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

Bulleyaconitine A multivesicular liposome and preparation method thereof

A technology of multivesicular liposomes and clathrin, which is applied in the directions of liposome delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve the problems of low utilization rate of drugs and low utilization rate of raw materials, etc.

Inactive Publication Date: 2010-06-23
SHANGHAI INST OF PHARMA IND
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The raw material utilization rate of this method is low, and the drug utilization rate is usually less than 40%.

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
  • Bulleyaconitine A multivesicular liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Step 1: In a clean glass vessel add 1 mL containing 19.8mM (14.85mg) lecithin, 4.2mM (3.13mg) dipalmitoylphosphatidylglycerol, 30mM (11.61mg) cholesterol and 3.75mM (3.32mg) trioleic acid Chloroform solution of glycerides. This solution is called the lipid phase.

[0059] Step 2: Add 1mL of the internal water phase of the aqueous solution of 120mM (15.86mg) ammonium sulfate into the above-mentioned glass container containing the lipid phase, and stir at a speed of 10,000rpm for 10 minutes with a high-speed shearer to obtain W / O type colostrum.

[0060] Step 3: 5 mL of a solution containing 5% (w / v) (250 mg) glucose and 40 mM (29.36 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 7500 rpm for 10 seconds to obtain W / O / W type double milk.

[0061]Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 7mL containing 5% (w / v) (350mg) glucose and 40mM (40.93mg) lysine, in a constant temperature water bath at 37°C, and make 8...

Embodiment 2

[0066] Step 1: Add 1 mL of 5 mM (3.96 mg) Hydrogenated Soy Lecithin, 0.5 mM (0.38 mg) Dipalmitate Phosphatidylserine, 10 mM (3.87 mg) Cholesterol and 0.155 mM (0.073 mg) Tricaprylic Glycerin to a clean glass container Esters in chloroform-ether solution. This solution is called the lipid phase.

[0067] Step 2: Add 0.5mL of the inner water phase of the aqueous solution of 10mM manganese sulfate (0.845mg) and 6% (w / v) (600mg) sucrose into the above-mentioned glass container containing the lipid phase, and use a high-speed shearing machine to Stir at a speed of 10,000 rpm for 10 minutes to obtain W / O colostrum.

[0068] Step 3: 7.5 mL of a solution containing 0.5% (w / v) (37.5 mg) mannitol and 80 mM (87.71 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 4500 rpm for 40 seconds to obtain W / O / W type double emulsion.

[0069] Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 9mL containing 0.5% (w / v) (45mg) mannitol and 80mM (...

Embodiment 3

[0074] Step 1: Add 1 mL of a dichloromethane solution containing 100 mM (75 mg) lecithin, 20 mM (8.49 mg) phosphatidic acid, 10 mM (3.87 mg) cholesterol and 13 mM (11.51 mg) triolein into a clean glass container. This solution is called the lipid phase.

[0075] Step 2: Add 1mL of the inner water phase of the aqueous solution with 1000mM (192.1mg) citric acid into the above-mentioned glass container containing the lipid phase, and stir at a speed of 10,000rpm for 10 minutes with a high-speed shearer to obtain a W / O type colostrum.

[0076] Step 3: 20 mL of a solution containing 10% (w / v) (2000 mg) mannitol and 20 mM (58.48 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 7500 rpm for 20 seconds to obtain W / O / W type double milk.

[0077] Step 4: Transfer the double emulsion to a 1000mL Erlenmeyer flask containing 22mL containing 10% (w / v) (2200mg) mannitol and 20mM (64.32mg) lysine. Flow through the suspension in the Erlenmeyer flask, slowly evapor...

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
particle sizeaaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses a bulleyaconitine A multivesicular liposome and a preparation method thereof. The bulleyaconitine A multivesicular liposome comprises medicament active components, namely bulleyaconitine A and blank multivesicular liposome which serve as carriers; the blank multivesicular liposome comprises the following components in part by mass: 1 part of lipid component and 0.1 to 50 parts of ion gradient regulator, wherein the lipid component comprises amphiphilic lipid and neutral lipid in a molar ratio of 5-36:1. In the preparation method, the blank multivesicular liposome which is packaged with a gradient regulator is used, bulleyaconitine A permeates a phospholipid film and enters a water phase in the blank multivesicular liposome by a transmembrane gradient active loading method to obtain the bulleyaconitine A multivesicular liposome. The bulleyaconitine A multivesicular liposome has the advantages of high utilization rate of raw materials, high loading concentration, excellent sustained release effect in in-vivo / in-vitro tests and better effect of resisting tumors.

Description

technical field [0001] The invention relates to the field of sustained-release preparations, in particular to an aconitin multivesicular liposome and a preparation method thereof. Background technique [0002] Bulleyaconitine A (Bulleyaconitine A) is a kind of alkaloid with significant analgesic effect isolated from Yunnan Aconitum (Aconitum bullyanum Diels), which is relatively The analgesic effect is 15 times that of morphine and 1208 times that of aspirin, and continuous medication does not produce analgesic tolerance. It is a non-addictive analgesic different from morphine. The drug is available in tablets, oral liquid, capsules and injections. Among them, the tablet and oral liquid have been included in the current edition of the Chinese Pharmacopoeia. Due to the short half-life of aconitin, the clinical use of existing preparations requires multiple administrations, poor patient compliance, and short analgesic effect which affects the curative effect. It is clinicall...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/439A61K47/26A61P25/04
Inventor 陆伟根陈亭亭杨耀杰虞丽芳李军王莉莉
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