← Back to Patent Explorer
US4722941A Expired / Lapsed US ⏱️ 0.0 years remaining

Readily absorbable pharmaceutical compositions of per se poorly absorbable pharmacologically active agents and preparation thereof

Assignee: AbbVie Pharmaceuticals GmbH
•
Filing: 1978-05-31
•
Granted: 1988-02-02
•
Expires: 1998-05-31
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

Abstract

Abstract A readily absorbable pharmaceutical composition of pharmacologically active agents, which per se are poorly absorbable, is disclosed which comprises a pharmacologically effective amount of at least one such pharmacologically active agent distributed in a vehicle comprising an absorption-enhancing amount of at least one fatty acid of medium chain length. The preparation is suited for formulating pharmacologically active bases, cardiac glycosides, steroids, antibiotics, sympathicomimetica, tranquilizing agents, or local anaesthetics.

Inventors

  • 👤 Theodor Eckert
  • 👤 Fritz H. Kemper
  • 👤 Martin Wischniewski
  • 👤 Reinhard Hempel

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 23:18
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/12; A61K47/14; A61K9/00; A61K9/48; A61K9/4841; A61K9/4858

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 110 words
A method of enhancing the absorption of an enterally or topically administered pharmacological active agent capable of eliciting a physiological effect in a human or animal subject, said active agent comprising a basic compound selected from the group consisting of antibiotics, antispasmodic agents, agents which are effective in improving coronary disorders, anti-inflammatory agents, sympathicomimetically active agents, tranquilizers and local anaesthetics, which method comprises the step of concurrently administering to the subject an amount of said active agent effective to produce the desired physiological effect and a vehicle comprising an absorption enhancing amount of a free fatty acid of medium chain length containing from about 6 to about 12 carbon atoms.
Claim 2
Independent Claim 110 words
A method of enhancing the absorption of an enterally or topically administered pharmacological active agent capable of eliciting a physiological effect in a human or animal subject, said active agent comprising a basic compound selected from the group consisting of antibiotics, antispasmodic agents, agents which are effective in improving coronary disorders, anti-inflammatory agents, sympathicomimetically active agents, tranquilizers and local anaesthetics, which method comprises the step of concurrently administering to the subject an amount of said active agent effective to produce the desired physiological effect and a vehicle comprising an absorption enhancing amount of a free fatty acid of medium chain length containing from about 6 to about 12 carbon atoms.
Claim 3
Dependent Claim 33 words
The method as defined in claim 1, wherein the per se poorly absorbable pharmacologically active basic agent is selected from the group consisting of valethamatebromide, bencyclane, dipyridamole, indomethacine, synephrine, diazepam, 7-chlor-1-methyl-2-(hydroxymethyl)-5-(2'-chlorophenyl)-1H-2,3-dihydro-1,4-benzodiazepine and procaine.
Claim 4
Dependent Claim 28 words
The method as defined in claim 1, wherein the amount of fatty acids of medium chain length is between about 1 and about 100% weight of the vehicle.
Claim 5
Dependent Claim 30 words
The method as defined in claim 3, wherein the total amount of fatty acids of medium chain length is from about 20 to about 100% by weight of the vehicle.
Claim 6
Dependent Claim 28 words
The method as defined in claim 1, wherein the pharmacologically active basic agent is administered in the form of an acid addition salt with a pharmaceutically acceptable acid.
Claim 7
Dependent Claim 23 words
The method as defined in claim 5, wherein the acid is a fatty acid containing from about 6 to about 18 carbon atoms.
Claim 8
Dependent Claim 23 words
The method as defined in claim 5, wherein the acid is a fatty acid containing from about 6 to about 12 carbon atoms.
Claim 9
Dependent Claim 73 words
The method as defined in claim 1, wherein the amount of the fatty acid of medium chain length in the vehicle is substantialy the amount which is necessary to form an acid addition salt of the pharmacologically active basic agent and wherein the vehicle further comprises at least one glyceride selected from the group of mono- and diglycerides of fatty acids containing from about 6 to about 18 carbon atoms and mixtures thereof.
Claim 10
Dependent Claim 14 words
The method as defined in claim 1, wherein said administering step comprises enteral administration.
Claim 11
Dependent Claim 14 words
The method as defined in claim 1, wherein said administering step comprises topical administration.
Claim 12
Dependent Claim 27 words
The method as defined in claim 1, wherein said vehicle further comprises at least one free fatty acid containing from about 12 to about 18 carbon atoms.
Claim 13
Dependent Claim 29 words
The method as defined in claim 1, wherein said vehicle further comprises at least one glyceride selected from the group consisting of tri-, di-, and monoglycerides or mixtures thereof
Claim 14
Dependent Claim 15 words
The methods as defined in claim 12, wherein the glyceride is a fatty acid glyceride.
Claim 15
Dependent Claim 26 words
The methods as defined in claim 13, wherein the glyceride is selected from the group consisting of mono- and diglycerides of fatty acids and mixtures thereof.
Claim 16
Dependent Claim 23 words
The method as defined in claim 13, wherein the fatty acid within the glyceride comprises from about 6 to about 18 carbon atoms.
Claim 17
Dependent Claim 22 words
The method as defined in claim 13, wherein at least part of the fatty acids within the glycerides are saturated fatty acids.
Claim 18
Dependent Claim 22 words
The method as defined in claim 13, wherein at least part of the fatty acids within the glycerides are unsaturated fatty acids.
Claim 19
Dependent Claim 29 words
The method as defined in claim 13, wherein the fatty acids are selected from the group consisting of capric acid, caprylic acid, palmitic acid, stearic acid, and oleic acid.
Claim 20
Dependent Claim 13 words
The method as defined by claim 1, wherein said active agent comprises diazepam.
Claim 21
Dependent Claim 13 words
The method as defined by claim 1, wherein said active agent comprises 7-chlor-1-methyl-2-(hydroxymethyl)-5-(2'-chlorophenyl)-1H-2,3-dihydro-1,4-benzodiazepine.
Claim 22
Dependent Claim 18 words
The method as defined by claim 1, wherein said active agent comprises an aliphatic or heterocyclic amine group.

References Cited (Backward Citations)

US3772446A Cited
US3551554A Cited
US3767801A Cited
DE2357389A1 Cited
GB1432784A Cited
US4202888A Cited
US4151304A Cited
US4250169A Cited
US4263313A Cited
US4230702A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-02-01 1991-08-03 1992-02-02 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-02-01 1995-08-03 1996-02-02 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-02-01 1999-08-03 2000-02-02 $7700.00 Window Closed / Lapsed

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag