US4568547A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Solid pharmaceutical compositions comprising MSM and their production
Assignee: CARDINAL ASSOCIATES Inc dba BERGSTROM NUTRITION
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Filing: 1984-02-28
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Granted: 1986-02-04
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Expires: 2004-02-28
Abstract
Abstract Methylsulfonylmethane (MSM) is useful as a tableting and granulating aid for pharmaceutically active agents, especially those which are unstable in the presence of moisture, mixtures therewith being or formable into free-flowing powders or granules which are readily compressible into tablets of improved properties. A preferred method of forming such powders or granules involves mixing the pharmaceutically active agent under substantially anhydrous conditions with molten MSM or with particulate solid MSM at its softening point, cooling the resultant mixture and, when the MSM was molten, forming the solidified melt into granules or a free flowing powder and thereafter, if desired, compressing the powder or granules into tablets.
Inventors
- 👤 Robert J. Herschler
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 20:00
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/16; A61K31/17; A61K31/095; A61K31/10; A61K31/70; A61K31/7004; A61K33/00; A61K33/14
Claims Analysis
Total Claims: 33
Claim 1
Independent Claim
86 words
In a solid pharmaceutical composition adapted for oral ingestion, in the form of tablets, granules or a free-flowing powder and consisting essentially of an intimate, physical mixture of at least one pharmaceutically systemically active agent which is storage unstable in the presence of moisture and a pharmaceutically acceptable carrier therefor, the improvement wherein the mixture is substantially anhydrous, the carrier consists essentially of methylsulfonylmethane (MSM) and the pharmaceutically active agent is dissolved in the MSM or adheringly bonded to the surface of particles of the MSM.
Claim 2
Dependent Claim
86 words
In a solid pharmaceutical composition adapted for oral ingestion, in the form of tablets, granules or a free-flowing powder and consisting essentially of an intimate, physical mixture of at least one pharmaceutically systemically active agent which is storage unstable in the presence of moisture and a pharmaceutically acceptable carrier therefor, the improvement wherein the mixture is substantially anhydrous, the carrier consists essentially of methylsulfonylmethane (MSM) and the pharmaceutically active agent is dissolved in the MSM or adheringly bonded to the surface of particles of the MSM.
Claim 3
Dependent Claim
18 words
A composition according to claim 1, wherein the carrier consists of at least 95% by weight of MSM.
Claim 4
Dependent Claim
13 words
A composition according to claim 1, in the form of a free-flowing powder.
Claim 5
Dependent Claim
11 words
A composition according to claim 1, in the form of granules.
Claim 6
Dependent Claim
11 words
A composition according to claim 1, in the form of tablets.
Claim 7
Dependent Claim
15 words
Tablets according to the composition of claim 5, wherein the pharmaceutically active agent is aspirin.
Claim 8
Dependent Claim
18 words
Tablets according to the composition of claim 5, wherein the pharmaceutically active agent comprises one or more vitamins.
Claim 9
Dependent Claim
33 words
A composition according to claim 1, wherein the carrier comprises up to 5% by weight thereof of at least one of colloidal or fumed silica, calcium carbonate and calcium mono-, di- or triphosphate.
Claim 10
Dependent Claim
23 words
A composition according to claim 1 in the form of tablets, wherein the carrier consists of at least 95% by weight of MSM.
Claim 11
Dependent Claim
101 words
A pharmaceutical formulation method for producing a solid pharmaceutical composition in the form of tablets, granules or a free-flowing powder, which comprises the steps of: (a) admixing a pharmaceutically active compound at a temperature from about 80° to about 110° C. at which it is stable, with (i) an amount of molten MSM effective to dissolve the former therein; or (ii) an amount of particulate solid MSM effective to adheringly bond the former thereto; and (b) cooling the resultant mixture to below its softening temperature and, when in Step a) the MSM was molten, reducing the solidified melt to particulate form.
Claim 12
Dependent Claim
101 words
A pharmaceutical formulation method for producing a solid pharmaceutical composition in the form of tablets, granules or a free-flowing powder, which comprises the steps of: (a) admixing a pharmaceutically active compound at a temperature from about 80° to about 110° C. at which it is stable, with (i) an amount of molten MSM effective to dissolve the former therein; or (ii) an amount of particulate solid MSM effective to adheringly bond the former thereto; and (b) cooling the resultant mixture to below its softening temperature and, when in Step a) the MSM was molten, reducing the solidified melt to particulate form.
Claim 13
Dependent Claim
23 words
A method according to claim 10, wherein in Step a) both the MSM and the pharmaceutically active agent are in solid particulate form.
Claim 14
Dependent Claim
27 words
A method according to claim 11, comprising the further step of filling the thus-produced particulate form into capsules or compressing the thus produced particulate form into tablets.
Claim 15
Dependent Claim
14 words
A method according to claim 10, wherein in Step (a), the MSM is molten.
Claim 16
Dependent Claim
17 words
A method according to claim 13, wherein in Step (b) the solidified melt is formed into granules.
Claim 17
Dependent Claim
19 words
A method according to claim 13, wherein in Step (b), the solidified melt is formed into a free-flowing powder.
Claim 18
Dependent Claim
17 words
A method according to claim 14 comprising the further step of compressing the thus-produced granules into tablets.
Claim 19
Dependent Claim
26 words
A method according to claim 15 comprising the further step of filling the thus-produced powder into ingestible capsules or compressing the thus-produced powder into ingestible tablets.
Claim 20
Dependent Claim
32 words
A method according to claim 10, wherein the carrier comprises up to 5% by weight of at least one of colloidal or fumed silica, calcium carbonate and calcium mono-, di- or triphosphate.
Claim 21
Dependent Claim
82 words
In a pharmaceutical formulation method for producing a solid pharmaceutical composition adapted for oral ingestion which comprises the step of forming an intimate physical mixture of at least one pharmaceutically systemically active agent which is storage unstable in the presence of moisture and a pharmaceutically acceptable carrier therefor, into tablets, granules or a free-flowing powder, the improvement wherein the mixture is substantially anhydrous, the carrier consists essentially of methylsulfonylmethane (MSM) and the pharmaceutically active agent is dissolved therein or adheringly bonded thereto.
Claim 22
Dependent Claim
82 words
In a pharmaceutical formulation method for producing a solid pharmaceutical composition adapted for oral ingestion which comprises the step of forming an intimate physical mixture of at least one pharmaceutically systemically active agent which is storage unstable in the presence of moisture and a pharmaceutically acceptable carrier therefor, into tablets, granules or a free-flowing powder, the improvement wherein the mixture is substantially anhydrous, the carrier consists essentially of methylsulfonylmethane (MSM) and the pharmaceutically active agent is dissolved therein or adheringly bonded thereto.
Claim 23
Dependent Claim
18 words
The method according to claim 19 wherein the carrier consists of at least 95% by weight of MSM.
Claim 24
Dependent Claim
13 words
The method according to claim 20 wherein the mixture is formed into granules.
Claim 25
Dependent Claim
15 words
The method according to claim 20 wherein the mixture is formed into a free-flowing powder.
Claim 26
Dependent Claim
13 words
The method according to claim 20 wherein the mixture is formed into granules.
Claim 27
Dependent Claim
21 words
The method according to claim 20 in the form of granules or a free-flowing powder, which is thereafter compressed into tablets.
Claim 28
Dependent Claim
32 words
The method according to claim 19, wherein the carrier comprises up to 5% by weight thereof of at least one colloidal or fumed silica, calcium carbonate and calcium mono-, di- or triphosphate.
Claim 29
Dependent Claim
91 words
In a pharmaceutical formulation method for producing a solid pharmaceutical composition adapted for oral ingestion which comprises the step of forming an intimate physical mixture of at least one pharmaceutically systemically active agent which is storage unstable in the presence of moisture and a pharmaceutically acceptable carrier therefor, into tablets, granules or a free-flowing powder, the improvement wherein the mixture is substantially anhydrous, the pharmaceutically active agent is in solid particulate form and the MSM is mixed therewith by condensing vapors thereof onto a moving bed of the pharmaceutically active agent.
Claim 30
Dependent Claim
91 words
In a pharmaceutical formulation method for producing a solid pharmaceutical composition adapted for oral ingestion which comprises the step of forming an intimate physical mixture of at least one pharmaceutically systemically active agent which is storage unstable in the presence of moisture and a pharmaceutically acceptable carrier therefor, into tablets, granules or a free-flowing powder, the improvement wherein the mixture is substantially anhydrous, the pharmaceutically active agent is in solid particulate form and the MSM is mixed therewith by condensing vapors thereof onto a moving bed of the pharmaceutically active agent.
Claim 31
Dependent Claim
10 words
The method according to claim 26 conducted at reduced pressure.
Claim 32
Dependent Claim
70 words
In a composition adapted for oral ingestion in the form of compressed units or a free-flowing powder and consisting essentially of an intimate physical mixture of at least one dietary component and a pharmaceutically acceptable carrier therefor, the improvement wherein the mixture is substantially anhydrous, the carrier consists essentially of methylsulfonylmethane and the agent is dissolved in the MSM or adheringly bonded to the surface of particles of the MSM.
Claim 33
Dependent Claim
70 words
In a composition adapted for oral ingestion in the form of compressed units or a free-flowing powder and consisting essentially of an intimate physical mixture of at least one dietary component and a pharmaceutically acceptable carrier therefor, the improvement wherein the mixture is substantially anhydrous, the carrier consists essentially of methylsulfonylmethane and the agent is dissolved in the MSM or adheringly bonded to the surface of particles of the MSM.
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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) | 1989-02-03 | 1989-08-05 | 1990-02-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-02-03 | 1993-08-05 | 1994-02-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-02-03 | 1997-08-05 | 1998-02-04 | $7700.00 | Window Closed / Lapsed |