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A kind of liposome preparation of picantron maleate and its preparation process

A technology of picentan maleate and liposome, which is applied in the directions of liposome delivery, medical preparations of inactive ingredients, antitumor drugs, etc. , difficult to adapt to scale and other issues

Inactive Publication Date: 2016-08-03
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 adopts the film dispersion method to prepare BBR2778 liposomes, which is difficult to adapt to the scale of industrial production, and the chloroform used in its technical solution also has greater toxicity and explosiveness, so its preparation process does not have industrialization potential

Method used

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  • A kind of liposome preparation of picantron maleate and its preparation process
  • A kind of liposome preparation of picantron maleate and its preparation process
  • A kind of liposome preparation of picantron maleate and its preparation process

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Embodiment 1BBR2778

[0051] Embodiment 1BBR2778 liposome

[0052] The composition of liposome membrane material is HSPC:CH:mPEG2000-DSPE=3:1:1 (w / w), and the substance for establishing gradient is citric acid-sodium citrate solution (concentration: 200mM, pH: 4.0).

[0053] 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 waving off part of the ethanol, inject a gradient material solution preheated to the same temperature at a medium speed to establish a substance solution, and incubate for 20min to obtain the initial liposome The product was initially mixed with 200W ultrasonic for 2min, then dispersed with 400W ultrasonic for 4min (working for 1s, intermittent for 1s), and passed through 0.8 and 0.45μm microporous membranes in sequence to obtain a blank liposome suspension. Take some blank liposome suspension, add appropriate amount of Na 3 PO...

Embodiment 2

[0055] The liposome membrane material is DSPC:CH=2:1 (w / w), and the gradient building material solution is malic acid-sodium malate solution (concentration: 100mM, pH: 4.0).

[0056] In a 50°C water bath, 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 minutes. , the primary product of liposome was prepared, after 2 minutes of preliminary mixing treatment with 200W ultrasonic wave, 400W ultrasonic dispersion for 4 minutes (working for 1 s, intermittent for 1 s), passing through 0.8 and 0.45 μm microporous membranes in turn to obtain a blank liposome suspension liquid. Take some blank liposome suspension, add appropriate amount of Na 3 PO 4 Solution (concentration: 500mM) and sterilized water for injection, mix evenly, adjust the pH of ...

Embodiment 3

[0058] The liposome membrane material is the same as in "Example 1", and the gradient building materials are selected from tartaric acid-sodium tartrate solution (200mM, pH 4.0) and sodium dihydrogen phosphate solution (200mM, 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 (12000psi for 2 cycles, 14000psi for 2 cycles), and then through 0.8, 0.45, 0.22, 0.10 , 0.05 μm microporous membrane to obtain a blank liposome suspension. Use Na 3 PO 4 (500mM) to adjust the pH value of the blank liposome suspension to 8.0, and mix the gradient liposome suspension with the BBR2778 solution (concentration: 4.0mg / mL) at a ratio of drug to lipid of 1:15 (w / w), Stir and incubate in a water bath at 60-65°C for 20 minutes, then take it out and place it in an ice-water bath to stop drug loading to obtain BBR2778 liposomes. Use tartaric acid-sodium tartrate solution as gradient to establish the ...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and discloses a liposome preparation of picantron maleate and a preparation process thereof. The preparation is prepared from picantecone maleate, phospholipids, cholesterol and gradient building substances. The preparation process includes the steps of preparing blank liposomes, gradient liposomes, loading drugs and the like. The preparation process is simple and easy, the obtained preparation has good stability and high encapsulation efficiency, and can improve the tumor targeting property of the medicine and reduce its toxic and side effects.

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 (BBR2778, CAS No. 144675-97-8). The drug was originally synthesized by researchers MilesP.Hacker and PaulA.Krapcho of the University of Vermont and subjected to in vitro cytotoxicity experiments. It was later developed by Italian...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/473A61K47/28A61P35/00
Inventor 邓意辉翟文君宋冠杉骆翔佘振南欧瀚杰
Owner SHENYANG PHARMA UNIVERSITY
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