Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Cetrorelix acetate injection and preparation method thereof

A technology of cetrorelix acetate and injection, which is applied in the field of pharmaceutical preparations, can solve the problems of increased contact between active ingredients and rubber stoppers, increased impurities, long reconstitution time, etc., to ensure curative effect and safety, and low initial impurity level , good physical and chemical stability

Pending Publication Date: 2021-11-09
南京锐志生物医药有限公司
View PDF7 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 1. If the freeze-dried powder has an overly dense block structure, the sample in this state can effectively avoid the contact between the active ingredient and the rubber stopper, reducing the risk of impurities, but the reconstitution time is longer, and a large number of aggregates adhere to the packaging material after reconstitution The inner wall leads to a low concentration of active ingredients in the reconstituted solution, and the effective dose injected into the patient cannot be guaranteed, which affects the effectiveness of the product;
[0005] 2. If the freeze-dried powder is in a powder state, or is easily broken into a loose block structure of powder, although the reconstitution time of the sample in this state is short, the contact chance of the active ingredient and the rubber stopper is greatly increased, and there are impurities related to the rubber stopper Increased risk; and the moisture value of the sample in this state is higher than that of the block structure sample, which is more likely to produce hydrolyzed impurities of cetrorelix, which affects product safety

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
  • Cetrorelix acetate injection and preparation method thereof
  • Cetrorelix acetate injection and preparation method thereof
  • Cetrorelix acetate injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Prescription: Weigh the raw and auxiliary materials according to the prescription quantity in the following table

[0105] Cetrorelix acetate 0.27g Mannitol 27g glacial acetic acid 10g Water for Injection 1 40g Water for injection 2 350g Water for injection 3 to 500mL

[0106] Preparation Process:

[0107] 1. Mix glacial acetic acid with water for injection 1 to obtain an aqueous solution of acetic acid;

[0108] 2. Dissolve cetrorelix acetate in the acetic acid aqueous solution in step 1, add water for injection 2 and mannitol, and dissolve until clear;

[0109] 3. Dilute to the target volume with water for injection 3;

[0110] 4. Use a filter with a pore size of 0.22 μm to sterilize and filter the medicinal solution in step 3;

[0111] 5. Divide the filtered medicinal liquid into 2mL vials with a volume of about 1mL, fill with nitrogen, and half-stopper;

[0112] 6. Freeze-drying. After the freeze-drying process is ov...

Embodiment 2

[0121] Prescription: Weigh the raw and auxiliary materials according to the prescription quantity in the following table

[0122] Cetrorelix acetate 0.27g Mannitol 54g glacial acetic acid 20g Water for Injection 1 30g Water for injection 2 350g Water for injection 3 to 500mL

[0123] Preparation Process:

[0124] 1. Mix glacial acetic acid with water for injection 1 to obtain an aqueous solution of acetic acid;

[0125] 2. Dissolve cetrorelix acetate in the acetic acid aqueous solution in step 1, add water for injection 2 and mannitol, and dissolve until clear;

[0126] 3. Dilute to the target volume with water for injection 3;

[0127] 4. Use a filter with a pore size of 0.22 μm to sterilize and filter the medicinal solution in step 3;

[0128] 5. Divide the filtered medicinal liquid into 2mL vials with a volume of about 1mL, fill with nitrogen, and half-stopper;

[0129] 6. Freeze-drying. After the freeze-drying process is ov...

Embodiment 3

[0138] Prescription: Weigh the raw and auxiliary materials according to the prescription quantity in the following table

[0139] Cetrorelix acetate 0.135g Mannitol 67.5g glacial acetic acid 5g Water for Injection 1 45g Water for injection 2 350g Water for injection 3 to 500mL

[0140] Preparation Process:

[0141] 1. Mix glacial acetic acid with water for injection 1 to obtain an aqueous solution of acetic acid;

[0142] 2. Dissolve cetrorelix acetate in the acetic acid aqueous solution in step 1, add water for injection 2 and mannitol, and dissolve until clear;

[0143] 3. Dilute to the target volume with water for injection 3;

[0144] 4. Use a filter with a pore size of 0.22 μm to sterilize and filter the medicinal solution in step 3;

[0145] 5. Divide the filtered medicinal liquid into 2mL vials with a volume of about 1mL, fill with nitrogen, and half-stopper;

[0146] 6. Freeze-drying. After the freeze-drying process is ...

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

No PUM Login to View More

Abstract

The invention provides a cetrorelix acetate injection and a preparation method thereof. By controlling the pre-freezing cooling rate and the primary drying vacuum degree, the obtained freeze-dried product is a blocky solid, the phenomenon of active ingredient aggregation after redissolution is avoided, and the impurity level of the freeze-dried product is reduced. The product disclosed by the invention is low in initial moisture and controllable in key quality attribute such as moisture, turbidity, pH, purity and the like in the storage process, and effectiveness and safety are better guaranteed.

Description

technical field [0001] The invention relates to a cetrorelix acetate injection and a preparation method thereof, in particular to a freeze-drying process that can significantly improve the physical and chemical stability of the product, and belongs to the field of pharmaceutical preparations. Background technique [0002] Cetrorelix acetate is a gonadotropin-releasing hormone (GnRH) antagonist developed by Asta Medica in Germany. It controls luteinizing hormone (LH) and stimulating hormone by competing with endogenous GnRH to bind to membrane receptors on pituitary cells. The release of follicle hormone (FSH), thereby controlling the stimulation of the ovary, preventing premature discharge of immature follicles, and helping conception. Studies have shown that cetrorelix acetate has a good curative effect on ovarian cancer, prostate cancer, uterine fibroids, endometriosis and other diseases, and can prevent and improve benign prostatic hypertrophy and ovarian hyperstimulation...

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): A61K38/09A61K9/19A61K47/12A61P15/08A61P35/00A61P15/00A61P13/08
CPCA61K38/09A61K9/19A61K9/0019A61K47/12A61P15/08A61P35/00A61P15/00A61P13/08
Inventor 孙蕴哲沙向阳万琴徐丽叶仕春
Owner 南京锐志生物医药有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com