Unlock instant, AI-driven research and patent intelligence for your innovation.

A kind of cabazitaxel injection and preparation method thereof

A technology for cabazitaxel and injection, which is applied to pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. question

Active Publication Date: 2019-09-13
SICHUAN KELUN PHARMA RES INST CO LTD
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The inventor found in the process of preparing large quantities of cabazitaxel injections that although the cabazitaxel concentrate provided in the latter stage can ensure stability and safety, during the preparation of such a cabazitaxel concentrate, When polysorbate 80 and cabazitaxel are directly mixed, dissolved and stirred evenly, because polysorbate 80 is a viscous liquid, it is not only difficult to stir and dissolve, but also the dissolved mixed solution is not easy to filter, and it is also very difficult to pack it into a container. The loss of raw materials is large, and the preparation method is difficult

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
  • A kind of cabazitaxel injection and preparation method thereof
  • A kind of cabazitaxel injection and preparation method thereof
  • A kind of cabazitaxel injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] The cabazitaxel injection was basically prepared according to the method of Example 7, but samples were taken at different time points of freeze-drying to detect the residual amount of absolute ethanol, and different residual amounts of absolute ethanol cabazitaxel injection were obtained, which were respectively samples 1, Sample 2, sample 3, and sample 4 were placed under the conditions of influencing factors (high temperature 60 degrees, light (illumination intensity 4500lx±500lx), room temperature) for 10 days, and compared the residual ethanol content of samples on day 0 and day 10 and the The results of single impurity and total impurity content are shown in Table 1.

[0101] Table 1 Stability results of four samples with different ethanol residues

[0102]

[0103] It can be seen from Table 1 that after being placed at room temperature for 10 days, the four samples with different ethanol residues showed no difference in related substances. ; Under high temper...

Embodiment 2

[0106] The cabazitaxel injection was prepared basically according to the method of Example 8, the difference was that different amounts of citric acid were added to adjust the pH value of the injection, and the amounts of citric acid added to samples 1-5 were 0, 0.15 g, 0.25 g, 0.4 g, respectively. g, 0.5 g, the pH values ​​of polysorbate 80 after adding citric acid were: 6.5, 3.67, 3.50, 3.29, 3.19, and the pH values ​​of the finally obtained injections are shown in Table 2.

[0107] Place different samples under the conditions of high temperature 60 degrees, light, and room temperature to investigate the stability, and obtain the single impurity content and total impurity content of the sample at 0 days, see Table 2, and the single impurity content and total impurity content of the sample at 10 days, see table 3.

[0108] Table 2 Results of Stability Investigation of Cabazitaxel Injection with Different pH Values ​​(Day 0)

[0109]

[0110] The stability investigation re...

Embodiment 3

[0114] The quality detection of embodiment 3 cabazitaxel injection

[0115] Carry out cabazitaxel preparation according to the raw material prescription of table 4, the preparation method of cabazitaxel injection is as follows:

[0116] (1) Take table 4 polysorbate 80 and citric acid, join citric acid in the polysorbate 80 solution and stir to disperse evenly, dissolve completely, the add-on of citric acid is to make the pH value of polysorbate 80 be controlled at Between 3.3 and 3.8;

[0117] (2) The absolute ethanol that takes the prescription amount of Table 4 is added to the above-mentioned uniformly dispersed polysorbate 80 solution and stirred until uniformly dispersed;

[0118] (3) Weigh the cabazitaxel raw material according to the prescription amount, add it to the solution obtained in step (2), and stir until completely dissolved;

[0119] (4) Add activated carbon accounting for 0.05% (W / W) of the total solution to the solution obtained in step 2, stir and adsorb f...

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
melting pointaaaaaaaaaa
boiling pointaaaaaaaaaa
Login to View More

Abstract

The invention relates to a cabazitaxel injection and a preparation method thereof. The cabazitaxel injection is prepared from cabazitaxel, polysorbate 80, absolute ethyl alcohol and an appropriate amount of citric acid serving as a pH regulator, wherein a weight ratio of polysorbate 80 to absolute ethyl alcohol is 0.5-3:1, and a weight ratio of polysorbate 80 to cabazitaxel is 10-56:1. By specific raw material adding proportions, raw material adding sequence, pH value regulation, nitrogen filled protection and the like according to the preparation method, the prepared cabazitaxel injection is low in total impurity content, colorless and clear in appearance and high in stability. According to accidental discoveries, in a preparation process of the cabazitaxel injection, a feeding ratio of polysorbate to absolute ethyl alcohol can be adjusted to make solution nonviscous so as to facilitate subsequent filter operations, and accordingly difficulty of the preparation method is lowered, and the preparation method is easy to operate and complete.

Description

technical field [0001] The invention relates to a paclitaxel pharmaceutical preparation, in particular to a cabazitaxel injection and a preparation method thereof. Background technique [0002] Prostate cancer is the most common malignant tumor of the male reproductive system. The incidence increases with age, and its incidence has obvious regional differences. The incidence is higher in Europe and the United States, and lower in Asia. The morbidity and mortality of prostate cancer are second only to lung cancer, ranking second in cancer death. Prostate cancer, which develops slowly in older men in most cases, is less common in Asia than in Western countries but has been rising rapidly in recent years. [0003] According to statistics from the American Cancer Society, prostate cancer accounts for a quarter of newly diagnosed cancer cases in the United States each year. In 2010, there were about 220,000 prostate cancer patients diagnosed, and more than 32,000 patients died o...

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
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/337A61K47/22A61K47/10A61K47/12A61P35/00
Inventor 朱朝清熊冠军赵栋何苗高国玉王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD