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Docetaxel for injection and preparation method thereof

A technology for docetaxel and injection, which is applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc., can solve the problems of low stability of nano-microspheres and improve the encapsulation efficiency and drug loading, optimizing pH regulation, and enhancing stability

Active Publication Date: 2022-01-28
THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] has overcome the deficiencies in the prior art, the present invention provides a kind of docetaxel nano microspheres, utilizes modified pectin to carry docetaxel, and screens the modified The type of pectin and the ratio of pectin to docetaxel are optimized for the preparation method, which solves the problem of low stability of nano-microspheres, improves the encapsulation efficiency and drug loading capacity of nano-microspheres, and reduces the content of related substances

Method used

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  • Docetaxel for injection and preparation method thereof
  • Docetaxel for injection and preparation method thereof
  • Docetaxel for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0026] Embodiment 1-6 docetaxel nano microspheres

[0027]

[0028] Preparation:

[0029] (1) dissolving the carrier material in a glycine-citric acid buffer solution with a pH of 4.0 at 30-40° C., adding 20 ml of dimethyl sulfoxide to aid dissolution, and preparing a 1%-5% solution to obtain a solution A;

[0030] (2) Slowly add docetaxel to solution A while stirring, and stir and reflux in a water bath at 25-30°C for 1-1.5h to obtain solution B;

[0031] (3) The solution B is dialyzed for 4-8 hours with a dialysis bag, and the outer solution of the dialysis is replaced every 2 hours, and the obtained nano-microspheres in the bag are vacuum-dried to obtain the final product.

[0032] Embodiment 1-6 is the screening optimization process to drug-loaded material, and its encapsulation efficiency is all greater than 80%, and drug loading capacity is all greater than 35%, and the docetaxel nano-microsphere encapsulation efficiency and drug loading capacity of embodiment 2 are ...

Embodiment 7-14

[0033] Embodiment 7-14 docetaxel nano microspheres

[0034]

[0035]

[0036] Preparation:

[0037] (1) dissolving the carrier material in a glycine-citric acid buffer solution with a pH of 4.0 at 30-40° C., adding 20 ml of dimethyl sulfoxide to aid dissolution, and preparing a 1%-5% solution to obtain a solution A;

[0038] (2) Slowly add docetaxel to solution A while stirring, and stir and reflux in a water bath at 25-30°C for 1-1.5h to obtain solution B;

[0039] (3) The solution B is dialyzed for 4-8 hours with a dialysis bag, and the outer solution of the dialysis is replaced every 2 hours, and the obtained nano-microspheres in the bag are vacuum-dried to obtain the final product.

[0040] Examples 7-14 are experimental screening of the dosage ratio of docetaxel and esterified pectin in docetaxel nano-microspheres, the encapsulation efficiency is greater than 80%, and finally found that the weight ratio of docetaxel and esterified pectin In the range of 1:2-5, the...

Embodiment 15-21

[0041] Embodiment 15-21 docetaxel nano microspheres

[0042]

[0043]

[0044] Preparation:

[0045] (1) dissolving the carrier material in a glycine-citric acid buffer solution with a pH of 4.0 at 30-40° C., adding 20 ml of dimethyl sulfoxide to aid dissolution, and preparing a 1%-5% solution to obtain a solution A;

[0046] (2) Slowly add docetaxel to solution A while stirring, and stir and reflux in a water bath at 25-30°C for 1-1.5h to obtain solution B;

[0047] (3) The solution B is dialyzed for 4-8 hours with a dialysis bag, and the outer solution of the dialysis is replaced every 2 hours, and the obtained nano-microspheres in the bag are vacuum-dried to obtain the final product.

[0048] Examples 15-21 are to screen the degree of esterification of the drug-loaded material esterified pectin. In the experiment, the esterified pectin with a degree of esterification of 60%-75% has a better shape during the preparation process and is less prone to aggregation and coa...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to docetaxel for injection and a preparation method thereof. According to the invention, the drug carrier is utilized to encapsulate the cetaxel in a self-assembly manner to form a nano-microsphere intermediate with the particle size of 50-350 nm, so that the stability is improved, and the cetaxel is further prepared into an injection; the modified pectin bears docetaxel, and the variety of the modified pectin and the proportion of the modified pectin to the docetaxel are screened to optimize the preparation method. The problem of low stability of the nano-microspheres is solved, the encapsulation efficiency and the drug loading capacity of the nano-microspheres are improved, and the content of related substances is reduced.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a docetaxel for injection and a preparation method thereof, more particularly to a docetaxel nano-microsphere for injection and a preparation method thereof. Background technique [0002] Docetaxel is a paclitaxel derivative synthesized during the structural modification of paclitaxel. It is a semi-synthetic taxane antineoplastic drug. Its effect is the same as that of paclitaxel. It is a cycle-specific drug in the M phase and promotes the polymerization of tubules into stable microtubules. And inhibit its aggregation, thereby significantly reducing the number of small tubules, and can destroy the microtubule network structure, and has a good effect on advanced breast cancer, ovarian cancer, and non-small cell lung cancer. It also has a certain effect on head and neck cancer, pancreatic cancer, small cell lung cancer, gastric cancer, melanoma, and soft tissue sa...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/337A61K47/36A61K47/38A61P35/00B82Y5/00B82Y40/00
CPCA61K31/337A61K9/0019A61K9/5161A61P35/00B82Y5/00B82Y40/00
Inventor 孙浩樊锐太刘俊启常宇于吉峰
Owner THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV
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