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US4016254A Expired / Lapsed US ⏱️ 0.0 years remaining

Pharmaceutical formulations

Assignee: Beecham Group PLC
•
Filing: 1976-04-05
•
Granted: 1977-04-05
•
Expires: 1996-04-05
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Abstract

Abstract Microcapsules which have an average diameter of from 100μ to 300μ and which comprise 94% to 99.9% of a medicament coated by 0.1% to 6% of a coating agent may be formed into a powder with 0% to 95% excipients or a tablet or capsule with a carrier.

Inventors

  • 👤 Harry Seager

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 16:23
CPC Classifications
B; B01; B01J; B01J13/00; B01J13/02; B01J13/04; B01J13/043; A; A61; A61K; A61K9/00; A61K9/20; A61K9/2072; A61K9/2077; A61K9/2081; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5026; A61K9/5036; A61K9/5042; A61K9/5047; A61K9/5052; A61K9/5057; A61K9/5089; Y; Y10; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2989

Claims Analysis

Total Claims: 51
Claim 1
Independent Claim 45 words
A powder comprising 0% to 95% of conventional pharmaceutical excipients and 5% to 100% of microcapsules, having an average diameter of from 100 μ to 300 μ and which consist of 94% to 99.9% of a β-lactam antibiotic coated by 0.1% to 6% of polyvinylpyrrolidone.
Claim 2
Dependent Claim 45 words
A powder comprising 0% to 95% of conventional pharmaceutical excipients and 5% to 100% of microcapsules, having an average diameter of from 100 μ to 300 μ and which consist of 94% to 99.9% of a β-lactam antibiotic coated by 0.1% to 6% of polyvinylpyrrolidone.
Claim 3
Dependent Claim 14 words
A powder according to claim 1 comprising 0% to 5% of conventional pharmaceutical excipients.
Claim 4
Dependent Claim 14 words
A powder according to claim 1 comprising 0% to 2% of conventional pharmaceutical excipients.
Claim 5
Dependent Claim 14 words
A powder according to claim 1 comprising 1% to 1% of conventional pharmaceutical excipients.
Claim 6
Dependent Claim 28 words
A powder according to claim 1 which contains 98% to 99.8% of ampicillin trihydrate or amoxycillin trihydrate as the β-lactam antibiotic coated by 0.2% to 2% of polyvinylpyrrolidone.
Claim 7
Dependent Claim 22 words
A powder according to claim 1 wherein the microcapsules comprise 98.0% to 99.8% of β-lactam antibiotic and 0.2% to 2.0% of polyvinylpyrrolidone.
Claim 8
Dependent Claim 22 words
A powder according to claim 6 wherein the microcapsules comprise 98.0% to 99.8% of β-lactam antibiotic and 0.2% to 2.0% of polyvinylpyrrolidone.
Claim 9
Dependent Claim 22 words
A powder according to claim 6 wherein the microcapsules comprise 99.0% to 99.8% of β-lactam antibiotic and 0.2% to 1.0% of polyvinylpyrrolidone.
Claim 10
Dependent Claim 22 words
A powder according to claim 8 wherein at least 90.0% of the microcapsules have diameters in the range of 75μ to 450μ.
Claim 11
Dependent Claim 22 words
A powder according to claim 6 wherein at least 95% of the microcapsules have diameters in the range of 75μ to 450μ.
Claim 12
Dependent Claim 22 words
A powder according to claim 6 wherein at least 99% of the microcapsules have diameters in the range of 75μ to 450μ.
Claim 13
Dependent Claim 22 words
A powder according to claim 11 wherein at least 80% of the microcapsules have diameters in the range of 100μ to 300μ.
Claim 14
Dependent Claim 16 words
A powder according to claim 12 wherein the average microcapsule diameter is from 150μ to 250μ.
Claim 15
Dependent Claim 16 words
A powder according to claim 13 wherein the average microcapsule diameter is from 175μ to 225μ.
Claim 16
Dependent Claim 51 words
A powder according to claim 4 comprising 98% to 100% of microcapsules, which microcapsules have an average diamter of at least 100μ, 90% of which microcapsules have diameter in the range of 75μ to 450μ, and which microcapsules consist of 0.1% to 2.5% polyvinylpyrrolidone and 97.5% to 99.9% of β-lactam antibiotic.
Claim 17
Dependent Claim 46 words
A powder according to claim 1 which microcapsules have an average diameter between 150μ to 250μ, 95% have diameters between 75μ to 450μ and 80% have diameters between 100μ to 300μ and which microcapsules consist of 98% to 99.9% β-lactam antibiotic and 0.2% to 2% polyvinylpyrrolidone.
Claim 18
Dependent Claim 16 words
A powder according to claim 16 in which the amount of polyvinylpyrrolidone is 0.2% to 1.0%.
Claim 19
Dependent Claim 46 words
A powder according to claim 1 comprising 10% to 95% of microencapsulated excipient and 5% to 90% of microencapsulated β-lactam antibiotic wherein the microcapsules have an average diameter of at least 100μ and 90% of which microcapsules have diameters in the range of 75μ to 450μ.
Claim 20
Dependent Claim 27 words
A powder according to claim 18 wherein the microcapsules containing the β-lactam antibiotic consist of 98% to 99.9% of β-lactam antibiotic and 0.2% to 2.00% of polyvinylpyrrolidone.
Claim 21
Dependent Claim 41 words
A powder according to claim 1 comprising 0% to 5% of conventional pharmaceutical excipients and 95% to 100% of microcapsules which have an average diameter of at least 100μ, 90% of which have diameters in the range of 75μ to 450μ.
Claim 22
Dependent Claim 33 words
A powder according to claim 20 consisting of microcapsules containing 98% to 99.8% of β-lactam antibiotic and 0.2% to 2.0% of polyvinylpyrrolidone, which microcapsules have an average diameter of from 150μ to 300μ.
Claim 23
Dependent Claim 33 words
A powder according to claim 20 wherein the β-lactam antibiotic is ampicillin, amoxycillin, isoxazolylpenicillin, an orally active ester of ampicillin or carbenicillin or a pharmaceutically-acceptable salt or hydrate of ampicillin, amoxycillin or isoxazolylpenicillin.
Claim 24
Dependent Claim 12 words
A powder according to claim 1 wherein the β-lactam antibiotic is ampicillin.
Claim 25
Dependent Claim 50 words
A powder according to claim 1 wherein the β-lactam antibiotic is ampicillin, amoxycillin, isoxyzolylpenicillin, an orally active ester of ampicillin or carbenicillin or a pharmaceutically-acceptable salt or hydrate of ampicillin, amoxycillin or isoxazolylpenicillin in the amount of 98% to 99.8% and wherein the amount of polyvinylpyrrolidone is 0.2% to 2.0%.
Claim 26
Dependent Claim 13 words
A powder according to claim 1 wherein the β-lactam antibiotic is ampicillin trihydrate.
Claim 27
Dependent Claim 12 words
Microcapsules according to claim 1 wherein the β-lactam antibiotic is amoxycillin trihydrate.
Claim 28
Dependent Claim 30 words
A powder which have an average diameter of from 100μ to 300μ and which consist of 94% to 99.9% of a β-lactam antibiotic coated by 0.1% to 6% of polyvinylpyrrolidone.
Claim 29
Dependent Claim 30 words
A powder which have an average diameter of from 100μ to 300μ and which consist of 94% to 99.9% of a β-lactam antibiotic coated by 0.1% to 6% of polyvinylpyrrolidone.
Claim 30
Dependent Claim 38 words
A free-flowing, finely-divided solid which consists of microcapsules which have an average diameter of from 150μ to 300μ and which consist of 98% to 99.8% of ampicillin trihydrate or amoxycillin trihydrate coated by 0.2% to 2% of polyvinylpyrrolidone.
Claim 31
Dependent Claim 38 words
A free-flowing, finely-divided solid which consists of microcapsules which have an average diameter of from 150μ to 300μ and which consist of 98% to 99.8% of ampicillin trihydrate or amoxycillin trihydrate coated by 0.2% to 2% of polyvinylpyrrolidone.
Claim 32
Dependent Claim 14 words
Microcapsules according to claim 27 wherein the amount of polyvinylpyrrolidone is 0.2% to 2.0%.
Claim 33
Dependent Claim 14 words
Microcapsules according to claim 27 wherein the amount of polyvinylpyrrolidone is 0.2% to 1.0%.
Claim 34
Dependent Claim 13 words
Microcapsules according to claim 27 in the form of a free-flowing, finely-divided solid.
Claim 35
Dependent Claim 49 words
Microcapsules according to claim 31 wherein the β-lactam antibiotic is ampicillin, amoxycillin, isoxazolylpenicillin, an orally active ester of ampicillin or carbenicillin or a pharmaceutically-acceptable salt or hydrate of ampicillin, amoxycillin or isoxazolylpenicillin in the amount of 98% to 99.8% and wherein the amount of polyvinylpyrrolidone is 0.2% to 2.0%.
Claim 36
Dependent Claim 12 words
Microcapsules according to claim 31 wherein the β-lactam antibiotic is ampicillin trihydrate.
Claim 37
Dependent Claim 12 words
Microcapsules according to claim 31 wherein the β-lactam antibiotic is amoxycillin trihydrate.
Claim 38
Dependent Claim 19 words
Microcapsules according to claim 27 which comprise 97.5% to 99.9% of β-lactam antibiotic and 0.1% to 2.5% of polyvinylpyrrolidone.
Claim 39
Dependent Claim 19 words
Microcapsules according to claim 35 which comprise 98.0% to 99.8% of β-lactam antibiotic and 0.2% to 2.0% of polyvinylpyrrolidone.
Claim 40
Dependent Claim 19 words
Microcapsules according to claim 27 which comprise 99.0% to 99.8% of β-lactam antibiotic and 0.2% to 1.0% of polyvinylpyrrolidone.
Claim 41
Dependent Claim 21 words
Microcapsules according to claim 37 wherein at least 90.0% of the microcapsules have diameters in the range of 75μ to 450μ.
Claim 42
Dependent Claim 21 words
Microcapsules according to claim 27 wherein at least 95% of the microcapsules have diameters in the range of 75μ to 450μ.
Claim 43
Dependent Claim 21 words
Microcapsules according to claim 27 wherein at least 99% of the microcapsules have diameters in the range of 75μ to 450μ.
Claim 44
Dependent Claim 21 words
Microcapsules according to claim 27 wherein at least 80% of the microcapsules have diameters in the range of 100μ to 300μ.
Claim 45
Dependent Claim 15 words
Microcapsules according to claim 27 wherein the average microcapsule diameter is from 150μ to 250μ.
Claim 46
Dependent Claim 15 words
Microcapsules according to claim 27 wherein the average microcapsule diameter is from 175μ to 225μ.
Claim 47
Dependent Claim 44 words
Microcapsules according to claim 27 which microcapsules have an average diameter of at least 100μ, 90% of which microcapsules have diameters in the range of 75μ to 450μ, and which microcapsules consist of 97.5% to 99.9% of β-lactam antibiotic and 0.1% to 2.5% polyvinylpyrrolidone.
Claim 48
Dependent Claim 45 words
Microcapsules according to claim 27 which microcapsules have an average diameter between 150μ to 250μ, 95% have diameters between 75μ and 450μ and 80% have diameters between 100μ to 300μ and which microcapsules consist of 98% to 99.9% β-lactam antibiotic and 0.2% to 2% polyvinylpyrrolidone.
Claim 49
Dependent Claim 15 words
Microcapsules according to claim 45 in which the amount of polyvinylpyrrolidone is 0.2% to 1.0%.
Claim 50
Dependent Claim 29 words
Microcapsules according to claim 27 which microcapsules have an average diameter of at least 100μ and 90% of which microcapsules have diameters in the range of 75μ to 450μ.
Claim 51
Dependent Claim 32 words
Microcapsules according to claim 27 wherein the β-lactam antibiotic is ampicillin, amoxycillin, isoxazolylpenicillin, an orally active ester of ampicillin or carbenicillin or a pharmaceutically-acceptable salt or hydrate of ampicillin, amoxycillin or isoxazolylpenicillin.

References Cited (Backward Citations)

US3639306A Cited
US3634586A Cited
GB1287431A Cited
US3725556A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-04-04 1980-10-04 1981-04-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-04-04 1984-10-04 1985-04-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-04-04 1988-10-04 1989-04-05 $7700.00 Window Closed / Lapsed

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