US4720387A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Sustained-release preparation of pinacidil
Assignee: Shionogi and Co Ltd
•
Filing: 1984-06-05
•
Granted: 1988-01-19
•
Expires: 2004-06-05
Abstract
Abstract Highly effective and orally administrable sustained-release preparation of an antihypertensive agent, pinacidil (N"-cyano-N-4-pyridyl-N'-1,2,2-trimethylpropylguanidine) comprising a rapid-release and a slow-release component at a ratio of about 7:3 to about 1:9 by pinacidil weight.
Inventors
- 👤 Teruo Sakamoto
- 👤 Sadao Kawai
- 👤 Kinzaburo Noda
- 👤 Toyohiko Takeda
- 👤 Toshihiro Ogura
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 20:46
CPC Classifications
C; C07; C07D; C07D491/00; C07D491/02; C07D491/04; C07D491/056; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K9/00; A61K9/48; A61K9/50; A61K9/5084
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
71 words
A sustained-release preparation of pinacidil which consists essentially of two different components: one is a rapid-release component dissolving rapidly in the stomach and the other is an enteric coated slow-release component containing hydrophilic additives at 40 to 90 wt% and hydrophobic additives at 30 to 2 wt% based on the slow-release component, wherein the ratio of pinacidil in the respective components is in a range of 4:6 to 1:9 by weight.
Claim 2
Dependent Claim
71 words
A sustained-release preparation of pinacidil which consists essentially of two different components: one is a rapid-release component dissolving rapidly in the stomach and the other is an enteric coated slow-release component containing hydrophilic additives at 40 to 90 wt% and hydrophobic additives at 30 to 2 wt% based on the slow-release component, wherein the ratio of pinacidil in the respective components is in a range of 4:6 to 1:9 by weight.
Claim 3
Dependent Claim
29 words
The sustained-release preparation as claimed in claim 1, wherein the hydrophilic additive is lactose, sucrose, glucose, D-mannitol, sorbitol, inositol, dextrin, xylose, starch, or crystalline cellulose, or the mixture thereof.
Claim 4
Dependent Claim
20 words
The sustained-release preparation as claimed in claim 1, wherein the hydrophobic additive is magnesium stearate, hydrogenated castor oil or both.
Claim 5
Dependent Claim
27 words
The sustained-release preparation as claimed in claim 1, wherein the slow-release component of pinacidil is covered with an enteric coating film soluble at pH 5.0 to 7.0.
Claim 6
Dependent Claim
21 words
The sustained-release preparation as claimed in claim 1, wherein the slow-release component of pinacidil is covered with a water-insoluble coating base.
Claim 7
Dependent Claim
62 words
The sustained-release preparation as claimed in claim 1, wherein the enteric coating film is composed of an ingredient selected from the group consisting of (a) methyl methacrylate methacrylic acid copolymer, (b) carboxymethylethylcellulose, (c) shellac and (d) hydroxypropylmethylcellulose phthalate, (e) cellulose acetate phthalate, (f) polyvinylacetate phthalate, (g) ethyl acrylate methacrylic acid copolymer, (h) vinylacetate crotonic acid copolymer, (i) methacrylate methacrylic acid methylmethacrylate copolymer.
Claim 8
Dependent Claim
29 words
The sustained-release preparation as claimed in claim 1, wherein the rapid-release component of pinacidil is in the form of powder, fine granules, granules, beads, tablets or a portion thereof.
Claim 9
Dependent Claim
25 words
The sustained-release preparation as claimed in claim 1, wherein the slow-release component of pinacidil is in the form of fine granules, granules, beads or tablets.
Claim 10
Dependent Claim
20 words
The sustained-release preparation as claimed in claim 1, which is formulated by covering the slow-release component with the rapid-release component.
Claim 11
Dependent Claim
19 words
The sustained-release preparation as claimed in claim 1, wherein said ratio is in a range of 3:7 to 2:8.
Claim 12
Dependent Claim
15 words
The sustained-release preparation according to claim 1 which is in the form of multi-layer tablets.
Claim 13
Dependent Claim
15 words
The sustained-release preparation according to claim 1 which is in the form of multi-layer granules.
Claim 14
Dependent Claim
15 words
The sustained-release preparation according to claim 1 which is in the form of multi-layer beads.
References Cited (Backward Citations)
US2953497A
Cited
US2996431A
Cited
US3044938A
Cited
US2809917A
Cited
US2951792A
Cited
US3115441A
Cited
US3275519A
Cited
US3634584A
Cited
US3906086A
Cited
US3922338A
Cited
US4057636A
Cited
US4173626A
Cited
US4353887A
Cited
US4409222A
Cited
US4524060A
Cited
US4454108A
Cited
US4600577A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-01-18 | 1991-07-20 | 1992-01-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-01-18 | 1995-07-20 | 1996-01-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-01-18 | 1999-07-20 | 2000-01-19 | $7700.00 | Window Closed / Lapsed |