US4701320A
Expired / Lapsed
US
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Composition stably containing minocycline for treating periodontal diseases
Assignee: Sunstar Inc
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Filing: 1985-11-26
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Granted: 1987-10-20
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Expires: 2005-11-26
Abstract
Abstract A pharmaceutical composition stably containing minocycline for treating periodontal diseases which comprises minocycline or a pharmaceutically acceptable salt thereof and a base composed of a polyhydric alcohol containing a magnesium compound. Optionally, the base can further contain a water soluble high molecular weight compound, ethyl methacrylate/chlrortrimethylammnoniumethyl methacrylate copolymer and its solubilizer. A method for treating periodontal diseases comprising topically applying the composition to the oral cavity is also disclosed.
Inventors
- 👤 Kenji Hasegawa
- 👤 Koichi Nakashima
- 👤 Tohru Eguchi
- 👤 Masako Ota
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 07:09
CPC Classifications
A; A61; A61Q; A61Q11/00; A61K; A61K31/00; A61K31/65; A61K47/00; A61K47/02; A61K47/06; A61K47/08; A61K47/10; A61K8/00; A61K8/18; A61K8/30; A61K8/40; A61K8/42; A61K9/00; A61K9/0012; A61K9/0053; A61K9/0063
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
80 words
A pharmaceutical composition in the form of non-aqueous paste stably containing minocycline for topical application to treat periodontal diseases which comprises: (a) 0.1 to 15% by weight of minocycline or a pharmaceutically acceptable salt thereof, and (b) a base comprising an alkane-diol or an alkane-triol having 2 to 6 carbon atoms, and 0.5 to 10% by weight of a magnesium compound selected from the group consisting of magnesium chloride, magnesium acetate, magnesium sulfate, magnesium carbonate, magnesium gluconate and hydrates thereof.
Claim 2
Dependent Claim
80 words
A pharmaceutical composition in the form of non-aqueous paste stably containing minocycline for topical application to treat periodontal diseases which comprises: (a) 0.1 to 15% by weight of minocycline or a pharmaceutically acceptable salt thereof, and (b) a base comprising an alkane-diol or an alkane-triol having 2 to 6 carbon atoms, and 0.5 to 10% by weight of a magnesium compound selected from the group consisting of magnesium chloride, magnesium acetate, magnesium sulfate, magnesium carbonate, magnesium gluconate and hydrates thereof.
Claim 3
Dependent Claim
123 words
A pharmaceutical composition according to claim 1, wherein the base (b) further includes 0.2 to 10% by weight of a water soluble high molecular weight compound selected from the group consisting of polyvinyl pyrrolidone, polyvinyl alcohol, carrageenan, locust bean gum, guar gum, hydroxyethyl cellulose, xanthan gum, tragacanth gum, starches and succinoglucan; 0.5 to 10% by weight of ethyl methacrylate/chlorotrimethylammoniumethyl methacrylate copolymer; and 5 to 25% by weight of a solubilizer selected from the group consisting of esters of an alkane-diol or alkane-triol having 2 to 4 carbon atoms and of a lower fatty acid having 2 to 4 carbon atoms and esters of a lower alcohol having 2 to 4 carbon atoms and of a dicarboxylic acid having 4 to 10 carbon atoms.
Claim 4
Dependent Claim
48 words
A pharmaceutical composition according to claim 2, wherein minocycline or a pharmaceutically acceptable salt thereof is incorporated into a mixture of the alkane-diol or alkane-triol having 2 to 6 carbon atoms, the magnesium compound, the water soluble high molecular weight compound, ethyl methacrylate/chlorotrimethylammoniumethyl methacrylate copolymer and a solubilizer.
Claim 5
Dependent Claim
57 words
A pharmaceutical composition according to claim 3, wherein the composition comprises a mixture of minocycline or a pharmaceutically acceptable salt and a base composed of the alkane-diol or alkane-triol having 2 to 6 carbon atoms, the magnesium compound and the water soluble high molecular weight compound, and a solution of ethyl methacrylate/chlorotrimethylammoniumethyl methacrylate copolymer in the solubilizer.
Claim 6
Dependent Claim
17 words
A pharmaceutical composition according to claim 1, wherein the magnesium compound is magnesium chloride or its hydrate.
Claim 7
Dependent Claim
36 words
A pharmaceutical composition according to claim 1, wherein the alkane-diol or alkane-triol is a member selected from the group consisting of glycerin, ethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, hexylene glycol, 1,5-pentanediol and 1,3-butylene glycol.
Claim 8
Dependent Claim
12 words
A pharmaceutical composition according to claim 6, wherein the alkane-triol is glycerin.
Claim 9
Dependent Claim
18 words
A pharmaceutical composition according to claim 2, wherein the water soluble high molecular weight compound is hydroxyethyl cellulose.
Claim 10
Dependent Claim
35 words
A pharmaceutical composition according to claim 2, wherein the solubilizer is a member selected from the group consisting of triacetin, tributyrin, ethylene glycol diacetate, diethyl sebacate, diethyl phthalate, dibutyl phthalate, diisopropyl adipate and dibutyl succinate.
Claim 11
Dependent Claim
12 words
A pharmaceutical composition according to claim 9, wherein the solubilizer is triacetin.
Claim 12
Dependent Claim
25 words
A pharmaceutical composition according to claim 2, wherein the weight ratio of the methacrylate copolymer: the solubilizer is in the range of 1:2 to 1:25.
Claim 13
Dependent Claim
32 words
A pharmaceutical composition according to claim 2, wherein the composition contains 0.2 to 3% by weight of the water soluble high molecular weight compound based on the weight of the polyhydric alcohol.
Claim 14
Dependent Claim
20 words
A pharmaceutical composition according to claim 1, wherein minocycline is incorporated into the base composed of glycerin containing magnesium chloride.
Claim 15
Dependent Claim
48 words
A pharmaceutical composition according to claim 13, wherein 0.1 to 5% by weight of minocycline based on the total weight of the composition is incorporated into the base composed of glycerin containing 1 to 5% by weight of magnesium chloride based on the total weight of the composition.
Claim 16
Dependent Claim
42 words
A pharmaceutical composition according to claim 2, wherein the composition comprises: ______________________________________
Minocycline hydrochloride
0.1-5.0 wt %
Hydroxyethyl cellulose 0.2-10.0 wt %
Magnesium chloride 0.5-10.0 wt %
Triacetin 5.0-25.0 wt %
Ethyl methacrylate/chlorotrimethyl-
0.5-10.0 wt %
ammoniumethyl methacrylate copolymer
Glycerin remainder.
______________________________________
Claim 17
Independent Claim
97 words
A method for topical application of minocycline for treating periodontal diseases which comprises topically applying a pharmaceutical composition in the form of non-aqueous paste stably containing an effective dose of minocycline in the oral cavity, said composition comprising: (a) 0.1 to 15% by weight of minocycline or a pharmaceutically acceptable salt thereof, and (b) a base comprising an alkane-diol or an alkane-triol having 2 to 6 carbon atoms, and 0.5 to 10% by weight of a magnesium compound selected from the group consisting of magnesium chloride, magnesium acetate, magnesium sulfate, magnesium carbonate, magnesium gluconate and hydrates thereof.
Claim 18
Independent Claim
97 words
A method for topical application of minocycline for treating periodontal diseases which comprises topically applying a pharmaceutical composition in the form of non-aqueous paste stably containing an effective dose of minocycline in the oral cavity, said composition comprising: (a) 0.1 to 15% by weight of minocycline or a pharmaceutically acceptable salt thereof, and (b) a base comprising an alkane-diol or an alkane-triol having 2 to 6 carbon atoms, and 0.5 to 10% by weight of a magnesium compound selected from the group consisting of magnesium chloride, magnesium acetate, magnesium sulfate, magnesium carbonate, magnesium gluconate and hydrates thereof.
Claim 19
Dependent Claim
119 words
A method according to claim 16, wherein the base (b) further includes 0.2 to 10% by weight of a water soluble high molecular weight compound selected from the group consisting of polyvinyl pyrrolidone, polyvinyl alcohol, carrageenan, locust bean gum, guar gum, hydroxyethyl cellulose, xanthan gum, traganth gum, starches and succinoglucan; 0.5 to 10% by weight of ethyl methacrylate/chlorotrimethylammoniumethyl methacrylate copolymer; and 5 to 25% by weight of a solubilizer selected from the group consisting of esters of an alkane-diol or alkane-triol having 2 to 4 carbon atoms and of a lower fatty acid having 2 to 4 carbon atoms and esters of lower alcohol having 2 to 4 carbon atoms and dicarboxylic acid having 4 to 10 carbon atoms.
Claim 20
Dependent Claim
47 words
A method according to claim 17, wherein minocycline or a pharmaceutically acceptable salt thereof is incorporated into a mixture of the alkane-diol or alkane-triol having 2 to 6 carbon atoms, the magnesium compound, the water soluble high molecular weight compound, ethyl methacrylate/chlorotrimethylammoniumethyl methacrylate copolymer and the solubilizer.
Claim 21
Dependent Claim
57 words
A method according to claim 17, wherein the composition comprises a mixture of minocycline or a pharmaceutically acceptable salt thereof and a base composed of the alkane-diol or alkane-triol having 2 to 6 carbon atoms, the magnesium compound and the water soluble high molecular weight compound, and a solution of ethyl methacrylate/chlorotrimethylammoniumethyl methacrylate copolymer in the solubilizer.
Claim 22
Dependent Claim
15 words
A method according to claim 16, wherein the composition is applied to a periodontal pocket.
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Cited
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Cited
EP0049422A2
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1990-10-19 | 1991-04-20 | 1991-10-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-10-19 | 1995-04-20 | 1995-10-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-10-19 | 1999-04-20 | 1999-10-20 | $7700.00 | Window Closed / Lapsed |