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

A technology for lyophilizing liposomes and water-soluble drugs, applied in the field of medicine, can solve problems such as leakage of water-soluble drugs, inability to store stably for a long time, aggregation and fusion encapsulation rate between particles, etc., so as to avoid drug leakage and improve stability. Effect

Active Publication Date: 2011-04-20
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
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Effect test

Embodiment 1

[0041] Raw and auxiliary drugs: water-soluble drug is doxorubicin hydrochloride 0.2g, phospholipid is HSPC 0.9g, polyethylene glycol derivatized phospholipid is DSPE-mPEG20000.4g, cholesterol is 0.25g, sugar lyoprotectant is sucrose 14.0 g. Cyclodextrin or cyclodextrin derivative lyoprotectant is 1.25 g of hydroxypropyl-β-cyclodextrin.

[0042] The preparation method is as follows:

[0043] Phospholipids, polyethylene glycol derivatized phospholipids, and cholesterol are dissolved in 500ml of organic solvent 99.5% ethanol to obtain transparent liquid A; transparent liquid A is put into a 60°C water bath, and 250ml of the first buffer ammonium sulfate solution (250mM ) was added to the transparent liquid A while stirring, and the obtained product was extruded with a high-pressure homogenizer to obtain a blank liposome D with an average particle diameter of about 90 nm; a second buffer was added to the blank liposome D obtained. Liquid histidine (10mM) 5000ml replaces the first...

Embodiment 2

[0046] Raw and auxiliary drugs: daunorubicin hydrochloride 0.2g, HSPC1.2g, DSPE-mPEG20000.6g, cholesterol 1.0g, sucrose 13.0g, hydroxypropyl-β-cyclodextrin 2.5g Preparation method: same as Example 1, wherein , the water bath temperature was 76°C, and the encapsulation temperature was 105°C.

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

Embodiment 3

[0048] Example 3 Primary and auxiliary drugs: 0.2g of doxorubicin hydrochloride, 0.32g of HSPC, 0.18g of DSPE-mPEG20000, 0.2g of cholesterol, 13.9g of sucrose, and 0.78g of hydroxypropyl-α-cyclodextrin.

[0049] Preparation method: Same as Example 1, the organic solvent is replaced by 99.5% methanol (1000ml), the second buffer is replaced by citrate (10mM) 250ml; other components remain unchanged; while the water bath temperature is 65 ° C, the encapsulation temperature is 80 ℃.

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

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Abstract

The invention discloses a freeze-dried liposome composition of water-soluble medicament. The composition comprises the following raw materials: water-soluble medicament, phospholipid, polyethylene glycol-phospholipid, cholesterol, carbohydrate freeze-drying protective agent and cyclodextrin or cyclodextrin derivative freeze-drying protective agent. In the invention, the carbohydrate and cyclodextrin or cyclodextrin derivative are used as the freeze-drying protective agent for the liposome dispersion liquid of the water-soluble medicament, and the entrapment rate of the obtained freeze-dried liposome of the water-soluble medicament is not less than 90%, the particle size is between 10 and 500 nm, all indexes conform to the requirements of the quality standard, and the period of validity isnot shorter than 24 months and is more than 4 months longer than that of the liposome of the water-soluble medicament on the market. Meanwhile, the invention also provides a preparation method of thefreeze-dried liposome composition of the water-soluble medicament.

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. Can be divided into unilamellar liposomes and multilamellar liposomes. Its structure has been described in many literatures and monographs. As a drug carrier, liposomes can meet many therapeutic requirements of pharmaceutical preparations and have many advantages. Liposomes can encapsulate drugs and bring them to the lesion; administration through liposomes can control the delivery of drugs in tissues in the body. The distribution of the drug can reduce the content of the drug in the blood and reduce the toxicity. [0003] There are also many preparation methods for liposomes, which are introduced in many documents and monographs, such as Szoka and apahadjopoulos, Ann.Re.Biophysics Bioeng.9: 467-508 (19...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/704A61K45/00A61K47/40A61K47/26A61P35/00A61P31/00A61P5/00A61J3/00
CPCA61K47/26A61K47/40A61K45/00A61K9/127A61K31/704A61J3/00A61K9/1271A61K9/19A61P31/00A61P35/00A61P5/00
Inventor 卢智俊刘旭伟
Owner REGENEX PHARMA LTD
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