Taxdol self assembled precusor liposome and its preparation method

A proliposome and self-assembly technology, which is applied in liposome delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of poor stability of preparation quality, incomplete local dissolution, complex preparation process, etc., and achieve stable product quality , stable and controllable quality, simple process effect

Active Publication Date: 2006-08-30
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 1. The preparation process is complicated, prone to bacterial contamination, poor reproducibility, difficult to industrialized large-scale production, and high manufacturing cost
[0007] 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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  • Taxdol self assembled precusor liposome and its preparation method
  • Taxdol self assembled precusor liposome and its preparation method
  • Taxdol self assembled precusor liposome and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] prescription:

[0062] Paclitaxel 0.6g

[0063] Soy Lecithin 37.5g

[0064] Polyoxyethylene hydrogenated castor oil (Cremophor RH40) 18.75g

[0065] Cholesterol 2.5g

[0066] Ethanol to 100ml

[0067] Preparation process: according to figure 1 As shown in the process flow chart, dissolve the prescribed amount of soybean lecithin in an appropriate amount of ethanol, then add the prescribed amount of drug, polyoxyethylene hydrogenated castor oil Cremophor RH40, cholesterol and the remaining amount of ethanol, and wait until the drug and other components are completely dissolved , 0.22 μm microporous membrane filter to sterilize, under aseptic conditions, the filtrate is sealed in nitrogen-filled ampoules or vials to obtain paclitaxel self-assembled proliposomes.

[0068] Adding the prepared paclitaxel self-assembled proliposomes to 50 times the amount (v / v) of 5% glucose injection can quickly form a paclitaxel liposome solution with an average particle size of 95 %...

Embodiment 2

[0070] prescription:

[0071] Paclitaxel 0.6g

[0072] Egg phospholipids 16.7g

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

[0074] PEG400 3.33g

[0075] Propylene glycol 25ml

[0076] Ethanol to 100ml

[0077] Preparation process: Dissolve the prescribed amount of 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 to obtain the paclitaxel self-assembled proliposome.

[0078] Adding the prepared paclitaxel self-assembled proliposomes to 75 times the amount (v / v) of sodium chloride injection can quickly form a paclitaxel liposome solution with an average particle size of 90 %.

Embodiment 3

[0080] prescription:

[0081] Paclitaxel 0.6g

[0082]Soy Lecithin 15g

[0083] Polyoxyethylene (23) lauryl ether 20.7g

[0084] Benzyl alcohol 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 to obtain paclitaxel self-assembled proliposomes.

[0088] Adding the prepared paclitaxel self-assembled proliposome to 25 times the volume (v / v) of water for injection can quickly form a paclitaxel liposome solution with an average particle size of 90%.

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Abstract

A self-assembled precursor liposome of taxusol is proportionally prepared from tausol, 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 self-assembled proliposome containing an insoluble anticancer drug paclitaxel, and also relates to a preparation method of the self-assembled proliposome. Background technique [0002] Paclitaxel is a unique diterpenoid anticancer compound extracted from the bark of Yew brevifolia. Paclitaxel stabilizes tubulin polymers and promotes microtubule assembly. Paclitaxel has been reported to be useful in the treatment of breast cancer, non-small cell lung cancer, head and neck cancer, and refractory ovarian cancer. [0003] Since the solubility of paclitaxel in water is 0.006mg / ml, it can be regarded as insoluble in water. The key to its intravenous infusion formulation is to solve its solubility in water. Paclitaxel injections currently on the market are solubilized by surfactants and diluted for use. For example, the current clinical application of paclitaxel injection ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/34A61K31/337A61P35/00A61K47/10A61K47/14A61K47/26A61K47/44
Inventor 周建平仝新勇谭燕张惠谢俊徐向阳曹春陵陈振飞
Owner CHINA PHARM UNIV
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