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|Title:||Modified release formulations of a bupropion salt|
|Abstract:||The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.|
|Inventor(s):||Oberegger; Werner (Mississauga, CA), Zhou; Fang (Davie, FL), Maes; Paul (Toronto, CA), Jackson; Graham (Co. Kildare, IE), Saleh; Mohammad Ashty (Oakville, CA)|
|Assignee:||Biovail Laboratories International S.r.l. (St. Michael, BB)|
1. A modified release tablet comprising (a) a core comprising (i) bupropion hydrobromide in an amount of from 40% to 99% by weight of the tablet dry weight; (ii) binder in an amount
of from 0.25% to 25% by weight of the tablet dry weight; and (iii) lubricant in an amount of from 0.1% to 6% by weight of the tablet dry weight; and (b) a control-releasing coat substantially surrounding said core.
2. The composition of claim 1 wherein the binder is selected from the group consisting of hydrogenated vegetable oil, castor oil, paraffin, higher aliphatic alcohols, higher alphatic acids, long chain fatty acids, fatty acid esters, fatty alcohols, fatty acid esters, fatty acid glycerides, hydrogenated fats, hydrocarbons, waxes, stearic acid, stearyl alcohol, hydrophobic and hydrophilic polymers having hydrocarbon backbones, modified starch, gelatin, polyvinylpyrrolidone, hydroxypropyl methylcellulose, hydroxypropyl cellulose, polyvinyl alcohol and mixtures thereof.
3. The composition of claim 2 wherein the binder is polyvinyl alcohol.
4. The composition of claim 1 wherein the lubricant is selected from the group consisting of glyceryl behenate, stearic acid, hydrogenated vegetable oils, stearyl alcohol, leucine, polyethylene glycol, magnesium stearate, glyceryl monostearate, ethylene oxide polymers, sodium lauryl sulfate, magnesium lauryl sulfate, sodium oleate, sodium stearyl fumarate, DL-leucine, colloidal silica, and mixtures thereof.
5. The composition of claim 4 wherein the lubricant is glyceryl behenate.
6. The composition of claim 1 wherein the coat comprises a water-insoluble polymer, and a water-soluble polymer.
7. The composition of claim 6 wherein the water-insoluble polymer is present in an amount of from 1% to 12% by weight of the tablet dry weight; and the water-soluble polymer is present in an amount of from 1.5% to 10% by weight of the tablet dry weight.
8. The composition of claim 6 wherein the water-insoluble polymer is selected from the group consisting of cellulose ethers, cellulose esters, and polyvinyl alcohol.
9. The composition of claim 8 wherein the water-insoluble polymer is ethyl cellulose.
10. The composition of claim 6 wherein the water-soluble polymer is selected from the group consisting of polyvinylpyrrolidone, hydroxypropyl methylcellulose, hydroxypropyl cellulose and mixtures thereof.
11. The composition of claim 10 wherein the water-soluble polymer is polyvinylpyrrolidone.
12. The composition of claim 6 further comprising a plasticizer.
13. The composition of claim 12 wherein the plasticizer is present in an amount of from 0.5% to 4% by weight of the tablet dry weight.
14. The composition of claim 12 wherein the plasticizer is selected from the group consisting of acetylated monoglycerides, acetyltributyl citrate, butyl phthalyl butyl glycolate, dibutyl tartrate, diethyl phthalate, dimethyl phthalate, ethyl phthalyl ethyl glycolate, glycerin, propylene glycol, triacetin, tripropioin, diacetin, dibutyl phthalate, acetyl monoglyceride, acetyltriethyl citrate, polyethylene glycols, castor oil, rape seed oil, olive oil, sesame oil, triethyl citrate; polyhydric alcohols, glycerol, glycerin sorbitol, acetate esters, gylcerol triacetate, acetyl triethyl citrate, dibenzyl phthalate, dihexyl phthalate, butyl octyl phthalate, diisononyl phthalate, butyl octyl phthalate, dioctyl azelate, epoxidized tallate, triisoctyl trimellitate, diethylhexyl phthalate, di-n-octyl phthalate, di-i-octyl phthalate, di-i-decyl phthalate, di-n-undecyl phthalate, di-n-tridecyl phthalate, tri-2-ethylhexyl trimellitate, di-2-ethylhexyl adipate, di-2-ethylhexyl sebacate, di-2-ethylhexyl azelate, dibutyl sebacate, diethyloxalate, diethylmalate, diethylfumerate, dibutylsuccinate, diethylmalonate, dibutylphthalate, dibutylsebacate, glyceroltributyrate, polyols, and mixtures thereof.
15. The composition of claim 14 wherein the plasticizer is selected from the group consisting of polyethylene glycol 4000, dibutyl sebacate, and a mixture thereof.
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