Pharmaceutical composition containing esomeprazole sodium and preparation method thereof

Abstract

The invention relates to a pharmaceutical composition containing esomeprazole sodium and a preparation method thereof. The pharmaceutical composition is freeze-dried powder for injection, and for every 1000 bottles, the pharmaceutical composition is composed of the following pharmaceutical ingredients of 20-40 grams of the esomeprazole sodium, 1.5 grams of disodium edetate, and 1 liter of water for injection. The preparation method of the pharmaceutical composition containing the esomeprazole sodium includes the steps of liquid preparation and freeze drying, wherein in the process of liquid preparation, the esmeprazole sodium, the disodium edetate, and the water for injection are mixed to prepare a liquid of a pH of 11.0 to 11.5; the step of freeze drying includes freeze control 1, freezecontrol 2, sublimation drying 1, sublimation drying 2 and desorption drying. The pharmaceutical composition containing the esomeprazole sodium has various advantages, such as having low moisture content, few metal ions and colored impurities and good stability, and having no significant increase in impurities accompanied by changes in solution color after long-term placement.

Description

technical field [0001] The invention relates to the field of pharmaceutical technology, more specifically, to a freeze-dried powder injection containing esomeprazole sodium and a preparation method thereof. Background technique [0002] The chemical name of Esomeprazole sodium is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl ] Sodium sulfinyl-1H-benzimidazole) has become the first choice drug for the treatment of acid-related diseases such as peptic ulcer and gastroesophageal reflux disease because of its strong gastric acid inhibitory effect, long-lasting effect and small side effects. In 2007, the China Food and Drug Administration approved the import preparation of AstraZeneca's esomeprazole sodium freeze-dried powder injection, the trade name is Nexium, and the specifications are 40mg and 20mg azole meter), the prescription is composed of esomeprazole sodium and edetate disodium, which is compatible with 0.9% sodium chloride solution for intravenous injecti...

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Problems solved by technology

[0004] CN102440965A Example 1 discloses a freeze-dried preparation composed of esomeprazole sodium and ethylenediaminetetraacetic acid, the activated carbon used to adsorb impurities in the preparation process has undergone specific finishing steps to release the activated carbon in advance Easy-to-release impurities in the product, so as to control the visible foreign matter and insoluble particles in the product to a lower level, but this method cannot further control the impurities in the product, especially the colored impurities

[0005] The prior art also improves the stability of the preparation by adding stabilizers such as amino acids, antioxidants such as sodium sulfite, or preparing phospholipid complexes in the prescription, in order to reduce the generation of impurities, but the addition of too many excipients increases the The probability of introducing exogenous impurities, and during the research process, the inventors found that the esomeprazole sodium freeze-dried powder injection had problems such as increased impurities, discoloration of the solution, and the preparation method, especially the freeze-drying process and drug The liquid treatment method has a great relationship, even with the same prescription, the products obtained by different preparation methods still have significant quality differences, and this point is often ignored in the prior art, so a stable and effective solution to the increase of colored impurities in products cannot be provided. , the method for the color change problem of the liquid medicine

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