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Freeze-dried liposome composition of water-soluble medicament and preparation method thereof

A technology of liposome freeze-drying and water-soluble drugs, which is applied in the field of medicine, can solve the problems of water-soluble drugs leakage, long-term stable storage, aggregation fusion encapsulation rate between particles, etc., to avoid drug leakage and improve stability Effect

Active Publication Date: 2013-09-18
REGENEX PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The purpose of the present invention is to provide a liposome freeze-dried composition of water-soluble drugs, which overcomes the fact that the liposome dispersion of water-soluble drugs in the prior art cannot be stored stably for a long time, and it is easy to cause water-soluble To solve the problems of drug leakage, interparticle aggregation and fusion, and low encapsulation efficiency, a water-soluble drug freeze-dried liposome with good stability, validity period ≥ 24 months, and encapsulation rate ≥ 90% is provided

Method used

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  • Freeze-dried liposome composition of water-soluble medicament and preparation method thereof
  • Freeze-dried liposome composition of water-soluble medicament and preparation method thereof
  • Freeze-dried liposome composition of water-soluble medicament and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Original adjuvant: water-soluble drug is 0.2g of doxorubicin hydrochloride, 0.9g of phospholipid, DSPE-mPEG2000 0.4g of polyethylene glycol derivatized phospholipid, 0.25g of cholesterol, sugar lyophilized protective agent is sucrose 14.0 g, Cyclodextrin or cyclodextrin derivative freeze-dried protective agent is 1.25g of hydroxypropyl-β-cyclodextrin.

[0042] The preparation method is as follows:

[0043] Dissolve phospholipids, polyethylene glycol derivatized phospholipids and cholesterol in 500ml of organic solvent 99.5% ethanol to obtain clear liquid A; put clear liquid A in a 60℃ water bath, and mix 250ml of the first buffer ammonium sulfate solution (250mM ) While stirring, add it to the transparent liquid A, and extrude the resultant with a high-pressure homogenizer to obtain a blank liposome D with an average particle diameter of about 90 nm; add a second buffer to the obtained blank liposome D Replace the first buffer ammonium sulfate of the external phase of blank...

Embodiment 2

[0046] Original adjuvants: Daunorubicin hydrochloride 0.2g, HSPC 1.2g, DSPE-mPEG2000 0.6g, cholesterol 1.0g, sucrose 13.0g, hydroxypropyl-β-cyclodextrin 2.5g Preparation method: same as in Example 1, wherein , The temperature of the water bath is 76℃, and the encapsulation temperature is 105℃.

[0047] Three batches of products were prepared, and the products obtained were Examples 2-1, 2-2, and 2-3 respectively.

Embodiment 3

[0048] Example 3 Original adjuvants: Doxorubicin hydrochloride 0.2g, HSPC 0.32g, DSPE-mPEG2000 0.18g, cholesterol 0.2g, sucrose 13.9g, hydroxypropyl-α-cyclodextrin 0.78g.

[0049] Preparation method: Same as in Example 1, the organic solvent was replaced with 99.5% methanol (1000ml), the second buffer was replaced with citrate (10mM) 250ml; the other components were unchanged; at the same time, the temperature of the water bath was 65°C and the encapsulation temperature was 80 ℃.

[0050] Three batches of products were prepared, and the products obtained were Example 3-1, Example 3-2, and Example 3-3.

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Abstract

Disclosed is a lyophilized liposome composition encapsulating a water-soluble drug and a preparation process thereof. The lyophilized liposome composition comprises a water-soluble drug, a phospholipid, a polyethylene glycol-derivatized phospholipid, cholesterol and a lyoprotectant, wherein the lyoprotectant comprises a saccharide and a cyclodextrin or cyclodextrin derivative. The encapsulation rate of the lyophilized liposome composition encapsulating the water-soluble drug is >=90%.

Description

Technical field [0001] The invention relates to the field of medicine, in particular to a water-soluble drug liposome freeze-dried composition and a preparation method thereof. Background technique [0002] Liposomes are bilayer vesicles composed of phospholipid molecules. It can be divided into unilamellar liposomes and multilamellar liposomes. Its structure is described in many documents and monographs. As a drug carrier, liposomes can meet many requirements for the treatment of pharmaceutical preparations and have many advantages. Liposomes can encapsulate drugs and bring them to the lesion; through liposome administration, they can control the drug in the body tissues. The distribution of the drug reduces the content of the drug in the blood and reduces the toxicity. [0003] There are many preparation methods of liposomes, which are introduced in many literatures and monographs, such as Szoka and apahadjopoulos, Ann. Re. Biophysics Bioeng. 9: 467-508 (1980), Liposome Techno...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/704A61K45/00A61K47/40A61K47/26A61P35/00A61P31/00A61P5/00A61J3/00
CPCA61K31/704A61K47/40A61K9/127A61K47/26A61K45/00A61J3/00A61K9/1271A61K9/19A61P31/00A61P35/00A61P5/00
Inventor 卢智俊刘旭伟
Owner REGENEX PHARMA LTD
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