← Back to Patent Explorer
US4547498A Expired / Lapsed US ⏱️ 0.0 years remaining

Pharmaceutical combination composition and associated method

Assignee: Mylan Pharmaceuticals Inc
•
Filing: 1984-02-17
•
Granted: 1985-10-15
•
Expires: 2004-02-17
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

Abstract

Abstract A novel combination pharmaceutical composition is described, together with a method for making the same, wherein the pharmaceutcially active ingredients are separately milled and then formed into separate granules, and only thereafter blended together to form the combination composition. The method for achieving this novel combination composition is also described. In particular, a novel combination composition of triamterene and hydrochlorothiazide having improved bioavialability and novel effectiveness to prevent or eliminate hypokalemic side effects is also described.

Inventors

  • 👤 Cheryl D. Blume
  • 👤 Paul H. Bonner

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 05:18
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5084; A61K31/00; A61K31/33; A61K31/395; A61K31/54; A61K9/20; A61K9/2072; A61K9/2077

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 169 words
A method for forming a granularly-heterogenous composition having combined pharmaceutically-effective diuretic anti-hypokalemic and antihypertensive activity comprising the steps of mixing finely-divided particles of a triamterene-active pteridine ingredient with at least one finely-divided pharmaceutically-acceptable inert ingredient to form a first mixture, and granulating said first mixture to form first granules composed of a homogeneous blend of the particles of said first mixture; separately mixing finely-divided particles of a hydrochlorothiazide-active benzothiadiazide ingredient with at least one finely-divided pharmaceutically-acceptable inert ingredient to form a second mixture, and separately granulating said second mixture to form second granules composed of a homogeneous blend of the particles of said second mixture; thereafter physically blending together said thusformed first and second granules while substantially retaining the respective identities of said first and second granules, in respective amounts such that in the resulting blended composition the weight ratio of said pteridine ingredient to said benzothiadiazide ingredient provides an effective bioavailable amount of said pteridine to control the hypokalemic condition induced by the dosage amount of said benzothiadiazide.
Claim 2
Independent Claim 169 words
A method for forming a granularly-heterogenous composition having combined pharmaceutically-effective diuretic anti-hypokalemic and antihypertensive activity comprising the steps of mixing finely-divided particles of a triamterene-active pteridine ingredient with at least one finely-divided pharmaceutically-acceptable inert ingredient to form a first mixture, and granulating said first mixture to form first granules composed of a homogeneous blend of the particles of said first mixture; separately mixing finely-divided particles of a hydrochlorothiazide-active benzothiadiazide ingredient with at least one finely-divided pharmaceutically-acceptable inert ingredient to form a second mixture, and separately granulating said second mixture to form second granules composed of a homogeneous blend of the particles of said second mixture; thereafter physically blending together said thusformed first and second granules while substantially retaining the respective identities of said first and second granules, in respective amounts such that in the resulting blended composition the weight ratio of said pteridine ingredient to said benzothiadiazide ingredient provides an effective bioavailable amount of said pteridine to control the hypokalemic condition induced by the dosage amount of said benzothiadiazide.
Claim 3
Dependent Claim 18 words
A method according to claim 1 wherein said pteridine ingredient is triamterene and said benzothiadiazine ingredient is hydrochlorothiazide.
Claim 4
Dependent Claim 16 words
A method according to claim 2 wherein the triamterene:hydrochlorothiazide weight ratio is from 1.25 to 1.75:1.
Claim 5
Dependent Claim 13 words
A method according to claim 3 wherein said weight ratio is about 1.5:1.
Claim 6
Dependent Claim 46 words
A method according to claim 2 wherein said finely-divided triamterene particles have a size range such that at least 95% pass through a 200 mesh screen, and said finely-divided hydrochlorothiazide particles have a size range such that at least 95% pass through a 100 mesh screen.
Claim 7
Dependent Claim 33 words
A method according to claim 5 wherein said granules have a size range from not more than 5% being larger than 2 mm to not more than 20% being smaller than 0.075 mm.
Claim 8
Dependent Claim 25 words
A method according to claim 6 wherein said granules have a size range such that not more than 5% have a dimension exceeding 1.5 mm.
Claim 9
Dependent Claim 24 words
A method according to claim 5 wherein said pharmaceutically-acceptable inert ingredients are of the class including wicking agents, disintegrants, surfactants, lubricants and compacting aids.
Claim 10
Dependent Claim 25 words
A method according to claim 8 wherein said wicking agent has a longitudinal dimension greater than would pass through a screen of about 200 mesh.

References Cited (Backward Citations)

US2853418A Cited
US3184386A Cited
US3081230A Cited
US3146167A Cited
US3220025A Cited
US4139589A Cited
US4168308A Cited
US4169885A Cited
US4255413A Cited
US4285947A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-10-14 1989-04-15 1989-10-15 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-10-14 1993-04-15 1993-10-15 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-10-14 1997-04-15 1997-10-15 $7700.00 Window Closed / Lapsed

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag