Acarbose for the Treatment of Diabetes Mellitus by W. Creutzfeldt (auth.), Prof. Dr. med. Dr. h.c. W.

By W. Creutzfeldt (auth.), Prof. Dr. med. Dr. h.c. W. Creutzfeldt (eds.)

New rules for the therapy of diabetes are defined during this quantity. specialists current experimental and medical information on therapy with acarbose, an alpha-glucosidase inhibitor that delays absorption of quick carbohydrates. Toxicologic, pharmacologic and metabolic results of acarbose are mentioned. A concluding part at the destiny points of alpha-glucosidase inhibition deals a good evaluate of healing possibilities.

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LCi of 14C-acarbose at steady state. (n = 6) 24 F. O. Miiller et al. seems to indicate that circulating acarbose metabolites, found after p. o. administration of the parent compound, originate in the gastrointestinal tract from whence they are more readily absorbed than the parent compound. We did not determine the amount of unlabelled acarbose excreted in faeces. The figure of 51 %, measured as total radioactivity, would include the approximately 16% of the administered dose previously found to be excreted unchanged in faeces measured as acarbose activity [7].

63 h correlates well with the value of approximately 9 h previously reported [6]. We did not detect any accumulation of acarbose in plasma with chronic administration. This is in agreement with published data [6-7]. Conclusion In humans, acarbose as such is poorly absorbed from the gastrointestinal tract. Less than 2% is excreted in urine as the parent compound. Inactive acarbose metabolites, possibly resulting from intraluminal biotransformation in the gastrointestinal tract, are apparently more readily absorbed and excreted by the kidneys, representing more than 30% of the total dose of acarbose administered.

Availability of acarbose previously described [6]. 7% ofthe orally administered dose is excreted as acarbose or "acarbose activity". 5% previously reported [6] but still negligible compared to the almost 90% after i. v. administration [6-7]. 3% of the daily ingested dose of acarbose was excreted in urine. The fact that apparent plasma-acarbose concentrations, derived from radioactivity in plasma, were greatly in excess of unlabelled plasma-acarbose concentrations, The Disposition and Pharmacokinetics of Acarbose in Man 23 40 30 CD (I) e "0 20 ....

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