Icatibant composition for injection and preparation method and preparation thereof

A technology for icatibant and injection, which is applied in the field of medicine, can solve problems such as high production cost, complex production line, and high product price, and achieve the effect of safe excipients and maintaining stability

Inactive Publication Date: 2014-09-17
ADLAI NORTYE BIOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

During the preparation of the existing icatibant injection for long-term storage, particle precipitation and discoloration will occur, which is more likely to cause the degradation of icatibant, resulting in an excessively high i

Method used

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  • Icatibant composition for injection and preparation method and preparation thereof
  • Icatibant composition for injection and preparation method and preparation thereof
  • Icatibant composition for injection and preparation method and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Preparation of icatibant injection composition

[0042] Weigh 30.0mg icatibant, 60.0mg freeze-dried protectant (mannitol) and 60.0mg solubilizer and stabilizer (glucose) in a sterile container, stir to dissolve the mixture with 1mL of water for injection, stir to dissolve, then use acetic acid Adjust the pH to 5.5, continue to dilute the volume to 3 mL with water for injection, filter with a 0.22μm microporous membrane under aseptic conditions, and freeze-dry to obtain it.

[0043] The freeze-drying process is as follows: ①In the pre-freezing stage, the sample reaches the set temperature of -25°C within half an hour and maintained for 2 hours, and then the sample reaches the pre-freezing temperature of -55°C within half an hour and maintained for 2 hours; ②Freezing sublimation In the primary drying stage, the sample will reach the set temperature of -10°C within 1 minute and maintain it for 25 hours; ③The freeze-sublimation secondary drying stage will bring the sam...

Embodiment 2

[0044] Example 2 Preparation of icatibant injection composition

[0045] Weigh 30.0mg icatibant, 60.0mg freeze-dried protectant (glucose) and 60.0mg solubilizer and stabilizer (sucrose) in a sterile container, stir to dissolve the mixture with 1mL water for injection, stir to dissolve, adjust with acetic acid The pH value is 5.5. Continue to dilute the volume to 3 mL with water for injection, filter with a 0.22μm microporous membrane under aseptic conditions, and freeze-dry it.

[0046] The freeze-drying process is as follows: ①In the pre-freezing stage, the sample reaches the set temperature of -25°C within half an hour and maintained for 2 hours, and then the sample reaches the pre-freezing temperature of -55°C within half an hour and maintained for 2 hours; ②Freezing sublimation In the primary drying stage, the sample will reach the set temperature of -10°C within 1 minute and maintain it for 25 hours; ③The freeze-sublimation secondary drying stage will bring the sample to the s...

Embodiment 3

[0047] Example 3 Preparation of icatibant injection composition

[0048] Weigh 30.0mg icatibant, 60.0mg freeze-dried protectant (sucrose) and 60.0mg solvent-promoting and stabilizer (glycerin) in a sterile container, stir to dissolve the mixture with 1mL water for injection, stir to dissolve, adjust with acetic acid The pH value is 5.5. Continue to dilute the volume to 3 mL with water for injection, filter with a 0.22μm microporous membrane under aseptic conditions, and freeze-dry it.

[0049] The freeze-drying process is as follows: ①In the pre-freezing stage, the sample reaches the set temperature of -25°C within half an hour and maintained for 2 hours, and then the sample is reached to the pre-freezing temperature of -55°C within half an hour and maintained for 2 hours; ②Freezing sublimation In the primary drying stage, the sample will reach the set temperature of -10°C within 1 minute and maintained for 25 hours; ③The freeze-sublimation secondary drying stage will bring the sam...

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Abstract

The invention relates to the technical field of medicine, and in particular relates to an Icatibant composition for injection and a preparation method and a preparation thereof. Icatibant composition for injection includes Icatibant, a freeze-drying protective agent, a cosolvent and stabilizer, and a pH regulator, wherein the mass ratio of Icatibant, the freeze-drying protective agent and the cosolvent and stabilizer is 1:(1-100):(1-100). The freeze-drying protective agent ensures that Icatibant does not degrade in the preparation and preservation processes; the cosolvent and stabilizer not only solves the problem of easy precipitation of Icatibant in solution state, but also plays the role of accelerating the re-dissolution of the freeze-dried injection powder preparation; the pH regulator can regulate the pH value of the Icatibant composition for injection after re-dissolution, and further maintains the stability of Icatibant. The Icatibant composition for injection provided by the invention has good stability, simple and reasonable formula and good re-dissolution performance, and can be prepared into the freeze-dried injection powder without being prepared into a pre-filled syringe; and the production process is simple.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to an icatibant injection composition and a preparation method and preparation thereof. Background technique [0002] Icatibant, the English name: Icatibant, is a decapeptide containing 5 non-protein-derived amino acids. The structural formula is as follows: [0003] [0004] The peptide sequence is: H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH. [0005] Hereditary angioedema (HAE), also known as C1 inhibitor deficiency, is a rare autosomal dominant genetic disease caused by genetic defects, with an incidence of 1 / 50000~1 / 10000. HAE is characterized by unpredictable episodic edema and swelling of the hands, feet, face, throat, and abdomen, leading to disfigurement, disability or death. Patients usually have a family history of the disease. HAE patients may develop rapid edema of the hands, feet, limbs, face, intestines, larynx, or trachea, which may cause respiratory tract ...

Claims

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Application Information

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IPC IPC(8): A61K38/08A61K9/19A61K47/26A61K47/10A61K47/42A61K47/36A61K47/34A61K47/02A61K47/18A61K47/22A61K47/12
Inventor 叶晓峰何南海林晓峰杨东晖路杨
Owner ADLAI NORTYE BIOPHARMA CO LTD
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