IP Library › Granted Patent US 7,645,802
Granted Patent B2
US 7,645,802 · App. 11/930,644 · Granted Jan 12, 2010

Bupropion hydrobromide and therapeutic applications

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Patent No.
US 7,645,802
App. No.
11/930,644
Granted
Jan 12, 2010
Kind
B2
Abstract

Bupropion hydrobromide formulations as well as their use for the treatment of conditions is described.

Claims (27)

1. A modified release bupropion hydrobromide composition comprising:

a core comprising a therapeutically effective amount of bupropion hydrobromide; and

a controlled release polymeric coat comprising from about 1% to about 12% by weight of tablet dry weight of a water-insoluble polymer and from about 1.5% to about 10% by weight of tablet dry weight of a water-soluble polymer;

wherein said coat at least partially surrounds said core; and

wherein said composition releases bupropion hydrobromide in a first dissolution medium consisting of 0.1 N HCl and 5%-40% v/v ethanol at a rate that is less than or equal to about 1.1 times the rate of release of bupropion hydrobromide from an identical modified release pharmaceutical composition in a second dissolution medium consisting of 0.1 N HCl, measured over a time period of at least from 0 to 2 hours measured using a USP Apparatus I at 75 rpm and at 37±0.5° C.

2. The modified release composition according to claim 1 wherein said composition releases bupropion hydrobromide in a first dissolution medium consisting of 0.1 N HCl and 5%-40% v/v ethanol at a rate that is less than or equal to the rate of release of bupropion hydrobromide from the identical modified release composition in a second dissolution medium consisting of 0.1 N HCl.

3. The modified release composition according to claim 2 wherein the first dissolution medium consists of 0.1 N HCl and 5% v/v ethanol.

4. The modified release composition according to claim 2 wherein the first dissolution medium consists of 0.1 N HCl and 40% v/v ethanol.

5. The modified release composition according to claim 1 wherein the time period is from 0 to 16 hours.

6. The modified release composition according to claim 1 wherein the composition is a tablet comprising 174 mg, 348 mg or 522 mg of bupropion hydrobromide.

7. The modified release bupropion hydrobromide composition according to claim 1 wherein said composition releases bupropion hydrobromide in a dissolution medium consisting of 0.1 N HCl and 40% v/v ethanol at a rate that is less than the rate of release of bupropion hydrochloride from a modified release bupropion hydrochloride composition, in the identical dissolution medium consisting of 0.1 N HCl and 40% v/v ethanol, measured over a time period of at least from 0 to 2 hours measured using a USP Apparatus I at 75 rpm and at 37±0.5° C.;

wherein the modified release bupropion hydrochloride composition comprises:

a core comprising bupropion hydrochloride, in an amount equimolar to the amount of bupropion hydrobromide in the modified release bupropion hydrobromide composition; and

the identical controlled release polymeric coat comprising a water-insoluble polymer and a water-soluble polymer, used in the bupropion hydrobromide composition; and

wherein the coat at least partially surrounds the core of the modified release bupropion hydrochloride composition.

8. A method of reducing alcohol-induced dose dumping of bupropion hydrobromide in a patient comprising administering to a patient the modified release pharmaceutical composition of claim 1 .

9. The method of claim 8 wherein the composition is a tablet comprising 174 mg, 348 mg or 522 mg of bupropion hydrobromide.

10. The modified release composition according to claim 1 , wherein said water insoluble polymer is selected from the group consisting of cellulose ethers, cellulose esters, polyvinyl alcohol, and mixtures thereof.

11. The modified release composition according to claim 1 , wherein said water soluble polymer is selected from the group consisting of polyvinylpyrrolidone, hydroxypropyl methylcellulose, hydroxypropyl cellulose, and mixtures thereof.

12. The modified release composition according to claim 1 wherein said water insoluble polymer is ethyl cellulose.

13. The modified release composition according to claim 1 wherein said water soluble polymer is polyvinylpyrrolidone.

14. The modified release composition according to claim 1 wherein said water insoluble polymer is ethyl cellulose and said water soluble polymer is polyvinylpyrrolidone.

15. A modified release bupropion hydrobromide composition comprising:

a core comprising a therapeutically effective amount of bupropion hydrobromide; and

a controlled release polymeric coat comprising from about 0.5% to about 10% by weight of tablet dry weight of a water-insoluble polymer and from about 1.5% to about 10% by weight of tablet dry weight of a water-soluble polymer;

wherein said coat at least partially surrounds said core; and

wherein said composition releases bupropion hydrobromide in a first dissolution medium consisting of 0.1 N HCl and 5%-40% v/v ethanol at a rate that is less than or equal to about 1.1 times the rate of release of bupropion hydrobromide from an identical modified release pharmaceutical composition in a second dissolution medium consisting of 0.1 N HCl, measured over a time period of at least from 0 to 2 hours measured using a USP Apparatus I at 75 rpm and at 37±0.5° C.

Assignments (26)
U.S. PATENT SECURITY AGREEMENT Recorded Nov 25, 2025
From: BAUSCH HEALTH IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 073715/0375 →
RELEASE OF SECURITY INTEREST Recorded Nov 20, 2025
From: THE BANK OF NEW YORK MELLON, AS NOTES COLLATERAL AGENT
To: BAUSCH HEALTH COMPANIES INC.; BAUSCH HEALTH, CANADA INC.; BAUSCH HEALTH IRELAND LIMITED; SOLTA MEDICAL IRELAND LIMITED
Reel/Frame 073654/0300 →
RELEASE OF SECURITY INTEREST Recorded Nov 20, 2025
From: THE BANK OF NEW YORK MELLON, AS NOTES COLLATERAL AGENT
To: ATON PHARMA, INC.; BAUSCH & LOMB INCORPORATED; BAUSCH & LOMB PHARMA HOLDINGS CORP.; COMMONWEALTH LABORATORIES, LLC; DOW PHARMACEUTICAL SCIENCES, INC.; ECR PHARMACEUTICALS CO., INC.; LABORATOIRE CHAUVIN S.A.S.; MEDICIS PHARMACEUTICAL CORPORATION; ONPHARMA INC.; ORAPHARMA, INC.; PRECISION DERMATOLOGY, INC.; SALIX PHARMACEUTICALS, LTD.; SALIX PHARMACEUTICALS, INC.; SANTARUS, INC.; SOLTA MEDICAL, INC.; SYNERGETICS USA, INC.; TECHNOLAS PERFECT VISION GMBH; VALEANT CANADA LP; VALEANT PHARMACEUTICALS INTERNATIONAL; VALEANT PHARMACEUTICALS INTERNATIONAL, INC.; VALEANT PHARMACEUTICALS NORTH AMERICA LLC; WIRRA IP PTY LIMITED; VALEANT PHARMA POLAND SP. Z O.O.; VALEANT PHARMACEUTICALS LUXEMBOURG S.A R.L.; VALEANT PHARMACEUTICALS IRELAND LIMITED
Reel/Frame 073637/0001 →
RELEASE OF SECURITY INTEREST Recorded Nov 20, 2025
From: THE BANK OF NEW YORK MELLON, AS NOTES COLLATERAL AGENT
To: BAUSCH HEALTH IRELAND LIMITED; BAUSCH HEALTH COMPANIES INC.; BAUSCH HEALTH, CANADA INC.; TECHNOLAS PERFECT VISION GMBH; VALEANT PHARMACEUTICALS LUXEMBOURG S.A R.L.; VALEANT PHARMA POLAND SPOLKA Z ORGANICZONA ODPOWIEDZIALNOSCIA; VALEANT SP. Z.O.O.
Reel/Frame 073637/0222 →
RELEASE OF SECURITY INTEREST Recorded Apr 8, 2025
From: BARCLAYS BANK PLC, AS COLLATERAL AGENT
To: SOLTA MEDICAL, INC.; PRECISION DERMATOLOGY, INC.; BAUSCH HEALTH IRELAND LIMITED (F/K/A/ VALEANT PHARMACEUTICALS IRELAND LIMITED); SALIX PHARMACEUTICALS, INC.; SALIX PHARMACEUTICALS, LTD; SANTARUS, INC.; MEDICIS PHARMACEUTICAL CORPORATION; HUMAX PHARMACEUTICAL S.A.; SOLTA MEDICAL IRELAND LIMITED; BAUSCH & LOMB MEXICO, S.A. DE C.V.; BAUSCH+LOMB OPS B.V.; BAUSCH HEALTH AMERICAS, INC.; BAUSCH HEALTH COMPANIES INC.; BAUSCH HEALTH HOLDCO LIMITED; BAUSCH HEALTH MAGYARORSZAG KFT (A/K/A BAUSCH HEALTH HUNGARY LLC); BAUSCH HEALTH POLAND SPOLKA Z OGRANICZONA ODPOWIEDZIALNOSCIA (F/K/A VALEANT PHARMA POLAND SPOLKA Z OGRANICZONA ODPOWIEDZIALNOSCIA); BAUSCH HEALTH US, LLC; BAUSCH HEALTH, CANADA INC. / SANTE BAUSCH, CANADA INC.; ICN POLFA RZESZOW SPOLKA AKCYJNA (A/K/A ICN POLFA RZESZOW S.A.); ORAPHARMA, INC.; PRZEDSIEBIORSTWO FARMACEUTYCZNE JELFA SPOLKA AKCYJNA (A/K/A PRZEDSIEBIORSTWO FARMACEUTYCZNE JELFA S.A.); SOLTA MEDICAL DUTCH HOLDINGS B.V.; V-BAC HOLDING CORP.; VRX HOLDCO LLC; 1261229 B.C. LTD.; 1530065 B.C. LTD.
Reel/Frame 070778/0199 →
SECURITY AGREEMENT (SECOND LIEN) Recorded Nov 4, 2022
From: BAUSCH HEALTH COMPANIES INC.; BAUSCH HEALTH IRELAND LIMITED; SOLTA MEDICAL IRELAND LIMITED
To: THE BANK OF NEW YORK MELLON, AS NOTES COLLATERAL AGENT
Reel/Frame 062078/0276 →
SECURITY AGREEMENT (FIRST LIEN) Recorded Nov 4, 2022
From: BAUSCH HEALTH COMPANIES INC.; BAUSCH HEALTH IRELAND LIMITED; SOLTA MEDICAL IRELAND LIMITED
To: THE BANK OF NEW YORK MELLON, AS NOTES COLLATERAL AGENT
Reel/Frame 061882/0708 →
SECURITY AGREEMENT (SECOND LIEN) Recorded Oct 5, 2022
From: BAUSCH HEALTH US, LLC; BAUSCH HEALTH AMERICAS, INC.; MEDICIS PHARMACEUTICAL CORPORATION; ORAPHARMA, INC.; PRECISION DERMATOLOGY, INC.; SALIX PHARMACEUTICALS, INC.; SALIX PHARMACEUTICALS, LTD.; SANTARUS, INC.; SOLTA MEDICAL, INC.
To: THE BANK OF NEW YORK MELLON, AS NOTES COLLATERAL AGENT
Reel/Frame 061606/0468 →
SECURITY AGREEMENT (FIRST LIEN) Recorded Oct 4, 2022
From: BAUSCH HEALTH US, LLC; BAUSCH HEALTH AMERICAS, INC.; MEDICIS PHARMACEUTICAL CORPORATION; ORAPHARMA, INC.; PRECISION DERMATOLOGY, INC.; SALIX PHARMACEUTICALS, INC.; SALIX PHARMACEUTICALS, LTD.; SANTARUS, INC.; SOLTA MEDICAL, INC.
To: THE BANK OF NEW YORK MELLON, AS NOTES COLLATERAL AGENT
Reel/Frame 061595/0066 →
SECURITY INTEREST Recorded Jun 13, 2022
From: BAUSCH HEALTH COMPANIES INC.; BAUSCH HEALTH, CANADA INC.; BAUSCH HEALTH IRELAND LIMITED; SOLTA MEDICAL IRELAND LIMITED
To: THE BANK OF NEW YORK MELLON
Reel/Frame 060346/0705 →
SECURITY INTEREST Recorded Oct 5, 2021
From: BAUSCH & LOMB IRELAND LIMITED; BAUSCH HEALTH COMPANIES INC.; DR. GERHARD MANN CHEM.-PHARM. FABRIK GMBH; TECHNOLAS PERFECT VISION GMBH
To: THE BANK OF NEW YORK MELLON, AS NOTES COLLATERAL AGENT
Reel/Frame 057821/0800 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Jul 3, 2019
From: BAUSCH HEALTH IRELAND LIMITED; BAUSCH HEALTH COMPANIES INC.; BAUSCH HEALTH, CANADA INC.; TECHNOLAS PERFECT VISION GMBH; VALEANT PHARMACEUTICALS LUXEMBOURG S.À R.L.; VALEANT PHARMA POLAND SPOLKA Z OGRANICZONA ODPOWIEDZIALNOSCIA; VALEANT SP. Z O. O.
To: THE BANK OF NEW YORK MELLON, AS COLLATERAL AGENT
Reel/Frame 049672/0652 →
SECURITY INTEREST Recorded Feb 26, 2018
From: ATON PHARMA, INC.; BAUSCH & LOMB INCORPORATED; BAUSCH & LOMB PHARMA HOLDINGS CORP.; COMMONWEALTH LABORATORIES, LLC; DOW PHARMACEUTICAL SCIENCES, INC.; ECR PHARMACEUTICALS CO., INC.; LABORATOIRE CHAUVIN S.A.S.; MEDICIS PHARMACEUTICAL CORPORATION; ONPHARMA INC.; ORAPHARMA, INC.; PRECISION DERMATOLOGY, INC.; SALIX PHARMACEUTICALS, LTD.; SALIX PHARMACEUTICALS, INC.; SANTARUS, INC.; SOLTA MEDICAL, INC.; SYNERGETICS USA, INC.; TECHNOLAS PERFECT VISION GMBH; VALEANT CANADA LP; VALEANT PHARMACEUTICALS INTERNATIONAL; VALEANT PHARMACEUTICALS INTERNATIONAL, INC.; VALEANT PHARMACEUTICALS NORTH AMERICA LLC; WIRRA IP PTY LIMITED; VALEANT PHARMA POLAND SP. Z O.O.; VALEANT PHARMACEUTICALS LUXEMBOURG S.A R.L.; VALEANT PHARMACEUTICALS IRELAND LIMITED
To: BARCLAYS BANK PLC, AS COLLATERAL AGENT
Reel/Frame 045444/0299 →
SECURITY INTEREST Recorded Feb 26, 2018
From: ATON PHARMA, INC.; BAUSCH & LOMB INCORPORATED; BAUSCH & LOMB PHARMA HOLDINGS CORP.; COMMONWEALTH LABORATORIES, LLC; DOW PHARMACEUTICAL SCIENCES, INC.; ECR PHARMACEUTICALS CO., INC.; LABORATOIRE CHAUVIN S.A.S.; MEDICIS PHARMACEUTICAL CORPORATION; ONPHARMA INC.; ORAPHARMA, INC.; PRECISION DERMATOLOGY, INC.; SALIX PHARMACEUTICALS, LTD.; SALIX PHARMACEUTICALS, INC.; SANTARUS, INC.; SOLTA MEDICAL, INC.; SYNERGETICS USA, INC.; TECHNOLAS PERFECT VISION GMBH; VALEANT CANADA LP; VALEANT PHARMACEUTICALS INTERNATIONAL; VALEANT PHARMACEUTICALS INTERNATIONAL, INC.; VALEANT PHARMACEUTICALS NORTH AMERICA LLC; WIRRA IP PTY LIMITED; VALEANT PHARMA POLAND SP. Z O.O.; VALEANT PHARMACEUTICALS LUXEMBOURG S.A R.L.; VALEANT PHARMACEUTICALS IRELAND LIMITED
To: THE BANK OF NEW YORK MELLON, AS COLLATERAL AGENT
Reel/Frame 045444/0634 →
NOTICE OF SUCCESSION OF AGENCY Recorded Jan 9, 2015
From: GOLDMAN SACHS LENDING PARTNERS, LLC
To: BARCLAYS BANK PLC, AS SUCCESSOR AGENT
Reel/Frame 034749/0689 →
CHANGE IN NAME AND COUNTRY OF INCORPORATION Recorded Aug 9, 2012
From: VALEANT INTERNATIONAL (BARBADOS) SRL
To: VALEANT INTERNATIONAL BERMUDA
Reel/Frame 028757/0052 →
SECURITY AGREEMENT Recorded Jul 18, 2011
From: VALEANT INTERNATIONAL (BARBADOS) SRL, A BARBADOS INTERNATIONAL SOCIETY WITH RESTRICTED LIABILITY; BIOVALE LABORATORIES INTERNATIONAL (BARBADOS) SRL, A BARBADOS INTERNATIONAL SOCIETY WITH RESTRICTED LIABILITY
To: GOLDMAN SACHS LENDING PARTNERS LLC, AS COLLATERAL AGENT
Reel/Frame 026605/0801 →
CHANGE OF NAME Recorded Jun 7, 2011
From: BIOVAIL LABORATORIES INTERNATIONAL SRL
To: VALEANT INTERNATIONAL (BARBADOS) SRL
Reel/Frame 026404/0095 →
PATENT SECURITY RELEASE AGREEMENT Recorded Mar 14, 2011
From: GOLDMAN SACHS LENDING PARTNERS LLC
To: BIOVAIL INTERNATIONAL LABORATORIES SRL; BIOVAIL INTERNATIONAL LABORATORIES (BARBADOS) SRL
Reel/Frame 025950/0073 →
RELEASE OF SECURITY AGREEMENT Recorded Oct 6, 2010
From: JPMORGAN CHASE BANK, N.A., TORONTO BRANCH
To: BIOVAIL CORPORATION; BIOVAIL LABORATORIES INTERNATIONAL SRL
Reel/Frame 025095/0479 →
SECURITY AGREEMENT Recorded Oct 4, 2010
From: BIOVAIL INTERNATIONAL LABORATORIES SRL; BIOVAIL INTERNATIONAL LABORATORIES (BARBADOS) SRL
To: GOLDMAN SACHS LENDING PARTNERS LLC, AS COLLATERAL AGENT
Reel/Frame 025084/0022 →
PATENT AND TRADEMARK SECURITY AGREEMENT Recorded Jun 11, 2009
From: BIOVAIL LABORATORIES INTERNATIONAL SRL
To: J.P. MORGAN CHASE BANK, N.A., TORONTO BRANCH, AS ADMINISTRATIVE AGENT
Reel/Frame 022813/0195 →
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNEE'S ADDRESS PREVIOUSLY RECORDED ON REEL 022250 FRAME 0123. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Feb 23, 2009
From: JACKSON, GRAHAM
To: BIOVAIL LABORATORIES INTERNATIONAL SRL.
Reel/Frame 022293/0725 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 12, 2009
From: JACKSON, GRAHAM
To: BIOVAIL LABORATORIES INTERNATIONAL S.R.L.
Reel/Frame 022250/0123 →
LICENSE Recorded Dec 24, 2008
From: BIOVAIL LABORATORIES INTERNATIONAL SRL
To: SANOFI-AVENTIS U.S. LLC
Reel/Frame 022024/0492 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 27, 2008
From: OBEREGGER, WERNER; MAES, PAUL; SALEH, MOHAMMAD ASHTY
To: BIOVAIL LABORATORIES INTERNATIONAL SRL
Reel/Frame 020708/0980 →