US4637930A
Expired / Lapsed
US
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Transdermal formulation of nicardipine hydrochloride
Assignee: Astellas Pharma Inc
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Filing: 1985-01-31
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Granted: 1987-01-20
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Expires: 2005-01-31
Abstract
Abstract A formulation is provided for the transdermal administration of nicardipine hydrochloride. The formulation is comprised of nicardipine hydrochloride dissolved or suspended in a mixed liquid composed of an urea and at least one compound selected from the group consisting of propylene glycol, a monohydric alcohol having 2 to 4 carbon atoms, lactic acid, thioglycol, a middle chain fatty acid glyceride and a sorbitan middle chain fatty acid ester compounded with a transdermal formulation base.
Inventors
- 👤 Yutaka Konno
- 👤 Hiroitsu Kawata
- 👤 Masayoshi Aruga
- 👤 Takashi Sonobe
- 👤 Mitsuo Mitomi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 04:02
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7084; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/12; A61K47/14; A61K47/16; A61K47/18; A61K47/20; A61K47/26; A61K9/0012; A61K9/0014
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
150 words
A transdermal formulation containing 1 to 20 weight percent of a nicardipine hydrochloride and wherein said nicardipine hydrochloride is dissolved or suspended in a mixed liquid comprised of, based on the weight of said formulation: (1) 0.3 to 30 weight percent of a urea, and (2) at least one member selected from the group consisting of (a) 0.5 to 15 weight percent of propylene glycol, (b) 0.3 to 30 weight percent of thioglycol, (c) 0.3 to 30 weight percent of a monohydric alcohol having from 2 to 4 carbon atoms, (d) 0.3 to 10 weight percent of lactic acid, (e) 0.5 to 20 weight percent of mono- or di-esters of glycerol and fatty acids having 6 to 12 carbon atoms, and (f) 0.5 to 20 weight percent of mono- or di-esters of sorbitol and fatty acids having 6 to 12 carbon atoms, and said formulation containing a pharmaceutically acceptable carrier.
Claim 2
Dependent Claim
150 words
A transdermal formulation containing 1 to 20 weight percent of a nicardipine hydrochloride and wherein said nicardipine hydrochloride is dissolved or suspended in a mixed liquid comprised of, based on the weight of said formulation: (1) 0.3 to 30 weight percent of a urea, and (2) at least one member selected from the group consisting of (a) 0.5 to 15 weight percent of propylene glycol, (b) 0.3 to 30 weight percent of thioglycol, (c) 0.3 to 30 weight percent of a monohydric alcohol having from 2 to 4 carbon atoms, (d) 0.3 to 10 weight percent of lactic acid, (e) 0.5 to 20 weight percent of mono- or di-esters of glycerol and fatty acids having 6 to 12 carbon atoms, and (f) 0.5 to 20 weight percent of mono- or di-esters of sorbitol and fatty acids having 6 to 12 carbon atoms, and said formulation containing a pharmaceutically acceptable carrier.
Claim 3
Dependent Claim
20 words
The transdermal formulation as claimed in claim 1, wherein the monohydric alcohol having 2 to 4 carbon atoms is ethanol.
Claim 4
Dependent Claim
13 words
The transdermal formulation as claimed in claim 1, wherein the urea is urea.
Claim 5
Dependent Claim
16 words
The transdermal formulation of claim 1 wherein said carrier is an oily base for an ointment.
Claim 6
Dependent Claim
18 words
The transdermal formulation of claim 1 wherein said carrier is an adhesive base for a tape or patch.
Claim 7
Dependent Claim
22 words
A process for the transdermal administration of nicardipine hydrochloride which comprises contacting the epidermal tissue with the transdermal formulation of claim 1.
Claim 8
Dependent Claim
14 words
The process of claim 6 wherein the transdermal formulation is contained on a tape.
Claim 9
Dependent Claim
14 words
The process of claim 6 wherein the transdermal formulation is contained on a patch.
Claim 10
Dependent Claim
163 words
A transdermal formulation containing 1 to 20 weight percent of a nicardipine hydrochloride and 0.5 to 10 weight percent of a crystallizing inhibitor for nicardipine hydrochloride, said nicardipine hydrochloride and inhibitor being dissolved or suspended in a mixed liquid comprised of, based on the weight of said formulation: (1) 0.3 to 30 weight percent of a urea, and (2) at least one member selected from the group consisting of (a) 0.5 to 15 weight percent of propylene glycol, (b) 0.3 to 30 weight percent of thioglycol, (c) 0.3 to 30 weight percent of a monohydric alcohol having from 2 to 4 carbon atoms, (d) 0.3 to 10 weight percent of lactic acid, (e) 0.5 to 20 weight percent of mono- or di-esters of glycerol and fatty acids having 6 to 12 carbon atoms, and (f) 0.5 to 20 weight percent of mono- or di-esters of sorbitol and fatty acids having 6 to 12 carbon atoms, and said formulation containing a pharmaceutically acceptable carrier.
Claim 11
Dependent Claim
163 words
A transdermal formulation containing 1 to 20 weight percent of a nicardipine hydrochloride and 0.5 to 10 weight percent of a crystallizing inhibitor for nicardipine hydrochloride, said nicardipine hydrochloride and inhibitor being dissolved or suspended in a mixed liquid comprised of, based on the weight of said formulation: (1) 0.3 to 30 weight percent of a urea, and (2) at least one member selected from the group consisting of (a) 0.5 to 15 weight percent of propylene glycol, (b) 0.3 to 30 weight percent of thioglycol, (c) 0.3 to 30 weight percent of a monohydric alcohol having from 2 to 4 carbon atoms, (d) 0.3 to 10 weight percent of lactic acid, (e) 0.5 to 20 weight percent of mono- or di-esters of glycerol and fatty acids having 6 to 12 carbon atoms, and (f) 0.5 to 20 weight percent of mono- or di-esters of sorbitol and fatty acids having 6 to 12 carbon atoms, and said formulation containing a pharmaceutically acceptable carrier.
Claim 12
Dependent Claim
38 words
The transdermal formulation as claimed in claim 9, wherein the crystallizing inhibitor of nicardipine hydrochloride is at least one compound selected from the group consisting of propylene glycol didecanoate, neopentyl glycol di-2-ethylhexanoate, and a polyoxyethylene-hardened caster oil derivative.
Claim 13
Dependent Claim
16 words
The transdermal formulation of claim 9 wherein said carrier is an oily base for an ointment.
Claim 14
Dependent Claim
18 words
The transdermal formulation of claim 9 wherein said carrier is an adhesive base for a tape or patch.
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) | 1990-01-19 | 1990-07-21 | 1991-01-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-01-19 | 1994-07-21 | 1995-01-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-01-19 | 1998-07-21 | 1999-01-20 | $7700.00 | Window Closed / Lapsed |