Insight into the Colonic Disposition of Sulindac in Humans
نویسندگان
چکیده
NSAIDs such as celecoxib and sulindac play a critical role in the treatment of colorectal cancer, yet it is not understood how sufficiently high concentrations are reached colonic tissue. We previously demonstrated that an incomplete small intestinal absorption enables gut driven drug accumulation caecal tissue, which most likely needed for inducing remission. However, multistage dissolution experiment suggested more extensive relative to celecoxib, though still incomplete. To study whether solely plasma or also driven, we performed exploratory clinical healthy volunteers. After intake tablet (200 mg; Arthrocine), two colonoscopies (1.0–2.5 h, 6.0–7.5 h after intake) were assess metabolites plasma, tissue contents. observed sulindac, even without use colon-targeted delivery strategy, can arrive at lumen due biliary excretion, microbiota catalyse production sulfide, then accumulates local manner These data be relevant development adenomas cancer.
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ژورنال
عنوان ژورنال: Journal of Pharmaceutical Sciences
سال: 2021
ISSN: ['0022-3549', '1520-6017']
DOI: https://doi.org/10.1016/j.xphs.2020.09.034