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Poly olefinic taxadol self assembled precusor liposome and its preparation method

A technology of proliposome and docetaxel, which is applied in the direction of liposome delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of incomplete local dissolution, poor preparation quality stability, poor reproducibility, etc., to achieve safety and Ease of purchase, stable product quality, stable and controllable quality effects

Active Publication Date: 2009-05-13
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 1. The preparation process is complicated, prone to bacterial contamination, poor reproducibility, difficult to industrialized large-scale production, and high manufacturing cost
[0006] 2. Poor preparation quality stability
In view of the fact that in the process of preparing solid proliposomes, the process of removing organic solvents is the main technical bottleneck to realize industrialization, and the hydration process of solid proliposomes will also objectively have a slow hydration rate and incomplete local dissolution , uneven dispersion and other problems, which lead to difficult effective control of main quality indicators such as drug encapsulation rate and average particle size, and difficult to meet the requirements of clinical use. So far, no such preparations have been marketed
In the existing published patents, research literature and reports on the preparation of liposomes and proliposomes, no preparation technology directly using liquid self-assembled proliposomes has been found.

Method used

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  • Poly olefinic taxadol self assembled precusor liposome and its preparation method
  • Poly olefinic taxadol self assembled precusor liposome and its preparation method
  • Poly olefinic taxadol self assembled precusor liposome and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] prescription:

[0062] Docetaxel 2g

[0063] Egg phospholipids 27.5g

[0064] Tween 80 12.5g

[0065] Cholesterol 1g

[0066] Add ethanol to 100ml

[0067] Preparation process: according to figure 1 The process flow shown (the same below) dissolves the prescribed amount of lecithin in an appropriate amount of ethanol, then adds the prescribed amount of docetaxel, Tween 80, cholesterol and the remaining amount of ethanol, and after the drug and other components are completely dissolved , 0.22 μm microporous membrane filter to sterilize, under aseptic conditions, the filtrate is sealed in a nitrogen-filled ampoule or a vial to obtain the docetaxel self-assembled proliposome.

[0068] The prepared docetaxel self-assembled proliposomes are added to 50 times the amount (v / v) of 5% glucose injection, and the docetaxel liposome solution can be formed rapidly, with an average particle diameter of 95%.

Embodiment 2

[0070] prescription:

[0071] Docetaxel 2g

[0072] Soy Lecithin 16.7g

[0073] Polyoxyethylene castor oil (Cremophor EL) 16.7g

[0074] PEG400 3.33g

[0075] Propylene glycol 30ml

[0076] Add ethanol to 100ml

[0077] Preparation process: dissolve the prescribed amount of soybean lecithin in an appropriate amount of ethanol, then add the prescribed amount of drug, polyoxyethylene castor oil Cremophor EL, PEG400, propylene glycol and the remaining amount of ethanol, after the drug and other components are completely dissolved, The 0.22 μm microporous membrane is filtered and sterilized, and the filtrate is filled and sealed in a nitrogen-filled ampoule or a vial under aseptic conditions, that is, the docetaxel self-assembled proliposome.

[0078] Adding the prepared docetaxel self-assembled proliposomes to 25 times the amount (v / v) of water for injection can quickly form a docetaxel liposome solution with an average particle size of 90 %.

Embodiment 3

[0080] prescription:

[0081] Docetaxel 3g

[0082] Soy Lecithin 20g

[0083] Polyoxyethylene (23) lauryl ether 15.7g

[0084] Benzyl alcohol 2.2g

[0085] Isopropanol 20ml

[0086] Ethanol to 100ml

[0087] Preparation process: dissolve the prescribed amount of soybean lecithin in an appropriate amount of ethanol, then add the prescribed amount of medicine, polyoxyethylene (23) lauryl ether, benzyl alcohol, isopropanol and the remaining amount of ethanol, and wait for the medicine and other components After all the parts are dissolved, the 0.22 μm microporous membrane is filtered to sterilize, and the filtrate is filled and sealed in a nitrogen-filled ampoule or a vial under aseptic conditions, that is, the docetaxel self-assembled proliposome.

[0088] Adding the prepared docetaxel self-assembled proliposomes to 100 times the amount (v / v) of sodium chloride injection can quickly form a docetaxel liposome solution with an average particle size of 90%.

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Abstract

A self-assembled precursor liposome of polyenic taxusol is proportionally prepared from polyenic taxusol, phosphatide, polyethylene glycol and dispersing medium through mixing, dispersing, press-filtering by millipore film, and pouring it in a container full of N2.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a docetaxel self-assembled proliposome, and also relates to a preparation method of the proliposome. Background technique [0002] Docetaxel (Docetaxel) is a new generation of taxane antineoplastic drugs. Its mechanism of action is unique, and its target is in the microtubules of the cytoplasm. The most effective single-agent chemotherapy drug for small cell lung cancer (NSCLC). (Liang Xiaoli, Pharmacology and Clinical Application of Docetaxel, Capital Medicine, 1999, 6(5): 28-29). [0003] The oral bioavailability of docetaxel alone is only 8%, and making it into injection is one of the means to improve the bioavailability (Zhang Xuenong, Foreign Medicine·Pharmacy, 2002, 29(6): 321-325). Due to the low solubility of docetaxel in water, its clinical use is limited. The current commercially available docetaxel injection has relatively severe hemolysis and allergic react...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/337A61K47/24A61K47/34A61K9/127A61P35/00A61K47/10
Inventor 周建平仝新勇徐向阳谭燕范博谢俊曹春陵陈振飞
Owner CHINA PHARM UNIV
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