US4855326A
Expired / Lapsed
US
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Rapidly dissoluble medicinal dosage unit and method of manufacture
Assignee: Valeant International Bermuda
•
Filing: 1988-03-18
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Granted: 1989-08-08
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Expires: 2008-03-18
Abstract
Abstract A melt spinnable carrier agent such as sugar is combined with a medicament then converted into fiber form by melt spinning with "cotton candy" fabricating equipment. The as-spun product is converted to compacted individual dosage units. For certain medicaments a binding agent is added to the carrier agent. Examples are presented for oral administration, topical application, systemic and non-systemic, intravenous and intra-muscular infusion via multicameral containers. All applications utilize the extraordinarily rapid entry into solution upon contact with a solvent.
Inventors
- 👤 Richard C. Fuisz
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 02:34
CPC Classifications
A; A61; A61K; A61K9/00; A61K8/00; A61K8/02; A61K8/0241; A61K8/027; A23; A23L; A23L13/00; A23L13/40; A23L13/42; A23L13/43; A23L33/00; A23L33/20; A23P; A23P10/00; A23P10/20; A23P10/25; A23P10/28; A61K8/18; A61K8/30; A61K8/40; A61K8/44; A61K8/445; A61K8/60; A61K8/72; A61K8/73; A61K8/735; A61K9/70; A61Q; A61Q17/00; A61Q17/04; A61Q5/00; A61Q5/12
Claims Analysis
Total Claims: 66
Claim 1
Independent Claim
35 words
A spun fibrous pharmaceutical composition comprising a mass of spun fibers of a material capable of being spun into fibers that are readily water-soluble and a medicament distributed on or incorporated in said fibrous mass.
Claim 2
Dependent Claim
35 words
A spun fibrous pharmaceutical composition comprising a mass of spun fibers of a material capable of being spun into fibers that are readily water-soluble and a medicament distributed on or incorporated in said fibrous mass.
Claim 3
Dependent Claim
19 words
A spun fibrous pharmaceutical composition according to claim 1, wherein said material is a sugar or a cellulosic material.
Claim 4
Dependent Claim
15 words
A spun fibrous pharmaceutical composition according to claim 2, wherein said material is a sugar.
Claim 5
Dependent Claim
15 words
A spun fibrous pharmaceutical composition according to claim 3, wherein said medicament is an analgesic.
Claim 6
Dependent Claim
18 words
A spun fibrous pharmaceutical composition according to claim 3, wherein said medicament is an antihistaminic labyrinthine function depressant.
Claim 7
Dependent Claim
15 words
A spun fibrous pharmaceutical composition according to claim 3, wherein said medicament is a decongestant.
Claim 8
Dependent Claim
14 words
A spun fibrous pharmaceutical composition according to claim 1, wherein said medicament is acetaminophen.
Claim 9
Dependent Claim
15 words
A spun fibrous pharmaceutical composition according to claim 1, wherein said medicament is diethylcarbamazine citrate.
Claim 10
Dependent Claim
26 words
A spun fibrous pharmaceutical composition according to claim 1, wherein said composition further comprises an adhesion promoter for promoting adhesion between said material and said medicament.
Claim 11
Dependent Claim
15 words
A spun fibrous pharmaceutical composition according to claim 9, wherein said adhesion promoter comprises polyvinylpyrrolidone.
Claim 12
Dependent Claim
15 words
A spun fibrous pharmaceutical composition according to claim 10, wherein said medicament comprises diethylcarbamazine citrate.
Claim 13
Dependent Claim
29 words
A spun fibrous pharmaceutical composition according to claim 3, wherein said sugar is selected from the group consisting of maltose, fructose, sorbitol, dextrose, mannitol, sucrose, lactose, and combinations thereof.
Claim 14
Dependent Claim
35 words
A spun fibrous pharmaceutical composition according to claim 12, wherein said mass of spun fibers is in the form of a compacted unit-dose body of said fibers where the fibers have retained their fibrous identity.
Claim 15
Dependent Claim
35 words
A spun fibrous pharmaceutical composition according to claim 1, wherein said mass of spun fibers is in the form of a compacted unit-dose body of said fibers where the fibers have retained their fibrous identity.
Claim 16
Dependent Claim
21 words
A spun fibrous pharmaceutical composition according to claim 3, wherein said sugar comprises at least 10% lactose and the remainder sucrose.
Claim 17
Dependent Claim
30 words
A spun fibrous pharmaceutical composition according to claim 12, wherein said medicament is of the type that is rapidly assimilated when in contact with the tissues of the oral cavity.
Claim 18
Dependent Claim
22 words
A pharmaceutical dosage unit comprising compacted spun fibers of a spinnable, readily water soluble material and an effective amount of a medicament.
Claim 19
Dependent Claim
22 words
A pharmaceutical dosage unit comprising compacted spun fibers of a spinnable, readily water soluble material and an effective amount of a medicament.
Claim 20
Independent Claim
76 words
A system for topical delivery of a medicament comprising a wafer containing a mass of fibers, and means for securing said wafer in contact with a dermal area to be treated, said mass of fibers, comprising a soluble fiber forming ingredient and a medicament where at least said fiber forming ingredient has been spun into fibers, and in said fiber form said ingredient has a solubility characteristic corresponding to that of spun sugar fibers in water.
Claim 21
Independent Claim
76 words
A system for topical delivery of a medicament comprising a wafer containing a mass of fibers, and means for securing said wafer in contact with a dermal area to be treated, said mass of fibers, comprising a soluble fiber forming ingredient and a medicament where at least said fiber forming ingredient has been spun into fibers, and in said fiber form said ingredient has a solubility characteristic corresponding to that of spun sugar fibers in water.
Claim 22
Dependent Claim
14 words
A system according to claim 18, wherein said ingredient in fiber form is hydrophilic.
Claim 23
Dependent Claim
12 words
A system according to claim 19, wherein said ingredient is essentially lactose.
Claim 24
Dependent Claim
13 words
A system according to claim 18, wherein said medicament is a dermatotropic agent.
Claim 25
Dependent Claim
13 words
A system according to claim 18, wherein said medicament includes an antibiotic agent.
Claim 26
Dependent Claim
12 words
A system according to claim 18, wherein said medicament includes a corticosteroid.
Claim 27
Dependent Claim
15 words
A system according to claim 18, wherein said medicament is characterized by transdermal systemic activity.
Claim 28
Dependent Claim
58 words
A multicameral container for intravenous or intra muscular administration comprising a first compartment containing a pharmaceutically acceptable solvent, and a second compartment containing a spun fibrous pharmaceutical composition comprising a mass of spun fibers of a material capable of being spun into fibers that are readily water-soluble and a medicament distributed on or incorporated in said fibrous mass.
Claim 29
Dependent Claim
58 words
A multicameral container for intravenous or intra muscular administration comprising a first compartment containing a pharmaceutically acceptable solvent, and a second compartment containing a spun fibrous pharmaceutical composition comprising a mass of spun fibers of a material capable of being spun into fibers that are readily water-soluble and a medicament distributed on or incorporated in said fibrous mass.
Claim 30
Dependent Claim
29 words
A multicameral container according to claim 25, wherein said material is a sugar selected from the group consisting of maltose, fructose, sorbitol, dextrose, mannitol, sucrose, lactose, and combinations thereof.
Claim 31
Dependent Claim
32 words
A multicameral container according to claim 26, wherein said mass of spun fibers is in the form of a compacted body of said fibers where the fibers have retained their fibrous identity.
Claim 32
Dependent Claim
18 words
A multicameral container according to claim 27, wherein said sugar comprises about 10% lactose and the remainder sucrose.
Claim 33
Dependent Claim
15 words
A spun fibrous pharmaceutical composition according to claim 29, wherein said material is methyl cellulose.
Claim 34
Dependent Claim
14 words
A spun fibrous pharmaceutical composition according to claim 29, wherein said medicament comprises dimenhydrinate.
Claim 35
Independent Claim
29 words
A method for preparing a pharmaceutical dosage unit for delivering a medicament, comprising producing a mass of medicament bearing spun fibers by melt spinning a composition containing said medicament.
Claim 36
Independent Claim
29 words
A method for preparing a pharmaceutical dosage unit for delivering a medicament, comprising producing a mass of medicament bearing spun fibers by melt spinning a composition containing said medicament.
Claim 37
Dependent Claim
41 words
A method according to claim 31, wherein said medicament is combined with a melt spinnable compatible water soluble carrier agent to provide an intermediate product, and said intermediate product is converted to a mass of spun fibers by melt spinning product.
Claim 38
Dependent Claim
17 words
A method according to claim 32, wherein said carrier agent comprises a mixture of sucrose and lactose.
Claim 39
Dependent Claim
22 words
A method according to claim 33, wherein said lactose is combined with said sucrose in the ratio of about 1:9 by weight.
Claim 40
Dependent Claim
49 words
A method according to claim 32, wherein said medicament has a higher melting point than said carrier agent, and said melt spinning is carried out at a temperature lying between the melting points of said medicament and said carrier agent but less than the melting point of said medicament.
Claim 41
Independent Claim
48 words
A method for preparing a rapidly dissoluble medicinal dosage unit for administering medication comprising in combination the steps of combining a medicament with a melt spinnable compatible carrier agent to provide an intermediate product, and producing a mass of medicament bearing fibers by melt spinning said intermediate product.
Claim 42
Independent Claim
48 words
A method for preparing a rapidly dissoluble medicinal dosage unit for administering medication comprising in combination the steps of combining a medicament with a melt spinnable compatible carrier agent to provide an intermediate product, and producing a mass of medicament bearing fibers by melt spinning said intermediate product.
Claim 43
Dependent Claim
24 words
A method according to claim 36, wherein said carrier agent is a sugar having a spinning temperature below the degradation temperature of said medicament.
Claim 44
Dependent Claim
37 words
A method according to claim 37, wherein said intermediate product is produced by coating granules of said sugar with a slurry of said medicament where the vehicle for said slurry is not a solvent for said sugar.
Claim 45
Dependent Claim
12 words
A method according to claim 38, wherein said vehicle is isopropyl alcohol.
Claim 46
Dependent Claim
30 words
A method according to claim 39, wherein said granules of sugar are added to said slurry and the slurry coated granules are thereafter dried then spun to produce said fibers.
Claim 47
Dependent Claim
29 words
A method according to claim 40, wherein said slurry is produced by admixing acetaminophen with isopropyl alcohol to produce a 60-70% w/v solution of said medicament in said vehicle.
Claim 48
Dependent Claim
43 words
A method according to claim 40, wherein said slurry is produced by adding 2-3% by weight of polyvinylpyrrolidone to isopropyl alcohol and admixing the resulting solution with diethylcarbamazine citrate to obtain a slurry containing about 60% w/v of said medicament in said vehicle.
Claim 49
Dependent Claim
47 words
A method according to claim 36, wherein the spun fiber product resulting from said melt spinning of said intermediate product is compacted to produce a body whose enclosed volume is substantially less than the as-spun enclosed volume, and the compacted product is thereafter subdivided into dosage units.
Claim 50
Dependent Claim
48 words
A method according to claim 43, wherein said compaction step is performed to produce said body with an enclosed volume at least 30% less than said as-spun enclosed volume, said compaction step being limited to less than that compaction which would result in noticeable fracturing of said fibers.
Claim 51
Dependent Claim
101 words
A rapidly dissoluble spun fibrous medicinal dosage unit for administering medication orally, sublingually, or buccally, consisting essentially of a compacted mass of spun fibers of a carrier agent capable of being spun into fibers that are readily water-soluble which dissolve in the saliva of the mouth, said mass having an enclosed volume that is at least 30% less than the as-spun enclosed volume, said carrier agent being selected from the group consisting of sugars, sugar alcohols and mixtures thereof, and an effective amount of an orally, sublingually, or buccally effective medicament distributed within or coated on said spun carrier agent fibers.
Claim 52
Dependent Claim
101 words
A rapidly dissoluble spun fibrous medicinal dosage unit for administering medication orally, sublingually, or buccally, consisting essentially of a compacted mass of spun fibers of a carrier agent capable of being spun into fibers that are readily water-soluble which dissolve in the saliva of the mouth, said mass having an enclosed volume that is at least 30% less than the as-spun enclosed volume, said carrier agent being selected from the group consisting of sugars, sugar alcohols and mixtures thereof, and an effective amount of an orally, sublingually, or buccally effective medicament distributed within or coated on said spun carrier agent fibers.
Claim 53
Dependent Claim
15 words
A rapidly dissoluble medicinal dosage unit according to claim 45, wherein said medicament is acetaminophen.
Claim 54
Dependent Claim
16 words
A rapidly dissoluble medicinal dosage unit according to claim 45, wherein said medicament is diethylcarbamazine citrate.
Claim 55
Dependent Claim
25 words
A rapidly dissoluble medicinal dosage unit according to claim 45, wherein said fibers consist essentially of a compound containing said carrier agent and said medicament.
Claim 56
Dependent Claim
23 words
A rapidly dissoluble medicinal dosage unit according to claim 48, wherein said fibers are the product resulting from melt spinning of said compound.
Claim 57
Dependent Claim
15 words
A rapidly dissoluble medicinal dosage unit according to claim 49, wherein said medicament is acetaminophen.
Claim 58
Dependent Claim
16 words
A rapidly dissoluble medicinal dosage unit according to claim 49, wherein said medicament is diethylcarbamazine citrate.
Claim 59
Dependent Claim
45 words
A rapidly dissoluble medicinal dosage unit according to claim 48, wherein said compound consists essentially of said carrier agent, said medicament, and adducts selected from the group consisting of coloring agents, flavoring agents, and promoters of adhesion between said carrier agent and the other constituents.
Claim 60
Dependent Claim
16 words
A rapidly dissoluble medicinal dosage unit according to claim 52, wherein said adhesion promoter comprises polyvinylpyrrolidine.
Claim 61
Dependent Claim
16 words
A rapidly dissoluble medicinal dosage unit according to claim 53, wherein said medicament comprises diethylcarbamazine citrate.
Claim 62
Dependent Claim
35 words
A rapidly dissoluble medicinal dosage unit according to claim 45, wherein said mass of spun fibers is in the form of a tablet of compacted spun fibers where the fibers have retained their fibrous identity.
Claim 63
Dependent Claim
25 words
A rapidly dissoluble medicinal dosage unit according to claim 55, wherein said fibers consist essentially of a compound containing said carrier agent and said medicament.
Claim 64
Dependent Claim
23 words
A rapidly dissoluble medicinal dosage unit according to claim 56, wherein said fibers are the product resulting from melt spinning of said compound.
Claim 65
Dependent Claim
15 words
A rapidly dissoluble medicinal dosage unit according to claim 57, wherein said medicament is acetaminophen.
Claim 66
Dependent Claim
16 words
A rapidly dissoluble medicinal dosage unit according to claim 57, wherein said medicament is diethylcarbamazine citrate.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-08-07 | 1993-02-06 | 1993-08-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-08-07 | 1997-02-06 | 1997-08-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-08-07 | 2001-02-06 | 2001-08-08 | $7700.00 | Window Closed / Lapsed |