Pixantrone maleate liposome preparation and preparation process thereof

A technology of picentan maleate and liposome, which is applied in the directions of liposome delivery, medical preparations of inactive ingredients, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2014-01-01
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, the patent ZL00814600.4 uses a film dispersion method to prepare BBR 2778 liposomes. This method is difficult to adapt to the scale of industrial production, and the chloroform used in its technical solution is also highly toxic and explosive, so its preparation process is not industrialized. potential

Method used

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  • Pixantrone maleate liposome preparation and preparation process thereof
  • Pixantrone maleate liposome preparation and preparation process thereof
  • Pixantrone maleate liposome preparation and preparation process thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0053] Example 1 BBR 2778 liposome

[0054] The composition of liposome membrane material was HSPC:CH:mPEG2000-DSPE=3:1:1 (w / w), and the gradient building material was citric acid-sodium citrate solution (200 mM concentration, pH 4.0).

[0055] In a water bath at 60~65°C, dissolve the membrane materials (ie HSPC, CH and mPEG) with ethanol 2000 -DSPE mixture), the ratio of the weight of phospholipids to the volume of ethanol is about 1:2, after evaporating part of the ethanol, inject a gradient material solution preheated to the same temperature at a medium speed, and incubate for 20 min to obtain liposomes The primary product was initially mixed with 200 W ultrasonic for 2 min, then dispersed by 400 W ultrasonic for 4 min (working for 1 s, intermittent for 1 s), and then passed through 0.8 and 0.45 μm microporous membranes to obtain a blank liposome suspension. liquid. Take some blank liposome suspension, add appropriate amount of Na 3 PO 4 Solution (concentration: 500 ...

Embodiment 2

[0057] The liposome membrane material was DSPC:CH=2:1 (w / w), and the gradient building material solution was malic acid-sodium malate solution (concentration: 100 mM, pH: 4.0).

[0058] In a water bath at 50°C, dissolve the prescribed amount of membrane material with ethanol. The ratio of the weight of phospholipids to the volume of ethanol is about 1:6. After waving off part of the ethanol, inject a gradient material solution preheated to the same temperature at a medium speed and incubate for 20 min, the primary product of liposome was prepared, after 200 W ultrasonic initial mixing treatment for 2 min, 400 W ultrasonic dispersion for 4 min (working for 1 s, intermittent for 1 s), passing through 0.8 and 0.45 μm microporous membranes successively, that is Obtain blank liposome suspension. Take some blank liposome suspension, add appropriate amount of Na 3 PO 4 Solution (concentration: 500 mM) and sterilized water for injection, mix evenly, adjust the pH of the outer aqueo...

Embodiment 3

[0060] The liposome membrane material was the same as that in "Example 1", and the materials used for gradient establishment were tartaric acid-sodium tartrate solution (200 mM, pH 4.0) and sodium dihydrogen phosphate solution (200 mM, pH 4.0). The preparation process of the liposome primary product is the same as "Example 1". The liposome primary product is treated with micro-jet (12000 psi for 2 cycles, 14000 psi for 2 cycles), and then through 0.8, 0.45, 0.22 , 0.10, 0.05 μm microporous membranes to obtain a blank liposome suspension. Use Na 3 PO 4 (500 mM) adjust the pH value of the blank liposome suspension to 8.0, and mix the gradient liposome suspension with BBR 2778 solution (concentration of 4.0 mg / mL) at a ratio of drug to lipid 1:15 (w / w) Mix, incubate with stirring in a water bath at 60-65°C for 20 min, then take it out and place it in an ice-water bath to stop drug loading to obtain BBR 2778 liposomes. The encapsulation efficiency of BBR 2778 liposomes obtained...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and discloses a pixantrone maleate liposome preparation and a preparation process thereof. The preparation is prepared from pixantrone maleate, phospholipid, cholesterol and a gradient establishment substance. The preparation process comprises: preparing a blank liposome, preparing a gradient liposome, loading a drug, and other steps. According to the present invention, the preparation process is simple and easy to perform, the obtained preparation has characteristics of good stability and high encapsulation efficiency, tumor targeting of drugs can be increased, and toxic-side effects of drugs can be reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a picantine maleate liposome preparation and a preparation process thereof. Background technique [0002] Pixantrone is a new generation of anthracycline antibiotics, which has a similar structure and comparable antitumor activity to mitoxantrone, and has less cardiotoxicity. It can be embedded between DNA bases to block DNA synthesis and transcription, resulting in cross-linking of DNA chains and damage to the chain structure; at the same time, it can inhibit the activity of type II topoisomerase, resulting in the disintegration of genomic DNA. The present pharmaceutical form of this compound is its maleate salt, picantron maleate (BBR 2778, CAS No. 144675-97-8). The drug was initially synthesized by researchers Miles P. Hacker and Paul A. Krapcho of the University of Vermont and subjected to in vitro cytotoxicity experiments. It was later developed by Ita...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/473A61K47/28A61P35/00
Inventor 邓意辉翟文君骆翔佘振南欧瀚杰
Owner SHENYANG PHARMA UNIVERSITY
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