US3976071A
Expired / Lapsed
US
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Methods of improving control of release rates and products useful in same
Assignee: Debiopharm SA
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Filing: 1974-01-07
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Granted: 1976-08-24
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Expires: 1994-01-07
Abstract
Abstract Improved processes for obtaining the sustained release of pharmaceuticals from polymer matrices comprising the utilization of such steps as will allow the formation of solid solutions between pharmaceutical and its matrix or, conversely and in a proper case, substantially avoiding formation of any solid solution between the matrix and pharmaceutical. The advantage of such processes is the greater predictability of qualitative and quantitative nature of release rates of products formed therewith.
Inventors
- 👤 Safik E. Sadek
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-22 23:33
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K9/204
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
85 words
Solid-shaped articles for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said articles formed of (1) an active pharmaceutical chemical agent and (2) an organic polymer matrix, said agent and polymer normally forming a composition wherein there is substantial insolubility of one in the other, wherein said articles are formed of a composition of said agent and said polymer which is a solid solution and comprises substantially all of said agent in solution.
Claim 2
Dependent Claim
85 words
Solid-shaped articles for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said articles formed of (1) an active pharmaceutical chemical agent and (2) an organic polymer matrix, said agent and polymer normally forming a composition wherein there is substantial insolubility of one in the other, wherein said articles are formed of a composition of said agent and said polymer which is a solid solution and comprises substantially all of said agent in solution.
Claim 3
Dependent Claim
15 words
Articles as defined in claim 1 wherein said active agent is an organic pharmaceutical chemical.
Claim 4
Dependent Claim
13 words
Articles as defined in claim 2 wherein said organic chemical is a steroid.
Claim 5
Dependent Claim
19 words
Articles as defined in claim 2 wherein said organic polymer matrix is a poly(glycolic acid) or a polylactic acid.
Claim 6
Dependent Claim
35 words
Articles as defined in claim 1 wherein said solid solution is a supercooled solution containing a quantity of a solute that have substantial insolubility with said matrix when said matrix is in the liquid state.
Claim 7
Dependent Claim
15 words
Articles as defined in claim 1 wherein said active agent is an organic pharmaceutical chemical.
Claim 8
Dependent Claim
13 words
Articles as defined in claim 6 wherein said organic chemical is a steroid.
Claim 9
Dependent Claim
18 words
Articles as defined in claim 6 wherein said organic polymer matrix is a poly(glycolic acid) a polylactic acid.
Claim 10
Dependent Claim
82 words
Solid-shaped articles for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said articles formed of (1) an active pharmaceutical chemical agent and (2) an organic polymer matrix, said agent and polymer normally forming a composition wherein there is substantial solubility of one in the other, wherein said articles are formed of a composition of said agent and said polymer which there is no substantial solution of one in the other.
Claim 11
Dependent Claim
82 words
Solid-shaped articles for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said articles formed of (1) an active pharmaceutical chemical agent and (2) an organic polymer matrix, said agent and polymer normally forming a composition wherein there is substantial solubility of one in the other, wherein said articles are formed of a composition of said agent and said polymer which there is no substantial solution of one in the other.
Claim 12
Dependent Claim
15 words
Articles as defined in claim 9 wherein said active agent is an organic pharmaceutical chemical.
Claim 13
Dependent Claim
13 words
Articles as defined in claim 10 wherein said organic chemical is a steroid.
Claim 14
Dependent Claim
18 words
Articles as defined in claim 10 wherein said organic polymer matrix is a poly(glycolic acid) a polylactic acid.
Claim 15
Dependent Claim
77 words
In a process for administering medication at more favorable dosage rates over an extended period of time by implanting into a host body a solid medicine-bearing implant formed of a polymeric matrix and an active medicinal agent which normally has substantial insolubility in said matrix, the improvement comprising the step of modifying the administering rate by implanting said matrix and agent in a composition which is a substantially complete solid solution of said matrix and said agent.
Claim 16
Dependent Claim
77 words
In a process for administering medication at more favorable dosage rates over an extended period of time by implanting into a host body a solid medicine-bearing implant formed of a polymeric matrix and an active medicinal agent which normally has substantial insolubility in said matrix, the improvement comprising the step of modifying the administering rate by implanting said matrix and agent in a composition which is a substantially complete solid solution of said matrix and said agent.
Claim 17
Dependent Claim
17 words
In a process as defined in claim 13 wherein said active agent is an organic pharmaceutical chemical.
Claim 18
Dependent Claim
15 words
In a process as defined in claim 14 wherein said organic chemical is a steroid.
Claim 19
Dependent Claim
21 words
In a process as defined in claim 14 wherein said organic polymer matrix is a poly(glycolic acid) or a polylactic acid.
Claim 20
Dependent Claim
101 words
A process for making a medicinal implant article for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said article being made from (1) a polymer matrix which is decomposable in a physiological environment into physiologically-tolerable decomposition products and (2) an organic pharmaceutical chemical which normally has substantial insolubility in said matrix polymer when said polymer is a solid state, said process comprising the mixing of said matrix and said polymer to form a solid solution which is stable under physiological conditions and free from said chemical in non-solute form.
Claim 21
Dependent Claim
101 words
A process for making a medicinal implant article for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said article being made from (1) a polymer matrix which is decomposable in a physiological environment into physiologically-tolerable decomposition products and (2) an organic pharmaceutical chemical which normally has substantial insolubility in said matrix polymer when said polymer is a solid state, said process comprising the mixing of said matrix and said polymer to form a solid solution which is stable under physiological conditions and free from said chemical in non-solute form.
Claim 22
Dependent Claim
23 words
A process as defined in claim 17 wherein said article is formed by making a supercooled solution of said solute in said matrix.
Claim 23
Dependent Claim
13 words
A process as defined in claim 17 wherein said pharmaceutical is a steroid.
Claim 24
Dependent Claim
18 words
A process as defined in claim 19 wherein said polymer is a poly(lactic acid) or a poly(glycolic acid).
Claim 25
Dependent Claim
96 words
A process for making a medicinal implant article for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said article being made from (1) a polymer matrix which is decomposable in a physiological environment into physiologically-tolerable decomposition products and (2) an organic pharmaceutical chemical which is normally soluble in said matrix polymer when said polymer is in a liquid state, said process comprising the mixing of said matrix and said polymer without liquifying and matrix and thereby maintaining said pharmaceutical entirely in a non-solute state.
Claim 26
Dependent Claim
96 words
A process for making a medicinal implant article for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said article being made from (1) a polymer matrix which is decomposable in a physiological environment into physiologically-tolerable decomposition products and (2) an organic pharmaceutical chemical which is normally soluble in said matrix polymer when said polymer is in a liquid state, said process comprising the mixing of said matrix and said polymer without liquifying and matrix and thereby maintaining said pharmaceutical entirely in a non-solute state.
Claim 27
Dependent Claim
75 words
In a process for administering medication at more favorable dosage rates over an extended period of time by implanting into a host body a solid medicine-bearing implant formed of a polymeric matrix and an active medicinal agent which normally has substantial solubility in said matrix, the improvement comprising the step of modifying the administering rate by implanting said matrix and agent as a composition substantially free from any solution of said agent in said matrix.
Claim 28
Dependent Claim
75 words
In a process for administering medication at more favorable dosage rates over an extended period of time by implanting into a host body a solid medicine-bearing implant formed of a polymeric matrix and an active medicinal agent which normally has substantial solubility in said matrix, the improvement comprising the step of modifying the administering rate by implanting said matrix and agent as a composition substantially free from any solution of said agent in said matrix.
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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) | 1979-08-24 | 1980-02-23 | 1980-08-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-08-24 | 1984-02-23 | 1984-08-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-08-24 | 1988-02-23 | 1988-08-24 | $7700.00 | Window Closed / Lapsed |