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Stable Tablet Formulation of Clopidogrel Salts Disclosure Number: IPCOM000128929D
Publication Date: 2005-Sep-21
Document File: 1 page(s) / 22K

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A stable formulation of the hydrobromide and napsylate salts of clopidogrel is described, which contains microcrystalline cellulose as filler and sodium stearyl fumarate as lubricant.

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Stable Tablet Formulation of Clopidogrel Salts

Clopidogrel, an inhibitor of platelet agglomeration is sold under
the tradename PlavixTM in a tablet formulation containing 97.875 mg
of clopidogrel bisulfate (equivalent to 75 mg of clopidogrel). A
stable formulation of clopidogrel bisulfate was described in pat-
ent US 6,914,141 B2, comprising a lubricant from the group con-
sisting of zinc stearate, sodium stearyl fumarate and stearic
acid, but excluding preferably microcrystalline cellulose, the
latter being described as inhibiting the dissolution of clopido-
grel bisulfate.

Stability and dissolution of formulations containing the hydrobro-
mide and napsylate salts of clopidogrel were tested. It was found
that the presence of microcrystalline cellulose as filler in
amounts of about 4% to 15% of the tablet weight did not signifi-
cantly affect the dissolution. Formulations containing magnesium
stearate as lubricant were less stable than formulations contain-
ing sodium stearyl fumarate as lubricant in amounts of about 0.5%
to 1.5%. Stable tablet formulations further included lactose mono-
hydrate, 15% to 35%, as filler, low substituted hydroxypropylcel-
lulose, 2% to 8%, as disintegrant, methylhydroxypropylcellulose,
1% to 6%, as binder, and silicium dioxide, 0.5% to 1.5%, as gli-

The tablets were manufactured by wet granulation and then coated
using a mixture of hypromellose, macrogol, lactose monohydrate,
titan (IV) oxide, talc and a colorant.