Solid pharmaceutical compositions comprising MSM and their production
First Claim
1. 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.
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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.
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Citations
28 Claims
- 1. 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.
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10. 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:
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(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. - View Dependent Claims (11, 12, 13, 14, 15, 16, 17, 18)
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- 19. 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.
- 26. 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.
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28. 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.
Specification