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
View PDF9 Cites 0 Cited by
  • 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 do

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

Example Embodiment

[0026] Example 1-6 Docetaxel Nanoparticles

[0027]

[0028] Preparation:

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

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

[0031] (3) Dialyze solution B using a dialysis bag for 4-8h, replace the outer dialysate solution every 2h, and vacuum dry the nano-microspheres in the obtained bag to obtain the final product.

[0032] Examples 1-6 are the screening and optimization process of drug-carrying materials. The encapsulation efficiency is greater than 80%, and the drug-loading capacity is greater than 35%. The encapsulation efficiency and drug-loading capacity of the docetaxel nano-microspheres in Example 2 are higher. Better than Example 1 and E...

Example Embodiment

[0033] Example 7-14 Docetaxel Nanospheres

[0034]

[0035]

[0036] Preparation:

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

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

[0039] (3) Dialyze solution B using a dialysis bag for 4-8h, replace the outer dialysate solution every 2h, and vacuum dry the nano-microspheres in the obtained bag to obtain the final product.

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

Example Embodiment

[0041] Example 15-21 Docetaxel Nanospheres

[0042]

[0043]

[0044] Preparation:

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

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

[0047] (3) Dialyze solution B using a dialysis bag for 4-8h, replace the outer dialysate solution every 2h, and vacuum dry the nano-microspheres in the obtained bag to obtain the final product.

[0048] Examples 15-21 are to screen the esterification degree of the drug-carrying material esterified pectin. In the experiment, the esterified pectin with an esterification degree of 60%-75% has a better shape in the preparation process, and is not easy to aggregate and coagulate. Happening.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap