Patent US4428883A successfully refreshed from Google Patents.
US4428883A
Expired / Lapsed
US
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Novel method of administering β-blockers and novel dosage forms containing same
Assignee: KENTUCKY LEXINGTON KY, University of, Trustees of
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Filing: 1981-03-06
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Granted: 1984-01-31
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Expires: 2001-03-06
Abstract
Abstract The invention provides a novel method of administering selected known adrenergic β-receptor blocking agents, such as dichloroisoproterenol, pronethalol, sotalol and alprenolol, which are of use in the treatment of angina pectoris, arrhythmias, hypertension and other cardiac conditions, and migraine. The invention further provides novel dosage forms of those β-blockers which are adapted for nasal administration and which include solutions, suspensions, gels and ointments.
Inventors
- 👤 Anwar A. Hussain
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 23:56
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0043
Claims Analysis
Total Claims: 66
Claim 1
Independent Claim
59 words
A method for eliciting a systemic therapeutic β-adrenergic blocking response in a warm-blooded animal, which comprises nasally administering to said animal a systemically therapeutically effective β-adrenergic blocking amount of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxolol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, or a nontoxic pharmaceutically acceptable salt thereof.
Claim 2
Independent Claim
59 words
A method for eliciting a systemic therapeutic β-adrenergic blocking response in a warm-blooded animal, which comprises nasally administering to said animal a systemically therapeutically effective β-adrenergic blocking amount of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxolol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, or a nontoxic pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
54 words
A method as defined by claim 1 for eliciting a systemic therapeutic β-adrenergic blocking response in a warm-blooded animal, which comprises nasally administering to said animal a systemically therapeutically effective β-adrenergic blocking amount of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, alprenolol, metoprolol, nadoxolol, timolol or bupranolol, or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
76 words
A method as defined by claim 1 for eliciting a systemic therapeutic β-adrenergic blocking response in a warm-blooded animal, which comprises nasally administering to said animal a systemically therapeutically effective β-adrenergic blocking amount of a long-chain carboxylic acid salt of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxolol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, the carboxylic acid portion of said salt containing 10 to 20 carbon atoms.
Claim 5
Independent Claim
32 words
A method for eliciting a systemic therapeutic β-adrenergic response in a warm-blooded animal which comprises nasally administering to said animal, a systemically therapeutically effective β-adrenergic blocking amount of a composition as defined.
Claim 6
Independent Claim
32 words
A method for eliciting a systemic therapeutic β-adrenergic response in a warm-blooded animal which comprises nasally administering to said animal, a systemically therapeutically effective β-adrenergic blocking amount of a composition as defined.
Claim 7
Dependent Claim
16 words
A method as defined by claim 1, wherein said warm-blooded animal is afflicted with angina pectoris.
Claim 8
Dependent Claim
15 words
A method as defined by claim 1, wherein said warm-blooded animal is afflicted with arrhythmias.
Claim 9
Dependent Claim
15 words
A method as defined by claim 1, wherein said warm-blooded animal is afflicted with hypertension.
Claim 10
Dependent Claim
15 words
A method as defined by claim 1, wherein said warm-blooded animal is afflicted with migraine.
Claim 11
Dependent Claim
109 words
A pharmaceutically acceptable, sustained release nasal composition, in dosage unit form, for nasal administration to obtain a systemic therapeutic β-adrenergic blocking response in a warm-blooded animal, consisting essentially of, per nasal dosage unit, (i) a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, the carboxylic acid portion of said salt containing 10 to 20 carbon atoms, and (ii) a nontoxic pharmaceutically acceptable nasal carrier therefor, said composition being in the form of a nasal ointment or a nasal gel.
Claim 12
Dependent Claim
109 words
A pharmaceutically acceptable, sustained release nasal composition, in dosage unit form, for nasal administration to obtain a systemic therapeutic β-adrenergic blocking response in a warm-blooded animal, consisting essentially of, per nasal dosage unit, (i) a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, the carboxylic acid portion of said salt containing 10 to 20 carbon atoms, and (ii) a nontoxic pharmaceutically acceptable nasal carrier therefor, said composition being in the form of a nasal ointment or a nasal gel.
Claim 13
Dependent Claim
13 words
The composition as defined by claim 9, wherein said salt is a stearate.
Claim 14
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of dichloroisoproterenol.
Claim 15
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of pronethalol.
Claim 16
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of sotalol.
Claim 17
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of oxprenolol.
Claim 18
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of pindolol.
Claim 19
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of metoprolol.
Claim 20
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of nadoxolol.
Claim 21
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of practolol.
Claim 22
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of butoxamine.
Claim 23
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of alprenolol.
Claim 24
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of metalol.
Claim 25
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of nifenalol.
Claim 26
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of acebutolol.
Claim 27
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of atenolol.
Claim 28
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of bunolol.
Claim 29
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of carteolol.
Claim 30
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of labetalol.
Claim 31
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of pamatolol.
Claim 32
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of timolol.
Claim 33
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of tiprenolol.
Claim 34
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of xipranolol.
Claim 35
Dependent Claim
27 words
The composition as defined by claim 9, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of a long chain carboxylic acid salt of bupranolol.
Claim 36
Dependent Claim
17 words
The composition as defined by claim 9, said composition being in the form of a nasal ointment.
Claim 37
Dependent Claim
17 words
The composition as defined by claim 9, said composition being in the form of a nasal gel.
Claim 38
Dependent Claim
102 words
A pharmaceutically acceptable nasal composition, in dosage unit form, for nasal administration to obtain a systemic therapeutic β-adrenergic blocking response in a warm-blooded animal, consisting essentially of, per nasal dosage unit, (i) a systemically therapeutically effective unit β-adrenergic blocking amount of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxolol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, or a nontoxic pharmaceutically acceptable salt thereof, and (ii) a nontoxic pharmaceutically acceptable nasal carrier therefor, said composition being in the form of a nasal ointment or a nasal gel adapted for sustained release to the nasal mucosa.
Claim 39
Dependent Claim
102 words
A pharmaceutically acceptable nasal composition, in dosage unit form, for nasal administration to obtain a systemic therapeutic β-adrenergic blocking response in a warm-blooded animal, consisting essentially of, per nasal dosage unit, (i) a systemically therapeutically effective unit β-adrenergic blocking amount of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxolol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, or a nontoxic pharmaceutically acceptable salt thereof, and (ii) a nontoxic pharmaceutically acceptable nasal carrier therefor, said composition being in the form of a nasal ointment or a nasal gel adapted for sustained release to the nasal mucosa.
Claim 40
Dependent Claim
17 words
The composition as defined by claim 35, said composition being in the form of a nasal ointment.
Claim 41
Dependent Claim
17 words
The composition as defined by claim 35, said composition being in the form of a nasal gel.
Claim 42
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of dichloroisoproterenol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 43
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of pronethalol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 44
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of sotalol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 45
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of oxprenolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 46
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of pindolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 47
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of metoprolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 48
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of nadoxolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 49
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of practolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 50
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of butoxamine or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 51
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of alprenolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 52
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of metalol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 53
Dependent Claim
28 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of nifenalol or nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 54
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of acebutolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 55
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of atenolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 56
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of bunolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 57
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of carteolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 58
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of labetalol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 59
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of pamatolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 60
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of timolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 61
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of tiprenolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 62
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of xipranolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 63
Dependent Claim
29 words
The composition as defined by claim 35, wherein (i) is a systemically therapeutically effective unit β-adrenergic blocking amount of bupranolol or a nontoxic pharmaceutically acceptable acid addition salt thereof.
Claim 64
Dependent Claim
43 words
A long chain carboxylic acid salt of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxolol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, the carboxylic acid portion of said salt containing 10 to 20 carbon atoms.
Claim 65
Dependent Claim
43 words
A long chain carboxylic acid salt of dichloroisoproterenol, pronethalol, sotalol, oxprenolol, pindolol, metoprolol, nadoxolol, practolol, butoxamine, alprenolol, metalol, nifenalol, acebutolol, atenolol, bunolol, carteolol, labetalol, pamatolol, timolol, tiprenolol, xipranolol or bupranolol, the carboxylic acid portion of said salt containing 10 to 20 carbon atoms.
Claim 66
Dependent Claim
12 words
A salt as defined by claim 60, said salt being a stearate.
References Cited (Backward Citations)
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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) | 1987-01-30 | 1987-08-01 | 1988-01-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-01-30 | 1991-08-01 | 1992-01-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-01-30 | 1995-08-01 | 1996-01-31 | $7700.00 | Window Closed / Lapsed |