US4727064A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical preparations containing cyclodextrin derivatives
Assignee: United States Department of Health and Human Services
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Filing: 1985-05-29
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Granted: 1988-02-23
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Expires: 2005-05-29
Abstract
Abstract The invention comprises pharmaceutical preparations consisting generally of a drug with a substantially low water solubility and an amorphous, water-soluble cyclodextrin-based mixtures. In these preparations a stable amorphous state can be achieved. This improves the dissolution properties of the drug and hence its absorption by the body. The required cyclodextrin-based mixtures were prepared from alpha -, beta -, or gamma -cyclodextrin which were rendered amorphous through non-selective alkylation. The alkylation agents suitable for that purposes are exemplified by propylene oxide, glycidol, iodoacetamide, chloroacetate, or 2-diethylaminoethylchloride; their reactions with cyclodextrins were performed in a manner to yield mixtures containing many components, a circumstance which effectively prevents crystallization processes within the above pharmaceutical preparation.
Inventors
- 👤 Josef Pitha
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 22:37
CPC Classifications
B; B82; B82Y; B82Y5/00; A; A61; A61K; A61K47/00; A61K47/50; A61K47/69; A61K47/6949; A61K47/6951; A61K31/00; A61K31/56; A61K31/565; A61K31/57; C; C08; C08B; C08B37/00; C08B37/0006; C08B37/0009; C08B37/0012
Claims Analysis
Total Claims: 31
Claim 1
Independent Claim
63 words
A method of producing a stablizing amorphous complex of a drug and a mixture of cyclodextrins which comprises the steps of: 1. Dissolving an intrinsically amorphous mixture of cyclodextrin deratives which are water soluble and capable of forming inclusion complexes with drugs in water; and 2. Solublizing lipophilic drugs into the aqueous media to form a solution and form a solublized drug/cyclodextrin complex.
Claim 2
Independent Claim
63 words
A method of producing a stablizing amorphous complex of a drug and a mixture of cyclodextrins which comprises the steps of: 1. Dissolving an intrinsically amorphous mixture of cyclodextrin deratives which are water soluble and capable of forming inclusion complexes with drugs in water; and 2. Solublizing lipophilic drugs into the aqueous media to form a solution and form a solublized drug/cyclodextrin complex.
Claim 3
Dependent Claim
24 words
A method of claim 1 wherein the solubilized complex is subjected to freeze-dried or evaporation to provide a solid cyclodextrin/drug complex in powder form.
Claim 4
Dependent Claim
24 words
A method of claim 1 wherein cyclodextrins used are substituted by at least one of the following substituents: hydroalkyl, carboxamide, diethylaminoethyl, carboxymethyl, and carboxyamidomethyl.
Claim 5
Dependent Claim
11 words
A method of claim 1 wherein the drug is a hormone.
Claim 6
Dependent Claim
15 words
A method of claim 4 wherein the drug is testosterone, an estrogen, or a progesterone.
Claim 7
Dependent Claim
14 words
A composition of matter which contains an amorphous complex of cylodextrin and a drug.
Claim 8
Dependent Claim
14 words
A composition of matter which contains an amorphous complex of cylodextrin and a drug.
Claim 9
Dependent Claim
13 words
A omposition of matter of claim 6 wherein the drug is a hormone.
Claim 10
Dependent Claim
19 words
A composition of claim 6 wherein the drug is at least one of testosterone, progesterone, and an estrogenic drug.
Claim 11
Dependent Claim
10 words
A composition of matter of claim 6 in solid form.
Claim 12
Dependent Claim
11 words
A composition of matter of claim 9 which is a tablet.
Claim 13
Dependent Claim
15 words
A composition of matter of claim 6 which is in a liquid or semi-liquid form.
Claim 14
Dependent Claim
22 words
A composition of matter for use in the process of claim 1 containing a mixture of substituted cyclodextrin derivatives in amorphous form.
Claim 15
Dependent Claim
13 words
A composition of matter of claim 6 wherein the drug is a vitamin.
Claim 16
Dependent Claim
16 words
A composition of matter of claim 6 wherein the drug is a salt of retinoic acid.
Claim 17
Dependent Claim
13 words
A composition of matter of claim 6 wherein the drug is a steroid.
Claim 18
Dependent Claim
13 words
A composition of matter of claim 6 wherein the drug is a spironolactone.
Claim 19
Dependent Claim
14 words
A composition of matter of claim 6 wherein the drug is an antiviral agent.
Claim 20
Dependent Claim
13 words
A composition of matter of claim 17 wherein the antiviral agent is acylovir.
Claim 21
Dependent Claim
13 words
A composition of matter of claim 6 wherein the drug is a diuretic.
Claim 22
Dependent Claim
12 words
A composition of matter of claim 19 wherein the diuretic is chlorthalidone.
Claim 23
Dependent Claim
13 words
A composition of matter of claim 6 wherein the drug is an anticoagulant.
Claim 24
Dependent Claim
12 words
A composition of matter of claim 21 wherein the anticoagulant is dicumerol.
Claim 25
Dependent Claim
13 words
A composition of matter of claim 6 wherein the drug is an anticonvulsant
Claim 26
Dependent Claim
12 words
A composition of matter of claim 23 wherein the drug is diphenylhydantoin.
Claim 27
Dependent Claim
14 words
A composition of matter of claim 6 wherein the drug is an antiinflammatory agent.
Claim 28
Dependent Claim
13 words
A composition of matter of claim 25 wherein the antiinflammatory agent is iproniazid.
Claim 29
Dependent Claim
12 words
A composition of matter of claim 16 wherein the drug is oxyprenolol.
Claim 30
Dependent Claim
32 words
A composition of matter in solid or semi-solid form comprising at least one of testosterone, progesterone, and estradiol as an inclusion complex with poly-β-cylodextin and/or hydroxypropyl-β-cyclodextrin adapted for administration by buccal route.
Claim 31
Dependent Claim
32 words
A composition of matter in solid or semi-solid form comprising at least one of testosterone, progesterone, and estradiol as an inclusion complex with poly-β-cylodextin and/or hydroxypropyl-β-cyclodextrin adapted for administration by buccal route.
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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) | 1991-02-22 | 1991-08-24 | 1992-02-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-02-22 | 1995-08-24 | 1996-02-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-02-22 | 1999-08-24 | 2000-02-23 | $7700.00 | Window Closed / Lapsed |