A kind of Fidaxomycin enteric-coated preparation

Abstract

The invention discloses a fidaxomicin enteric-coated preparation, which contains 40-400 mg of fidaxomicin; the fidaxomicin enteric-coated preparation includes a drug inner core, an isolation coat layer and an enteric coat layer; the isolation coat layer includes A copolymer of polyvinyl alcohol and polyethylene glycol, the weight of which is 0.3wt% to 2.5wt% of the drug inner core; the enteric coating layer includes enteric materials dissolved at pH 4.5 to 6.8, whose weight is 0.3% to 2.5wt% of the drug inner core 5wt% ~ 25wt%. The enteric-coated preparation of the present invention remains intact in the gastric juice, does not leak the drug, and effectively avoids the degradation and consumption of fidaxomicin under the action of gastric acid; and when the enteric-coated preparation leaves the stomach and enters the pylorus, the enteric coating and isolation coat can quickly Disintegration and rapid release of Fidaxomycin, Fidaxomicin in the enteric-coated preparation reaches the therapeutic concentration in a short time after reaching the intestinal tract, there is no time lag effect, prolonging the residence time of the drug in the human body, making The bactericidal effect is maximized, thereby effectively improving the bioavailability and bactericidal efficacy of the drug.

Description

technical field [0001] The invention relates to a fidaxomicin enteric-coated preparation, which belongs to the technical field of western medicine preparations. Background technique [0002] Clostridium difficile infection (CDI) is a serious illness caused by the bacterium Clostridium difficile infecting the lining of the colon and producing toxins that can cause colon inflammation, severe diarrhea and even death. Clostridium difficile infection is a significant medical problem in hospitals, nursing homes and communities. It affects more than 700,000 people per year in the United States alone. Not only the number of severe cases, recurrence rate and mortality rate have increased significantly, but also drug-resistant strains are also increasing. The traditional CDI treatment drugs are metronidazole and vancomycin, but the treatment effect is not satisfactory, and the recurrence rate is high. [0003] Fidaxomicin is a macrolide antibiotic with an 18-membered ring structure, ...

AI Technical Summary

Problems solved by technology

Because the existing formulations of Fidaxomycin are not stable enough in gastric acid and prone to degradation, Fidaxomicin is consumed in the stomach and the content of Fidaxomicin entering the intestinal tract is reduced, which leads to the clinical administration of Fidaxomicin The increase in the amount of Fidaxomycin and the emergence of various degradation impurities have also brought hidden dangers to the safety of Fidaxomycin

[0014] After Fidaxomycin is made into ordinary enteric-coated preparations, the drug can be kept intact and not destroyed in gastric acid, but the enteric coating layer of enteric-coated preparations will form a film that is difficult to dissolve under the action of acid; when the drug leaves When it enters the stomach and intestinal tract, it still cannot disintegrate and release quickly; even in the intestinal environment with a pH greater than 5.0, it still takes a while to dissolve and release, resulting in a time-lag effect in drug release, slow drug onset, and reduced The residence time of the drug in the human body is affected, which affects the efficacy of the drug

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