Patent US4383992A successfully refreshed from Google Patents.
US4383992A
Expired / Lapsed
US
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Water-soluble steroid compounds
Assignee: Individual
•
Filing: 1982-02-08
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Granted: 1983-05-17
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Expires: 2002-02-08
Abstract
Abstract Beta-cyclodextrin forms a water-soluble complex or inclusion compound with steroid compounds having a molecular structure smaller than the interior cavity in the doughnut-shaped molecular structure of beta-cyclodextrin. The resulting inclusion compounds can be used for a variety of applications including aqueous topical ophthalmic preparations and topical dermatological ointments.
Inventors
- 👤 John M. Lipari
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 14:48
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/50; A61K47/69; A61K47/6949; A61K47/6951; A61K31/00; A61K31/56; A61K31/565; A61K31/57; B; B82; B82Y; B82Y5/00; C; C08; C08B; C08B37/00; C08B37/0006; C08B37/0009; C08B37/0012; C08B37/0015
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
27 words
A water-soluble inclusion compound formed by complexing beta-cyclodextrin with a steroid compound having a molecular structure smaller than the inside dimension of the internal cavity of beta-cyclodextrin.
Claim 2
Dependent Claim
27 words
A water-soluble inclusion compound formed by complexing beta-cyclodextrin with a steroid compound having a molecular structure smaller than the inside dimension of the internal cavity of beta-cyclodextrin.
Claim 3
Dependent Claim
193 words
A water-soluble inclusion compound according to claim 1 wherein said steroid has the following general chemical structure: ##STR7## wherein R 1 is H, ═O, OH, OCH 3 OR 11 , or bridged with R 2 ##STR8## R 2 is H, CHOR 11 or bridged with R 1 as noted above; R 3 is H or CH 3 ; R 4 is H, CH 3 , F, Cl, or Br; R 5 is H, F, Cl, or Br; R 6 is H, ═O, or OR 11 R 7 is H, CH 3 or C 2 H 5 ; R 8 is OH, ═O, C.tbd.CH, R 11 , --OR 11 or ##STR9## R 9 is H, OH, CH 3 , C 2 H 5 , C.tbd.CH, OR 11 or bridged with R 10 as ##STR10## R 10 is H, CH 3 , or OR 11 ; R 11 is H, or ##STR11## R 12 is ##STR12## x is O or a positive integer of 1-10; y is O or a positive integer of at least 1; z is a positive integer of 1-3; and the dotted lines indicate the alternate positions of the double bond.
Claim 4
Dependent Claim
18 words
A water-soluble inclusion compound according to claim 2 wherein said steroid compound is dexamethasone, prednisolone acetate or hydrocortisone.
Claim 5
Dependent Claim
45 words
An anti-inflammatory pharmaceutical preparation comprising an effective amount of one or more inclusion compounds formed by complexing beta-cyclodextrin and an anti-inflammatory steroid compound having a molecular structure smaller than the inside dimension of the internal cavity of beta-cyclodextrin and mixed with a non-toxic pharmaceutical carrier.
Claim 6
Dependent Claim
45 words
An anti-inflammatory pharmaceutical preparation comprising an effective amount of one or more inclusion compounds formed by complexing beta-cyclodextrin and an anti-inflammatory steroid compound having a molecular structure smaller than the inside dimension of the internal cavity of beta-cyclodextrin and mixed with a non-toxic pharmaceutical carrier.
Claim 7
Dependent Claim
21 words
An anti-inflammatory preparation according to claim 4 wherein said steroid compound has the general chemical structure set forth in claim 1.
Claim 8
Dependent Claim
41 words
An anti-inflammatory preparation according to claim 4 wherein said preparation is adapted to treat ocular inflammation, said carrier is an aqueous medium, said inclusion compound is dissolved in an aqueous medium and said steroid compound is dexamethasone, prednisolone acetate or hydrocortisone.
Claim 9
Dependent Claim
26 words
An anti-inflammatory preparation according to claim 6 wherein the concentration of said steroid compound is within the range of about 0.1 to about 1.0 volume %.
Claim 10
Independent Claim
41 words
A method for preparing a water-soluble inclusion compound of a steroid compound comprising the steps of admixing in an aqueous medium beta-cyclodextrin and a steroid compound having a molecular structure smaller than the inside dimension of the internal cavity of beta-cyclodextrin.
Claim 11
Independent Claim
41 words
A method for preparing a water-soluble inclusion compound of a steroid compound comprising the steps of admixing in an aqueous medium beta-cyclodextrin and a steroid compound having a molecular structure smaller than the inside dimension of the internal cavity of beta-cyclodextrin.
Claim 12
Dependent Claim
21 words
A method according to claim 8 wherein the molar ratio of said steroid compound to beta-cyclodextrin is about 1:1 or less.
Claim 13
Dependent Claim
20 words
A method according to claim 9 wherein said steroid compound has the general chemical structure set forth in claim 1.
References Cited (Backward Citations)
US3079410A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-05-16 | 1986-11-15 | 1987-05-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-05-16 | 1990-11-15 | 1991-05-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-05-16 | 1994-11-15 | 1995-05-17 | $7700.00 | Window Closed / Lapsed |