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Lodine XL
(etodolac extended-release tablets)
400 mg, 500 mg, 600 mg
] only
DESCRIPTION
Lodine XL (etodolac extended-release tablets) contains etodolac, which is a member of the
pyranocarboxylic acid group of nonsteroidal anti-inflammatory drugs (NSAIDs). Each tablet contains
etodolac for oral administration. Etodolac is a racemic mixture of [+]S and [-]R-enantiomers. It is a
white crystalline compound, insoluble in water, but soluble in alcohols, chloroform, dimethyl
sulfoxide, and aqueous polyethylene glycol.
The chemical name is (±) 1,8-diethyl-1,3,4,9-tetrahydropyrano-[3,4-b] indole-1-acetic acid. The
molecular weight is 287.37. Its molecular formula is C17H21NO3 and it has the following structural
formula:
The inactive ingredients in Lodine XL include: dibasic sodium phosphate, ethylcellulose,
hypromellose, lactose, magnesium stearate, polyethylene glycol, and titanium dioxide. In addition, the
400 mg tablets also contain FD&C Red #40, and FD&C Yellow #6 as color additives and
polysorbate 80. The 500 mg tablets also contain D&C Yellow #10, FD&C Blue #2, and iron oxide as
color additives and polysorbate 80. The 600 mg tablets also contain hydroxy-propyl cellulose and iron
oxide.
CLINICAL PHARMACOLOGY
Pharmacodynamics
Lodine XL is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory,
analgesic, and antipyretic activities in animal models. The mechanism of action of Lodine XL, like that
of other NSAIDs, is not completely understood, but may be related to prostaglandin synthetase
inhibition.
Pharmacokinetics
Absorption
Lodine XL and Lodine both contain etodolac, but differ in their release characteristics. The systemic
availability of etodolac from Lodine XL is generally greater than 80%. Etodolac does not undergo
NDA 20-584/S-004, S-006, S-007
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significant first-pass metabolism following oral administration. After oral administration of Lodine XL
in doses up to 800 mg once daily, peak concentra