Omeprazole sodium freeze-dried powder injection and preparation method thereof

Abstract

The invention discloses an omeprazole sodium freeze-dried powder injection and a preparation method thereof. The omeprazole sodium freeze-dried powder injection contains an active ingredient, namely, omeprazole sodium monohydrate, and auxiliary materials, namely, calcium disodium edetate and sodium hydroxide. The preparation method of the omeprazole sodium freeze-dried powder injection is characterized by comprising the following steps: weighing the calcium disodium edetate of prescription amount and dissolving the calcium disodium edetate in water for injection, stirring, dissolving, and regulating pH value to 10.0-12.0 by using 10% of sodium hydroxide solution; weighing omeprazole sodium of the prescription amount and adding the omeprazole sodium in the mixture, stirring at room temperature for dissolution, supplementing and adding the water for injection to full amount; adding active carbon, stirring at room temperature for decoloration and endotoxin removal, conducting rough filtration to remove carbon firstly, and then conducting refining filtration by using a filter membrane of 0.22 Mum; taking refining filtrate to test intermediate, conducting encapsulation after meeting requirements; and freeze-drying and unboxing, thus obtaining the omeprazole sodium freeze-dried powder injection. The freeze-drying technology of the omeprazole sodium freeze-dried powder injection takes temperature below minus 40 DEG C as pre-freezing temperature; after pre-freezing for at least two hours, sublimation is started, wherein the sublimation temperature is 5-12 DEG C, the sublimation time is over 14 hours; and then drying is conducted for over 2 hours at the temperature of 20-35 DEG C. Unboxing is carried out after a stopper is added and a cover is put in place, thus obtaining the finished product of the omeprazole sodium freeze-dried powder injection.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a proton pump inhibitor omeprazole sodium freeze-dried powder injection and a preparation method thereof. Background technique [0002] Omeprazole sodium is the sodium salt of the benzimidazole compound omeprazole, the chemical name is 5-methoxy-2-{[(4-methoxy-3,5-dimethyl-2-pyridine Base)-methyl]-sulfinyl}-1H-benzimidazole sodium, its parent compound omeprazole reduces the secretion of gastric acid through the specific effect on the parietal cell proton pump, and the inhibitory effect is dose-related, and the effect is reversible. The principle is that omeprazole is a weakly alkaline substance, which is concentrated and converted into an active form in the acidic environment in the parietal cells, inhibiting H+, K + -ATPase. [0003] There are multiple forms of omeprazole preparations currently on the market, such as oral dosage forms such as tablets, capsules, and pellets. Be...

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Problems solved by technology

However, the preparation of this patent application adds disodium edetate as an auxiliary material, which can complex calcium ions in the blood, resulting in a decrease in blood calcium in the human body, so it is not conducive to clinical use

[0007] The application number is CN200810062160.3 Chinese patent application discloses a freeze-dried powder injection of omeprazole sodium, with omeprazole as the main active ingredient, containing a skeleton agent, a metal ion complexing agent, a stabilizer, an antioxidant, pH value regulator, the pH value of the preparation is adjusted to 10.8-11.2 and the Chinese patent application with application number CN200810211501.9 discloses a freeze-dried preparation of omeprazole sodium for injection, which is made of the following raw materials in parts by weight : Omeprazole sodium 20-40 parts, dextran 20-200 parts, stabilizer 5-60 parts, sodium sulfite 5-40 parts, polymethyl methacrylate 40-400 parts, freeze-dried matrix agent 10-500 parts and disclosed its preparation method. The preparations of the two patent applications contain more excipients, which not only increases the production cost of the preparation, but also greatly increases the potential risk of adverse reactions in clinical application.

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