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Imipenem and cilastatin sodium sterile powder preparation for injection and preparation method thereof

A technology of cilastatin and imipenem, applied in the field of medicine, can solve the problems of difficulty in powder injection for injection, increase the dosage of auxiliary materials, increase the risk of hemolysis, etc., and achieve the effects of reducing toxic side effects, increasing solubility, and avoiding organic solvent residues

Active Publication Date: 2016-12-07
泊诺(天津)创新医药研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Imipenem and cilastatin sodium compound preparation is one of the anti-severe infection drugs with high clinical evaluation. However, due to the poor solubility of imipenem in aqueous solution, the existing domestic marketed drugs are all made of the two powders mixed. It is obtained by dispensing in large infusion bottles. It is difficult to directly produce injection powder injections with bottle freezing technology, and a series of solubilizers or co-solvents need to be added. This method virtually increases the amount of excipients and increases the injection time. Chance of risk of hemolysis
In addition, imipenem and cilastatin sodium are sensitive to heat. In addition to the easy decomposition of the β-lactam ring, the molecular structure also contains sulfur, which is easily oxidized to form impurities in the form of sulfoxide, and is relatively unstable in the solution.

Method used

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  • Imipenem and cilastatin sodium sterile powder preparation for injection and preparation method thereof
  • Imipenem and cilastatin sodium sterile powder preparation for injection and preparation method thereof
  • Imipenem and cilastatin sodium sterile powder preparation for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Imipenem cilastatin sodium sterile powder preparation for injection

[0030] Prescription (1000 bottles):

[0031]

[0032] Preparation Process:

[0033] (1) Under sterile conditions, dissolve 10 g of sodium bicarbonate in 500 mL of water for injection to make a pH regulator for use.

[0034] (2) Dissolve 20 g of sodium bicarbonate in 500 mL of water for injection under sterile conditions, add 100 g of imipenem and 100 g of cilastatin sodium, and stir to dissolve. Add 5g of sodium sulfite, stir to dissolve, and add the pH regulator obtained in (1), pH = 7.1.

[0035] (3) The solution obtained in (2) was filtered with a 0.2 μm filter membrane, and then equally divided into 1000 sterilized vials.

[0036] (4) Place the vial in a freeze dryer, pre-freeze at -40±5°C for 3 hours, then adjust the temperature to -10±5°C for sublimation drying, and then raise the temperature to 5±5°C for re-drying after 5 hours , a white lyophilized product was obtained after 3 hours. S...

Embodiment 2

[0037] Example 2 imipenem cilastatin sodium sterile powder preparation for injection

[0038] Prescription (1000 bottles):

[0039]

[0040] Preparation Process:

[0041] (1) Under sterile conditions, dissolve 30 g of sodium bicarbonate in 400 mL of water for injection to make a pH regulator for use.

[0042] (2) Dissolve 70g of sodium bicarbonate in 600mL of water for injection under sterile conditions, add 250g of imipenem and 250g of cilastatin sodium, and stir to dissolve. Add 12g of sodium sulfite, stir to dissolve, and add the pH regulator obtained in (1), pH = 7.7.

[0043] (3) The solution obtained in (2) was filtered with a 0.2 μm filter membrane, and then equally divided into 1000 sterilized vials.

[0044](4) Place the vial in a freeze dryer, pre-freeze at -40±5°C for 3 hours, then adjust the temperature to -10±5°C for sublimation drying, and then raise the temperature to 5±5°C for re-drying after 6 hours , a white lyophilized product was obtained after 3 hou...

Embodiment 3

[0045] Example 3 imipenem cilastatin sodium sterile powder preparation for injection

[0046] Prescription (1000 bottles):

[0047]

[0048]

[0049] Preparation Process:

[0050] (1) Under sterile conditions, dissolve 80g of sodium bicarbonate in 800mL of water for injection to make a pH regulator for use.

[0051] (2) Dissolve 170g of sodium bicarbonate in 2000mL of water for injection under sterile conditions, add 500g of imipenem and 500g of cilastatin sodium, and stir to dissolve. Add 25g of sodium sulfite, stir to dissolve, and add the pH regulator obtained in (1), pH = 7.9.

[0052] (3) The solution obtained in (2) was filtered with a 0.2 μm filter membrane, and then equally divided into 1000 sterilized vials.

[0053] (4) Place the vial in a freeze dryer, pre-freeze at -40±5°C for 5 hours, then adjust the temperature to -10±5°C for sublimation drying, and then raise the temperature to 5±5°C for re-drying after 8 hours , a white lyophilized product was obtaine...

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Abstract

The invention provides an imipenem and cilastatin sodium sterile powder preparation for injection and a preparation method thereof. The solubilizing effect of a pH regulator of sodium bicarbonate on imipenem is utilized; the solubility of the imipenem in a water solution is increased; antioxidants are added, so that the oxidative deterioration of the imipenem and the cilastatin sodium sterile powder preparation in production and storage processes is reduced; the use of medical auxiliary materials is reduced; the manufacturing process is simplified; the cost is reduced; meanwhile, the contents of relevant substances are reduced; the production of the stable-quality imipenem and cilastatin sodium sterile powder preparation for injection can be ensured.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a sterile powder preparation of imipenem and cilastatin sodium for injection and a preparation method thereof. Background technique [0002] Imipenem: (+)–(5R,6S)-3[[2-(iminomethylamino)ethyl]thio]-6-[(R)-1-cyanoethyl]-7- Oxo-1-azabicyclo[3.2.0]hept-2-ene-2carboxylic acid monohydrate, imipenem, the first stably existing thiamycin derivative, is a new β - Lactam antibiotics, which show broad-spectrum and high-efficiency antibacterial activity by specifically inhibiting the synthesis of bacterial cell wall peptidoglycan, and have effects on Gram-positive and negative bacteria, including anaerobic bacteria, especially Staphylococcus aureus, The antibacterial activity of Streptococcus faecalis, Pseudomonas aeruginosa and Bacteroides fragilis is much better than that of the third-generation cephems such as cefzozirone. [0003] [0004] Cilastatin sodium: (+)-(Z)-7-[[(R)-2-amino-2-carboxy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/407A61K31/198A61K9/19A61P31/04
CPCA61K9/0019A61K9/19A61K31/198A61K31/407A61K2300/00
Inventor 沈载宽郑林海
Owner 泊诺(天津)创新医药研究有限公司
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