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US4151273A Expired / Lapsed US ⏱️ 0.0 years remaining

Increasing the absorption rate of insoluble drugs

Assignee: University of California, San Diego
•
Filing: 1978-06-13
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Granted: 1979-04-24
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Expires: 1998-06-13
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Abstract

Abstract The absorption in body fluids of poorly soluble drugs is enhanced by forming a glassy solid matrix of a carrier and the drug. A solution of the drug and the carrier is formed at an elevated temperature either with or without a solvent and chilled rapidly to form a solid mass which can be ground to a powder for oral administration in a tablet or capsule.

Inventors

  • 👤 Sidney Riegelman
  • 👤 Win L. Chiou

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 15:11
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/141; A61K9/146; A61K31/00; A61K31/33; A61K31/335; A61K31/34; A61K9/20; A61K9/2095; A61K9/48; A61K9/4841; A61K9/4866

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 103 words
In the art of obtaining an effective concentration of griseofulvin of a single, oral dosage in humans, the improvement of administering to a human subject an effective concentration dosage of griseofulvin which has been prepared by forming a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin, heating the mixture to an elevated temperature sufficient to dissolve the griseofulvin without decomposition in the polyethylene glycol and rapidly cooling instantaneously within 2 to 3 minutes, the griseofulvin-polyethylene glycol mixture to produce a solid solution of griseofulvin in the polyethylene glycol.
Claim 2
Dependent Claim 103 words
In the art of obtaining an effective concentration of griseofulvin of a single, oral dosage in humans, the improvement of administering to a human subject an effective concentration dosage of griseofulvin which has been prepared by forming a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin, heating the mixture to an elevated temperature sufficient to dissolve the griseofulvin without decomposition in the polyethylene glycol and rapidly cooling instantaneously within 2 to 3 minutes, the griseofulvin-polyethylene glycol mixture to produce a solid solution of griseofulvin in the polyethylene glycol.
Claim 3
Dependent Claim 16 words
The method according to claim 1, wherein the solid solution is ground to a fine powder.
Claim 4
Dependent Claim 75 words
In a process for making a solid solution of polyethylene glycol and griseofulvin comprising heating to an elevated temperature without decomposition of the griseofulvin a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin, the step of rapidly cooling instantaneously within 2 to 3 minutes the polyethylene glycolgriseofulvin mixture to produce a solid solution of the griseofulvin in the polyethylene glycol.
Claim 5
Dependent Claim 75 words
In a process for making a solid solution of polyethylene glycol and griseofulvin comprising heating to an elevated temperature without decomposition of the griseofulvin a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin, the step of rapidly cooling instantaneously within 2 to 3 minutes the polyethylene glycolgriseofulvin mixture to produce a solid solution of the griseofulvin in the polyethylene glycol.
Claim 6
Dependent Claim 9 words
The product prepared by the process of claim 3.
Claim 7
Dependent Claim 81 words
A process for making a solid solution of polyethylene glycol and griseofulvin comprising forming a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin, heating the mixture to an elevated temperature sufficient to dissolve the griseofulvin without decomposition in the polyethylene glycol, and rapidly cooling instantaneously within 2 to 3 minutes the polyethylene glycol-griseofulvin mixture to produce a solid solution of the griseofulvin in the polyethylene glycol.
Claim 8
Dependent Claim 81 words
A process for making a solid solution of polyethylene glycol and griseofulvin comprising forming a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin, heating the mixture to an elevated temperature sufficient to dissolve the griseofulvin without decomposition in the polyethylene glycol, and rapidly cooling instantaneously within 2 to 3 minutes the polyethylene glycol-griseofulvin mixture to produce a solid solution of the griseofulvin in the polyethylene glycol.
Claim 9
Dependent Claim 9 words
The product prepared by the process of claim 5.
Claim 10
Dependent Claim 83 words
A process for making a solid solution of polyethylene glycol and griseofulvin comprising adding a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin to a mutual solvent, heating the polyethylene glycol-griseofulvin-solvent mixture to form a solution, removing substantially all of the solvent, and rapidly cooling instantaneously within 2 to 3 minutes, the resultant polyethylene glycol-griseofulvin mixture to produce a solid solution of the griseofulvin in the polyethylene glycol.
Claim 11
Dependent Claim 83 words
A process for making a solid solution of polyethylene glycol and griseofulvin comprising adding a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin to a mutual solvent, heating the polyethylene glycol-griseofulvin-solvent mixture to form a solution, removing substantially all of the solvent, and rapidly cooling instantaneously within 2 to 3 minutes, the resultant polyethylene glycol-griseofulvin mixture to produce a solid solution of the griseofulvin in the polyethylene glycol.
Claim 12
Dependent Claim 9 words
The product prepared by the process of claim 7.
Claim 13
Dependent Claim 103 words
In the art of obtaining an effective concentration of griseofulvin of a single, oral dosage in humans, the improvement of administering to a human subject an effective concentration dosage of griseofulvin which has been prepared by adding a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin to a mutual solvent, heating the polyethylene glycol-griseofulvin-solvent mixture to form a solution, removing substantially all of the solvent, and rapidly cooling instantaneously within 2 to 3 minutes, the griseofulvin-polyethylene glycol mixture to produce a solid solution of griseofulvin in polyethylene glycol.
Claim 14
Dependent Claim 103 words
In the art of obtaining an effective concentration of griseofulvin of a single, oral dosage in humans, the improvement of administering to a human subject an effective concentration dosage of griseofulvin which has been prepared by adding a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin to a mutual solvent, heating the polyethylene glycol-griseofulvin-solvent mixture to form a solution, removing substantially all of the solvent, and rapidly cooling instantaneously within 2 to 3 minutes, the griseofulvin-polyethylene glycol mixture to produce a solid solution of griseofulvin in polyethylene glycol.
Claim 15
Dependent Claim 16 words
The method according to claim 9, wherein the solid solution is ground to a fine powder.
Claim 16
Dependent Claim 93 words
In the art of obtaining an effective concentration of griseofulvin of a single, oral dosage in humans, the improvement of administering to a human subject an effective concentration dosage of griseofulvin which has been prepared by heating to an elevated temperature without decomposition of the griseofulvin, a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin, and rapidly cooling instantaneously within 2 to 3 minutes, the griseofulvin-polyethylene glycol mixture to produce a solid solution of griseofulvin in polyethylene glycol.
Claim 17
Dependent Claim 93 words
In the art of obtaining an effective concentration of griseofulvin of a single, oral dosage in humans, the improvement of administering to a human subject an effective concentration dosage of griseofulvin which has been prepared by heating to an elevated temperature without decomposition of the griseofulvin, a mixture of polyethylene glycol having an average molecular weight of from 1,000 to 20,000 and from about 2% to about 50% of griseofulvin, and rapidly cooling instantaneously within 2 to 3 minutes, the griseofulvin-polyethylene glycol mixture to produce a solid solution of griseofulvin in polyethylene glycol.
Claim 18
Dependent Claim 16 words
The method according to claim 11, wherein the solid solution is ground to a fine powder.

References Cited (Backward Citations)

US2149005A Cited
US2698822A Cited
DE1083985B Cited
US3330727A Cited
US3325362A Cited
US3297804A Cited
US3308217A Cited
US3374146A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1982-04-23 1982-10-23 1983-04-24 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1986-04-23 1986-10-23 1987-04-24 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1990-04-23 1990-10-23 1991-04-24 $7700.00 Window Closed / Lapsed

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