Check patentability & draft patents in minutes with Patsnap Eureka AI!

Decitabine long-circulating liposome lyophilized preparation and preparation method thereof

A long-circulation liposome and liposome freeze-drying technology, which can be used in liposome delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problem of reducing the rapid phagocytosis of the reticuloendothelial system Slow down plastid clearance rate, prolonged drug action time and other problems, to achieve the effect of good appearance, small integrity and good stability

Active Publication Date: 2016-01-06
XIAN LIBANG ZHAOXIN BIOTECH CO LTD
View PDF8 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can prevent liposomes from being recognized by opsonins in the blood, reduce the rapid phagocytosis and uptake of the reticuloendothelial system, thereby slowing down the clearance rate of liposomes, prolonging the residence time in the blood, and prolonging the drug action time

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
  • Decitabine long-circulating liposome lyophilized preparation and preparation method thereof
  • Decitabine long-circulating liposome lyophilized preparation and preparation method thereof
  • Decitabine long-circulating liposome lyophilized preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0045] 1、地西他滨长循环脂质体制剂的制备实施例

[0046] (1)不同配比磷脂制备的地西他滨长循环脂质体制剂

[0047] 例1.1处方:

[0048]

[0049] Preparation:

[0050] (1)秤取处方量的地西他滨、PG、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶剂中,然后旋转蒸发仪在30℃以下减压旋转下除去有机溶剂,使脂质体在器壁上形成薄膜。

[0051] (2)加入磷酸盐缓冲液,进行振摇,则可形大多层脂质体,其粒径范围约1-5um。

[0052] (3)再将其用高压均质机挤压,压力1000bar,均质4遍,便可得地西他滨长循环脂质体。

[0053] 例1.2处方:

[0054]

[0055] Preparation:

[0056] (1)秤取处方量的地西他滨、PS、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶剂中,然后旋转蒸发仪在30℃以下减压旋转下除去有机溶剂,使脂质体在器壁上形成薄膜。

[0057] (2)加入磷酸盐缓冲液,进行振摇,则可形大多层脂质体,其粒径范围约1-5um。

[0058] (3)再将其用高压均质机挤压,压力800bar,均质8遍,便可得地西他滨长循环脂质体。

[0059] 例1.3处方:

[0060]

[0061] Preparation:

[0062] (1)秤取处方量的地西他滨、HSPC、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶剂中,然后旋转蒸发仪在30℃以下减压旋转下除去有机溶剂,使脂质体在器壁上形成薄膜。

[0063] (2)加入磷酸盐缓冲液,进行振摇,则可形大多层脂质体,其粒径范围约1-5um。

[0064] (3)再将其用高压均质机挤压,压力1000bar,均质5遍,便可得地西他滨长循环脂质体。

[0065] (2)不同配比胆固醇制备的地西他滨长循环脂质体制剂

[0066] 例2.1处方:

[0067]

[0068]

[0069] Preparation:

[0070] (1)秤取处方量的地西他滨、HSPC、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶...

example 22

[0073] 例2.2处方

[0074]

[0075] Preparation:

[0076] (1)秤取处方量的地西他滨、HSPC、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶剂中,然后旋转蒸发仪在30℃以下减压旋转下除去有机溶剂,使脂质体在器壁上形成薄膜。

[0077] (2)加入磷酸盐缓冲液,进行振摇,则可形大多层脂质体,其粒径范围约1-5um。

[0078] (3)再将其用高压均质机挤压,压力1000bar,均质3遍,便可得地西他滨长循环脂质体。

example 23

[0079] 例2.3处方

[0080]

[0081] Preparation:

[0082] (1)秤取处方量的地西他滨、HSPC、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶剂中,然后旋转蒸发仪在30℃以下减压旋转下除去有机溶剂,使脂质体在器壁上形成薄膜。

[0083] (2)加入磷酸盐缓冲液,进行振摇,则可形大多层脂质体,其粒径范围约1-5um。

[0084] (3)再将其用高压均质机挤压,压力1000bar,均质4遍,便可得地西他滨长循环脂质体。

[0085] (3)不同PH值磷酸盐缓冲液制备的地西他滨长循环脂质体制剂

[0086] 例3.1处方:

[0087]

[0088]

[0089] Preparation:

[0090] (1)秤取处方量的地西他滨、PG、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶剂中,然后旋转蒸发仪在30℃以下减压旋转下除去有机溶剂,使脂质体在器壁上形成薄膜。

[0091] (2)加入磷酸盐缓冲液,进行振摇,则可形大多层脂质体,其粒径范围约1-5um。

[0092] (3)再将其用高压均质机挤压,压力700bar,均质8遍,便可得地西他滨长循环脂质体。

[0093] 例3.2处方:

[0094]

[0095] Preparation:

[0096] (1)秤取处方量的地西他滨、PG、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶剂中,然后旋转蒸发仪在30℃以下减压旋转下除去有机溶剂,使脂质在器壁上形成薄膜。

[0097] (2)加入磷酸盐缓冲液,进行振摇,则可形大多层脂质体,其粒径范围约1-5um。

[0098] (3)再将其用高压均质机挤压,压力1000bar,均质3遍,便可得地西他滨长循环脂质体。

[0099] 例3.3处方:

[0100]

[0101] Preparation:

[0102] (1)秤取处方量的地西他滨、PG、PEG-DSPE、胆固醇,将其溶解于处方量氯仿和甲醇的混合溶剂中,然后旋转蒸发仪在30℃以下减压旋转下除去有机溶剂,使脂质体在器壁上形成薄膜。

[0103] (2)加入磷酸盐缓冲液,进行...

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 sizeaaaaaaaaaa
Particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a decitabine long-circulating liposome lyophilized preparation and a preparation method thereof. The decitabine long-circulating liposome is obtained by mixing decitabine, phosphatide, a long-circulating membrane material, cholesterol and phosphate buffered solution, and then the obtained liposome as well as a lyophilized protective agent and a compound cosolvent are mixed and lyophilized, so that the decitabine long-circulating liposome lyophilized preparation is obtained. The decitabine long-circulating liposome lyophilized preparation has the advantages that the long-circulating liposome can avoid a mononuclear phagocyte system from rapidly swallowing liposome, blood circulation time is prolonged, relative accumulation quantity of liposome arrived at a diseased region can be conveniently increased, namely a half-life period of the liposome in blood plasma is prolonged, bioavailability of medicine is improved, and the decitabine long-circulating liposome lyophilized preparation can be used for treating primary or secondary myelodysplastic syndrome (MDS) and has broad spectrum antitumour activity on hemic malignant canceration and solid tumours.

Description

technical field [0001] The invention relates to a technology for producing freeze-dried drug liposomes, in particular to a freeze-dried decitabine long-circulation liposome preparation and a preparation method thereof. Background technique [0002] Decitabine, also known as 5-aza-2-deoxycytidine, is the strongest DNA methylation-specific inhibitor known so far. Blocking DNA methylation can cause gene activation and induce cell differentiation . Approved by the European EMEA and the US Food and Drug Administration in April and May 2006, respectively, it is a drug for the treatment of primary and secondary myelodysplastic syndromes (MDS). Its mechanism of action is mainly through phosphorylation, and then directly penetrates into DNA, thereby imitating DNA methyltransferase, then, this can play an anti-tumor effect through DNA hypomethylation and cell differentiation or apoptosis. Clinical reports show that it has broad-spectrum antitumor activity against hematologic maligna...

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): A61K9/127A61K31/706A61P35/00A61P7/00
Inventor 马玉樊陈涛王汝涛
Owner XIAN LIBANG ZHAOXIN BIOTECH CO LTD
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com