Micelle containing taxane drugs as well as preparation method and application of thereof

A taxane and micelle technology, applied in the field of medicine, can solve the problems of ineffective preparation, high drug loading and the like, and achieve the effects of reducing systemic side effects, good stability and high stability

Pending Publication Date: 2022-01-11
SHANGHAI WHITTLONG PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved by the present invention is to overcome the problem that the prior art cannot effectively prepare taxane drug nanomicelle preparations with high drug loading, high encapsulation efficiency and good stability; Micelle of alkanes drug, its preparation method and application

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  • Micelle containing taxane drugs as well as preparation method and application of thereof
  • Micelle containing taxane drugs as well as preparation method and application of thereof
  • Micelle containing taxane drugs as well as preparation method and application of thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] Example 1 Preparation and Stability Investigation of Docetaxel Nano-micelle Preparation

[0088] See Table 1 for the prescription:

[0089] Table 1 Example 1 Docetaxel nano-micelle preparation prescription

[0090] drug Lipid / drug (mass ratio) Drug concentration (mg / mL) Hydration solvent Docetaxel 15:1 6 Deionized water Docetaxel 5:1 6 Deionized water

[0091] Preparation process: Weigh docetaxel and polyethylene glycol 2000 distearoylphosphatidylethanolamine (PEG2000-DSPE, purchased from Avanti Company) according to the above prescription ratio and place them in a rotary steamer bottle, add an appropriate amount of ethanol and shake gently to make the drug and lipids can be completely dissolved to obtain a clear and transparent solution. Drain the organic solvent in the rotary evaporator on a vacuum rotary evaporator with a rotation speed of 90r / min and a water bath temperature of 40°C. After the organic solvent is drained, the li...

Embodiment 2

[0094] Example 2: Preparation and Stability Investigation of Cabazitaxel Nano-micelle Preparation

[0095] See Table 2 for the prescription:

[0096] Table 2 embodiment 2 cabazitaxel nano-micelle preparation prescription

[0097] drug Lipid / drug (mass ratio) Drug concentration (mg / mL) Hydration solvent Cabazitaxel 10:1 8 Deionized water

[0098] Preparation process: weigh cabazitaxel and polyethylene glycol 2000 distearoylphosphatidylethanolamine according to the above prescription ratio and place them in a rotary steamer, add an appropriate amount of ethanol and gently shake to dissolve the drug and lipids, and obtain a clear and transparent solution. Drain the organic solvent in the rotary evaporator on the vacuum rotary evaporator, the rotation speed is 90r / min, and the temperature of the water bath is 40°C. After the organic solvent is drained, the lipids and drugs are evenly distributed on the inner wall of the rotary evaporator, and then the...

Embodiment 3

[0099] Example 3: The encapsulation efficiency of paclitaxel nanomicelle is high, but the stability is poor and cannot meet the needs of clinical medication

[0100] See Table 3 for the prescription:

[0101] Table 3 Example 3 paclitaxel nanomicelle preparation prescription

[0102] drug Lipid / drug (mass ratio) Drug concentration (mg / mL) Hydration solvent paclitaxel 15:1 5 Deionized water

[0103] Preparation process: Weigh paclitaxel and polyethylene glycol 2000 distearoylphosphatidylethanolamine according to the above prescription ratio and put them in a rotary steamer, add an appropriate amount of ethanol and shake gently to dissolve the drug and lipids to obtain a clear and transparent solution, and rotate in a vacuum Drain the organic solvent in the rotary evaporator on the evaporator, the speed is 90r / min, and the temperature of the water bath is 40°C. After the organic solvent is drained, the lipids and drugs are evenly distributed on the i...

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Abstract

The invention discloses micelle containing taxane drugs, and a preparation method and application thereof. The invention provides a micelle containing a substance A, which comprises the following components in parts by weight: 1 part of the substance A and 5-25 parts of polyethylene glycol derivatized phospholipid; the substance A is docetaxel and / or cabazitaxel, the polyethylene glycol derivative phospholipid comprises a polyethylene glycol part and a phospholipid part, and the phospholipid part is di (C12-C24 fatty acyl) phosphatidyl ethanolamine. The micelle containing taxane drugs can contain a therapeutically effective amount of the taxane drugs, and the drug loading capacity is as high as 6.25%-9.09%; the stability is good; and the problems in clinical application of the traditional Chinese medicine composition can be effectively solved.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a taxane-containing micelle, a preparation method and application thereof. Background technique [0002] Taxanes are a large class of natural medicines obtained from plants, and belong to diterpenoids in structural classification. Both cabazitaxel and docetaxel belong to the class of taxanes and are fat-soluble compounds. Due to their poor water solubility, short half-life and high toxicity, their clinical application is limited. At present, the docetaxel injection and cabazitaxel injection marketed at home and abroad are all dissolved in Tween-80. In clinical application, it is necessary to strictly use a special injection solvent to dilute it, and the operation requirements are strict. It is also necessary to use special infusion devices during infusion. Not only is the method of use cumbersome, but also because the preparation contains a large amount of Tween-80, it is ver...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/337A61K47/24A61K47/26A61P35/00
CPCA61K9/1075A61K31/337A61K47/24A61K47/26A61P35/00
Inventor 于继兵梁伟赵晓东王浩
Owner SHANGHAI WHITTLONG PHARMA INST
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