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CA2433915A1 - Improved controlled release oral dosage form - Google Patents

Improved controlled release oral dosage form Download PDF

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Publication number
CA2433915A1
CA2433915A1 CA002433915A CA2433915A CA2433915A1 CA 2433915 A1 CA2433915 A1 CA 2433915A1 CA 002433915 A CA002433915 A CA 002433915A CA 2433915 A CA2433915 A CA 2433915A CA 2433915 A1 CA2433915 A1 CA 2433915A1
Authority
CA
Canada
Prior art keywords
dosage form
composition
polymer
methacrylic acid
hydroxypropyl methylcellulose
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CA002433915A
Other languages
French (fr)
Other versions
CA2433915C (en
Inventor
Boyong Li
Chih-Ming Chen
Xiu Xiu Cheng
Avinash Nangia
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Andrx Pharmaceuticals LLC
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Priority to CA2685214A priority Critical patent/CA2685214C/en
Publication of CA2433915A1 publication Critical patent/CA2433915A1/en
Application granted granted Critical
Publication of CA2433915C publication Critical patent/CA2433915C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)

Abstract

A once a day bupropion hydrochloride formulation comprising applying a bupropion/cellulose ether suspension to inert spheres wherein the spheres ar e further divided and coated with two types of film being, an enteric coating and a hydrophobic coating, wherein the active drug is then released at vario us pH throughout the gastrointestinal tract maintaining a therapeutic range ove r an extended period of time.

Claims (37)

1. A pelletized or extruded composition comprising:
a core which comprises (a) a carrier, and (b) at least one aminoketone antidepressant.
2. The composition of claim 1 wherein said core further comprises at least one binder.
3. The composition of claim 2 wherein said binder comprises hydroxypropyl methylcellulose.
4. The composition of claim 1 further comprising at least one polymer for controlled release delivery of said aminoketone antidepressant.
5. The composition of claim 4 wherein said polymer is selected from the group consisting of shellac, methacrylic acid copolymers, hydroxypropyl cellulose, hydroxypropyl methylcellulose, ethylcellulose, cellulose acetate, cellulose acetate butyrate, cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate trimellitate, polyvinyl acetate phthalate and mixtures thereof.
6. The composition of claim 4 wherein said polymer is water insoluble.
7. The composition of claim 6 wherein said water insoluble polymer comprises ethyl a methacrylic acid copolymer.
8. The composition of claim 6 wherein said water insoluble polymer comprises ethylcellulose.
9. The composition of claim 4 wherein said polymer is insoluble below about pH 7.
10. The composition as of claim 4 wherein said composition has a coating comprising a polymer.
11. A pelletized or extruded dosage form comprising at least one composition of claim 1.
12. The dosage form of claim 11 wherein said composition further compirses at least one binder.
13. The dosage form of claim 12 wherein said binder is hydroxypropyl methylcellulose.
14. The dosage form of claim 11 further comprising at least one polymer for controlled release delivery.
15. The dosage form of claim 14 wherein said polymer is selected from the group consisting of shellac, methacrylic acid copolymers, hydroxypropyl cellulose, hydroxypropyl methylcellulose, ethylcellulose, cellulose acetate, cellulose acetate butyrate, cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, cellulose acetate trimellitate, polyvinyl acetate phthalate and mixtures thereof.
16. The dosage form of claim 15 wherein said polymer is water insoluble.
17. The dosage form of claim 16 wherein said water insoluble polymer comprises ethylcellulose.
18. The dosage form of claim 14 wherein said polymer is insoluble below about pH 7.
19. The dosage form of claim 14 wherein said dosage form is for once daily administration.
20. The dosage form of claim 11 wherein said dosage form is a tablet, caplet, capsule or pelletized tablet.
21. The dosage form of claim 11 comprising at least two distinct compositions of claim 1.
22. The dosage form of claim 21 wherein at least one distinct composition is for controlled release.
23. A once daily dosage form comprising 150 mg of an aminoketone antidepressant, said dosage form providing an in vivo plasma profile selected from:
(a) Mean T max of about 5 or more hours (b) Mean C max of less than about 90 ng/ml, and (c) Mean AUC0-120h of more than about 350 (ng-h)ml.
24. The once daily dosage form of Claim 23 wherein said mean C max is less than about 80 ng/ml.
25. The once daily dosage form of claim 23 wherein said mean C max is less than about 70 ng/ml.
26. The once daily dosage form of claim 23 wherein said mean C max is less than about 60 ng/ml.
27. The once daily dosage form of claim 23 wherein said mean C max is less than about 50 ng/ml.
28. The once daily dosage form of claim 23 wherein said mean C max is less than about 40 ng/ml.
29. A pellet comprising:

(a) a core comprising (1) an inert carrier; (2) bupropion, its salts or isomers, or a pharmaceutically acceptable aminoketone antidepressant agent; and (3) a binder; and (b) a coating comprising a pH dependent coating agent selected from the group consisting of hydroxypropyl methylcellulose phthalate and a methacrylic acid copolymer.
30. A pellet comprising:
(a) a core comprising (1) an inert carrier; (2) bupropion, its salts or isomers, or a pharmaceutically acceptable aminoketone antidepressant agent; and (3) a binder; and (b) a coating comprising a methacrylic acid copolymer and a water insoluble polymer.
31. A dosage form of claim 11, said dosage form comprising a first pellet having a coating comprising methacrylic acid copolymer and a second pellet having a coating comprising methacrylic acid copolymer.
32. The dosage form of claim 31 wherein said methacrylic acid copolymer of said first pellet is pH independent.
33. The dosage form of claim 31 wherein said methacrylic acid copolymer of said second pellet is pH independent.
34. A dosage form comprising 150 mg of an aminoketone antidepressant wherein the aminoketone antidepressant has a dissolution profile as measured in pH 7.5 buffer at 1 hour between about 20% and 35%, at 4 hours between about 50 and 80% and at 8 hours between about 75 and 95%.
35. A dosage form comprising 150 mg of an aminoketone antidepressant wherein the aminoketone antidepressant has a dissolution profile of the active as measured in SGF 1.5 pH of less than 25% at 8 hours, of between about 25 and 45% at 10 hours and between about 50 and 80%
at 18 hours.
36. A dosage form as defined in Claim 34 wherein said aminoketone antidepressant comprises bupropion or a salt of bupropion.
37. A dosage form as defined in Claim 35 wherein said aminoketone antidepressant comprises bupropion or a salt of bupropion.
CA2433915A 2001-02-08 2002-02-08 Improved controlled release oral dosage form Expired - Fee Related CA2433915C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2685214A CA2685214C (en) 2001-02-08 2002-02-08 Improved controlled release oral dosage form

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US26745701P 2001-02-08 2001-02-08
US26745601P 2001-02-08 2001-02-08
US60/267,457 2001-02-08
US60/267,456 2001-02-08
PCT/US2002/003523 WO2002062299A2 (en) 2001-02-08 2002-02-08 Improved controlled release oral dosage form

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2685214A Division CA2685214C (en) 2001-02-08 2002-02-08 Improved controlled release oral dosage form

Publications (2)

Publication Number Publication Date
CA2433915A1 true CA2433915A1 (en) 2002-08-15
CA2433915C CA2433915C (en) 2010-04-20

Family

ID=26952450

Family Applications (3)

Application Number Title Priority Date Filing Date
CA2685214A Expired - Fee Related CA2685214C (en) 2001-02-08 2002-02-08 Improved controlled release oral dosage form
CA2433915A Expired - Fee Related CA2433915C (en) 2001-02-08 2002-02-08 Improved controlled release oral dosage form
CA2796884A Abandoned CA2796884A1 (en) 2001-02-08 2002-02-08 Improved controlled release oral dosage form

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CA2685214A Expired - Fee Related CA2685214C (en) 2001-02-08 2002-02-08 Improved controlled release oral dosage form

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2796884A Abandoned CA2796884A1 (en) 2001-02-08 2002-02-08 Improved controlled release oral dosage form

Country Status (3)

Country Link
EP (1) EP1357898A4 (en)
CA (3) CA2685214C (en)
WO (1) WO2002062299A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7537784B2 (en) 2003-08-08 2009-05-26 Biovail Laboratories International Srl Modified release tablet of bupropion hydrochloride

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8545880B2 (en) 1999-02-26 2013-10-01 Andrx Pharmaceuticals, Llc Controlled release oral dosage form
JP5020931B2 (en) * 2005-03-14 2012-09-05 サン・ファーマ・アドバンスド・リサーチ・カンパニー・リミテッド Oral drug delivery system
JP2010510320A (en) 2006-11-21 2010-04-02 マクニール−ピーピーシー・インコーポレーテツド Modified release analgesic suspension
US9833510B2 (en) 2007-06-12 2017-12-05 Johnson & Johnson Consumer Inc. Modified release solid or semi-solid dosage forms
JP2012528799A (en) * 2009-06-02 2012-11-15 ダウ グローバル テクノロジーズ エルエルシー Sustained release formulation
CN110200947A (en) * 2019-06-27 2019-09-06 深圳市泛谷药业股份有限公司 A kind of Bupropion enteric sustained-release pellet capsule and preparation method thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69331906T2 (en) * 1992-08-05 2002-12-19 F.H. Faulding & Co. Ltd., Underdale GRANULATED PHARMACEUTICAL COMPOSITION
GB9217295D0 (en) * 1992-08-14 1992-09-30 Wellcome Found Controlled released tablets
US6270805B1 (en) * 1998-11-06 2001-08-07 Andrx Pharmaceuticals, Inc. Two pellet controlled release formulation for water soluble drugs which contains an alkaline metal stearate
US6210716B1 (en) * 1999-02-26 2001-04-03 Andrx Pharmaceuticals, Inc. Controlled release bupropion formulation

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7537784B2 (en) 2003-08-08 2009-05-26 Biovail Laboratories International Srl Modified release tablet of bupropion hydrochloride

Also Published As

Publication number Publication date
WO2002062299A2 (en) 2002-08-15
EP1357898A4 (en) 2005-07-13
CA2685214A1 (en) 2002-08-15
CA2796884A1 (en) 2002-08-15
EP1357898A2 (en) 2003-11-05
WO2002062299A3 (en) 2003-04-24
CA2433915C (en) 2010-04-20
CA2685214C (en) 2013-01-22

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EEER Examination request
MKLA Lapsed

Effective date: 20210831

MKLA Lapsed

Effective date: 20200210