US4869904A
Expired / Lapsed
US
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Sustained release drug preparation
Assignee: NISSHIN FLOUE MILLING Co Ltd 19-12 NIHONBASHI KOAMI-CHO CHUO-KU TOKYO JAPAN
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Filing: 1987-12-02
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Granted: 1989-09-26
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Expires: 2007-12-02
Abstract
Abstract Now is provided a new sustained release drug preparation comprising such an inclusion complex of a medical compound with a hydrophobic cyclodextrin derivative, e.g. ethylated cyclodextrins, which sustains or retards the dissolution and release of the medical compound at a controlled rate from the inclusion complex and hence from the drug preparation containing the inclusion complex, so as to maintain the concentration of the medical compound in blood at an effective level for prolonged time. This drug preparation may further contain a second type of an inclusion complex of the medical compound with a hydrophilic cyclodextrin or hydrophilic cyclodextrin derivative, in mixture with the first type of the inclusion complex of the medical compound with a hydrophobic cyclodextrin derivative, to maintain the controlled release of the medical compound from the drug.
Inventors
- 👤 Kaneto Uekama
- 👤 Yoshiyuki Tahara
- 👤 Takanori Ijitsu
- 👤 Tadashi Yamada
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 15:30
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/16; A61K31/18; B; B82; B82Y; B82Y5/00; A61K47/00; A61K47/50; A61K47/69; A61K47/6949; A61K47/6951
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
46 words
A sustained release drug preparation, which comprises an inclusion complex composed of at least one medical compound complexed with at least one hydrophobic alkylated cyclodextrin, as the active ingredient, said medical compound being capable of complexing with said hydrophobic alkylated cyclodextrin to form said inclusion complex.
Claim 2
Dependent Claim
46 words
A sustained release drug preparation, which comprises an inclusion complex composed of at least one medical compound complexed with at least one hydrophobic alkylated cyclodextrin, as the active ingredient, said medical compound being capable of complexing with said hydrophobic alkylated cyclodextrin to form said inclusion complex.
Claim 3
Dependent Claim
136 words
A sustained release pharmaceutical composition in the form of compressed tablets or granules, which comprises (1) a inclusion complex of diltiazem or its acid addition salt, isosorbide or its acid addition salt or dicardipin or its acid addition salt with a hydrophobic alkylated cyclodextrin at a molar ratio of the medical compound to the cyclodextrin derivative of 1:1 to 1:10, plus (ii) an inclusion complex of a medical compound with a hydrophilic cyclodextrin or a hydrophilic cyclodextrin derivative, said medical compound being capable of complexing with a hydrophilic cyclodextrin or a hydrophilic cyclodextrin derivative, at a molar ratio of 1:1 to 1:10, as the active ingredient, and which is in the form of a physical mixture of the inclusion complex (i) with the inclusion complex (ii) at a mixing ratio of 1:2 to 1:0.1 by weight.
Claim 4
Dependent Claim
136 words
A sustained release pharmaceutical composition in the form of compressed tablets or granules, which comprises (1) a inclusion complex of diltiazem or its acid addition salt, isosorbide or its acid addition salt or dicardipin or its acid addition salt with a hydrophobic alkylated cyclodextrin at a molar ratio of the medical compound to the cyclodextrin derivative of 1:1 to 1:10, plus (ii) an inclusion complex of a medical compound with a hydrophilic cyclodextrin or a hydrophilic cyclodextrin derivative, said medical compound being capable of complexing with a hydrophilic cyclodextrin or a hydrophilic cyclodextrin derivative, at a molar ratio of 1:1 to 1:10, as the active ingredient, and which is in the form of a physical mixture of the inclusion complex (i) with the inclusion complex (ii) at a mixing ratio of 1:2 to 1:0.1 by weight.
Claim 5
Dependent Claim
19 words
The sustained release drug preparation as claimed in claim 1, wherein the hydrophobic alkylated cyclodextrin is an ethylated cyclodextrin.
Claim 6
Dependent Claim
23 words
The sustained release drug preparation as claimed in claim 3, wherein the ethylated cyclodextrin is heptakis(2,3-di-O-ethyl)-β-cyclodextrin, heptakis(2,6-di-O-ethyl)-.beta.-cyclodextrin or heptakis (2,3,6-tri-O-ethyl)-β-cyclodextrin, or mixtures thereof.
Claim 7
Dependent Claim
21 words
The sustained release drug preparation as claimed in claim 1 wherein comprises further a pharmaceutically acceptable carrier for said inclusion complex.
Claim 8
Dependent Claim
20 words
The sustained release drug preparation as claimed in claim 1, wherein the hydrophobic alkylated cyclodextin is a mixed methylated/ethylated cyclodextrin.
Claim 9
Dependent Claim
31 words
The sustained release drug preparation as claimed in claim 1, further comprising an inclusion complex composed of a medical compound complexed with a hydrophilic naural cyclodextrin or a hydrophilic cyclodextrin derivative.
Claim 10
Dependent Claim
89 words
A sustained release drug preparation, which comprises (i) an inclusion complex of a medical compound with a hydrophobic alkylated cyclodextrin, said medical compound being capable of complexing with said hydrophobic alkylated cyclodextrin and (ii) an inclusion complex of a medical compound with a hydrophilic cyclodextrin or a hydrophilic cyclodextrin, said medical compound being capable of complexing with said hydrophilic cyclodextrin or hydrophilic cyclodextrin derivative, as a mixture of the complex (i) with the complex (ii) at a mixing ratio of 1:2 to 1:0.1 by weight, as the active ingredient.
Claim 11
Dependent Claim
89 words
A sustained release drug preparation, which comprises (i) an inclusion complex of a medical compound with a hydrophobic alkylated cyclodextrin, said medical compound being capable of complexing with said hydrophobic alkylated cyclodextrin and (ii) an inclusion complex of a medical compound with a hydrophilic cyclodextrin or a hydrophilic cyclodextrin, said medical compound being capable of complexing with said hydrophilic cyclodextrin or hydrophilic cyclodextrin derivative, as a mixture of the complex (i) with the complex (ii) at a mixing ratio of 1:2 to 1:0.1 by weight, as the active ingredient.
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) | 1992-09-25 | 1993-03-27 | 1993-09-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-09-25 | 1997-03-27 | 1997-09-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-09-25 | 2001-03-27 | 2001-09-26 | $7700.00 | Window Closed / Lapsed |