DESCRIPTION
Avandia (rosiglitazone maleate) is an oral antidiabetic
agent which acts primarily by increasing insulin sensitivity.
Avandia is used in the management of type 2 diabetes mellitus
(also known as non-insulin-dependent diabetes mellitus (NIDDM)
or adult-onset diabetes). Avandia improves glycemic control
while reducing circulating insulin levels.
Pharmacological studies in animal models indicate that rosiglitazone
improves sensitivity to insulin in muscle and adipose tissue
and inhibits hepatic gluconeogenesis. Rosiglitazone maleate
is not chemically or functionally related to the sulfonylureas,
the biguanides, or the alpha-glucosidase inhibitors.
Chemically, rosiglitazone maleate is (±)-5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-
2,4-thiazolidinedione,(Z)-2-butenedioate (1:1) with a molecular
weight of 473.52 (357.44 free base). The molecule has a
single chiral center and is present as a racemate. Due to
rapid interconversion, the enantiomers are functionally
indistinguishable.
The molecular formula is C18H19N3O3S·C4H4O4. Rosiglitazone
maleate is a white to off- white solid with a melting point
range of 122o to 123o C. The pKa values of rosiglitazone
maleate are 6.8 and 6.1. It is readily soluble in ethanol
and a buffered aqueous solution with pH of 2.3; solubility
decreases with increasing pH in the physiological range.
Each pentagonal film-coated TiltabÒ tablet contains
rosiglitazone maleate equivalent to rosiglitazone, 2 mg,
4 mg, or 8 mg, for oral administration. Inactive ingredients
are: hydroxypropyl methylcellulose, lactose monohydrate,
magnesium stearate, microcrystalline cellulose, polyethylene
glycol 3000, sodium starch glycolate, titanium dioxide,
triacetin, and one or more of the following: synthetic red
and yellow iron oxides and talc.
DESCRIPTION
Avandia (rosiglitazone maleate) is an oral antidiabetic
agent which acts primarily by increasing insulin sensitivity.
Avandia is used in the management of type 2 diabetes mellitus
(also known as non-insulin-dependent diabetes mellitus (NIDDM)
or adult-onset diabetes). Avandia improves glycemic control
while reducing circulating insulin levels.
Pharmacological studies in animal models indicate that rosiglitazone
improves sensitivity to insulin in muscle and adipose tissue
and inhibits hepatic gluconeogenesis. Rosiglitazone maleate
is not chemically or functionally related to the sulfonylureas,
the biguanides, or the alpha-glucosidase inhibitors.
Chemically, rosiglitazone maleate is (±)-5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-
2,4-thiazolidinedione,(Z)-2-butenedioate (1:1) with a molecular
weight of 473.52 (357.44 free base). The molecule has a
single chiral center and is present as a racemate. Due to
rapid interconversion, the enantiomers are functionally
indistinguishable.
The molecular formula is C18H19N3O3S·C4H4O4. Rosiglitazone
maleate is a white to off- white solid with a melting point
range of 122o to 123o C. The pKa values of rosiglitazone
maleate are 6.8 and 6.1. It is readily soluble in ethanol
and a buffered aqueous solution with pH of 2.3; solubility
decreases with increasing pH in the physiological range.
Each pentagonal film-coated TiltabÒ tablet contains
rosiglitazone maleate equivalent to rosiglitazone, 2 mg,
4 mg, or 8 mg, for oral administration. Inactive ingredients
are: hydroxypropyl methylcellulose, lactose monohydrate,
magnesium stearate, microcrystalline cellulose, polyethylene
glycol 3000, sodium starch glycolate, titanium dioxide,
triacetin, and one or more of the following: synthetic red
and yellow iron oxides and talc.
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