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US4013784A Expired / Lapsed US ⏱️ 0.0 years remaining

Delayed release pharmaceutical preparations

Assignee: Individual
•
Filing: 1974-10-02
•
Granted: 1977-03-22
•
Expires: 1994-10-02
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Abstract

Abstract A novel delayed release pharmaceutical preparation which is free of added enzymes and thus is stable on storage is provided. The preparation comprises particles of the therapeutically effective agent, a water-soluble calcium salt, and, if desired, a filler material, stabilizer, and other additives uniformly embedded in a triglyceride of fatty acids with 12 to 18 carbon atoms, thereby forming a granular preparation of a grain size between about 0.1 mm. and about 1.0 mm. A process of producing such a preparation is also disclosed.

Inventors

  • 👤 Peter Speiser

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-28 21:16
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2013; A61K9/14; A61K9/16; A61K9/1605; A61K9/1617

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 146 words
A delayed release pharmaceutical preparation in granular form comprising intermixed particles of at least one orally administrable therapeutically active agent and a substantially non-toxic water-soluble calcium salt selected from the group consisting of calcium levulinate, calcium gluconate, calcium citrate and calcium chloride, at least part of said particles of said agent and said salt being enveloped by solidifying a melt of at least one triglyceride of a fatty acid of 12 to 18 carbon atoms, said salt being present in an amount to provide at least 11/2 moles of calcium ion for each mole of said triglyceride and forming a substantially insoluble calcium soap with the fatty acid produced upon hydrolysis of said triglyceride in the intestinal tract, the granules of said preparation being of a grain size between about 0.1 mm. and about 1.0 mm. and containing between about 1 and 50% of said agent.
Claim 2
Dependent Claim 146 words
A delayed release pharmaceutical preparation in granular form comprising intermixed particles of at least one orally administrable therapeutically active agent and a substantially non-toxic water-soluble calcium salt selected from the group consisting of calcium levulinate, calcium gluconate, calcium citrate and calcium chloride, at least part of said particles of said agent and said salt being enveloped by solidifying a melt of at least one triglyceride of a fatty acid of 12 to 18 carbon atoms, said salt being present in an amount to provide at least 11/2 moles of calcium ion for each mole of said triglyceride and forming a substantially insoluble calcium soap with the fatty acid produced upon hydrolysis of said triglyceride in the intestinal tract, the granules of said preparation being of a grain size between about 0.1 mm. and about 1.0 mm. and containing between about 1 and 50% of said agent.
Claim 3
Dependent Claim 24 words
The pharmaceutical preparation of claim 1, wherein the triglyceride is selected from the group consisting of trilaurin, trimyristin, tripalmitin, and mixtures of said triglycerides.
Claim 4
Dependent Claim 19 words
The pharmaceutical preparation of claim 1, wherein the fatty acid triglyceride is present in the form of its β-modification.
Claim 5
Dependent Claim 32 words
The pharmaceutical preparation of claim 1, wherein the proportion of therapeutically active agent and calcium salt to fatty acid triglyceride in the preparation is between about 5% and about 30% by volume.
Claim 6
Dependent Claim 56 words
The pharmaceutical preparation of claim 1, wherein the preparation is in the form of spherical pellets of a diameter between about 0.1 mm. and about 1 mm. and wherein the ratio of the particle size of the active agent to the size of the pellet is between about 1 : 20 and about 1 : 100.
Claim 7
Dependent Claim 12 words
The pharmaceutical preparation of claim 1, additionally containing physiologically inert filler materials.
Claim 8
Dependent Claim 25 words
The pharmaceutical preparation of claim 1, additionally containing physiologically inert filler materials, preserving agents, stabilizers, aroma imparting and taste improving agents, and disintegration promoting agents.
Claim 9
Dependent Claim 16 words
A delayed release pharmaceutical composition having the preparation of claim 1 enclosed in a gelatin capsule.
Claim 10
Dependent Claim 20 words
A delayed release pharmaceutical composition in readily disintegrating tablet form containing the preparation of claim 1 and conventional tabletting adjuvants.
Claim 11
Dependent Claim 30 words
A delayed release pharmaceutical composition in aqueous dispersion form containing the granules of the preparation of claim 1 suspended in an aqueous medium containing a physiologically compatible, viscosity increasing agent.

References Cited (Backward Citations)

US2793979A Cited
US2805977A Cited
US2875130A Cited
US2987445A Cited
US3062720A Cited
US3146167A Cited
US3400197A Cited
US3629393A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-03-21 1980-09-20 1981-03-22 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-03-21 1984-09-20 1985-03-22 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-03-21 1988-09-20 1989-03-22 $7700.00 Window Closed / Lapsed

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