US5368852A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Prolonged-release liquid type of pharmaceutical preparation comprising drug-resin complex and benzoate preservative
Assignee: Rohto Pharmaceutical Co Ltd
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Filing: 1993-03-31
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Granted: 1994-11-29
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Expires: 2013-03-31
Abstract
Abstract The present invention provides a prolonged-release liquid type of pharmaceutical preparation prepared by coating a pharmaceutically active drug-ion exchange resin complex which was treated previously with an impregnating agent, with a water permeable diffusion barrier material, followed by suspending the coated complex in a solution containing preservatives. The formulation of the present invention does not develop the rupture of the diffusion barrier film even in a solution containing preservatives. Therefore the formulation of the present invention is a prolonged-release liquid type of pharmaceutical preparation which is stable and does not lose the controlled release of the active ingredient.
Inventors
- 👤 Mitsuo Umemoto
- 👤 Kiyotsugu Higashi
- 👤 Youko Mitani
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 09:09
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0087; A61K9/0095; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/585; A61K9/14; A61K9/16; A61K9/1605; A61K9/1617; A61K9/1629; A61K9/1641; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5036; A61K9/5042; A61K9/5047; A61P; A61P11/00; A61P11/14; A61K9/0012; A61K9/0048
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
250 words
A prolonged-release liquid type of pharmaceutical preparation comprising: (a) 0.1-45.0 w/v % of diffusion barrier-coated complex particles, which are prepared by adsorbing a pharmacologically active drug onto ion exchange resin particles to form drug-resin complex particles, treating the drug-resin complex particles with an impregnating agent to form treated complex particles, and then coating the treated complex particles with ethylcellulose, wherein said ethylcellulose has an ethoxyl group content of 44.0-47.5%; (b) a preservative selected from the group consisting, (i) one of para-hydroxybenzoic acid esters, wherein if methyl para-hydroxybenzoate is chosen, the preparation contains it at a concentration of 0.05-0.75 w/v %; if ethyl para-hydroxybenzoate is chosen, the preparation contains it at a concentration of 0.05-0.075 w/v %; if propyl para-hydroxybenzoate is chosen, the preparation contains it at a concentration of 0.03-0.05 w/v %; and if butyl para-hydroxybenzoate is chosen, the preparation contains it at a concentration of 0.01-0.015 w/v %; (ii) a mixture of two or more of para-hydroxybenzoic acid esters, wherein if a mixture of methyl para-hydroxybenzoate and propyl para-hydroxybenzoate is chosen, the preparation contains the former at a concentration of 0.05-0.10 w/v % and the latter at a concentration of 0.01-0.02 w/v %, respectively; and (iii) sodium benzoate at a concentration of 0.1-0.5 w/v %; and the percent dissolution of the drug from the drug-resin complex changes minimally upon storage at 25° C. for a long period of time, (c) a solvent, wherein said preparation can be stably stored for a long time without loss of its controlled-release property.
Claim 2
Dependent Claim
250 words
A prolonged-release liquid type of pharmaceutical preparation comprising: (a) 0.1-45.0 w/v % of diffusion barrier-coated complex particles, which are prepared by adsorbing a pharmacologically active drug onto ion exchange resin particles to form drug-resin complex particles, treating the drug-resin complex particles with an impregnating agent to form treated complex particles, and then coating the treated complex particles with ethylcellulose, wherein said ethylcellulose has an ethoxyl group content of 44.0-47.5%; (b) a preservative selected from the group consisting, (i) one of para-hydroxybenzoic acid esters, wherein if methyl para-hydroxybenzoate is chosen, the preparation contains it at a concentration of 0.05-0.75 w/v %; if ethyl para-hydroxybenzoate is chosen, the preparation contains it at a concentration of 0.05-0.075 w/v %; if propyl para-hydroxybenzoate is chosen, the preparation contains it at a concentration of 0.03-0.05 w/v %; and if butyl para-hydroxybenzoate is chosen, the preparation contains it at a concentration of 0.01-0.015 w/v %; (ii) a mixture of two or more of para-hydroxybenzoic acid esters, wherein if a mixture of methyl para-hydroxybenzoate and propyl para-hydroxybenzoate is chosen, the preparation contains the former at a concentration of 0.05-0.10 w/v % and the latter at a concentration of 0.01-0.02 w/v %, respectively; and (iii) sodium benzoate at a concentration of 0.1-0.5 w/v %; and the percent dissolution of the drug from the drug-resin complex changes minimally upon storage at 25° C. for a long period of time, (c) a solvent, wherein said preparation can be stably stored for a long time without loss of its controlled-release property.
Claim 3
Dependent Claim
26 words
The pharmaceutical preparation according to claim 1 wherein the pharmacologically active drug is selected from the group consisting of codeine, dihydrocodeine, dextromethorphan, phenylpropanolamine, methylephedrine, and hydrocodone.
Claim 4
Dependent Claim
23 words
The pharmaceutical preparation according to claim 1 wherein the ion exchange resin particles are a gel type divinylbenzene sulfonic acid cation exchange resin.
Claim 5
Dependent Claim
14 words
The pharmaceutical preparation according to claim 1 wherein the impregnating agent is polyethylene glycol.
Claim 6
Dependent Claim
17 words
The pharmaceutical preparation according to claim 1 wherein the ethoxyl group content of ethylcellulose is within 45.0-46.5%.
Claim 7
Dependent Claim
27 words
The pharmaceutical preparation according to claim 1 wherein 5.0-30.0 parts by weight of ethylcellulose is coated relative to 100 parts by weight of the impregnated complex particles.
Claim 8
Dependent Claim
13 words
The pharmaceutical preparation according to claim 1 wherein the preservative is methyl para-hydroxybenzoate.
Claim 9
Dependent Claim
13 words
The pharmaceutical preparation according to claim 1 wherein the preservative is ethyl para-hydroxybenzoate.
Claim 10
Dependent Claim
13 words
The pharmaceutical preparation according to claim 1 wherein the preservative is propyl para-hydroxybenzoate.
Claim 11
Dependent Claim
13 words
The pharmaceutical preparation according to claim 1 wherein the preservative is butyl para-hydroxybenzoate.
Claim 12
Dependent Claim
19 words
The pharmaceutical preparation according to claim 1 wherein the preservative is a mixture of methyl para-hydroxybenzoate and propyl para-hydroxybenzoate.
Claim 13
Dependent Claim
13 words
The pharmaceutical preparation according to claim 1 wherein the preservative is sodium benzoate.
Claim 14
Dependent Claim
20 words
The pharmaceutical preparation according to claim 1 which further contains a viscosity-increasing agent, pH-adjusting agent, sweetening agent, and/or flavoring agent.
Claim 15
Dependent Claim
14 words
The pharmaceutical preparation according to claim 1, wherein the solvent is an aqueous solvent.
Claim 16
Dependent Claim
14 words
The pharmaceutical preparation according to claim 1, wherein the solvent is an oily solvent.
References Cited (Backward Citations)
DE171528C
Cited
GB925890A
Cited
DE1908946A1
Cited
US4221778A
Cited
EP0171528A2
Cited
EP0294103A1
Cited
US5032393A
Cited
EP0367746A2
Cited
US4996047A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-11-28 | 1998-05-30 | 1998-11-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-11-28 | 2002-05-30 | 2002-11-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-11-28 | 2006-05-30 | 2006-11-29 | $7700.00 | Window Closed / Lapsed |