文档介绍：PRECOSE®
(acarbose tablets)
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DESCRIPTION
PRECOSE® (acarbose tablets) is an oral alpha-glucosidase inhibitor for use in the management of type 2
diabetes mellitus. Acarbose is an oligosaccharide which is obtained from fermentation processes of a
microorganism, Actinoplanes utahensis, and is chemically known as O-4,6-dideoxy­
4-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-α-D-glucopyranos
yl-(1 → 4)-O-α-D-glucopyranosyl-(1 → 4)-D-glucose. It is a white to off-white powder with a
molecular weight of . Acarbose is soluble in water and has a pKa of . Its empirical formula is
C25H43NO18 and its chemical structure is as follows:
PRECOSE is available as 25 mg, 50 mg and 100 mg tablets for oral use. The inactive ingredients are
starch, microcrystalline cellulose, magnesium stearate, and colloidal silicon dioxide.
CLINICAL PHARMACOLOGY
Acarbose is a complex oligosaccharide that delays the digestion of ingested carbohydrates,
thereby resulting in a smaller rise in blood glucose concentration following meals. As a consequence of
plasma glucose reduction, PRECOSE reduces levels of glycosylated hemoglobin in patients with type 2
diabetes mellitus. Systemic non-enzymatic protein glycosylation, as reflected by levels of glycosylated
hemoglobin, is a function of average blood glucose concentration over time.
Mechanism of Action
In contrast to sulfonylureas, PRECOSE does not enhance insulin secretion. The antihyperglycemic
action of acarbose results from a competitive, reversible inhibition of pancreatic alpha-amylase and
membrane-bound intestinal a