DIPENTUM olsalazine sodium capsule gelatin coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

olsalazine sodium (UNII: Y7JEW0XG7I) (olsalazine - UNII:ULS5I8J03O)

Available from:

Alaven Pharmaceutical LLC

INN (International Name):

olsalazine sodium

Composition:

olsalazine sodium 250 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application

Summary of Product characteristics

DIPENTUM- OLSALAZINE SODIUM CAPSULE, GELATIN COATED
ALAVEN PHARMACEUTICAL LLC
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DIPENTUM
(OLSALAZINE SODIUM CAPSULES)
Rx Only
DESCRIPTION
The active ingredient in DIPENTUM Capsules (olsalazine sodium) is the
sodium salt of a salicylate,
disodium 3,3'-azobis (6-hydroxybenzoate) a compound that is
effectively bioconverted to 5-
aminosalicylic acid (5-ASA), which has anti-inflammatory activity in
ulcerative colitis. Its empirical
formula is C
H N Na O with a molecular weight of 346.21.
The structural formula is:
Olsalazine sodium is a yellow crystalline powder, which melts with
decomposition at 240°C. It is the
sodium salt of a weak acid, soluble in water and DMSO, and practically
insoluble in ethanol,
chloroform, and ether. Olsalazine sodium has acceptable stability
under acidic or basic conditions.
DIPENTUM is supplied in hard gelatin capsules for oral administration.
The inert ingredient in each
250 mg capsule of olsalazine sodium is magnesium stearate. The capsule
shell contains the following
inactive ingredients: black iron oxide, caramel, gelatin, and titanium
dioxide.
CLINICAL PHARMACOLOGY
After oral administration, olsalazine has limited systemic
bioavailability. Based on oral and intravenous
dosing studies, approximately 2.4% of a single 1.0 g oral dose is
absorbed. Less than 1% of olsalazine
is recovered in the urine. The remaining 98 to 99% of an oral dose
will reach the colon, where each
molecule is rapidly converted into two molecules of 5-aminosalicylic
acid (5-ASA) by colonic bacteria
and the low prevailing redox potential found in this environment. The
liberated 5-ASA is absorbed
slowly resulting in very high local concentrations in the colon.
The conversion of olsalazine to mesalamine (5-ASA) in the colon is
similar to that of sulfasalazine,
which is converted into sulfapyridine and mesalamine. It is thought
that the mesalamine component is
therapeutically active in ulcerative colitis (A.K. Azad-Kahn et al,
_LANCET_, 2:892-895, 1977). The
usual dose of sulfasalazine for maintenance of remi