Stable elaioplast compositions

A liposome composition and liposome technology are applied in the direction of liposome delivery, drug combination, active ingredients of heavy metal compounds, etc., which can solve problems such as hypersensitivity and expensive phospholipids, so as to improve tolerance and reduce systemic Toxicity, the effect of simple preparation process

Inactive Publication Date: 2007-04-18
SHANGHAI ALLIST PHARM CO LTD
View PDF4 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But this phospholipid is very expensive
Paclitaxel liposomes for injection that are already on the market in China, such as Lipusu produced by Nanjing Cisco Pharmaceutical Co., Ltd., still have the risk of hypersensitivity reactions, and need to inject dexamethasone in advance for anti-allergic pretreatment

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
  • Stable elaioplast compositions
  • Stable elaioplast compositions
  • Stable elaioplast compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The preparation of embodiment 1 paclitaxel liposome

[0034] prescription:

[0035] Paclitaxel 0.15g

[0036] Hydrogenated Soy Lecithin 4g

[0037] Cholesterol 0.6g

[0038] Vitamin E 25mg

[0039] Sucrose 12g

[0040] Water for injection 120ml

[0041] Weigh the prescribed amount of paclitaxel, hydrogenated soybean lecithin, cholesterol, and vitamin E and add 100ml of absolute ethanol, after dissolving, drain the solvent with a rotary evaporator in the presence of nitrogen, prepare a film, and place it in a vacuum desiccator overnight , to remove residual solvent. Add sucrose solution dissolved in water for injection, 55°C water bath, magnetically stir for 1 hour, ultrasonically disperse, homogenize with a high-pressure homogenizer, filter aseptically with a 0.22-micron PVDF membrane, divide into vials, and freeze-dry. Ventilate the vial with nitrogen, and seal it with a gland.

[0042] The electron micrograph of the liposome made is shown in Fig. 1 (magnificat...

Embodiment 2

[0045] The preparation of embodiment 2 paclitaxel liposomes

[0046] prescription:

[0047] Paclitaxel 0.15g

[0048] Hydrogenated Lecithin 4g

[0049] Cholesterol 1g

[0050] Vitamin E 20mg

[0051] Sucrose 15g

[0052] Water for injection 150ml

[0053] Weigh the prescribed amount of paclitaxel, hydrogenated soybean lecithin, cholesterol, and vitamin E, add 100ml of absolute ethanol, dissolve, prepare a film with a rotary evaporator, and place it in a vacuum desiccator overnight to remove the residual solvent. Add sucrose solution dissolved in water for injection, 58 ° C water bath, magnetic stirring for 1 hour, ultrasonic dispersion, sequentially use 0.8, 0.4, 0.2 micron polycarbonate film, extrude with extruder under high pressure, divide into vials, freeze dry , gland seal.

[0054] Measured in the same manner as in Example 1, the average particle diameter of the sample before freeze-drying was 164.6 nm, and the encapsulation efficiency was 92.1%.

Embodiment 3

[0055] The preparation of embodiment 3 paclitaxel liposomes

[0056] prescription:

[0057] Paclitaxel 0.15g

[0058] Hydrogenated soybean lecithin 3.5g

[0059] Cholesterol 1.5g

[0060] Vitamin E 16mg

[0061] Sucrose 5g

[0062] Water for injection 50ml

[0063] Weigh the prescribed amount of paclitaxel, hydrogenated soybean lecithin, cholesterol, and vitamin E, add 100ml of absolute ethanol, dissolve, prepare a film with a rotary evaporator, and place it in a vacuum desiccator overnight to remove the residual solvent. Add sucrose solution dissolved in water for injection, 60°C water bath, magnetically stir for 1 hour, ultrasonically disperse, homogenize with a high-pressure homogenizer, extrude with a 0.2-micron polycarbonate membrane, filter aseptically with a 0.22-micron PVDF membrane, and dispense into Vials, freeze-dried, sealed with a gland.

[0064] Measured in the same manner as in Example 1, the average particle diameter of the sample before freeze-drying wa...

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 sizeaaaaaaaaaa
Login to view more

Abstract

A stable liposome composition used as the carrier of anticancer medicine taxol is prepared from saturated phosphatide, cholesterol, VE and cane sugar through thin-film evaporation and freeze-drying.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a stable liposome composition, in particular to a liposome composition with saturated phospholipids and cholesterol as membrane-forming lipids, and in particular to a liposome composition containing paclitaxel thing. Background technique [0002] The main components and structure of liposomes are similar to those of human cell membranes, with excellent biocompatibility, and have been widely used as carriers for drug delivery. Lipid materials commonly used in liposomes include natural lecithin and natural soybean phospholipids. Because these lipids contain unsaturated fatty acid groups in their molecules, they are easily oxidized and hydrolyzed into peroxides, malondialdehyde, fatty acids and lysophospholipids, and the latter can be further hydrolyzed into glycerol phosphate complexes and fatty acids. Oxidative hydrolysis of phospholipids can also reduce membrane fluidit...

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): A61K9/127A61K31/337A61K31/282A61K33/24A61K47/24A61K47/28A61P35/00
Inventor 郭建辉刘善奎翟晨淏
Owner SHANGHAI ALLIST PHARM CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products