Patent US2715618A successfully refreshed from Google Patents.
Patent US4867985A successfully refreshed from Google Patents.
US4867985A
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US
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Spheroids
Assignee: Euro Celtique SA
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Filing: 1988-03-01
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Granted: 1989-09-19
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Expires: 2008-03-01
Abstract
Abstract A controlled release pharmaceutical composition contains a number of spheroids, the spheroids containing a water-insoluble drug dispersed in a controlled release matrix. The matrix contains between 70% and 99.5% (by weight) of microcrystalline cellulose, between 0.5% and 4% (by weight) of a cellulose derivative and, optionally, up to 26% of a sugar or a sugar alcohol. The water insoluble drug must dissolve in water (pH 5) at 20° C. to a concentration of less than 1.0 mg ml-1, preferably less than 0.5 mg ml-1. Preferred drugs are non-steroidal anti-inflammatory agents, especially fenprofen calcium, ibuprofen, ketoprofen, naproxen, diclofenac sodium, fenbufen, flurbiprofen, indomethancin, oxyphenbutazone, phenylbutazone or piroxicam.
Inventors
- 👤 Joanne Heafield
- 👤 Stewart T. Leslie
- 👤 Sandra T. A. Malkowska
- 👤 Philip J. Neale
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 16:25
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1652
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
88 words
A controlled release pharmaceutical composition comprising a plurality of spheroids, the spheroids comprising a water-insoluble drug selected from the group consisting of benzocaine, nifedipine, bendrofluazide, benzthiazide, chlorothiazide, chlorthalidone, cyclopenthiazide, frusemide, hydrochlorothiazide, hydroflumethiazide, spironolactone, reserpine, chlorpropamide, glibenclamide, betamethasone, cortisone acetate, dexamethasone, hydrocortisone, prednisone, trimethoprim, digoxin, haloperidol, phenytoin, pindolol, clofibrate, fenoprofen calcium, ibuprofen, ketoprofen, naproxen, diclofenac sodium, fenbufen, flurbiprofen, indomethacin, oxyphenbutazone, phenylbutazone, prioxicam, dispsersed in a controlled release matrix, whereinthe matrix comprises between 70% and 99.5% of microcrystalline cellulose and between 0.5% and 4% of at least one cellulose derivative.
Claim 2
Dependent Claim
88 words
A controlled release pharmaceutical composition comprising a plurality of spheroids, the spheroids comprising a water-insoluble drug selected from the group consisting of benzocaine, nifedipine, bendrofluazide, benzthiazide, chlorothiazide, chlorthalidone, cyclopenthiazide, frusemide, hydrochlorothiazide, hydroflumethiazide, spironolactone, reserpine, chlorpropamide, glibenclamide, betamethasone, cortisone acetate, dexamethasone, hydrocortisone, prednisone, trimethoprim, digoxin, haloperidol, phenytoin, pindolol, clofibrate, fenoprofen calcium, ibuprofen, ketoprofen, naproxen, diclofenac sodium, fenbufen, flurbiprofen, indomethacin, oxyphenbutazone, phenylbutazone, prioxicam, dispsersed in a controlled release matrix, whereinthe matrix comprises between 70% and 99.5% of microcrystalline cellulose and between 0.5% and 4% of at least one cellulose derivative.
Claim 3
Dependent Claim
15 words
A composition according to claim 1 wherein the water-insoluble drug comprises a non-steroidal anti-inflammatory agent.
Claim 4
Dependent Claim
29 words
A composition according to claim 2 wherein the water-insoluble drug comprises at least one of fenprofen calcium, ibuprofen, ketoprofen, naproxen, diclofenac sodium, fenbufen, flurbiprofen, indomethacin, oxyphenbutazone, phenylbutazone and piroxicam.
Claim 5
Dependent Claim
12 words
A composition according to claim 3 wherein the water-insoluble drug comprises naproxen.
Claim 6
Dependent Claim
12 words
A composition according to claim 3 wherein the water-insoluble drug comprises indomethacin.
Claim 7
Dependent Claim
17 words
A composition according to claim 1 wherein the at least one cellulose derivative comprises a hydratable cellulose.
Claim 8
Dependent Claim
19 words
A composition according to claim 6 wherein the at least on cellulose drivative comprises a hydroxy lower alkyl cellulose.
Claim 9
Dependent Claim
22 words
A composition according to claim 7 wherein the at least one cellulose derivative comprises at least one of hydroxypropylcellulose and hydroxypropylmethyl cellulose.
Claim 10
Dependent Claim
25 words
A composition according to claim 1 wherein the ratio of the microcrystalline cellulose to the at least one cellulose derivative is between 20:1 and 100:1.
Claim 11
Dependent Claim
14 words
A composition according to claim 9 wherein the ratio is between 30:1 and 70:1.
Claim 12
Dependent Claim
23 words
A composition according to claim 1 wherein the controlled release matrix further comprises at least one sugar or at least one sugar alcohol.
Claim 13
Dependent Claim
11 words
A composition according to claim 11 wherein the sugar comprises lactose.
Claim 14
Dependent Claim
28 words
A composition according to claim 11 wherein the controlled release matrix contains up to 26% (by weight) of at least one sugar or at least one sugar alcohol.
Claim 15
Dependent Claim
13 words
A controlled release pharmaceutical composition according to claim 1 in unit dosage form.
Claim 16
Dependent Claim
15 words
A composition according to claim 14 in the form of a capsule, cachet of sachet.
Claim 17
Dependent Claim
134 words
A process for the preparation of a controlled release pharmaceutical composition according to claim 1 comprising (a) blending a mixture comprising a water-insoluble drug, a predetermined amount of microcrystalline cellulose, a predetermined amount of at least one cellulose derivative and water, (b) granulating and extruding the blended mixture to give a uniform, free-flowing extrudate, (c) spheronising the extrudate until spheroids are formed, (d) drying the spheroids, and (e) optionally, film coating the spheroids, to form a plurality of spheroids, the spheroids comprising a water-insoluble drug dispersed in a controlled release matrix wherein the amounts of the microcrystalline cellulose and the at least one cellulose derivative are so determined that the matrix comprises between 70% and 99.5% by weight of microcrystalline cellulose and between 0.5% and 4% by weight of at least one cellulose derivative.
Claim 18
Dependent Claim
25 words
A process according to claim 16 wherein the spheroids are dried until the moisture content is between 0% and 5% of the total spheroid weight.
References Cited (Backward Citations)
US4681765A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-09-18 | 1993-03-20 | 1993-09-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-09-18 | 1997-03-20 | 1997-09-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-09-18 | 2001-03-20 | 2001-09-19 | $7700.00 | Window Closed / Lapsed |