Freeze-dried injection of proton pump inhibitor

Abstract

The invention relates to a proton pump inhibitor frozen powder injection agent and a preparation method thereof. The proton pump inhibitor frozen powder injection agent prepared by the method can be taken as a medicine for treating gastric ulcer, duodenal ulcer, erosive gastroesophageal reflux disease, helicobacter pylori and Zollinger-Ellison Syndrome. The proton pump inhibitor frozen powder injection agent is prepared through taking a proton pump inhibitor as an active ingredient, adopting crystallized filtration, freezing and drying. The preparation process comprises the following steps of: adding water for injection and alkali to the proton pump inhibitor, stirring to dissolve and mix uniformly; performing the crystallized filtration; after measuring the content, adjusting pH value of filtrate; using the water for injection for fixing volume and a millipore filter with 0.22 mu m for filtration; filling, partially arranging corks, arranging in trays, freezing out, pressing the corks, taking out from boxes, rolling openings, checking quality and packaging. The prepared proton pump inhibitor frozen powder injection agent has excellent re-dissolving performance, is more stable when used together with transfusion in clinical use, can not separate out, and has better inspection result for visible foreign matters and insoluble particles.

Description

technical field [0001] The present invention relates to a kind of proton pump inhibitor composition freeze-dried powder injection and preparation method thereof, the lansoprazole freeze-dried powder injection prepared by the method can be used as gastric ulcer, duodenal ulcer, erosive gastric- Drugs for the treatment of esophageal reflux disease, Helicobacter pylori, and Zollimger-ellison syndrome. Background technique [0002] Digestive system disease is one of common frequently-occurring diseases, and wherein ulcer disease is the most common, and its total sickness rate accounts for 10~12% of total population approximately, and main onset age is 30~50 years old. There are 400,000 people in the United States suffering from peptic ulcers every year, mainly due to smoking, drinking, emotional stress, and drug stimulation (such as ASP, indomethacin, and peptic ulcer). The incidence rate of American men is 10%, and that of women is 5%. %. The gastrointestinal incidence rate ...

AI Technical Summary

Problems solved by technology

[0005]Because proton pump inhibitors are easily degraded in acidic environment, the usual oral preparations of proton pump inhibitors adopt enteric coating to prevent the active ingredients from being exposed to gastric acid While the enteric coating protects the active ingredients, it also delays the acid-suppressing effect of proton pump inhibitors, which is not conducive to timely treatment and rapid relief of patients’ pain. Therefore, it needs to be prepared into injections, but due to proton pump inhibitors The injection solution has poor stability and cannot be sterilized at high temperature, so it can only be prepared by freeze-drying

During the development process, it was found that foreign matter and insoluble particles could be seen after reconstitution of the proton pump inhibitor freeze-dried powder injection prepared by common preparation methods, and the inspection results of insoluble particles were unsatisfactory. Particles of 5-20 microns and above can block blood flow when passing through pulmonary capillaries, causing complications such as pulmonary embolism and even death. Exogenous particles can also form phlebitis at the injection site, and may also cause venous vessel obstruction and Patient injury, seriously affecting the safety of clinical medication

The lansoprazole ( ) injection marketed in the United States is proposed to be equipped with a disposable filter with a pore size of 1.2 μm to filter out the The above-mentioned fine particles did not fundamentally solve the above-mentioned defects, and greatly increased the cost of the preparation, increased the economic burden on the patient, and the sterility guarantee level of the disposable filter also increased the risk of bacterial contamination, which is not an ideal solution. Scheme; commercially available omeprazole sodium freeze-dried powder injection and pantoprazole sodium freeze-dried powder injection adopt the way of being equipped with special solvent, but bring trouble to clinical use and packaging transportation, other known technologies do not improve above defect suggestion

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