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

Bulleyaconitine A liposome and preparation method thereof

A technology for clathrate and clathrate, which is applied in the field of clathrate liposome and its preparation, can solve the problems of no large-scale industrial production, unsuitable for intramuscular injection, complicated preparation process and the like, and achieves controllability. Good reproducibility and reproducibility, few preparation steps, and the effect of improving compliance

Inactive Publication Date: 2010-11-17
SHANGHAI INST OF PHARMA IND
View PDF0 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The particle size of the disclosed multivesicular liposomes of aconitin is relatively large, at the micron level, and is used as a subcutaneous injection, and its preparation process is relatively complicated, and there is no feasibility for large-scale industrial production
The above-mentioned aconitin liposome preparations are not suitable for intramuscular injection

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Step 1: Dissolve 450mg of distearoylphosphatidylcholine, 150mg of dipalmitoylphosphatidylglyceride, 150mg of cholesterol, and 20mg of vitamin E in 50ml of ether, and evaporate under reduced pressure at a temperature of 25°C to form a uniform film , add 0.2M pH3.8 acetate buffer, shake until the membrane is completely hydrated to obtain primary blank liposomes. Homogenize the primary blank liposomes by high pressure (600bar homogenization 5 times) to obtain liposomes with small particle size, i.e. secondary blank liposomes, adjust the pH to 7.0 with 0.1M sodium hydroxide solution to obtain blank lipids finished product.

[0030] Step 2: Weigh 40mg of aconitin and dissolve it in 2ml of 0.1M, pH3.5 acetate buffer.

[0031] Step 3: Mix the blank liposome in step 1 and the aconitin solution in step 2, and place it at 65° C. for 30 minutes to obtain the product.

[0032] The Nicomp 380 nanometer particle size analyzer was used to measure the particle size, and the measured ...

Embodiment 2

[0034]Step 1: Dissolve 350mg of dipalmitoylphosphatidylcholine, 150mg of distearoylphosphatidylcholine, 150mg of cholesterol, and 15mg of vitamin E in 50ml of ethyl acetate, and rotary evaporate under reduced pressure at a temperature of 30°C to form a uniform Add 0.3M pH 4.0 citric acid buffer to the membrane, and shake until the membrane is completely hydrated to obtain primary blank liposomes. The primary blank liposomes were homogenized under high pressure (600bar homogenization 5 times) to obtain liposomes with small particle size, i.e. secondary blank liposomes, and the pH was adjusted to 7.2 with 0.1M sodium carbonate solution to obtain blank liposomes finished product.

[0035] Step 2: Weigh 40mg of aconitin and dissolve it in 2ml of 0.1M, pH4.0 citrate buffer.

[0036] Step 3: Same as Example 1.

[0037] The average particle diameter of the aconitin liposome was measured to be 113nm, and the encapsulation efficiency was 85.5%.

Embodiment 3

[0039] Step 1: Dissolve 550 mg of dipalmitoylphosphatidylcholine, 60 mg of phosphatidylethanolamine, 100 mg of cholesterol and 20 mg of vitamin E in 50 ml of ethanol to obtain an organic phase. The organic phase was gradually added dropwise to a 0.3M pH4.5 sodium phosphate buffer at a temperature of 45° C. with magnetic stirring (stirring speed 100 rpm), and the residual organic solvent was evaporated to obtain primary blank liposomes. The primary blank liposomes were homogenized under high pressure (600bar homogenization 5 times) to obtain liposomes with small particle size, that is, the secondary blank liposomes, and the pH was adjusted to 8.0 with 0.1M sodium hydroxide solution to obtain blank liposomes finished product.

[0040] Step 2: Weigh 40mg of aconitin and dissolve it in 2ml of 0.3M, pH7.0 sodium phosphate buffer.

[0041] Step 3: Same as Example 1.

[0042] The measured particle diameter of the aconitin liposome is about 140nm, and the encapsulation efficiency is...

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
The average particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a bulleyaconitine A liposome, which comprises the following components in part by mass: 0.01 to 1 part of bulleyaconitine A, 1 part of phospholipid, 0.05 to 1 part of cholesterol and 0.001 to 0.03 part of vitamin E. In the method, the bulleyaconitine A liposome is prepared by adopting a unique two-step method; and the preparation method has the advantages of a few steps, simple and convenient operation and high controllability and reproducibility. The medicament entrapment efficiency of the bulleyaconitine A liposome prepared by the method can reach over 85 percent. The choice of the adopted phospholipids is wide; and natural phospholipids or soybean phospholipids can be used, and synthesized neutral phospholipids or electronegative phospholipids can also be used. The grain size of the bulleyaconitine A liposome is lower than 200 nm; and a preliminary toxicity test shows that the bulleyaconitine A liposome can reduce the toxicity and irritation of the bulleyaconitine A, and improve the compliance of a patient; and therefore, the bulleyaconitine A liposome is particularly suitable to be used as an intramuscular injection.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an aconitin liposome and a preparation method thereof. Background technique [0002] Bulleyaconitine A, also known as Dianxi duraine A, is a diterpene diester alkaloid isolated and extracted from Aconitum Longtounense T.L.Ming, a plant of the genus Ranunculaceae. Pain and obvious anti-inflammatory effect. Its relative analgesic effect is 15 times that of morphine and 1208 times that of aspirin, and continuous administration does not produce analgesic effect tolerance. It is a non-addictive analgesic different from morphine. Due to the long duration of analgesic effect of orthoconitin, it is more suitable for the treatment of various chronic pain diseases. Both animal experiments and clinical applications have shown that aconitin has a good curative effect on rheumatic and rheumatoid arthritis, frozen shoulder, benign arthralgia and pain caused by various e...

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): A61K9/127A61K31/439A61K47/28A61P29/00A61P23/02
Inventor 奉建芳邵红霞祝林李瑞新战丹
Owner SHANGHAI INST OF PHARMA IND
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