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US5536508A
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Pharmaceutical compositions in the form of particles suitable for the controlled release of pharmacologically active substances and process for preparing the same compositions
Assignee: Vectorpharma International SpA
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Filing: 1993-10-21
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Granted: 1996-07-16
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Expires: 2013-10-21
Abstract
Abstract Pharmaceutical compositions in the form of particles comprising a biodegradable polymer and/or a polysaccharide jellifying and/or bioadhesive polymer, an amphiphilic polymer, an agent modifying the interface properties of the particles and a pharmacologically active substance. Said compositions exhibit improved biocompatibility features and allow a controlled release of the active substance.
Inventors
- 👤 Tiziana Canal
- 👤 Mara Lucia Lovrecich
- 👤 Fabio Carli
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 18:26
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1652; A61K9/1617; A61K9/1641; A61K9/1647; Y; Y10; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2991
Claims Analysis
Total Claims: 36
Claim 1
Independent Claim
99 words
A pharmaceutical composition, in the form of particles having a diameter from 0.1 to 150 μm, suitable for the controlled release of a pharmaceutically active substance, comprising a biodegradable polymer, an amphiphilic polymer, an agent modifying the interface properties at a concentration between 0.1 and 99.9%, and a therapeutically effective amount of the pharmaceutically active substance at a concentration between 0.01 and 99.9% for those in need thereof, wherein said particles have separate intraparticle polymeric phases with different thermal characteristics when the content of the amphiphilic polymer is from 30 to 50% by weight relative to the biodegradable polymer.
Claim 2
Dependent Claim
99 words
A pharmaceutical composition, in the form of particles having a diameter from 0.1 to 150 μm, suitable for the controlled release of a pharmaceutically active substance, comprising a biodegradable polymer, an amphiphilic polymer, an agent modifying the interface properties at a concentration between 0.1 and 99.9%, and a therapeutically effective amount of the pharmaceutically active substance at a concentration between 0.01 and 99.9% for those in need thereof, wherein said particles have separate intraparticle polymeric phases with different thermal characteristics when the content of the amphiphilic polymer is from 30 to 50% by weight relative to the biodegradable polymer.
Claim 3
Dependent Claim
38 words
The pharmaceutical composition according to claim 1, wherein said biodegradable polymer is selected from the group consisting of polylactic acid, polyglycolic acid and co-polymers thereof, polyhydroxybutyric acid, polycaprolacton, polyorthoesters, polyanhydrides, chitins, chitosans, hyaluronic acid, collagen and co-polymers thereof.
Claim 4
Dependent Claim
22 words
The pharmaceutical composition according to claim 1, wherein said amphiphilic polymer is selected from the group consisting of polyethyleneglycol, polyvinylpyrrolidone, and polyvinylalcohol.
Claim 5
Dependent Claim
30 words
The pharmaceutical composition according to claim 1, wherein said agents modifying the interface properties are agents selected from the group consisting of sorbitan esters, polysorbates, lecithins, stearic acid and stearates.
Claim 6
Dependent Claim
45 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is selected from the group consisting of central nervous system active medicaments, cardiovasculars, hypotensives, diuretics, antiphlogistics, analgesics, antipyretics, antiasthma, bronchodilatators, antitussives, mucolytics, antibiotics, chemotherapeutics, antivirus, hormones, antineoplastics, immunosuppressors, immunostimulants, proteins, polypeptides and vaccines.
Claim 7
Dependent Claim
14 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is calcitonin.
Claim 8
Dependent Claim
20 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is selected from the group of LH-RH analogues.
Claim 9
Dependent Claim
22 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is (Des-Gly, D-Trp 6 , Pro 9 -ethylamide) LH-RH analogue.
Claim 10
Dependent Claim
14 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is somatostatin.
Claim 11
Dependent Claim
14 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is somatotropin.
Claim 12
Dependent Claim
17 words
The pharmaceutically composition according to claim 1, wherein said pharmaceutically active substances are broxaterol and hydrochloride thereof.
Claim 13
Dependent Claim
14 words
The pharmaceutically composition according to claim 1, wherein said pharmaceutically active substance is nicergoline.
Claim 14
Dependent Claim
15 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is megesterol acetate.
Claim 15
Dependent Claim
14 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is adriamycin.
Claim 16
Dependent Claim
14 words
The pharmaceutical composition according to claim 1, wherein said pharmaceutically active substance is levonorgestrel.
Claim 17
Dependent Claim
30 words
The pharmaceutical composition according to claim 1, wherein the agent modifying the interface properties is present in an amount of between 0.1% and 50% by weight relative to the polymers.
Claim 18
Dependent Claim
27 words
The pharmaceutical composition according to claim 1, wherein the pharmaceutically active substance in the composition is present in an amount of between 1% and 50% by weight.
Claim 19
Dependent Claim
93 words
A pharmaceutical composition in the form of particles having a diameter from 0.1 to 150 μm, suitable for the controlled release of a pharmaceutically active substance, and having separate polymeric phases with different thermal characteristics, comprising a biodegradable polymer, an amphiphilic polymer present in an amount of from 30 to 50% by weight relative to said biodegradable polymer, an agent modifying the interface properties at a concentration between 0.1% and 99.9%, and a therapeutically effective amount of said pharmaceutically active substance at a concentration between 0.01% and 99.9% for those in need thereof.
Claim 20
Dependent Claim
93 words
A pharmaceutical composition in the form of particles having a diameter from 0.1 to 150 μm, suitable for the controlled release of a pharmaceutically active substance, and having separate polymeric phases with different thermal characteristics, comprising a biodegradable polymer, an amphiphilic polymer present in an amount of from 30 to 50% by weight relative to said biodegradable polymer, an agent modifying the interface properties at a concentration between 0.1% and 99.9%, and a therapeutically effective amount of said pharmaceutically active substance at a concentration between 0.01% and 99.9% for those in need thereof.
Claim 21
Dependent Claim
38 words
The pharmaceutical composition according to claim 18, wherein said biodegradable polymer is selected from the group consisting of polylactic acid, polyglycolic acid and co-polymers thereof, polyhydroxybutyric acid, polycaprolacton polyorthoesters, polyanhydrides, chitins, chitosans, hyaluronic acid, collagen and co-polymers thereof.
Claim 22
Dependent Claim
22 words
The pharmaceutical composition according to claim 18, wherein said amphiphilic polymer is selected from the group consisting of polyethyleneglycol, polyvinylpyrrolidone and polyvinylalcohol.
Claim 23
Dependent Claim
30 words
The pharmaceutical composition according to claim 18, wherein said agents modifying the interface properties are agents selected from the group consisting of sorbitan esters, polysorbates, lecithins, stearic acid and stearates.
Claim 24
Dependent Claim
45 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is selected from the group consisting of central nervous system active medicaments, cardiovasculars, hypotensives, diuretics, antiphlogistics, analgesics, antipyretics, antiasthma, bronchodilatators, antitussives, mucolytics, antibiotics, chemotherapeutics, antivirus, hormones, antineoplastics, immunosuppressors, immunostimulants, proteins, polypeptides and vaccines.
Claim 25
Dependent Claim
14 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is calcitonin.
Claim 26
Dependent Claim
20 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is selected from the group of LH-RH analogues.
Claim 27
Dependent Claim
22 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is (Des-Gly, D-Trp 6 , Pro 9 -ethylamide) LH-RH analogue.
Claim 28
Dependent Claim
14 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is somatostatin.
Claim 29
Dependent Claim
14 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is somatotropin.
Claim 30
Dependent Claim
17 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substances are broxaterol and hydrochloride thereof.
Claim 31
Dependent Claim
14 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is nicergoline.
Claim 32
Dependent Claim
15 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is megesterol acetate.
Claim 33
Dependent Claim
14 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is adriamycin.
Claim 34
Dependent Claim
14 words
The pharmaceutical composition according to claim 18, wherein said pharmaceutically active substance is levonorgestrel.
Claim 35
Dependent Claim
30 words
The pharmaceutical composition according to claim 18, wherein the agent modifying the interface properties is present in an amount of between 0.1% and 50% by weight relative to the polymers.
Claim 36
Dependent Claim
27 words
The pharmaceutical composition according to claim 18, wherein the pharmaceutically active substance in the composition is present in an amount of between 1% and 50% by weight.
References Cited (Backward Citations)
US4293539A
Cited
US4962091A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1999-07-16 | 2000-01-15 | 2000-07-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2003-07-16 | 2004-01-15 | 2004-07-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2007-07-16 | 2008-01-15 | 2008-07-16 | $7700.00 | Window Closed / Lapsed |