US3758679A
Expired / Lapsed
US
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Propoxyphene napsylate timed release particles
Assignee: Eli Lilly and Co
•
Filing: 1972-02-22
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Granted: 1973-09-11
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Expires: 1992-02-22
Abstract
Abstract A pharmaceutical preparation is described which comprises particles of propoxyphene napsylate having timed-release properties.
Inventors
- 👤 W Seidler
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 22:17
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K31/00; A61K31/21; A61K31/215; A61K31/22
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
63 words
The pharmaceutical preparation of claim 1 wherein said intimate admixture is comprised of from about 50 to about 80 percent propoxyphene napsylate; from about 0 to about 5 percent gelatinized starch; from about 0 to about 25 percent microcrystalline cellulose; and from about 0 to about 30 percent of a saccharide selected from the class consisting of sucrose, dextrose, lactose, fructose, and maltose.
Claim 2
Dependent Claim
14 words
rotating said plate at a speed sufficient to overcome the inertia of said strands;
Claim 3
Dependent Claim
4 words
2.5 percent gelatinized starch,
Claim 4
Dependent Claim
20 words
imparting velocity to said strands such that said strands move in a curved path toward the periphery of said plate;
Claim 5
Dependent Claim
31 words
The pharmaceutical preparation of claim 1 comprised of from about 96 to about 99.6 percent of said intimate admixture and from about 0.4 to about 4 percent of said granulating agent.
Claim 6
Dependent Claim
5 words
12.5 percent microcrystalline cellulose, and
Claim 7
Dependent Claim
49 words
The pharmaceutical preparation of claim 1 comprised of (a) about 98.75 percent of an intimate admixture of about 70 percent propoxyphene napsylate; and 2.5 percent gelatinized starch; about 12.5 percent microcrystalline cellulose; and about 15 percent sucrose, and (b) about 1.25 percent of sodium carboxymethylcellulose as a granulating agent.
Claim 8
Dependent Claim
9 words
establishing a moving toroidal ring of said strands; and
Claim 9
Dependent Claim
72 words
15 percent sucrose; b. blending said intimate admixture of (a) with about 25 milliliters of about a 5 percent aqueous dispersion of sodium carboxymethylcellulose per 100 grams of said intimate admixture; c. extruding the blend of (b) under a pressure of from about 25 to about 600 psig through a perforated plate into elongated strands having a longitudinal dimension greater than the cross-sectional dimension; d. reducing the extruded strands of (c) by:
Claim 10
Dependent Claim
32 words
continuing such movement until said strands are reduced into particles having essentially equal cross-sectional and longitudinal axes; and e. drying the particles of (d) to a moisture content of about 5 percent.
Claim 11
Independent Claim
135 words
A method of preparing a timed-release pharmaceutical preparation for oral administration comprising: a. combining propoxyphene napsylate in an intimate admixture with an excipient or a combination of excipients selected from the group consisting of gelatinized starch, microcrystalline cellulose, and a saccharide selected from the class consisting of sucrose, dextrose, lactose, fructose and maltose; b. blending the intimate admixture of (a) with an aqueous dispersion of a granulating agent selected from the group consisting of partially hydrolyzed starch, sodium carboxymethylcellulose, methylcellulose, hydroxypropylmethylcellulose, and polyvinylpyrrolidone; c. extruding the blend of (b) under pressure through a perforated plate forming an extrudate of elongated strands having a length generally exceeding the cross-sectional dimension; d. reducing the strands of extrudate (c) into particles having essentially equal cross-sectional and longitudinal axes; e. removing the excess water from the particles of (d).
Claim 12
Dependent Claim
62 words
The method of claim 5 wherein the intimate admixture of (a) is comprised of from about 50 to about 80 percent propoxyphene napsylate, 0 to about 5 percent gelatinized starch, 0 to about 25 percent microcrystalline cellulose, and 0 to about 30 percent of a saccharide selected from the class consisting of sucrose, dextrose, lactose, fructose, or maltose, or a combination thereof.
Claim 13
Dependent Claim
34 words
The method of claim 5 wherein the intiMate admixture of (a) is comprised of about 70 percent propoxyphene napsylate, about 2.5 percent gelatinized starch, about 12.5 percent microcrystalline cellulose, and about 15 percent sucrose.
Claim 14
Dependent Claim
48 words
The method of claim 5 wherein the aqueous dispersion of a granulating agent of (b) is selected from the groups consisting of about 1.0 to about 10 percent partially hydrolyzed starch paste, and about 1.0 to about 5.0 percent aqueous dispersions of sodium carboxymethylcellulose methylcellulose, hydroxypropylmethylcellulose, and polyvinylpyrrolidone.
Claim 15
Dependent Claim
37 words
The method of claim 5 wherein the aqueous dispersion of a granulating agent of (b) is employed in an amount of from about 10 to about 40 milliliters per 100 grams of the intimate admixture of (a).
Claim 16
Dependent Claim
30 words
The method of claim 5 wherein 100 grams of the intimate mixture of (a) is blended with about 25 milliliters of a 5 percent aqueous dispersion of sodium carboxymethyl cellulose.
Claim 17
Dependent Claim
24 words
The method of claim 5 wherein the strands of extrudate (c) are formed at a pressure of from about 25 to about 600 psig.
Claim 18
Dependent Claim
73 words
The method of claim 5 wherein the reduction (d) of the strands of extrudate is accomplished by contacting said extrudate with a moving frictional plate; moving said frictional plate at a velocity sufficient to overcome the inertia of said extrudate; imparting velocity to said extrudate such that said extrudate moves in a rolling, tumbling bed; and continuing such movement until said extrudate is reduced into particles having essentially equal longitudinal and cross-sectional axes.
Claim 19
Dependent Claim
24 words
The method of claim 12 wherein the moving frictional plate is a circular frictional plate mounted horizontally in a vertically disposed stationary cylindrical vessel.
Claim 20
Dependent Claim
12 words
The method of claim 5 comprising: a. combining in an intimate admixture
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1976-09-10 | 1977-03-12 | 1977-09-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1980-09-10 | 1981-03-12 | 1981-09-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1984-09-10 | 1985-03-12 | 1985-09-11 | $7700.00 | Window Closed / Lapsed |