US4851228A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Multiparticulate controlled porosity osmotic
Assignee: Merck and Co Inc
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Filing: 1987-07-15
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Granted: 1989-07-25
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Expires: 2007-07-15
Abstract
Abstract The instant invention is directed to a multiparticulate osmotic pump, for the controlled release of a pharmaceutically active agent to an environment of use, said pump comprising: (I) a carrier medium which does not maintain its integrity in the environment of use; (II) a multiple of tiny osmotic pump elements each consisting essentially of: (A) a core comprises at least one pharmacologically active agent soluble in an external fluid, or a mixture of an agent having a limited solubility in the external fluid with an osmotically effective solute that is soluble in the fluid, which exhibit an osmotic pressure gradient across the wall against the external fluid surrounded by (B) a rate controlling water insoluble wall, having a fluid permeability of 6.96x10-18 to 6.96x1014 cm3 sec/g and a reflection coefficient of less than 0.5, prepared from: (i) a polymer permeable to water but impermeable to solute and (ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
Inventors
- 👤 Gaylen M. Zentner
- 👤 Kenneth J. Himmelstein
- 👤 Gerald S. Rork
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 21:56
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0002; A61K9/0004
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
172 words
A multiparticulate osmotic pump, for the controlled release of a pharmaceutically active agent to an environment of use, said pump comprising: (I) a carrier medium which does not maintain its integrity in the environment of use; (II) a multiple of tiny osmotic pump elements each consisting essentially of: (A) a core comprises at least one pharmacologically active agent soluble in an external fluid, or a mixture of an agent having a limited solubility in the external fluid with an osmotically effective solute that is soluble in the fluid, which exhibit an osmotic pressure gradient across the wall against the external fluid surrounded by (B) a rate controlling water insoluble wall, having a fluid permeability of 6.96×10 -18 to 6.96×10 -14 cm 3 sec/g and a reflection coefficient of less than 0.5, prepared from: (i) a polymer permeable to water but impermeable to solute and (ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
Claim 2
Dependent Claim
172 words
A multiparticulate osmotic pump, for the controlled release of a pharmaceutically active agent to an environment of use, said pump comprising: (I) a carrier medium which does not maintain its integrity in the environment of use; (II) a multiple of tiny osmotic pump elements each consisting essentially of: (A) a core comprises at least one pharmacologically active agent soluble in an external fluid, or a mixture of an agent having a limited solubility in the external fluid with an osmotically effective solute that is soluble in the fluid, which exhibit an osmotic pressure gradient across the wall against the external fluid surrounded by (B) a rate controlling water insoluble wall, having a fluid permeability of 6.96×10 -18 to 6.96×10 -14 cm 3 sec/g and a reflection coefficient of less than 0.5, prepared from: (i) a polymer permeable to water but impermeable to solute and (ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
Claim 3
Dependent Claim
60 words
The osmotic pump of claim 1, wherein said pore forming additive comprises: (a) 0.1 to 50%, by weight, solid additive, based on the total weight of (i) and (ii), and/or (b) 0.1 to 40%, by weight, liquid additive, based on the total weight of (i) and (ii), not to exceed a total weight % of pore forming additive of 60%.
Claim 4
Dependent Claim
14 words
The osmotic pump of claim 1, wherein said reflection coefficient is less than 0.1.
Claim 5
Dependent Claim
42 words
The osmotic pump of claim 1, further comprising: (C) 0 to 50 parts per 100 parts of (i) and (ii) of plasticizer and flux regulating additives and (D) 0 to 40 parts per 100 parts of (i) and (ii), of surfactant additive.
Claim 6
Dependent Claim
36 words
The osmotic pump of claim 1, wherein said water insolube wall is 1 to 1,000 microns thick and wherein 5 to 95% of the resulting wall pores are between 10 angstroms and 100 microns in diameter.
Claim 7
Dependent Claim
28 words
The osmotic pump of claim 5 wherein said wall is 20 to 500 microns thick and said wall pores are between 10 angstroms and 25 microns in diameter.
Claim 8
Dependent Claim
16 words
The osmotic pump of claim 1, wherein at least 0.05 ng of active agent are used.
Claim 9
Dependent Claim
16 words
The osmotic pump of claim 7, wherein at lest 1 microgram of active agent is used.
Claim 10
Dependent Claim
37 words
The osmotic pump of claim 1, wherein said polymer is selected from the group consisting of cellulose esters, acryalted polysaccharides, polyurethane, polymers of acrylic and methacrylic acid and esters thereof, poly (ortho ester)s, polyacetals and mixtures thereof.
Claim 11
Dependent Claim
21 words
The osmotic pump of claim 9, wherein said polymer is selected from the group consisting of cellulose esters and acylated polysaccharides.
Claim 12
Dependent Claim
27 words
The osmotic pump of claim 9 wherein said polymer is selected from the group consisting of polyurethanes and polymers of acrylic and methacrylic acid and esters thereof.
Claim 13
Dependent Claim
20 words
The osmotic pump of claim 9, wherein said polymer is selected from the group consisting of poly(ortho ester)s and polyacetals.
Claim 14
Dependent Claim
34 words
The osmotic pump of claim 1, wherein said pore forming additive is selected from the group consisting of water, alkali metal salts, alkaline earth metal salts, saccharides, aliphatic polyols, aromatic polyols and mixtures thereof.
Claim 15
Dependent Claim
19 words
The osmotic pump of claim 1, wherein 0.1 to 50%, by weight, of said pore forming additive is used.
Claim 16
Dependent Claim
27 words
The osmotic pump of claim 1, wherein said pH insensitive pore forming additive is selected from the group consisting of polyethylene glycol, sorbitol, glucose and mixtures thereof.
Claim 17
Dependent Claim
25 words
The osmotic pump of claim 1, wherein said active agent is selected from the group consisting of potassium chloride, sodium indomethacin trihydrate and cyclobenzaprine HCl.
Claim 18
Dependent Claim
30 words
The osmotic pump of claim 1, wherein said active agent is selected from the group consisting of quinoline carboxylic acids, naphthyridine carboxylic acids, pyrimidine carboxylic acids, and cinnoline carboxylic acids.
Claim 19
Dependent Claim
12 words
The osmotic pump of claim 1 wherein the carrier medium is solid.
Claim 20
Dependent Claim
19 words
The osmotic pump of claim 18 wherein the solid carrier medium is a soluble gelatin capsule or tablet matrix.
Claim 21
Dependent Claim
16 words
The osmotic pump of claim 19 wherein the solid carrier medium is a soluble gelatin capsule.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-07-24 | 1993-01-23 | 1993-07-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-24 | 1997-01-23 | 1997-07-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-24 | 2001-01-23 | 2001-07-25 | $7700.00 | Window Closed / Lapsed |