US4189469A
Expired / Lapsed
US
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Pharmaceutical compositions
Assignee: Hoechst AG
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Filing: 1976-05-06
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Granted: 1980-02-19
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Expires: 1996-05-06
Abstract
Abstract A pharmaceutical composition for oral administration in dosage unit form which comprises at least one xanthine derivative selected from the group consisting of (a) (ω-1(-hydroxyalkyl-dialkylxanthines wherein the (ω-1)-hydroxyalkyl group contains 5 or 6 carbon atoms and is in the 1- or 7-position, the alkyl group in the other of the 1- and 7-position contains from 1 to 12 carbon atoms and the alkyl group in the 3-position contains from 1 to 4 carbon atoms, (b) (ω-1)-oxoalkyl-dimethylxanthines wherein the (ω-1)-oxoalkyl group contains 5 or 6 carbon atoms and is in the 1- or 7-position, (c) dimethylxanthine derivatives having an additional alkyl group containing from 4 to 12 carbon atoms in the 1- or 7-position, and (d) dimethylxanthine derivatives having an additional benzyl group in the 1- or 7-position and a saliva forming agent, each dosage unit containing at least 300 mg of xanthine derivative, and the weight ratio of xanthine derivative to saliva forming agent being in the range from 1:2 to 10:1 and a method for the preparation of said composition.
Inventors
- 👤 Klaus Gleixner
- 👤 Roland Muller
- 👤 Franz Lehrach
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 04:58
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; A61K31/52; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2027; A61K9/205; A61K9/2054
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
53 words
An orally-administrable pharmaceutical composition in unit-dosage form which comprises an amount of pharmaceutically-active component having a degree of gastro-intestinal-tract incompatibility which renders it unsafe for oral administration in combination with a sufficient amount of swelling agent to reduce such incompatibility to a level at which the unit dosage is safe for oral administration.
Claim 2
Dependent Claim
53 words
An orally-administrable pharmaceutical composition in unit-dosage form which comprises an amount of pharmaceutically-active component having a degree of gastro-intestinal-tract incompatibility which renders it unsafe for oral administration in combination with a sufficient amount of swelling agent to reduce such incompatibility to a level at which the unit dosage is safe for oral administration.
Claim 3
Dependent Claim
166 words
A pharmaceutical composition as claimed in claim 1 for oral administration in dosage unit form which comprises at least one xanthine derivative selected from the group consisting of (a) (107 -1)-hydroxyalkyl-dialkylxanthine wherein the (ω-1)-hydroxyalkyl group contains 5 to 6 carbon atoms and is in the 1- or 7-position, the alkyl group in the other of the 1- and 7-positions contains from 1 to 12 carbon atoms, and the alkyl group in the 3-position contains from 1 to 4 carbon atoms, (b) (ω-1)-oxoalkyl-dimethylxanthine wherein the (ω-1)-oxoalkyl group contains 5 to 6 carbon atoms and is in the 1- or 7-position, (c) dimethylxanthine derivative having an additional alkyl group containing from 4 to 12 carbon atoms in the 1- or 7-position, and (d) dimethylxanthine derivative having an additional benzyl group in the 1- or 7-position and a swelling agent, each dosage unit containing at least 300 mg of xanthine derivative, and the weight ratio of xanthine derivative to swelling agent being in the range from 1:2 to 10:1.
Claim 4
Dependent Claim
13 words
A composition as claimed in claim 2 wherein the xanthine derivative is water-soluble.
Claim 5
Dependent Claim
19 words
A composition as claimed in claim 2 wherein each dosage unit contains at least 400 mg of xanthine derivative.
Claim 6
Dependent Claim
19 words
A composition as claimed in claim 2 wherein each dosage unit contains up to 1200 mg of an (ω-1)-oxoalkyl-dimethylxanthine.
Claim 7
Dependent Claim
15 words
A composition as claimed in claim 2 wherein the xanthine derivative comprises 1-(5-oxohexyl)-3,7-dimethylxanthine or 7-(5-oxohexyl)-1,3-dimethylxanthine.
Claim 8
Dependent Claim
33 words
A composition as claimed in claim 2 wherein the swelling agent is a member selected from the group consisting of guar powder, galacto-mannane, an alginate, an acrylic acid powder and a cellulose derivative.
Claim 9
Dependent Claim
27 words
A composition as claimed in claim 2 which additionally contains a further excipient selected from the group consisting of polyvinyl pyrrolidone, polyvinyl acetate, talcum and magnesium stearate.
Claim 10
Dependent Claim
10 words
A composition as claimed in claim 2 in tablet form.
Claim 11
Dependent Claim
19 words
A pharmaceutical composition as claimed in claim 2 wherein the xanthine derivative is in admixture with the swelling agent.
Claim 12
Dependent Claim
13 words
A composition as claimed in claim 2 wherein the xanthine derivative is 1-(5-hydroxyhexyl)-3,7-dimethylxanthine.
Claim 13
Dependent Claim
13 words
A composition as claimed in claim 2 wherein the xanthine derivative is 7-(5-hydroxyhexyl)-1,3-dimethylxanthine.
Claim 14
Dependent Claim
25 words
A pharmaceutical composition as claimed in claim 2, which is safe for oral administration in dosage unit form and wherein the xanthine derivative is (a).
Claim 15
Dependent Claim
25 words
A pharmaceutical composition as claimed in claim 2, which is safe for oral administration in dosage unit form and wherein the xanthine derivative is (b).
Claim 16
Dependent Claim
25 words
A pharmaceutical composition as claimed in claim 2, which is safe for oral administration in dosage unit form and wherein the xanthine derivative is (c).
Claim 17
Dependent Claim
25 words
A pharmaceutical composition as claimed in claim 2, which is safe for oral administration in dosage unit form and wherein the xanthine derivative is (d).
Claim 18
Dependent Claim
61 words
In a method for preparing a pharmaceutical composition in oral dosage form with a pharmaceutically-active component having a degree of gastro-intestinal-tract incompatibility which renders in unsafe for oral administration, the improvement which comprises admixing the pharmaceutically-active component with a sufficient amount of swelling agent to reduce such incompatibility to a level at which the pharmaceutical composition is safe for oral administration.
Claim 19
Dependent Claim
61 words
In a method for preparing a pharmaceutical composition in oral dosage form with a pharmaceutically-active component having a degree of gastro-intestinal-tract incompatibility which renders in unsafe for oral administration, the improvement which comprises admixing the pharmaceutically-active component with a sufficient amount of swelling agent to reduce such incompatibility to a level at which the pharmaceutical composition is safe for oral administration.
Claim 20
Dependent Claim
79 words
In a method for preparing a pharmaceutical composition in oral unit-dosage form with a pharmaceutically-active component having a degree of gastro-intestinal-tract incompatibility which renders it unsafe for oral administration in excess of a particular unit dosage, the improvement which comprises admixing a higher unit dosage of the pharmaceutically-active component with a sufficient amount of swelling agent to reduce such incompatibility to a level at which the oral unit-dosage form with the higher unit dosage is safe for oral administration.
Claim 21
Dependent Claim
79 words
In a method for preparing a pharmaceutical composition in oral unit-dosage form with a pharmaceutically-active component having a degree of gastro-intestinal-tract incompatibility which renders it unsafe for oral administration in excess of a particular unit dosage, the improvement which comprises admixing a higher unit dosage of the pharmaceutically-active component with a sufficient amount of swelling agent to reduce such incompatibility to a level at which the oral unit-dosage form with the higher unit dosage is safe for oral administration.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-02-18 | 1983-08-20 | 1984-02-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-02-18 | 1987-08-20 | 1988-02-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-02-18 | 1991-08-20 | 1992-02-19 | $7700.00 | Window Closed / Lapsed |