US4859469A
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Novel galenic forms of verapamil, their preparation and medicines containing said novel galenic forms
Assignee: Galephar P R Inc Ltd
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Filing: 1986-09-18
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Granted: 1989-08-22
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Expires: 2006-09-18
Abstract
Abstract The invention relates to a novel galenic form of verapamil which show an excellent bioavailability. The novel galenic form comprises microgranules containing a verapamil addition salt with an acid, associated to at least one wetting agent. The microgranules are coated with a porous membrane constituted of a synthetic polymer associated to an adjuvant.
Inventors
- 👤 Philippe Baudier
- 👤 Arthur De Boeck
- 👤 Jacques Fossion
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 10:53
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5026; A61K31/00; A61K31/275; A61K9/14; A61K9/16; A61K9/1605; A61K9/1617; A61K9/1623; A61K9/5073
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
111 words
Galenic form of verapamil chlorhydrate with sustained release of said compounds, comprising a microgranules containing verapamil chlorhydrate and at least one wetting agent selected from the group consisting of sucrose, polyvinylpyrrolidone, C 12 to C 20 fatty acid esters of sucrose and xylose, sucrose glycerides, fatty acid esters of polyoxyethylene, fatty alcohol ethers of polyoxyethylene, sorbitan esters, polyoxyethylene sorbitan esters, polyglycides-glycerides, polyglycides-alcohols esters and lecithins, said microgranules being coated with a microporous membrane constituted of at least a synthetic polymerisate of acrylic acid ethylesters and methacrylic acid methylesters and at least a pharmacologically acceptable adjuvant selected from the group consisting of plastifying agents, pigments, fillers, wetting agents, lubricants and anti-foaming agents.
Claim 2
Dependent Claim
111 words
Galenic form of verapamil chlorhydrate with sustained release of said compounds, comprising a microgranules containing verapamil chlorhydrate and at least one wetting agent selected from the group consisting of sucrose, polyvinylpyrrolidone, C 12 to C 20 fatty acid esters of sucrose and xylose, sucrose glycerides, fatty acid esters of polyoxyethylene, fatty alcohol ethers of polyoxyethylene, sorbitan esters, polyoxyethylene sorbitan esters, polyglycides-glycerides, polyglycides-alcohols esters and lecithins, said microgranules being coated with a microporous membrane constituted of at least a synthetic polymerisate of acrylic acid ethylesters and methacrylic acid methylesters and at least a pharmacologically acceptable adjuvant selected from the group consisting of plastifying agents, pigments, fillers, wetting agents, lubricants and anti-foaming agents.
Claim 3
Dependent Claim
34 words
Galenic form of verapamil chlorhydrate according to claim 1, wherein said active substance, containing microgranules are present in the form of spherules, the diameter of which is comprised between 0.1 mm and 2 mm.
Claim 4
Dependent Claim
28 words
Galenic form of verapamil chlorhydrate according to claim 1, wherein said microporous membrane weight makes from 5 to 22% of the weight of the microgranules coated by same.
Claim 5
Dependent Claim
34 words
Galenic form of verapamil chlorhydrate according to claim 1, wherein said active substance containing microgranules are present in the form of spherules the diameter of which is comprised between 0.05 mm and 3 mm.
Claim 6
Dependent Claim
28 words
Medicine containing verapamil chlorhydrate to be administered through oral way, Comprising a galenic form according to claim 1 contained in a capsule, a bag or a dosage dispenser.
Claim 7
Dependent Claim
125 words
Galenic form of verapamil chlorhydrate according to claim 1, wherein the pharmacologically acceptable adjuvant of said microporous membrane coating said microgranules is a plastifying agent selected from the group consisting of triacetine, dibutylphthalate, dibutylsebacate, citric acid esters, polyethyleneglycols, polypropyleneglycols and polyvinylpyrrolidone; or a contingently colored pigment selected from the group consisting of iron oxides and titanium oxido; or a filler selected from the group consisting of lactose and sucrose; or a wetting agent selected from the group consisting of fatty acid partial esters anhydrides of hexitols derivated from sorbitol contingently containing polyoxyethylenic chains and the polyethylene glycols; or a lubricant selected from the group consisting of magnesium stearate and talc; or a silicone oil as antifoaming agent or; a colloidal aluminum oxide as antistatic agent.
Claim 8
Dependent Claim
50 words
Galenic form of verapamil chlorhydrate according to claim 6, wherein said microporous membrane contains, in addition to the polymer(s), talc and/or magnesium stearate, as a lubricant, polyvinylpyrrolidone as a plastifying agent, titanium dioxide as a pigment, colloidal aluminum oxide as an antistatic agent and silicone oil as an antifoaming agent.
Claim 9
Dependent Claim
64 words
Galenic form of verapamil chlorhydrate according to claim 1, wherein said microgranules contain, by weight, 20 to 90% of verapamil chlorhydrate, as well as 5 to 30% of C 12 to C 20 fatty acid esters of saccharose, 4 to 50% of microcrystalline celluloses, 0 to 35% sucrose 0 to 10% hydroxy-propylmethylcellulose and 0 to 15% polyvinylpyrrolidone, as wetting agents and carriers or excipients.
Claim 10
Dependent Claim
40 words
Galenic form of verapamil chlorhydrate according to claim 8, wherein said microgranules contain, by weight, about 65% verapamil chlorhydrate, as well as 25% sucrose, 5% of microcrystalline celluloses, 4% hydroxypropylmethylcellulose and 1% polyvinylpyrrolidone, as wetting agents and carriers or excipients.
Claim 11
Dependent Claim
45 words
Galenic form of verapamil chlorhydrate according to claim 8, wherein said microgranules contain, by weight, about 80% verapamil chlorhydrate as well as 10% of C 12 to C 20 fatty acid esters of saccharose as wetting agent and 10% microcrystalline cellulose as carrier or excipient.
Claim 12
Dependent Claim
62 words
Galenic form of verapamil chlorhydrate according to claim 6, wherein said microporous membrane coating said microgranules contains, by weight, 5 to 95% of at least said polymerisate, 1 to 25% talc or magnesium stearate, 0 to 4% colloidal aluminum oxide, 0 to 15% polyvinylpyrrolidone, 0 to 2% silicone oil and 0 to 0.5% of sorbitan fatty acid polyoxyethylene ester as wetting agent.
Claim 13
Dependent Claim
46 words
Galenic form of verapamil chlorhydrate according to claim 6, wherein said microporous membrane coating said microgranules comprises, by weight, 70 to 80% of at least said polymerisate, 6% magnesium stearate, 4 to 6% titanium dioxide, 4 to 6% polyvinylpyrrolidone and 0.1% sorbitan fatty acid polyoxyethylene esters.
Claim 14
Dependent Claim
39 words
Galenic form of verapamil chlorhydrate according to claim 6, wherein said microporous membrane contains by weight, 60 to 80% of at least said polymerisate, 10 to 25% talc, 1 to 5% polyvinylpyrrolidone and 0.05% sorbitan fatty acid polyoxyethylene ester.
Claim 15
Dependent Claim
18 words
Galenic form of verapamil chlorhydrate according to claim 1, wherein said microporous membrane itself contains also verapamil chlorhydrate.
Claim 16
Dependent Claim
28 words
Galenic form of verapamil chlorhydrateU according to claim 1, wherein said microporous membrane weight makes from 2 to 35% of the weight of the microgranules coated by same.
Claim 17
Dependent Claim
23 words
Medicine according to claim 5, wherein said medicine is in the form of unit dosages containing from 20 to 400 mg verapamil chlorhydrate.
Claim 18
Dependent Claim
23 words
Medicine according to claim 5 wherein said medicine is in the form of unit dosage containing from 50 to 360 mg verapamil chlorhydrate.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-08-21 | 1993-02-20 | 1993-08-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-08-21 | 1997-02-20 | 1997-08-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-08-21 | 2001-02-20 | 2001-08-22 | $7700.00 | Window Closed / Lapsed |