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US4129649A Expired / Lapsed US ⏱️ 0.0 years remaining

Process for producing easily absorbable amorphous steryl glucoside monopalmitates and preparations thereof

Assignee: Nippon Shinyaku Co Ltd
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Filing: 1976-05-05
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Granted: 1978-12-12
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Expires: 1996-05-05
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Abstract

Abstract A process for producing amorphous preparations of steryl glucoside monopalmitates, wherein steryl glucoside monopalmitates are heated at a temperature above 110° C up to about 145° C or the compounds are dissolved in an organic solvent in which they are soluble with a solvent which is then distilled off, and the compounds then pulverized and mixed with physiologically harmless organic or inorganic fine particles in a proportion of 0.5 times (by weight) of the compounds or more, thereby homogeneously dispersing the amorphous compounds in the fine particles or uniformtly adsorbing the compounds on the fine particles, and the resulting preparations which have hemostatic properties and are readily absorbable upon ingestion. The starting steryl glucoside monopalmitates are obtained in crystalline form as from soy beans or other vegetable sources.

Inventors

  • 👤 Sho Inoue
  • 👤 Masanobu Kawamata
  • 👤 Hirokazu Ushimaru
  • 👤 Koichi Nakamichi
  • 👤 Yutaka Takahashi

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-26 17:24
CPC Classifications
C; C07; C07J; C07J17/00; C07J17/005

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 141 words
A process for the production of pharmaceutical composition having hemostatic activity which comprises converting a crystalline steryl glucoside monopalmitate to amorphous form by heating it to a temperature above 110° C. and in the range of 125°-145° C. and for a period of time of about 2-30 minutes to effect such conversion or by dissolving the crystalline steryl glucoside monopalmitate in an organic solvent in which it is soluble and distilling off the solvent, and admixing the thus formed amorphous steryl glucoside monopalmitate with physiologically harmless organic or inorganic fine particles to form a homogeneous dispersion having enhanced absorbability upon ingestion or administration and in which the amorphous steryl glucoside monopalmitate is absorbed on or dispersed in the physiologically harmless organic or inorganic fine particles in the proportion of at least 0.5 parts per part of steryl glucoside monopalmitate, by weight.
Claim 2
Dependent Claim 141 words
A process for the production of pharmaceutical composition having hemostatic activity which comprises converting a crystalline steryl glucoside monopalmitate to amorphous form by heating it to a temperature above 110° C. and in the range of 125°-145° C. and for a period of time of about 2-30 minutes to effect such conversion or by dissolving the crystalline steryl glucoside monopalmitate in an organic solvent in which it is soluble and distilling off the solvent, and admixing the thus formed amorphous steryl glucoside monopalmitate with physiologically harmless organic or inorganic fine particles to form a homogeneous dispersion having enhanced absorbability upon ingestion or administration and in which the amorphous steryl glucoside monopalmitate is absorbed on or dispersed in the physiologically harmless organic or inorganic fine particles in the proportion of at least 0.5 parts per part of steryl glucoside monopalmitate, by weight.
Claim 3
Dependent Claim 27 words
A process according to claim 1 wherein 0.5 to 10 parts of the fine particles are admixed with one part of the steryl glucoside monopalmitate, by weight.
Claim 4
Dependent Claim 43 words
A process according to claim 1 wherein the fine particles are selected from starch, cellulose, lactose, polyvinyl pyrrolidone, methyl cellulose, polyethyleneglycol, acacia, magnesium aluminate silicate, silicic acid anhydride, synthetic aluminum silicate, magnesium alumina hydroxide and aluminum hydroxide gel, individually and in mixtures thereof.
Claim 5
Dependent Claim 59 words
A method according to claim 1 wherein the fine particles are selected from starch, cellulose, lactose, polyvinyl pyrrolidone, methyl cellulose, polyethyleneglycol, acacia, magnesium aluminate silicate, silicic acid anhydride, synthetic aluminum silicate, magnesium alumina hydroxide and aluminum hydroxide gel, individually and in mixtures thereof and the steryl glucoside monopalmitate is selected from a 6-monopalmitate of β-sitosteryl-β-D-glucoside, stigmasteryl-β-D-glucoside, compesteryl-β-D-glucoside, or cholesteryl-β-D-glucoside.
Claim 6
Dependent Claim 59 words
A pharmaceutical composition having hemostatic activity comprising an amorphous steryl glucoside monopalmitate obtained from a crystalline steryl glucoside monopalmitate and adsorbed on or dispersed in physiologically harmless fine organic or inorganic particles, the said composition having enhanced absorbability upon ingestion or administration and the proportion of fine particles to steryl glucoside monopalmitate being from 0.5:1 to 10:1, by weight.
Claim 7
Dependent Claim 59 words
A pharmaceutical composition having hemostatic activity comprising an amorphous steryl glucoside monopalmitate obtained from a crystalline steryl glucoside monopalmitate and adsorbed on or dispersed in physiologically harmless fine organic or inorganic particles, the said composition having enhanced absorbability upon ingestion or administration and the proportion of fine particles to steryl glucoside monopalmitate being from 0.5:1 to 10:1, by weight.
Claim 8
Dependent Claim 21 words
A pharmaceutical composition according to claim 5 wherein the steryl glucoside monopalmitate is a 6-monopalmitate of β-sitosteryl-β-D-glucoside, stigmasteryl-β-D-glucoside, compesteryl-β-D-glucoside, or cholesteryl-β-D-glucoside.
Claim 9
Dependent Claim 44 words
A pharmaceutical composition according to claim 5 wherein the fine particles are selected from starch, cellulose, lactose, polyvinyl pyrrolidone, methyl cellulose, polyethyleneglycol, acacia, magnesium aluminate silicate, silicic acid anhydride, synthetic aluminum silicate, magnesium alumina hydroxide and aluminum hydroxide gel, individually and in mixtures thereof.

References Cited (Backward Citations)

US2746957A Cited
US3036060A Cited
US3238104A Cited
US3753975A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-12-11 1982-06-12 1982-12-12 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-12-11 1986-06-12 1986-12-12 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-12-11 1990-06-12 1990-12-12 $7700.00 Window Closed / Lapsed

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