US4002718A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Gelatin-encapsulated digoxin solutions and method of preparing the same
Assignee: Arnar-Stone Labs Inc
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Filing: 1974-10-16
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Granted: 1977-01-11
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Expires: 1994-10-16
Abstract
Abstract Digoxin solutions are disclosed which are compatible with gelatin and which are of relatively high concentration, thereby permitting encapsulation of therapeutic amounts of digoxin in soft gelatin capsules of moderate size. The digoxin is first micronized and then dissolved in a vehicle consisting predominately of polyethylene glycol having a molecular weight no greater than about one thousand and having a melting temperature no greater than about 35° C., to provide a digoxin concentration of at least one-half milligram per milliliter and preferably one milligram per milliliter. Solutions composed of various solvent blends are disclosed, including solutions which are highly viscous (semi-solid) at room temperature.
Inventors
- 👤 Libero A. Gardella
- 👤 Helen Kesler
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 04:17
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/4841; A61K9/4858; A61K31/00; A61K31/70; A61K31/7042; A61K31/7048
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
105 words
A method for preparing digoxin in encapsulated therapeutic dosage form, comprising the steps of reducing the size of digoxin particles to an average size no larger than about 10 microns, then mixing the micronized particles of digoxin with a solvent essentially alcohol-free and consisting predominantly of polyethylene glycol of a molecular weight no greater than about 1000, and heating the mixture at a temperature below the decomposition temperature of the drug until at least 0.5 milligrams of digoxin is dissolved in each milliliter of solvent, and then encapsulating therapeutic doses of the dissolved digoxin in gelatin capsules soluble in water but insoluble in said solvent.
Claim 2
Independent Claim
105 words
A method for preparing digoxin in encapsulated therapeutic dosage form, comprising the steps of reducing the size of digoxin particles to an average size no larger than about 10 microns, then mixing the micronized particles of digoxin with a solvent essentially alcohol-free and consisting predominantly of polyethylene glycol of a molecular weight no greater than about 1000, and heating the mixture at a temperature below the decomposition temperature of the drug until at least 0.5 milligrams of digoxin is dissolved in each milliliter of solvent, and then encapsulating therapeutic doses of the dissolved digoxin in gelatin capsules soluble in water but insoluble in said solvent.
Claim 3
Dependent Claim
21 words
The method of claim 1 in which substantially none of said particles following said size-reducing step exceeds 75 microns in size.
Claim 4
Dependent Claim
27 words
The method of claim 1 in which said solvent consists of at least 80% by weight of polyethylene glycol having a molecular weight no greater than 1000.
Claim 5
Dependent Claim
24 words
The method of claim 3 in which said solvent also includes a minor proportion of polyethylene glycol having a molecular weight greater than 1000.
Claim 6
Dependent Claim
14 words
The method of claim 4 in which said solvent is semisolid at room temperature.
Claim 7
Dependent Claim
16 words
The method of claim 3 in which said solvent also contains a minor proportion of glycerin.
Claim 8
Dependent Claim
17 words
The method of claim 3 in which said solvent also contains a minor proportion of propylene glycol.
Claim 9
Dependent Claim
16 words
The method of claim 3 in which said solvent also contains a minor proportion of polyvinylpyrrolidone.
Claim 10
Dependent Claim
15 words
The method of claim 1 in which the material of said capsules is soft gelatin.
Claim 11
Dependent Claim
26 words
The method of claim 1 in which said digoxin is encapsulated in each of said capsules at a therapeutic dosage level of 0.125 to 0.5 milligrams.
Claim 12
Dependent Claim
28 words
The method of claim 1 in which said step of dissolving is continued until at least 1 milligram of digoxin is dissolved in each milliliter of said solvent.
Claim 13
Dependent Claim
18 words
The method of claim 1 in which said solvent has a melting temperature no greater than 35° C.
Claim 14
Dependent Claim
24 words
A digoxin preparation prepared 2 accordance with the method of claim 1, in which said digoxin concentration exceeds 0.5 milligrams per milliliter of solvent.
Claim 15
Dependent Claim
18 words
The preparation of claim 13 in which said solvent has a melting temperature no greater than 35° C.
Claim 16
Dependent Claim
26 words
The preparation of claim 14 in which said solvent comprises at least 80% by weight of polyethylene glycol having a molecular weight no greater than 1000.
Claim 17
Dependent Claim
31 words
The preparation of claim 15 in which said solvent also includes a minor proportion of polyethylene glycol having a molecular weight greater than 1000, said solvent being semi-solid at room temperature.
Claim 18
Dependent Claim
16 words
The preparation of claim 15 in which said solvent also contains a minor proportion of glycerin.
Claim 19
Dependent Claim
17 words
The preparation of claim 15 in which said solvent also contains a minor proportion of propylene glycol.
Claim 20
Dependent Claim
16 words
The preparation of claim 15 in which said solvent also contains a minor proportion of polyvinylpyrrolidone.
Claim 21
Dependent Claim
19 words
The preparation of claim 13 in which said digoxin concentration is at least 1 milligram per milliliter of solvent.
Claim 22
Dependent Claim
17 words
The preparation of claim 13 in which said therapeutic dose of digoxin is 0.125 to 0.5 milligrams.
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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) | 1980-01-11 | 1980-07-12 | 1981-01-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-01-11 | 1984-07-12 | 1985-01-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-01-11 | 1988-07-12 | 1989-01-11 | $7700.00 | Window Closed / Lapsed |