Synthesis and properties of methylprednisolone-21sulfate sodiumas as a colon-specific prodrug of methylprednisolone

Corticosteroids have been used most frequently for inflammatory bowel disease. To reduce side effects by the systemic absorption, colon-specific delivery is highly desirable. We expected that conversion of 21-hydroxyl in glucocorticoids into a sulfate ester sodium will greatly increase the hydrophilicity, which consequently restrict the gastrointestinal absorption. Once delivered to the colon, sulfate ester will be hydrolyzed by the sulfatase originated from microbes and release the parent compound, glucocorticoids. In this study, we prepared methylprednisolone 21-sulfate sodium (MPS) and investigated its suitability as a colon-specific prodrug on methylprednisolone (MP). (omitted)