Stable rabeprazole sodium freeze-dried preparation and preparation method thereof

Abstract

The invention relates to the field of medicament preparations, and particularly relates to a stable rabeprazole sodium freeze-dried preparation and a preparation method thereof. The freeze-dried powder injection consists of active component rabeprazole sodium, a pharmaceutically acceptable excipient and a pH regulator, wherein the pH regulator ensures that the pH of a solution is maintained in a range of between 10.5 and 12.5 when being dissolved once again before the solution is not freeze-dried and after the solution is freeze-dried. The rabeprazole sodium freeze-dried preparation has the characteristic of high stability.

Description

technical field

[0001] The invention relates to a stable freeze-dried preparation of rabeprazole sodium and a preparation method thereof. Background technique

[0002] In the past ten years, the research on anti-ulcer drugs has tended to the drugs that can selectively inhibit gastric acid secretion, and these drugs can be roughly divided into the following four categories: (1) cholinergic M-receptor antagonists, such as pirenzepine; (2) Histamine H2-receptor antagonists, such as cimetidine and ranitidine; (3) mucosal protection promoters, such as prostaglandin analogues PGE2, etc.; (4) proton pump inhibitor (PPI)-H+ / K+ - APTase inhibitors such as omeprazole and rabeprazole sodium. M-receptor antagonists are gradually replaced by H2-receptor antagonists because of their large side effects and weak anti-ulcer effect. Although the latter are currently in the ascendant and have been improved several times, they have defects such as unsuitable indications and side effects. Pros...

Examples

Embodiment 1

[0050] prescription:

[0051] Rabeprazole Sodium 21.24g

[0052] Mannitol 40g

[0053] Appropriate amount of sodium hydroxide

[0054] Add water for injection to 2000ml

[0055]

[0056] Makes 1000 bottles

[0057] Take the prescribed amount of mannitol and rabeprazole sodium, put them in a sterile container, add water for injection, stir to dissolve, and mix well. Sodium hydroxide, a pH regulator, is added to adjust the medicinal solution within the range of 10.5 to 12.5, and the water for injection is supplemented to the prescribed amount. After complete dissolution, add 0.05% activated carbon to stir and adsorb for 20 minutes, decarbonize, sterilize and filter to measure the content of intermediates. After passing the test, the filtrate can be filled in sterile vials, half stoppered, and freeze-dried.

Embodiment 2

[0059] prescription:

[0060] Rabeprazole Sodium 21.24g

[0061] Mannitol 60g

[0062] Potassium hydroxide appropriate amount

[0063] Add water for injection to 2000ml

[0064]

[0065] Makes 1000 bottles

[0066] Take the prescribed amount of mannitol and rabeprazole sodium, put them in a sterile container, add water for injection, stir to dissolve, and mix well. Add a pH regulator potassium hydroxide to adjust the medicinal solution within the range of 11.0±0.5, and make up the water for injection to the prescribed amount. After complete dissolution, add 0.05% activated carbon to stir and adsorb for 20 minutes, decarbonize, sterilize and filter to measure the content of intermediates. After passing the test, the filtrate can be filled in sterile vials, half stoppered, and freeze-dried.

Embodiment 3

[0068] prescription:

[0069] Rabeprazole Sodium 21.24g

[0070] Dextran 40 40g

[0071] Appropriate amount of sodium hydroxide

[0072] Add water for injection to 2000ml

[0073]

[0074] Makes 1000 bottles

[0075] Dissolve dextran 40 in hot water (above 80°C), cool to room temperature, add the main ingredient and stir to dissolve, add pH regulator sodium hydroxide to adjust the pH to 11.0±0.5 after it is completely dissolved, and make up enough water for injection. Add 0.05% activated carbon, stir and adsorb for 20 minutes, decarburize, sterilize and filter, measure the content of intermediates, and after passing the test, the filtrate can be filled in sterile vials, half stoppered, and freeze-dried.

technical field

[0001] The invention relates to a stable freeze-dried preparation of rabeprazole sodium and a preparation method thereof. Background technique

[0002] In the past ten years, the research on anti-ulcer drugs has tended to the drugs that can selectively inhibit gastric acid secretion, and these drugs can be roughly divided into the following four categories: (1) cholinergic M-receptor antagonists, such as pirenzepine; (2) Histamine H2-receptor antagonists, such as cimetidine and ranitidine; (3) mucosal protection promoters, such as prostaglandin analogues PGE2, etc.; (4) proton pump inhibitor (PPI)-H+ / K+ - APTase inhibitors such as omeprazole and rabeprazole sodium. M-receptor antagonists are gradually replaced by H2-receptor antagonists because of their large side effects and weak anti-ulcer effect. Although the latter are currently in the ascendant and have been improved several times, they have defects such as unsuitable indications and side effects. Pros...

Examples

Embodiment 1

[0050] prescription:

[0051] Rabeprazole Sodium 21.24g

[0052] Mannitol 40g

[0053] Appropriate amount of sodium hydroxide

[0054] Add water for injection to 2000ml

[0055]

[0056] Makes 1000 bottles

[0057] Take the prescribed amount of mannitol and rabeprazole sodium, put them in a sterile container, add water for injection, stir to dissolve, and mix well. Sodium hydroxide, a pH regulator, is added to adjust the medicinal solution within the range of 10.5 to 12.5, and the water for injection is supplemented to the prescribed amount. After complete dissolution, add 0.05% activated carbon to stir and adsorb for 20 minutes, decarbonize, sterilize and filter to measure the content of intermediates. After passing the test, the filtrate can be filled in sterile vials, half stoppered, and freeze-dried.

Embodiment 2

[0059] prescription:

[0060] Rabeprazole Sodium 21.24g

[0061] Mannitol 60g

[0062] Potassium hydroxide appropriate amount

[0063] Add water for injection to 2000ml

[0064]

[0065] Makes 1000 bottles

[0066] Take the prescribed amount of mannitol and rabeprazole sodium, put them in a sterile container, add water for injection, stir to dissolve, and mix well. Add a pH regulator potassium hydroxide to adjust the medicinal solution within the range of 11.0±0.5, and make up the water for injection to the prescribed amount. After complete dissolution, add 0.05% activated carbon to stir and adsorb for 20 minutes, decarbonize, sterilize and filter to measure the content of intermediates. After passing the test, the filtrate can be filled in sterile vials, half stoppered, and freeze-dried.

Embodiment 3

[0068] prescription:

[0069] Rabeprazole Sodium 21.24g

[0070] Dextran 40 40g

[0071] Appropriate amount of sodium hydroxide

[0072] Add water for injection to 2000ml

[0073]

[0074] Makes 1000 bottles

[0075] Dissolve dextran 40 in hot water (above 80°C), cool to room temperature, add the main ingredient and stir to dissolve, add pH regulator sodium hydroxide to adjust the pH to 11.0±0.5 after it is completely dissolved, and make up enough water for injection. Add 0.05% activated carbon, stir and adsorb for 20 minutes, decarburize, sterilize and filter, measure the content of intermediates, and after passing the test, the filtrate can be filled in sterile vials, half stoppered, and freeze-dried.

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