Patent US4794000A successfully refreshed from Google Patents.
US4794000A
Expired / Lapsed
US
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Coacervate-based oral delivery system for medically useful compositions
Assignee: Quixote Corp
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Filing: 1987-01-08
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Granted: 1988-12-27
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Expires: 2007-01-08
Abstract
Abstract The present invention provides for an oral drug delivery system based on a two phase liquid coacervate system prepared from water and one or more surfactants selected from anionic, cationic, amphoteric, and non-toxic surfactants, polysaccharides, synthetic polymers and polysorbates and their derivatives, and in which a pharmaceutical component is incorporated. The delivery system may be prepared in the form of a microemulsion as well as other forms including encapuslated microparticles. The claimed oral composition is useful to delivery oral dosage forms of drugs, their salts and derivatives thereof; biologicals, enzymes, and other pharmocologically active compositions. A method to prepare the oral drug delivery system is also disclosed.
Inventors
- 👤 Bernard Ecanow
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 22:12
CPC Classifications
B; B82; B82Y; B82Y5/00; A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5089
Claims Analysis
Total Claims: 33
Claim 1
Independent Claim
129 words
A method of preparing a composition for oral delivery of a pharmaceutical component; said method based upon a non-toxic liquid aqueous two phase coacervate system; (a) one of said phases being an aqueous colloid rich phase, semi-polar to non-polar in character; (b) the other of said phases being an aqueous colloid poor phase, semi-polar to polar in character; (c) said colloid rich phase being insoluble and in equilibrium with said colloid poor phase; (d) said two phase system prepared from water and one or more surfactants selected from the group consisting of anionic, cationic, amphoteric, and non-ionic surfactants, polysaccharides, synthetic polymers, polysorbates and their derivatives and mixtures thereof; (e) said two phase system further prepared to contain a pharmaceutical component in the colloid poor phase of the coacervate system.
Claim 2
Independent Claim
129 words
A method of preparing a composition for oral delivery of a pharmaceutical component; said method based upon a non-toxic liquid aqueous two phase coacervate system; (a) one of said phases being an aqueous colloid rich phase, semi-polar to non-polar in character; (b) the other of said phases being an aqueous colloid poor phase, semi-polar to polar in character; (c) said colloid rich phase being insoluble and in equilibrium with said colloid poor phase; (d) said two phase system prepared from water and one or more surfactants selected from the group consisting of anionic, cationic, amphoteric, and non-ionic surfactants, polysaccharides, synthetic polymers, polysorbates and their derivatives and mixtures thereof; (e) said two phase system further prepared to contain a pharmaceutical component in the colloid poor phase of the coacervate system.
Claim 3
Dependent Claim
33 words
The composition according to claim 1, wherein the pharmaceutical component is selected from drugs, their salts and derivatives thereof; biologicals, enzymes and any other pharmacologically active compositions and their derivatives, and mixtures thereof.
Claim 4
Dependent Claim
39 words
The composition according to claim 1 or 2, wherein the colloid rich phase comprises from 0.5% to 99.5% by volume, and the colloid poor phase comprises from 99.5% to 0.5% by volume of the two phase liquid aqueous system.
Claim 5
Dependent Claim
19 words
The composition according to claim 1, wherein the surfactant comprises a mixture of a polysaccharide and a synthetic polymer.
Claim 6
Dependent Claim
18 words
The composition according to claim 4, wherein the polysaccharide is dextran and the synthetic polymer is polyethylene glycol.
Claim 7
Dependent Claim
31 words
The composition according to any of claims 1, wherein the colloid rich phase is separated from the colloid poor phase and the pharmaceutical component is added to said colloid rich phase.
Claim 8
Dependent Claim
22 words
The composition according to claim 6, wherein the pharmaceutical component contains a glyceride selected from a monoglyceride, diglyceride, triglyceride and mixtures thereof.
Claim 9
Dependent Claim
26 words
The composition according to claim 7, wherein the two phases are recombined and emulsified to yield a drug delivery system in the form of an emulsion.
Claim 10
Dependent Claim
37 words
The composition according to claims 6 or 7, wherein lecithin is dispersed into the colloid rich phase; and the two phases are recombined and microemulsified to yield a drug delivery system in the form of a microemulsion.
Claim 11
Dependent Claim
44 words
The composition according to claims 6 or 7, wherein lecithin, albumin and the colloid poor phase are combined with the colloid rich phase and microemulsified; said microemulsion being further subjected to a heating or chemical step to yield a sustained release drug delivery system.
Claim 12
Dependent Claim
26 words
A composition as defined according to claims 6 to 8, wherein the final product is in any appropriate dosage form including liquid, granule, tablet and suspension.
Claim 13
Independent Claim
125 words
A method of preparing a composition useful as an oral delivery system; said method based upon a non-toxic liquid aqueous two phase coacervate system; (a) one of said phases being an aqueous colloid rich phase, semi-polar to non-polar in character; (b) the other of said phases being an aqueous colloid poor phase, semi-polar to polar in character; (c) said colloid rich phase being insoluble and in equilibrium with said colloid poor phase; (d) said two phase system prepared from water and one or more surfactants selected from the group comprising anionic, cationic, amphoteric, and non-ionic surfactants, polysaccharides, synthetic polymers, and polysorbates and their derivatives; (e) said two phase system further prepared to contain a pharmaceutical component in the colloid poor phase of the coacervate system.
Claim 14
Independent Claim
125 words
A method of preparing a composition useful as an oral delivery system; said method based upon a non-toxic liquid aqueous two phase coacervate system; (a) one of said phases being an aqueous colloid rich phase, semi-polar to non-polar in character; (b) the other of said phases being an aqueous colloid poor phase, semi-polar to polar in character; (c) said colloid rich phase being insoluble and in equilibrium with said colloid poor phase; (d) said two phase system prepared from water and one or more surfactants selected from the group comprising anionic, cationic, amphoteric, and non-ionic surfactants, polysaccharides, synthetic polymers, and polysorbates and their derivatives; (e) said two phase system further prepared to contain a pharmaceutical component in the colloid poor phase of the coacervate system.
Claim 15
Dependent Claim
33 words
The method according to claim 12, wherein the pharmaceutical component is selected from drugs, their salts and derivatives thereof; biologicals, enzymes and any other pharmacologically active compositions and their derivatives, and mixtures thereof.
Claim 16
Dependent Claim
18 words
The method according to claim 12, wherein the surfactant is a mixture of a polysaccharide and a polysorbate.
Claim 17
Dependent Claim
17 words
The method according to claim 14, wherein the polysaccharide is dextran and the polysorbate is polyethylene glycol.
Claim 18
Dependent Claim
89 words
The method according to claim 15, including the steps of: (a) mixing a solution of dextran into a solution of polyethylene glycol; (b) storing the mixture undisturbed and at room temperature or under conventional refrigeration for from 6 to 24 hours until the composition of step (a) separates into two layers, one above the other, the lower phase being the colloid rich phase, the upper phase being the colloid poor phase; separating the two phases; and mixing a desired quantity of the pharmaceutical component into the colloid poor phase.
Claim 19
Dependent Claim
27 words
The method according to claim 16, further including the step of adding a solution of NaCl to the mixture dropwise to aid in separating the two phases.
Claim 20
Independent Claim
129 words
A method of preparing a composition for oral delivery of a pharmaceutical component; said method based upon a non-toxic liquid aqueous two phase coacervate system; (a) one of said phases being an aqueous colloid rich phase, semi-polar to non-polar in character; (b) the other of said phases being an aqueous colloid poor phase, semi-polar to polar in character; (c) said colloid rich phase being insoluble and in equilibrium with said colloid poor phase; (d) said two phase system prepared from water and one or more surfactants selected from the group consisting of anionic, cationic, amphoteric, and non-ionic surfactants, polysaccharides, synthetic polymers, polysorbates and their derivatives and mixtures thereof; (e) said two phase system further prepared to contain a pharmaceutical component in the colloid rich phase of the coacervate system.
Claim 21
Independent Claim
129 words
A method of preparing a composition for oral delivery of a pharmaceutical component; said method based upon a non-toxic liquid aqueous two phase coacervate system; (a) one of said phases being an aqueous colloid rich phase, semi-polar to non-polar in character; (b) the other of said phases being an aqueous colloid poor phase, semi-polar to polar in character; (c) said colloid rich phase being insoluble and in equilibrium with said colloid poor phase; (d) said two phase system prepared from water and one or more surfactants selected from the group consisting of anionic, cationic, amphoteric, and non-ionic surfactants, polysaccharides, synthetic polymers, polysorbates and their derivatives and mixtures thereof; (e) said two phase system further prepared to contain a pharmaceutical component in the colloid rich phase of the coacervate system.
Claim 22
Dependent Claim
41 words
The method according to claim 18, further including the additional steps of: recombining the colloid poor phase with the colloid rich phase, and emulsifying the combined colloid poor and colloid rich phases to produce an oral delivery composition in emulsion form.
Claim 23
Dependent Claim
40 words
The method according to claim 18, further including adding a solubilizing agent to the colloid rich phase; mixing the colloid poor phase with the colloid rich phase and emulsifying the product to produce an oral delivery composition in microemulsion form.
Claim 24
Dependent Claim
13 words
The method according to claim 20, wherein the solubilizing agent is a phospholipid.
Claim 25
Dependent Claim
74 words
The method according to claim 18, further including the steps of adding a phospholipid and a protein to the colloid rich phase; mixing the colloid poor phase with the colloid rich phase; emulsifying the composition to produce a microemulsion of the colloid rich phase in particles containing the pharmaceutical component; and encapsulating the particles using a chemical crosslinking agent or heat, to produce an oral drug delivery system in the form of encapsulated microparticles.
Claim 26
Dependent Claim
11 words
The method according to claim 21, wherein the protein is albumin.
Claim 27
Dependent Claim
14 words
The method according to claim 21, wherein the cross-linking agent is a non-toxic aldehyde.
Claim 28
Dependent Claim
14 words
The method of claim 21, which yields sustained release particles containing the pharmaceutical component.
Claim 29
Dependent Claim
48 words
The method according to claim 22, wherein the pharmaceutical component is dissolved in a monoglyceride, diglyceride or triglyceride solution or a mixture thereof prior to addition to the colloid rich phase to provide time release particles containing the pharmaceutical component; ranging from prompt release to sustained release particles.
Claim 30
Dependent Claim
33 words
The method according to claim 12, wherein the pharmaceutical component is selected from drugs, their salts and derivatives thereof; biologicals, enzymes and any other pharmacologically active compositions and their derivatives, and mixtures thereof.
Claim 31
Dependent Claim
10 words
The method of claim 21 wherein the phospholipid is lecithen.
Claim 32
Independent Claim
66 words
A method of introducing a pharmaceutical component into a circulatory system comprising orally ingesting a composition comprising an aqueous coacervate system including water, a surface active agent and an effective amount of the pharmaceutical component, said coacervate system including an aqueous coacervate-based film encapsulating the pharmaceutical compound; said aqueous coacervate-based film comprising an aqueous colloid-rich phase, or an aqueous colloid poor phase, or a combination thereof.
Claim 33
Independent Claim
66 words
A method of introducing a pharmaceutical component into a circulatory system comprising orally ingesting a composition comprising an aqueous coacervate system including water, a surface active agent and an effective amount of the pharmaceutical component, said coacervate system including an aqueous coacervate-based film encapsulating the pharmaceutical compound; said aqueous coacervate-based film comprising an aqueous colloid-rich phase, or an aqueous colloid poor phase, or a combination thereof.
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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) | 1991-12-27 | 1992-06-27 | 1992-12-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-12-27 | 1996-06-27 | 1996-12-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-12-27 | 2000-06-27 | 2000-12-27 | $7700.00 | Window Closed / Lapsed |