US4835142A
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US
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Powdery pharmaceutical composition suitable for application to mucosa of oral or nasal cavity
Assignee: Teijin Ltd
•
Filing: 1988-02-04
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Granted: 1989-05-30
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Expires: 2008-02-04
Abstract
Abstract A powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity including: (a) a base selected from the group consisting of lower alkyl ethers of cellulose; (b) a pharmaceutically effective amount of a drug selected from the group consisting of steroid or glycyrrhizic acid type anti-inflammatory agents; and (c) a stabilizer for the drug composed of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 or more carbon atoms, aliphatic polycarboxylic acid, hydroxy aliphatic polycarboxylic acids, aromatic carboxylic acids, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and cellulose derivatives having carboxyl group. This powdery pharmaceutical composition has extremely excellent stability in the steroid or glycyrrhizic acid type anti-inflammatory agent contained therein, low irritation of the mucosa of the oral or nasal cavity, and sustained release of the drug over an extended period of time.
Inventors
- 👤 Yoshiki Suzuki
- 👤 Hiroshi Ikura
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 01:53
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/12; A61K47/30; A61K47/36; A61K47/38; A61K9/00; A61K9/0012; A61K9/0043; A61K9/0053; A61K9/006; A61P; A61P27/00; A61P27/16
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
149 words
A powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity comprising: (a) a base selected from the group consisting of lower alkyl ethers of cellulose; (b) a pharmaceutically effective amount of a drug selected from the group consisting of steroidal anti-inflammatory agents or glycyrrhizic acid anti-inflammatory agents; and (c) a stabilizer for the drug in the form of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hydroxyl aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose, said stabilizer being present in an amount of 0.05% to 5% by weight in the composition.
Claim 2
Dependent Claim
149 words
A powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity comprising: (a) a base selected from the group consisting of lower alkyl ethers of cellulose; (b) a pharmaceutically effective amount of a drug selected from the group consisting of steroidal anti-inflammatory agents or glycyrrhizic acid anti-inflammatory agents; and (c) a stabilizer for the drug in the form of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hydroxyl aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose, said stabilizer being present in an amount of 0.05% to 5% by weight in the composition.
Claim 3
Dependent Claim
31 words
A powdery pharmaceutical composition as claimed in claim 1, wherein at least about 90% by weight of the stabilizer particles has an effective particle diameter of about 75 μm or less.
Claim 4
Dependent Claim
76 words
A powdery pharmaceutical composition for application to the mucosa of the oral cavity as claimed in claim 1, wherein said stabilizer is at least one member selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic dicarboxylic acids having 4 to 6 carbon atoms, hydroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, and carboxymethyl cellulose and carboxymethylethyl cellulose.
Claim 5
Dependent Claim
41 words
A powdery pharmaceutical composition for application to the mucosa of the nasal cavity as claimed in claim 1, wherein said stabilizer is a saturated higher aliphatic monocarboxylic acid having 12 or more carbon atoms or a cellulose derivative having carboxyl groups.
Claim 6
Dependent Claim
27 words
A powdery pharmaceutical composition as claimed in claim 1, wherein said saturated higher aliphatic hydrocarbon monocarboxylic acid is stearic acid, palmitic acid, lauric acid, or myristic acid.
Claim 7
Dependent Claim
23 words
A powdery pharmaceutical composition as claimed in claim 1, wherein said aliphatic hydrocarbon dicarboxylic acid is succinic acid, fumaric acid, or maleic acid.
Claim 8
Dependent Claim
24 words
A powdery pharmaceutical composition as claimed in claim 1, wherein said hydroxy aliphatic hydrocarbon di- or tricarboxylic acid is tartaric acid or citric acid.
Claim 9
Dependent Claim
24 words
A powdery pharmaceutical composition as claimed in claim 1, wherein said benzoic acid and its derivatives is benzoic acid, parahydroxybenzoic acid, or salicylic acid.
Claim 10
Dependent Claim
33 words
A powdery pharmaceutical composition as claimed in claim 1, wherein said steroid type anti-inflammatory agent is beclomethasone dipropionate, betamethasone, betamethasone valerate, triamcinolone, triamcinolone acetonide, dexamethasone, fluocinolone acetonide, fluocinonide, flumethasone, hydrocortisone, prednisolone, or prednisone.
Claim 11
Dependent Claim
31 words
A powdery pharmaceutical composition as claimed in claim 1, wherein the moisture content of the lower alkyl ether of cellulose is within the range of from 3% to 9% by weight.
Claim 12
Dependent Claim
25 words
A powdery pharmaceutical composition as claimed in claim 1, wherein said lower alkyl ether of cellulose is hydroxypropyl cellulose, methyl cellulose, or hydroxypropyl methyl cellulose.
Claim 13
Dependent Claim
35 words
A powdery pharmaceutical composition as claimed in claim 1, wherein at least about 90% by weight of the powder particles of the pharmaceutical composition has an effective particle diameter of about 20 to 250 μm.
Claim 14
Dependent Claim
27 words
A powdery pharmaceutical preparation in unit dosage form for application to the mucosa of the oral or nasal cavity comprising the powdery pharmaceutical composition of claim 1.
Claim 15
Dependent Claim
18 words
A powdery pharmaceutical preparation as claimed in claim 13, wherein said pharmaceutical composition is filled in a capsule.
Claim 16
Dependent Claim
18 words
A powdery pharmaceutical composition as claimed in claim 1, wherein the drug is a glycyrrhizic acid anti-inflammatory agent.
Claim 17
Dependent Claim
29 words
A powdery pharmaceutical composition as claimed in claim 15, wherein said glycyrrhizic acid anti-inflammatory agent is glycyrrhizic acid, disodium glycyrrhizinate, trisodium glycyrrhizinate, monopotassium glycyrrhizinate, dipotassium glycyrrhizinate or monoammonium glycyrrhizinate.
Claim 18
Dependent Claim
26 words
A powdery pharmaceutical composition as claimed in claim 1, wherein said base is present in an amount of 89.374% to 99.925% by weight in the composition.
Claim 19
Independent Claim
158 words
A method for preparing a powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity, comprising the step of mechanically mixing: (a) a base selected from the group consisting of lower alkyl ethers of cellulose; (b) a pharmaceutically effective amount of a drug selected from the group consisting of steroidal anti-inflammatory agents or glycyrrhizic acid anti-inflammatory agents; and (c) a stabilizer for the drug in the form of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hydroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose, said stabilizer being present in an amount of 0.05% to 5% by weight in the composition.
Claim 20
Independent Claim
158 words
A method for preparing a powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity, comprising the step of mechanically mixing: (a) a base selected from the group consisting of lower alkyl ethers of cellulose; (b) a pharmaceutically effective amount of a drug selected from the group consisting of steroidal anti-inflammatory agents or glycyrrhizic acid anti-inflammatory agents; and (c) a stabilizer for the drug in the form of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hydroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose, said stabilizer being present in an amount of 0.05% to 5% by weight in the composition.
Claim 21
Dependent Claim
22 words
A method as claimed in claim 18, wherein the mixed composition is compressed under pressure and, then, the compressed mixture is pulverized.
Claim 22
Independent Claim
162 words
A method for preparing a powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity, comprising the steps of: impregnating the lower alkyl ethers of cellulose with a solution or dispersion, in an organic solvent, of a pharmaceutically effective amount of a drug selected from the group consisting of steroidal anti-inflammatory agents or glycyrrhizic acid anti-inflammatory agents and a stabilizer for the drug in the form of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hydroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose, said stabilizer being present in an amount of 0.05% to 5% by weight in the composition, and drying the impregnated product.
Claim 23
Independent Claim
162 words
A method for preparing a powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity, comprising the steps of: impregnating the lower alkyl ethers of cellulose with a solution or dispersion, in an organic solvent, of a pharmaceutically effective amount of a drug selected from the group consisting of steroidal anti-inflammatory agents or glycyrrhizic acid anti-inflammatory agents and a stabilizer for the drug in the form of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hydroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose, said stabilizer being present in an amount of 0.05% to 5% by weight in the composition, and drying the impregnated product.
Claim 24
Independent Claim
181 words
A method for preparing a powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity comprising the steps of: dissolving or dispersing, in an organic solvent, water, or the mixture thereof (a) the lower alkyl ethers of cellulose, (b) a pharmaceutically effective amount of a drug selected from the group consisting of steroidal anti-inflammatory agents or glycyrrhizic acid anti-inflammatory agents, and (c) a stabilizer for the drug in the form of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hyroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose, said stabilizer being present in an amount of 0.05% to 5% by weight in the composition, evaporating the organic solvent, water, or the mixture thereof from the resultant solution or dispersion; and pulverizing the evaporated product.
Claim 25
Independent Claim
181 words
A method for preparing a powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity comprising the steps of: dissolving or dispersing, in an organic solvent, water, or the mixture thereof (a) the lower alkyl ethers of cellulose, (b) a pharmaceutically effective amount of a drug selected from the group consisting of steroidal anti-inflammatory agents or glycyrrhizic acid anti-inflammatory agents, and (c) a stabilizer for the drug in the form of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hyroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose, said stabilizer being present in an amount of 0.05% to 5% by weight in the composition, evaporating the organic solvent, water, or the mixture thereof from the resultant solution or dispersion; and pulverizing the evaporated product.
Claim 26
Independent Claim
163 words
A method for stabilizing a powdery pharmaceutical composition containing a steroidal anti-inflammatory agent or glycyrrhizic acid anti-inflammatory agent for application to the mucosa of the oral or nasal cavity, comprising incorporating at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hydroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose into a mixture of lower alkyl ethers of cellulose and a pharmaceutically effective amount of a drug selected from the group consisting of said steroidal anti-inflammatory agent or glycyrrhizic acid anti-inflammatory agents, said at least one low irritant solid organic acid being a stabilizer for the drug and being present in an amount of 0.05% to 5% by weight of the composition.
Claim 27
Independent Claim
163 words
A method for stabilizing a powdery pharmaceutical composition containing a steroidal anti-inflammatory agent or glycyrrhizic acid anti-inflammatory agent for application to the mucosa of the oral or nasal cavity, comprising incorporating at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 to 24 carbon atoms, aliphatic hydrocarbon dicarboxylic acids having 4 to 6 carbon atoms, hydroxy aliphatic hydrocarbon di- or tricarboxylic acids having 4 to 8 carbon atoms, benzoic acid and its derivatives, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and carboxymethyl cellulose and carboxymethylethyl cellulose into a mixture of lower alkyl ethers of cellulose and a pharmaceutically effective amount of a drug selected from the group consisting of said steroidal anti-inflammatory agent or glycyrrhizic acid anti-inflammatory agents, said at least one low irritant solid organic acid being a stabilizer for the drug and being present in an amount of 0.05% to 5% by weight of the composition.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-05-29 | 1992-11-28 | 1993-05-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-05-29 | 1996-11-28 | 1997-05-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-05-29 | 2000-11-28 | 2001-05-30 | $7700.00 | Window Closed / Lapsed |