the tetrandrine lipid nanoparticle ophthalmic preparation. The preparation has the advantages that the membrane superficial area is large, the drug loading capacity is big; the resistance time of drugs in eyes is prolonged, the bioavailability is improved, the eye irritation and the systemic toxicity caused by repeated administration and high concentration of the drugs are avoided. The cationic material can be degraded in vivo. The long-term stability of the preparation ishigh, the solubility is improved and the drug absorption is enhanced. The preparation has a microstructure similar to a biological membrane and is suitable as a carrier of a mucosal drug delivery system.

Description

Technical field [0001] The invention relates to the field of medicine, in particular to a tetrandrine lipid nanoparticle ophthalmic preparation and a preparation method thereof. Background technique [0002] With the continuous development of science and technology and information exchange, video terminals are becoming more and more popular, and people use their eyes for a longer time. It is easy to cause eye fatigue and poor blood circulation and various eye diseases, such as optic neuropathy, macular degeneration, and primary diseases. Glaucoma and dry eye. Failure to receive effective treatment will result in blindness. Studies have shown that tetrandrine has strong anti-inflammatory, anti-oxidant, anti-fibrosis and lowering intraocular pressure effects, and has great application prospects in preventing glaucoma, cataracts and macular degeneration. [0003] Traditional tetrandrine ophthalmic preparations have problems such as short pre-corneal retention time, poor corneal perm...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/51A61K47/36A61K31/4748A61P27/06A61P27/12A61P27/02
CPCA61K9/0048A61K9/5161A61K31/4748A61P27/02A61P27/06A61P27/12
Inventor 刘睿张玲玲金鑫杨洋
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com