소염효소제 장용정(브로멜라인)의 분할 및 분쇄 시 위액 pH에서의 안정성

Abstract

Bromelain is an oral antiinflammatory enzyme with a dosage form of enteric coated tablet to keep enzyme from inactivating in gastric pH. There are no stability data in gastric pH for enteric coated bromelain as a half tablet and powder, since there is no regulation in the Korean Pharmacopoeia. Stability of enzymes are concerned when the enteric coated tablets are prescribed as a half tablet or powder to patients. In this study, an in vitro study was performed to assess the stability of bromelain in gastric pH as a half tablet and powder form. Bromelain was prepared as a whole tablet, a half tablet and powder titrated from a whole tablet in duplicate samples. The samples were stored at room temperature or in the refrigerator. The storage periods were 0, 1, 3, 6, 8, 10, 20, 30 days, respectively. After each storage period, bromelain was eluted in artificial gastric juice(pH 1.2, 37℃, 500ml) for 60 minutes. Then, bromelain activity was measured using enzyme-substrate reaction method in the Korean Pharmacopoeia. As results, a whole tablet was intact in gastric juice and the activity was remained. A half tablet was eluted in gastric juice and the activity was decreased to less than 30%. Powder did not have any activity in all storage conditions and periods. In conclusion, bromelain lost activity significantly with a half tablet or powder form in gastric juice. Enteric coated antiinflammatory enzymes should be taken as an intact whole tablet to keep enzyme activity. We suggested that the pharmaceutical company develop enteric coated granules or capsules that filled up with those granules.