Glucotrol XL

[Glipizide]

Drug Description
DESCRIPTION

GLUCOTROL XL

Glipizide is an oral blood-glucose-lowering drug of the sulfonylurea class. The Chemical Abstracts name of glipizide is 1-cyclohexyl-3-[[ p-[ 2-( 5-methylpyrazinecarboxamido) ethyl] phenyl] sulfonyl] urea. The molecular formula is C21H27N5O4S; the molecular weight is 445.55

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Glipizide is a whitish, odorless powder with a pKa of 5.9. It is insoluble in water and alcohols, but soluble in 0.1 N NaOH; it is freely soluble in dimethylformamide. GLUCOTROL XL ® is a registered trademark for glipizide GITS. Glipizide GITS (Gastrointestinal Therapeutic System) is formulated as a once-a-day controlled release tablet for oral use and is designed to deliver 2.5, 5, or 10 mg of glipizide.

Inert ingredients in the 2.5 mg, 5 mg and 10 mg formulations are: polyethylene oxide, hydroxypropyl methylcellulose, mag-nesium stearate, sodium chloride, red ferric oxide, cellulose acetate, polyethylene glycol, opadry blue (OY-LS-20921)( 2.5 mg tablets), opadry white (YS-2-7063)( 5 mg and 10 mg tablet) and black ink (S-1-8106).

System Components and Performance GLUCOTROL XL Extended Release Tablet is similar in appearance to a conventional tablet. It consists, however, of an osmotically active drug core surrounded by a semipermeable membrane. The core itself is divided into two layers: an "active" layer containing the drug, and a "push" layer containing pharmacologically inert (but osmotically active) components. The membrane surrounding the tablet is permeable to water but not to drug or osmotic excipients.

As water from the gastrointestinal tract enters the tablet, pressure increases in the osmotic layer and "pushes" against the drug layer, resulting in the release of drug through a small, laser-drilled orifice in the membrane on the drug side of the tablet. The GLUCOTROL XL Extended Release Tablet is designed to provide a controlled rate of delivery of glipizide into the gas-trointestinal lumen which is independent of pH or gastrointestinal motility.

The function of the GLUCOTROL XL Extended Release Tablet depends upon the existence of an osmotic gradient between the contents of the bi-layer core and fluid in the GI tract. Drug delivery is essentially constant as long as the osmotic gradient remains constant, and then gradually falls to zero. The bio-logically inert components of the tablet remain intact during GI transit and are eliminated in the feces as an insoluble shell.