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US4335097A Expired / Lapsed US ⏱️ 0.0 years remaining

Stabilized, prostaglandin-containing tablets with controlled rate of solubility, for local use and process for the preparation thereof

Assignee: Chinoin Private Co Ltd
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Filing: 1981-01-15
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Granted: 1982-06-15
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Expires: 2001-01-15
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Abstract

Abstract The invention relates to stabilized, prostaglandin-containing tablets with controlled rate of solubility, for local use and a process for the preparation thereof. The tablets according to the invention comprise 0.2 to 20% by weight of one or more natural or synthetic prostaglandins, 0.4 to 40% by weight of a non-toxic buffer, which adjusts the pH of the liquid film formed on the surface of the solid phase due to air humidity, to 3 to 5, 1 to 50% by weight of stearic acid, 0 to 15% by weight of an alkali earth metal stearate, 10 to 95% by weight of lactose and/or mannite, 0 to 15% by weight of a further granulation aid, 1 to 30% by weight of a disintegrating agent and optionally 0.5 to 10% by weight of a flavoring and aroma substance and are prepared under a pressure of 500 to 2000 kp./cm 2 . (49.03 to 196.13 MPa).

Inventors

  • 👤 Agoston David
  • 👤 Tibor Horvath
  • 👤 Csaba Kiss
  • 👤 Gabor Nagy
  • 👤 Kalman Simon
  • 👤 Ilona Simonidesz nee Vermes
  • 👤 Agnes Udvardi
  • 👤 Sandor Virag

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 09:27
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0034; A61K31/00; A61K31/557; A61K9/0053; A61K9/006; A61K9/20; A61K9/2004

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 130 words
A stablized, prostaglandin-containing tablet with controlled rate of solubility, for local use, comprising 0.2 to 20% by weight of at least one natural or synthetic prostaglandin, 0.4 to 40% by weight of a non-toxic buffer for adjusting the pH of the liquid film formed on the surface of the solid phase due to air humidity to 3 to 5, 1 to 50% by weight of stearic acid, 0 to 15% by weight of an alkali earth metal stearate, 10 to 95% by weight of lactose and/or mannite, 0 to 15% by weight of a further granulation aid, 1 to 30% by weight of a disintegrating agent and optionally 0.5 to 10% by weight of a flavoring and aromatizing substance, tabletted under a pressure of 500 to 2000 kp/cm 2 .
Claim 2
Dependent Claim 130 words
A stablized, prostaglandin-containing tablet with controlled rate of solubility, for local use, comprising 0.2 to 20% by weight of at least one natural or synthetic prostaglandin, 0.4 to 40% by weight of a non-toxic buffer for adjusting the pH of the liquid film formed on the surface of the solid phase due to air humidity to 3 to 5, 1 to 50% by weight of stearic acid, 0 to 15% by weight of an alkali earth metal stearate, 10 to 95% by weight of lactose and/or mannite, 0 to 15% by weight of a further granulation aid, 1 to 30% by weight of a disintegrating agent and optionally 0.5 to 10% by weight of a flavoring and aromatizing substance, tabletted under a pressure of 500 to 2000 kp/cm 2 .
Claim 3
Dependent Claim 29 words
A process for loosening the cervical os and/or inducing labor or abortion, which comprises placing tablets as defined in claim 1 into the cervical canal or administering them sublingually.
Claim 4
Dependent Claim 140 words
A process for the preparation of stabilized, prostaglandin-containing tablets with controlled rate of solubility, for local use, which comprises granulating 0.2 to 20% by weight of at least one natural or synthetic prostaglandin, 0.4 to 40% by weight of a non-toxic buffer, which adjusts the pH of the liquid film formed on the surface of the solid phase due to air humidity, to 3 to 5, 1 to 50% by weight of stearic acid, 0 to 15% by weight of an alkali metal stearate, 10 to 95% by weight of lactose and/or mannite, 0 to 15% by weight of a further granulation aid, 1 to 30% by weight of a disintegrating agent and optionally 0.5 to 10% by weight of a flavouring and aroma substance, and tabletting the granulate obtained under a pressure of 500 to 2000 kp./cm 2 .
Claim 5
Dependent Claim 140 words
A process for the preparation of stabilized, prostaglandin-containing tablets with controlled rate of solubility, for local use, which comprises granulating 0.2 to 20% by weight of at least one natural or synthetic prostaglandin, 0.4 to 40% by weight of a non-toxic buffer, which adjusts the pH of the liquid film formed on the surface of the solid phase due to air humidity, to 3 to 5, 1 to 50% by weight of stearic acid, 0 to 15% by weight of an alkali metal stearate, 10 to 95% by weight of lactose and/or mannite, 0 to 15% by weight of a further granulation aid, 1 to 30% by weight of a disintegrating agent and optionally 0.5 to 10% by weight of a flavouring and aroma substance, and tabletting the granulate obtained under a pressure of 500 to 2000 kp./cm 2 .
Claim 6
Dependent Claim 16 words
A process as claimed in claim 3, which comprises using PGF 2 α as the prostaglandin.
Claim 7
Dependent Claim 17 words
A process as claimed in claim 3, which comprises using 15-methyl-prostaglandin F 2 α as the prostaglandin.
Claim 8
Dependent Claim 19 words
A process as defined in claim 3, which comprises using an alkali metal citrate/citric acid system as said buffer.
Claim 9
Dependent Claim 20 words
A process as defined in claim 3 which comprises using a dialkali metal hydrogen phosphate/tartaric acid system as said buffer.
Claim 10
Dependent Claim 17 words
A process as defined in claim 3 which comprises using magnesium or calcium stearate in the granulate.
Claim 11
Dependent Claim 26 words
A process as defined in claim 3 which comprises using an aroma β-cyclodextrin inclusion complex and saccharin as an aromatizing and flavoring substance in said granulate.

References Cited (Backward Citations)

US3937801A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1985-06-14 1985-12-14 1986-06-15 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1989-06-14 1989-12-14 1990-06-15 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1993-06-14 1993-12-14 1994-06-15 $7700.00 Window Closed / Lapsed

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