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US4681765A Expired / Lapsed US ⏱️ 0.0 years remaining

Rapid releasing triamterene containing gelatin capsule dosage forms for once daily antihypertensive use

Assignee: Wyeth LLC
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Filing: 1984-09-13
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Granted: 1987-07-21
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Expires: 2004-09-13
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Abstract

Abstract A gelatin capsule dosage form containing triamterene, 2,4,7-triamino-6-phenylpteridine, which results in rapid dissolution of the active ingredient. The dosage form comprises the pharmaceutical binder methylcellulose in combination with low doses of a surfactant or a carbonate salt as disintegrants.

Inventors

  • 👤 Paul C. Guley

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 07:02
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K9/00; A61K9/48; A61K9/4841; A61K9/50; A61K9/5084

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 77 words
Method of producing triamterene and hydrochlorothiazide capsules by mixed granulation comprising the steps: (1) blending triamterene, methylcellulose, lactose, sodium starch glycolate, microcrystalline cellulose, and talc (2) adding water to the blend of step 1 and mixing till granulated (3) milling and drying the wet granulation of step 2 (4) blending the dried granulation of step 3 with hydrochlorothiazide, calcium carbonate, sodium croscarmellose and magnesium stearate and (5) milling, and blending the blend of step 4 and encapsulating.
Claim 2
Dependent Claim 77 words
Method of producing triamterene and hydrochlorothiazide capsules by mixed granulation comprising the steps: (1) blending triamterene, methylcellulose, lactose, sodium starch glycolate, microcrystalline cellulose, and talc (2) adding water to the blend of step 1 and mixing till granulated (3) milling and drying the wet granulation of step 2 (4) blending the dried granulation of step 3 with hydrochlorothiazide, calcium carbonate, sodium croscarmellose and magnesium stearate and (5) milling, and blending the blend of step 4 and encapsulating.
Claim 3
Dependent Claim 66 words
Method of treating hypertension by the administration of a gelatin capsule dosage unit comprising triamterene, propranolol long acting spheres, hydrochlorothiazide, and (a) a rapid dispersing amount of a calcium, magnesium, ammonium, aminoacid, or alkali metal nontoxic carbonate or bicarbonate salt in the presence of adjunctive disintegrant aids selected from the group consisting of sodium starch glycolate, sodium croscarmellose and methylcellulose in the absence of a surfactant.
Claim 4
Dependent Claim 66 words
Method of treating hypertension by the administration of a gelatin capsule dosage unit comprising triamterene, propranolol long acting spheres, hydrochlorothiazide, and (a) a rapid dispersing amount of a calcium, magnesium, ammonium, aminoacid, or alkali metal nontoxic carbonate or bicarbonate salt in the presence of adjunctive disintegrant aids selected from the group consisting of sodium starch glycolate, sodium croscarmellose and methylcellulose in the absence of a surfactant.
Claim 5
Dependent Claim 61 words
An improved rapid dispersing gelatin capsule dosage unit comprising triamterene in the presence of adjunctive disintegrant aids selected from the group consisting of sodium starch glycolate, sodium croscarmellose, and methylcellulose, wherein the improvement comprises the addition of a rapid dispersing amount of a calcium, magnesium, ammonium, aminoacid, or alkali metal nontoxic carbonate or bicarbonate salt in the absence of a surfactant.
Claim 6
Dependent Claim 61 words
An improved rapid dispersing gelatin capsule dosage unit comprising triamterene in the presence of adjunctive disintegrant aids selected from the group consisting of sodium starch glycolate, sodium croscarmellose, and methylcellulose, wherein the improvement comprises the addition of a rapid dispersing amount of a calcium, magnesium, ammonium, aminoacid, or alkali metal nontoxic carbonate or bicarbonate salt in the absence of a surfactant.
Claim 7
Dependent Claim 14 words
The gelatin capsule of claim 3 in which the carbonate salt is calcium carbonate.
Claim 8
Dependent Claim 62 words
The gelatin capsule of claim 4 in which the triamterene is present in an amount of from 5 mg. to 100 mg., the carbonate salt is present in an amount of from about 4% to about 40% and the adjunctive disintegrant aids are present in an amount of from about 2% to about 15% by weight of the ingredients in the formula.
Claim 9
Dependent Claim 63 words
An improved rapid dispersing gelatin capsule dosage unit comprising triamterene and hydrochlorothiazide in the presence of adjunctive disintegrant aids selected from the group consisting of sodium starch glycolate, sodium croscarmellose, and methylcellulose, wherein the improvement comprises the addition of a rapid dispersing amount of a calcium, magnesium, ammonium, aminoacid, or alkali metal nontoxic carbonate or bicarbonate salt in the absence of a surfactant.
Claim 10
Dependent Claim 63 words
An improved rapid dispersing gelatin capsule dosage unit comprising triamterene and hydrochlorothiazide in the presence of adjunctive disintegrant aids selected from the group consisting of sodium starch glycolate, sodium croscarmellose, and methylcellulose, wherein the improvement comprises the addition of a rapid dispersing amount of a calcium, magnesium, ammonium, aminoacid, or alkali metal nontoxic carbonate or bicarbonate salt in the absence of a surfactant.
Claim 11
Dependent Claim 14 words
The gelatin capsule of claim 6 in which the carbonate salt is calcium carbonate.
Claim 12
Dependent Claim 77 words
The gelatin capsule of claim 6 in which the triamterene is present in an amount of from 5 mg. to 100 mg. and the hydrochlorothiazide is present in an amount of from 2 mg. to 250 mg., the carbonate salt is present in an amount of from about 4% to about 40% and the adjunctive ingredient aids are present in an amount of from about 2% to about 15% by weight of the ingredients in the formula.
Claim 13
Dependent Claim 65 words
An improved rapid dispersing gelatin capsule dosage unit comprising triamterene, hydrochlorothiazide and propranolol hydrochloride in the presence of adjunctive disintegrant aids selected from the group consisting of sodium starch glycolate, sodium croscarmellose, and methylcellulose, wherein the improvement comprises the addition of a rapid dispersing amount of a calcium, magnesium, ammonium, aminoacid, or alkali metal nontoxic carbonate or bicarbonate salt in the absence of a surfactant.
Claim 14
Dependent Claim 65 words
An improved rapid dispersing gelatin capsule dosage unit comprising triamterene, hydrochlorothiazide and propranolol hydrochloride in the presence of adjunctive disintegrant aids selected from the group consisting of sodium starch glycolate, sodium croscarmellose, and methylcellulose, wherein the improvement comprises the addition of a rapid dispersing amount of a calcium, magnesium, ammonium, aminoacid, or alkali metal nontoxic carbonate or bicarbonate salt in the absence of a surfactant.
Claim 15
Dependent Claim 14 words
The gelatin capsule of claim 9 in which the carbonate salt is calcium carbonate.
Claim 16
Dependent Claim 98 words
The gelatin capsule of claim 9 in which the triamterene is present in an amount of from about 5 mg. to about 100 mg. and the hydrochlorothiazide is present in an amount of from about 2 mg. to about 250 mg., and the propranolol long acting spheroids are present in an amount from 60 mg. to 320 mg., the carbonate salt is present in an amount of from about 4% to about 40% and the adjunctive disintegrant aids are present in an amount of from about 2% to about 15% by weight of the ingredients in the formula.

References Cited (Backward Citations)

US2883327A Cited
US4138475A Cited
US4248856A Cited
US4255413A Cited
US4444769A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-07-20 1991-01-19 1991-07-21 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-07-20 1995-01-19 1995-07-21 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-07-20 1999-01-19 1999-07-21 $7700.00 Window Closed / Lapsed

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