Fidaxomicin enteric-coated preparation

Abstract

The invention discloses a fidaxomicin enteric-coated preparation. The fidaxomicin enteric-coated preparation contains 40-400mg of fidaxomicin; the fidaxomicin enteric-coated preparation comprises an inner medicinal core, an isolation coating layer and a casing layer, wherein the isolation coating layer comprises a copolymer of polyvinyl alcohol and polyethylene glycol; the weight of the isolation coating layer is 0.3-2.5wt% of that of the inner medicinal core; the casing layer comprises an enteric-coated material dissolved under the pH of 4.5-6.8; and the weight of the casing layer is 5-25wt% of that of the inner medicinal core. The enteric-coated preparation disclosed by the invention is kept integrated in gastric juice, so that medicines cannot be leaked; degradation and consumption of fidaxomicin under gastric acid action are effectively avoided; when the enteric-coated preparation leaves a stomach and enters a pylorus, a casing and an isolation coating can be disintegrated rapidly, so that fidaxomicin is released rapidly; the therapeutical concentration of fidaxomicin in the enteric-coated preparation after entering an intestinal tract is achieved within a short time; the time-lag effect is avoided; the medicine retention time in human bodies is prolonged; the sterilization effect is the best, and thus, the bioavailability and the sterilization curative effect of medicines are effectively increased.

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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