Cetrorelix preparation and preparation method thereof

A technology of cetrorelix and cetrorelix acetate, which is applied in the field of biomedicine, can solve problems such as poor stability, and achieve the effects of ensuring stability, shortening drying time, and reducing production costs

Pending Publication Date: 2021-05-18
南京康舟医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because most cetrorelix acetate for injection on the market has long-term storage, poor stability in accelerated tests, and a large increase in related substances, the US FDA requires its storage temperature to be 2-8°C

Method used

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  • Cetrorelix preparation and preparation method thereof
  • Cetrorelix preparation and preparation method thereof
  • Cetrorelix preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The present invention provides a kind of preparation method of cetrorelix preparation, it comprises the following steps:

[0051] (1) Prepare a mixed solution containing mannitol and cetrorelix acetate:

[0052] Table 1 raw material ratio

[0053]

[0054] According to the components shown in Table 1 and the proportioning ratio thereof, raw materials are obtained;

[0055] Add cetrorelix acetate to 30% acetic acid solution (100mL) to dissolve completely, add 600ml water for injection and mix well; then add mannitol to dissolve and mix well; add water for injection to a total volume of 1000mL to obtain Mixed solution of trerelix. The solution was filtered through a 0.2 μm filter.

[0056] (2) freezing:

[0057] Divide the mannitol and cetrorelix acetate acetic acid solution obtained in step (1) into containers (1.0 mL / cartridge), and perform the following steps:

[0058] The first stage: the cooling rate is 0.5°C / min, the temperature of the plate layer is lowered...

Embodiment 2

[0064] The present invention provides a kind of preparation method of cetrorelix preparation, it comprises the following steps:

[0065] (1) Preparation of mannitol, cetrorelix acetate acetic acid solution:

[0066] According to the components shown in Table 1 and the proportioning ratio thereof, raw materials are obtained;

[0067] Add cetrorelix acetate to 30% acetic acid solution (100mL) to dissolve completely, then add 600mL water for injection and mix well; then add mannitol to dissolve and mix well; add water for injection to a total volume of 1000mL to obtain Mixed solution of cetrorelix. The solution was filtered through a 0.2 μm filter.

[0068] (2) freezing:

[0069] Divide the obtained mannitol and cetrorelix acetate acetic acid solution (1.0mL / cartridge) into containers, and perform the following steps:

[0070] The first stage: the cooling rate is 0.5°C / min, the temperature of the plate layer is lowered to -40°C, and the holding time is 1 hour;

[0071] The s...

Embodiment 3

[0076] The present invention provides a kind of preparation method of cetrorelix preparation, it comprises the following steps:

[0077] (1) Preparation of mannitol, cetrorelix acetate acetic acid solution:

[0078] According to the components shown in Table 1 and the proportioning ratio thereof, raw materials are obtained;

[0079] Add cetrorelix acetate to 30% acetic acid solution (100mL) to dissolve completely, add 600mL water for injection and mix well; then add mannitol to dissolve and mix well; add water for injection to a total volume of 1000mL to obtain Mixed solution of trerelix. The solution was filtered through a 0.2 μm filter.

[0080] (2) freezing:

[0081] Divide the obtained mannitol and cetrorelix acetate acetic acid solution (1.0mL / cartridge) into containers, and perform the following steps:

[0082] The first stage: the cooling rate is 1°C / min, the temperature of the plate layer is lowered to -30°C, and the holding time is 1 hour;

[0083] The second sta...

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Abstract

The invention discloses a cetrorelix preparation and a preparation method thereof, and relates to the technical field of biological medicines. The preparation method comprises the steps that a mixed solution containing mannitol and cetrorelix acetate is subjected to first-stage freezing, second-stage freezing and third-stage freezing, wherein the conditions of the first stage are that after the temperature is decreased to -20 DEG C to -40 DEG C, heat preservation is conducted for 0.1-2 h; the conditions of the second stage are as follows are that the temperature is raised to -20 DEG C to -5 DEG C, heat preservation is performed for 0.1-2 hours; and the conditions of the third stage are that after the temperature is reduced to -20 DEG C to -40 DEG C, heat preservation is performed for 0.1-2 hours. According to the method, the temperature is lowered to be close to the glass transition temperature of the solution, the temperature is kept for a period of time, and the temperature is lowered again until the solution is completely frozen after the temperature is raised to a certain temperature, so that the stability of the cetrorelix preparation product can be ensured to the greatest extent. Meanwhile, after the freezing treatment, a relatively high drying temperature can be selected for drying in the drying stage, so that the product quality is not influenced, the drying time is shortened, and the production cost is reduced.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a cetrorelix preparation and a preparation method thereof. Background technique [0002] Cetrorelix is ​​a gonadotropin-releasing hormone (LHRH) antagonist developed by Germany's ASTA MEDICA company, which can control the stimulation of the ovary, prevent premature discharge of immature follicles, and help conception. It is mainly used for patients undergoing controlled ovarian stimulation to prevent premature ovulation, and then perform egg collection and assisted reproductive technology treatment. [0003] The existing patent CN94101378.2 discloses a preparation method of cetrorelix freeze-dried pharmaceutical composition. The disclosed preparation method is to dissolve cetrorelix with acetic acid, dilute with water for injection, and then add mannitol to obtain manna Alcohol, cetrorelix solution, filter the solution, and freeze-dry. The preparation method mainly solves t...

Claims

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Application Information

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IPC IPC(8): A61K38/08A61K9/19A61K47/26A61P5/24A61P15/08
CPCA61K38/08A61K9/19A61K47/26A61P5/24A61P15/08
Inventor 孙浩张瑾谢应成徐健峰苏晴
Owner 南京康舟医药科技有限公司
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