Patent US5567431A successfully refreshed from Google Patents.
US5567431A
Expired / Lapsed
US
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Polylactic acid-based implant susceptible of bioresorption containing and antibiotic
Assignee: Centre National de la Recherche Scientifique
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Filing: 1992-03-13
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Granted: 1996-10-22
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Expires: 2012-03-13
Abstract
Abstract Implantable poly(lactic acid)-based pharmaceutical composition which comprises at least one water soluble antibiotic in particle form with controlled dimensions, less than 100 μm uniformly dispersed in an amorphous poly(lactic acid) matrix, said composition being in ground powder or thin film form. Application especially in initiating local internal antibiotic therapy by the gradual release of the antibiotic substance.
Inventors
- 👤 Michel Vert
- 👤 Jacques Mauduit
- 👤 Niels Bukh
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 07:08
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0024; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61K9/70; A61K9/7007
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
136 words
A bioresorbable pharmaceutical composition comprising poly(lactic acid), said composition being implantable so as to implement a local internal antibiotherapy for those in need thereof, said composition comprising an antibiotically effective amount of at least one water-soluble antibiotic in the form of particles of controlled size less than 100 μm dispersed homogeneously in a poly(lactic acid) matrix, said composition being provided in the form of (i) either a ground powder obtained by grinding a homogeneous dispersion of said antibiotic in an amorphous poly(lactic acid) matrix having a mean molecular mass ranging from 10,000 to 300,000 or (ii) a thin film whose poly(lactic acid) matrix is made of a mixture of (1) an amorphous poly(lactic acid) having a mean molecular mass greater than 20,000 and (2) an amorphous poly(lactic acid) having a mean molecular mass less than 5,000.
Claim 2
Dependent Claim
136 words
A bioresorbable pharmaceutical composition comprising poly(lactic acid), said composition being implantable so as to implement a local internal antibiotherapy for those in need thereof, said composition comprising an antibiotically effective amount of at least one water-soluble antibiotic in the form of particles of controlled size less than 100 μm dispersed homogeneously in a poly(lactic acid) matrix, said composition being provided in the form of (i) either a ground powder obtained by grinding a homogeneous dispersion of said antibiotic in an amorphous poly(lactic acid) matrix having a mean molecular mass ranging from 10,000 to 300,000 or (ii) a thin film whose poly(lactic acid) matrix is made of a mixture of (1) an amorphous poly(lactic acid) having a mean molecular mass greater than 20,000 and (2) an amorphous poly(lactic acid) having a mean molecular mass less than 5,000.
Claim 3
Dependent Claim
42 words
The pharmaceutical composition of claim 1 wherein said amorphous poly(lactic acid) matrix comprises a mixture of units derived from a D- and L-lactic acid, the amount of each of said D- and L-units being sufficient for said poly(lactic acid) to be amorphous.
Claim 4
Dependent Claim
19 words
The pharmaceutical composition of claim 2 wherein said poly(lactic acid) contains from 20 to 80 percent of D-lactic units.
Claim 5
Dependent Claim
21 words
The pharmaceutical composition of claim 3 wherein said poly(lactic acid) contains units derived from D- and L-lactic acids in equal proportions.
Claim 6
Dependent Claim
28 words
The pharmaceutical composition of claim 1 in the form of a ground powder wherein said amorphous poly(lactic acid) matrix has a molecular mass at least equal to 10,000.
Claim 7
Dependent Claim
28 words
The pharmaceutical composition of claim 1 in the form of a ground powder wherein said amorphous poly(lactic acid) matrix has a molecular mass ranging from 10,000 to 30,000.
Claim 8
Dependent Claim
20 words
The pharmaceutical composition of claim 1 wherein said ground powder has a particle size ranging from 0.1 to 1 mm.
Claim 9
Dependent Claim
37 words
The pharmaceutical composition of claim 7 wherein said ground powder comprises a mixture of (a) particles having a size ranging from 0.1 to 0.2 mm and (b) particles having a size ranging from 0.5 to 1 mm.
Claim 10
Dependent Claim
60 words
The pharmaceutical composition of claim 8 wherein the concentration of said antibiotic is sufficient for the amount of antibiotic released, in an isotonic phosphate buffer of pH 7.4 at 37° C., at the end of 24 hours, to be at least equal to 20 percent of the initial amount of antibiotic and less than 70 percent of the initial amount.
Claim 11
Dependent Claim
20 words
The pharmaceutical composition of claim 9 wherein the amount of said antibiotic ranges from 5 and 30 percent by weight.
Claim 12
Dependent Claim
37 words
The pharmaceutical composition of claim 1 wherein the amount of said amorphous poly(lactic acid) having a molecular mass less than 5,000 is sufficient for a glass transition of said mixture of polymers being less than 37° C.
Claim 13
Dependent Claim
91 words
The pharmaceutical composition of claim 1 wherein the amount of the water-soluble antibiotic or the low molecular mass poly(lactic acid) or mixture thereof is sufficiently high for the amount of antibiotic released, in an isotonic phosphate buffer of pH 7.4, at 37° C., at the end of 24 hours, to be as least equal to 20 percent of the initial amount, for a film having an initial thickness of 0.3 mm, and wherein said amounts are sufficiently low for said amount released being less than 70 percent of the initial amount.
Claim 14
Dependent Claim
18 words
The pharmaceutical composition of claim 1 wherein said film has a thickness in the range of 0.05-1 mm.
Claim 15
Dependent Claim
16 words
The pharmaceutical composition of claim 1 wherein said film is provided with a plurality of perforations.
Claim 16
Dependent Claim
27 words
The pharmaceutical composition of claim 14 wherein the surface area of said perforations represents from 10 to 70 percent of the total surface area of said film.
Claim 17
Dependent Claim
24 words
The pharmaceutical composition of claim 1 wherein said water-soluble antibiotic in the form of particles have a size ranging from 0.01 to 50 μm.
Claim 18
Dependent Claim
19 words
The pharmaceutical composition of claim 1 wherein said antibiotic is present in the form of a pharmaceutically acceptable salt.
Claim 19
Dependent Claim
80 words
A process for preparing an implantable and bioresorbable pharmaceutical composition in the form of a powder, said composition comprising poly(lactic acid) and an antibiotically effective amount of at least one water-soluble antibiotic in the form of particles of controlled size less than 100 μm, said antibiotic being dispersed homogeneously in an amorphous poly(lactic acid) matrix, said process comprising grinding a homogeneous dispersion of said antibiotic in said amorphous poly(lactic acid) matrix having a molecular mass ranging from 10,000 to 300,000.
Claim 20
Dependent Claim
80 words
A process for preparing an implantable and bioresorbable pharmaceutical composition in the form of a powder, said composition comprising poly(lactic acid) and an antibiotically effective amount of at least one water-soluble antibiotic in the form of particles of controlled size less than 100 μm, said antibiotic being dispersed homogeneously in an amorphous poly(lactic acid) matrix, said process comprising grinding a homogeneous dispersion of said antibiotic in said amorphous poly(lactic acid) matrix having a molecular mass ranging from 10,000 to 300,000.
Claim 21
Dependent Claim
79 words
A process for preparing an implantable and bioresorbable pharmaceutical composition in the form of a thin film, said composition comprising poly (lactic acid) and at least one water-soluble antibiotic in the form of particles of controlled size less than 100 μm, said antibiotic being dispersed homogeneously in an amorphous poly(lactic acid) matrix, said process comprising admixing said amorphous poly(lactic acid) having a molecular mass greater than 20,000 with an amorphous poly(lactic acid) having a molecular mass less than 5,000.
Claim 22
Dependent Claim
79 words
A process for preparing an implantable and bioresorbable pharmaceutical composition in the form of a thin film, said composition comprising poly (lactic acid) and at least one water-soluble antibiotic in the form of particles of controlled size less than 100 μm, said antibiotic being dispersed homogeneously in an amorphous poly(lactic acid) matrix, said process comprising admixing said amorphous poly(lactic acid) having a molecular mass greater than 20,000 with an amorphous poly(lactic acid) having a molecular mass less than 5,000.
Claim 23
Dependent Claim
41 words
The process of claim 19 further comprising mixing said water-soluble antibiotic particles and said amorphous poly(lactic acid) matrix in a solvent of a polymer wherein said antibiotic is insoluble, said solvent being evaporated and the resulting composition being ground or calendered.
Claim 24
Dependent Claim
34 words
The process of claim 20 wherein said mixing comprises kneading said at least one water-soluble antibiotic in the form of particles with said amorphous poly(lactic acid) to produce a film, and calendering said film.
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EP0251680A2
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US5180765A
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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) | 1999-10-22 | 2000-04-22 | 2000-10-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2003-10-22 | 2004-04-22 | 2004-10-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2007-10-22 | 2008-04-22 | 2008-10-22 | $7700.00 | Window Closed / Lapsed |