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
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  • 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...

Method used

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  • 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 ...

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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

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Application Information

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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
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