| US 7,537,784 B2 | ||
| Modified release tablet of bupropion hydrochloride | ||
| Werner Oberegger, Mississauga (Canada); Okponanabofa Eradiri, Ashburn, Va. (US); Fang Zhou, Centreville, Va. (US); and Paul Maes, Toronto (Canada) | ||
| Assigned to Biovail Laboratories International SRL, St. Michael (Barbados) | ||
| Filed on Jun. 13, 2006, as Appl. No. 11/451,496. | ||
| Application 11/451496 is a continuation of application No. 10/507525, abandoned, previously published as PCT/US03/24700, filed on Aug. 08, 2003. | ||
| Prior Publication US 2006/0228415 A1, Oct. 12, 2006 | ||
| Int. Cl. A61K 9/20 (2006.01); A61K 9/22 (2006.01); A61K 9/24 (2006.01); A61K 9/28 (2006.01); A61K 9/30 (2006.01); A61K 9/36 (2006.01); A61K 9/42 (2006.01) | ||
| U.S. Cl. 424—468 [424/464; 424/465; 424/472; 424/474; 424/475; 424/476; 424/479; 424/480] | 16 Claims |
| 1. A modified-release tablet comprising:
(i) a core comprising an effective amount of bupropion hydrochloride, polyvinyl alcohol, and glyceryl behenate, wherein said
bupropion hydrochloride is present in an amount of at least about 94% by weight of the core dry weight, said polyvinyl alcohol
is present in an amount of about 3% by weight of the core dry weight, and said glyceryl behenate is present in an amount of
about 3% by weight of each core dry weight;
(ii) a control-releasing coat completely surrounding and contacting said core, said control-releasing coat comprising ethyl
cellulose grade PR 100, polyethylene glycol 1450, and polyvinylpyrrolidone, wherein said ethyl cellulose grade PR 100 is present
in an amount of from about 45% to about 50% by weight of the control-releasing coating dry weight, said polyethylene glycol
1450 is present in an amount of about 12% by weight of the control-releasing coating dry weight, and said polyvinylpyrrolidone
is present in an amount of from about 25% to about 50% of the control-releasing coat dry weight, wherein the amount of said
control-releasing coat applied is from about 9% to about 15% by weight of the dry tablet core; and
(iii) a moisture barrier surrounding said control-releasing coat, said moisture barrier comprising methacrylic acid copolymer,
polyethylene glycol 1450, triethyl citrate and silicon dioxide, wherein said methacrylic acid copolymer is present in an amount
of about 66% by weight of said moisture barrier dry weight, said polyethylene glycol 1450 and triethyl citrate is present
in an amount of about 10% by weight of said moisture barrier dry weight in a proportion of 1 part triethyl citrate to 2 parts
polyethylene glycol 1450, and said silicon dioxide is present in an amount of about 25% by weight of said moisture barrier
dry weight, wherein the amount of the said moisture barrier applied is no more than about 2.5% of the tablet dry weight,
wherein the tablet provides an extended-release of the bupropion hydrochloride such that after about 2 hours about 5% of the
bupropion hydrochloride content is released, after about 4 hours about 32% of the bupropion hydrochloride content is released,
after about 8 hours about 74% of the bupropion hydrochloride content is released and after about 16 hours no less than about
99% of the bupropion hydrochloride content is released,
and wherein the ratio of the ethyl cellulose grade PR 100:polyethylene glycol 1450:polyvinylpyrrolidone is from about 3:1:4
to about 5:1:3.
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