ENTOCORT EC- budesonide capsule

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

BUDESONIDE (UNII: Q3OKS62Q6X) (BUDESONIDE - UNII:Q3OKS62Q6X)

Available from:

Physicians Total Care, Inc.

INN (International Name):

BUDESONIDE

Composition:

BUDESONIDE 3 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

ENTOCORT EC is indicated for - the treatment of mild to moderate active Crohn's disease involving the iluem and/or the ascending colon and - the maintenance of clinical remission of mild to moderate Crohn's disease involving the ileum and/or the ascending colon for up to 3 months. the maintenance of clinical remission of mild to moderate Crohn's disease involving the ileum and/or the ascending colon for up to 3 months. ENTOCORT EC is contraindicated in patients with known hypersensitivity to budesonide.

Product summary:

ENTOCORT EC 3 mg capsules are hard gelatin capsules with an opaque light grey body and an opaque pink cap, coded with ENTOCORT EC 3 mg on the capsule. They are supplied as follows: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) [See USP Controlled Room Temperature]. Keep container tightly closed.

Authorization status:

New Drug Application

Summary of Product characteristics

ENTOCORT EC- BUDESONIDE CAPSULE
PHYSICIANS TOTAL CARE, INC.
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ENTOCORT® EC
(BUDESONIDE)
CAPSULES
DESCRIPTION SECTION
Budesonide, the active ingredient of ENTOCORT EC capsules, is a
synthetic corticosteroid. It is
designated chemically as (RS)-11β, 16α,
17,21-tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-
acetal with butyraldehyde. Budesonide is provided as a mixture of two
epimers (22R and 22S). The
empirical formula of budesonide is C
H O and its molecular weight is 430.5. Its structural formula
is:
Budesonide is a white to off-white, tasteless, odorless powder that is
practically insoluble in water and
heptane, sparingly soluble in ethanol, and freely soluble in
chloroform. Its partition coefficient between
octanol and water at pH 5 is 1.6 x 10
ionic strength 0.01.
Each capsule contains 3 mg of micronized budesonide with the following
inactive ingredients:
ethylcellulose, acetyltributyl citrate, methacrylic acid copolymer
type C, triethyl citrate, antifoam M,
polysorbate 80, talc, and sugar spheres. The capsule shells have the
following inactive ingredients:
gelatin, iron oxide, and titanium dioxide.
CLINICAL PHARMACOLOGY
Budesonide has a high topical glucocorticosteroid (GCS) activity and a
substantial first pass
®
25
34
6
3
elimination. The formulation contains granules which are coated to
protect dissolution in gastric juice,
but which dissolve at pH >5.5, ie, normally when the granules reach
the duodenum. Thereafter, a matrix
of ethylcellulose with budesonide controls the release of the drug
into the intestinal lumen in a time-
dependent manner.
PHARMACOKINETICS
_ABSORPTION_
The absorption of ENTOCORT EC seems to be complete, although C
and T
are variable. Time
to peak concentration varies in individual patients between 30 and 600
minutes. Following oral
administration of 9 mg of budesonide in healthy subjects, a peak
plasma concentration of approximately
5 nmol/L is observed and the area under the plasma concentration time
curve is approximately 30
nmol hr/L. The systemic availability a