US4849227A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical compositions
Assignee: EURASIAM LABORATORIES Inc
•
Filing: 1987-03-03
•
Granted: 1989-07-18
•
Expires: 2007-03-03
Abstract
Abstract A composition adapted to administer a pharmocologically effective amount of a pharmaceutical agent when ingested orally comprising (a) a pharmaceutical agent; (b) a lipid coating materials; and (c) an enteric coating materials optionally comprising water soluble coating materials; emulsifying and solubilizing agents; binding agents; stabilizing and enzyme inhibiting agents surfactants and antimicrobial agents. The composition can also include a low density lipoprotein composition and lipolytic enzymes.
Inventors
- 👤 Young W. Cho
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 01:34
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K38/00; A61K38/16; A61K38/17; A61K38/22; A61K38/28; A61K9/1605; A61K9/1617; A61K9/1623; A61K9/1629; A61K9/1652; A61K9/48; A61K9/50; A61K9/5005; A61K9/5015; A61K9/5021; A61K9/5026; A61K9/5073; A61K9/5078
Claims Analysis
Total Claims: 84
Claim 1
Independent Claim
87 words
A composition adapted for the oral administration of a selected proteinaceous material in biologically active form, said composition comprising: (a) particles having an average diameter of approximately 1 to about 100 microns and consisting essentially of a solid emulsifying agent and a surfactant; (b) a selected biologically active proteinaceous material bound to the surface of said particles with a binder agent; and (c) a lipid coating having a thickness of approximately 0.05 to about 1.0 microns surrounding said particles having said proteinaceous material bound to their surfaces.
Claim 2
Dependent Claim
87 words
A composition adapted for the oral administration of a selected proteinaceous material in biologically active form, said composition comprising: (a) particles having an average diameter of approximately 1 to about 100 microns and consisting essentially of a solid emulsifying agent and a surfactant; (b) a selected biologically active proteinaceous material bound to the surface of said particles with a binder agent; and (c) a lipid coating having a thickness of approximately 0.05 to about 1.0 microns surrounding said particles having said proteinaceous material bound to their surfaces.
Claim 3
Dependent Claim
20 words
A composition according to claim 1 further including: (d) an enteric coating layer surrounding said lipid coating on said surfaces.
Claim 4
Dependent Claim
11 words
A composition of claim 2 wherein the proteinaceous material is insulin.
Claim 5
Dependent Claim
53 words
A composition according to claim 1 wherein the solid emulsifying agent is selected from the group consisting of cholesterol, glyceryl monostearate, oleic acid, polyethylene 50 stearate, polyoxy 40 stearate, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, propylene glycol diacetate, propylene glycol monostearate, arginine HCl, gum acacia, cholesterol ester, phospholipids, and fatty acids.
Claim 6
Dependent Claim
30 words
A composition according to claim 1 wherein the surfactant is selected from the group consisting of sodium lauryl sulfate, sodium stearate, stearic acid, sorbitan monolaurate, sorbitan monostearate and emulsifying wax.
Claim 7
Dependent Claim
38 words
The composition of claim 1 wherein the biologically active proteinaceous composition is selected from the group consisting of insulin, urokinase, Factor VIII, leuprolid, gangliocides, vincristine, belomyein, lidocaine, gentamicin, bretylium tosylate, cetiedile, cyclandelate, erythromycin, chloramphenicol, adriamycin, streptokinase, and cephalosporidines.
Claim 8
Dependent Claim
33 words
A composition according to claim 1 wherein the composition includes a binder agent that comprises materials selected from the group consisting of sodium carboxymethylcellulose, microcrystalline cellulose, ethylcellulose, gelatin, hydroxypropylmethylcellulose, methylcellulose, povidone, and hydroxypropylcellulose.
Claim 9
Dependent Claim
42 words
A composition according to claim 1 wherein the lipid coating comprises materials selected from the group consisting of polyethylene glycol fatty acid esters, glycerophosphatides, phosphatidylophosphates, egg yolk lecithin, oleic acid, mono, di, and tri-glycerides, stearic acid, palmitate, cholesterol, cholesterol ester, and thromethan.
Claim 10
Dependent Claim
31 words
A composition according to claim 2 wherein the enteric coating layer comprises materials selected from the group consisting of hydroxypropyl methylcellulose phthalate, polyethylene glycol-6000 shellac, cellulose phthalate, and polyvinyl acetate phthalate.
Claim 11
Dependent Claim
13 words
A composition according to claim 1 wherein said particles further include anti-microbial agents.
Claim 12
Dependent Claim
37 words
A composition according to claim 10 wherein the anti-microbial agents are selected from the group consisting of dehydroacetic acid, methylparaben, ethylparaben, phenol, phenylethyl alcohol, propylparaben, sodium benzoate, sorbic acid, thymol, thimerosal, sodium dehydroacetate, benzyl alcohol and butylparaben.
Claim 13
Dependent Claim
9 words
The composition of claim 1 including a lipolytic enzyme.
Claim 14
Dependent Claim
24 words
The composition of claim 12 wherein the lipolytic enzyme is selected from the group consisting of lipase, pancreatic lipase, amylase, protease, and bile salts.
Claim 15
Dependent Claim
13 words
A composition according to claim 1 wherein the composition further includes enzyme inhibitors.
Claim 16
Dependent Claim
36 words
A composition according to claim 14 wherein the enzyme inhibitors are selected from the group consisting of stearylamine, stearyl alcohol, triethylamine HCl, citric acid, lactic acid, pyrophosphate, triethanolamine, ethylamine tetraacetate, iodoacetamide, phenylhydrazine, hydroxylamine 3 and 8-hydroquinoline.
Claim 17
Dependent Claim
13 words
A composition according to claim 1 wherein the composition further includes antifoaming agents.
Claim 18
Dependent Claim
21 words
A composition according to claim 16 wherein the antifoaming agents are selected from the group consisting of stearyl alcohol and silicones.
Claim 19
Dependent Claim
107 words
A composition adapted for the oral administration of insulin in biologically active form, said composition comprising: (a) particles having an average diameter of from about 1 to about 100 microns and consisting essentially of cholesterol, sodium lauryl sulfate and, methyl and propylparabens; (b) insulin bound to the surface of said particles with a solution consisting essentially of hydroxypropylcellulose, sodium lauryl sulfate, triethylamine HCl and citric acid; (c) a lipid coating having a thickness of from about 0.1 to 0.3 microns; and (d) an enteric coating layer comprising hydroxypropylmethylcellulose phthalate, shellac and PEG-6000 with the thickness of 0.1 microns surrounding said polyethylene glycol monostearate coating on said particles.
Claim 20
Dependent Claim
107 words
A composition adapted for the oral administration of insulin in biologically active form, said composition comprising: (a) particles having an average diameter of from about 1 to about 100 microns and consisting essentially of cholesterol, sodium lauryl sulfate and, methyl and propylparabens; (b) insulin bound to the surface of said particles with a solution consisting essentially of hydroxypropylcellulose, sodium lauryl sulfate, triethylamine HCl and citric acid; (c) a lipid coating having a thickness of from about 0.1 to 0.3 microns; and (d) an enteric coating layer comprising hydroxypropylmethylcellulose phthalate, shellac and PEG-6000 with the thickness of 0.1 microns surrounding said polyethylene glycol monostearate coating on said particles.
Claim 21
Independent Claim
92 words
A method for the preparation of compositions adapted for oral administration of selected proteinaceous material in biologically active form comprising the steps: (a) forming particles having an average diameter of from about 1 micron to 1/2 millimeter and consisting essentially of a solid emulsifying agent and a surfactant; (b) binding a selected biologically active proteinaceous material to the surfaces of said particles with a binder agent; and (c) coating said particles having said proteinaceous material bound to their surfaces with a lipid coating layer having a thickness of 0.05 to 1.0 microns.
Claim 22
Independent Claim
92 words
A method for the preparation of compositions adapted for oral administration of selected proteinaceous material in biologically active form comprising the steps: (a) forming particles having an average diameter of from about 1 micron to 1/2 millimeter and consisting essentially of a solid emulsifying agent and a surfactant; (b) binding a selected biologically active proteinaceous material to the surfaces of said particles with a binder agent; and (c) coating said particles having said proteinaceous material bound to their surfaces with a lipid coating layer having a thickness of 0.05 to 1.0 microns.
Claim 23
Dependent Claim
25 words
The method according to claim 19 further including the step of (d) coating said particles with an enteric coating layer surrounding said lipid coating layer.
Claim 24
Dependent Claim
26 words
The method according to claim 19 further including the step of (d) coating the particles with a water soluble coating before the lipid coating is applied.
Claim 25
Dependent Claim
8 words
The product of the process of claim 19.
Claim 26
Dependent Claim
8 words
The product of the process of claim 20.
Claim 27
Dependent Claim
8 words
The product of the process of claim 21.
Claim 28
Dependent Claim
65 words
A composition adapted for the oral administration of insulin in biologically active form comprising: particles having an average diameter of approximately 1 to 100 microns consisting essentially of an emulsifying agent and a surfactant; insulin bound to the surface of the particles; a lipid coating surrounding the particles having the proteinaceous material bond to their surfaces; and an enteric coating layer surrounding the lipid coating.
Claim 29
Dependent Claim
65 words
A composition adapted for the oral administration of insulin in biologically active form comprising: particles having an average diameter of approximately 1 to 100 microns consisting essentially of an emulsifying agent and a surfactant; insulin bound to the surface of the particles; a lipid coating surrounding the particles having the proteinaceous material bond to their surfaces; and an enteric coating layer surrounding the lipid coating.
Claim 30
Independent Claim
58 words
A method of orally administering insulin comprising: providing a composition for oral ingestion comprising insulin bound to a surface of a solid emulsifier/solubilizing particle, the insulin and particles being coated with a lipid coating, the particles having an average diameter of approximately 1 micron to about 100 microns, and the lipid coating being coated by an enteric coating.
Claim 31
Independent Claim
58 words
A method of orally administering insulin comprising: providing a composition for oral ingestion comprising insulin bound to a surface of a solid emulsifier/solubilizing particle, the insulin and particles being coated with a lipid coating, the particles having an average diameter of approximately 1 micron to about 100 microns, and the lipid coating being coated by an enteric coating.
Claim 32
Independent Claim
41 words
A method orally administering insuling composition: providing a composition for oral ingestion comprising insulin bound to a surface of lipoprotein particles, the insulin and particles being coated by a lipid coating, and the lipid coating being coated by an enteric coating.
Claim 33
Independent Claim
41 words
A method orally administering insuling composition: providing a composition for oral ingestion comprising insulin bound to a surface of lipoprotein particles, the insulin and particles being coated by a lipid coating, and the lipid coating being coated by an enteric coating.
Claim 34
Dependent Claim
13 words
The method of claim 27 including the step of administering a lipolytic enzyme.
Claim 35
Dependent Claim
19 words
The method of claim 27 including orally administering at least one second capsule containing at least one lipolytic enzyme.
Claim 36
Dependent Claim
50 words
A composition adapted for the oral administration of a selected proteinaceous material in biologically active form, said composition comprising: (a) a lipoprotein composition; (b) a selected biologically active proteinaceous material bound to the surface of the lipoprotein composition; and (c) a lipid coating surrounding said lipoprotein composition and proteinaceous material.
Claim 37
Dependent Claim
50 words
A composition adapted for the oral administration of a selected proteinaceous material in biologically active form, said composition comprising: (a) a lipoprotein composition; (b) a selected biologically active proteinaceous material bound to the surface of the lipoprotein composition; and (c) a lipid coating surrounding said lipoprotein composition and proteinaceous material.
Claim 38
Dependent Claim
24 words
The composition of claim 30 including a water soluble coating surrounding the lipoprotein and proteinaceous material, the lipid coating coating the water soluble coating.
Claim 39
Dependent Claim
12 words
The composition of claim 30 wherein the liproprotein is low density lipoprotein.
Claim 40
Dependent Claim
14 words
The composition of claim 30 wherein the lipoprotein comprises at least one amino acid.
Claim 41
Dependent Claim
19 words
The composition of claim 30 including a gel capsule, the lipid coating material being packed into the gel capsule.
Claim 42
Dependent Claim
15 words
The composition of claim 34 wherein the gel capsule is coated with an enteric coating.
Claim 43
Dependent Claim
38 words
The composition of claim 30 wherein the biologically active proteinaceous composition is selected from the group consisting of insulin, urokinase, Factor VIII, leuprolid, gangliocides, vincristine, belomyein, lidocaine, gentamicyin, bretylium, tosylate, cetiedile, cyclandelate, erythromycin, chloroamphenicol, adriamycin, streptokinase, and cephalosporidines.
Claim 44
Dependent Claim
9 words
The composition of claim 30 including a lipolytic enzyme.
Claim 45
Dependent Claim
24 words
The composition of claim 37 wherein the lipolytic enzyme is selected from the group consisting of lipase, pancreatic lipase, amylase, protease, and bile salts.
Claim 46
Dependent Claim
14 words
The composition of claim 38 wherein the lipolytic enzyme comprises lipase and bile salts.
Claim 47
Dependent Claim
42 words
A composition according to claim 30 wherein the lipid coating comprises materials selected from the group consisting of polyethylene glycol fatty acid esters, glycerophosphatides, phosphatidylophosphates, egg yolk lecithin, oleic acid, mono, di, and tri-glycerides, stearic acid, palmitate, cholesterol, cholesterol ester, and thromethan.
Claim 48
Dependent Claim
31 words
A composition according to claim 35 wherein the enteric coating layer comprises materials selected from the group consisting of hydroxypropyl methylcellulose phthalate, polyethylene glycol-6000 shellac, cellulose phthalate, and polyvinyl acetate phthalate.
Claim 49
Dependent Claim
13 words
A composition according to claim 30 wherein said particles further include anti-microbial agents.
Claim 50
Dependent Claim
37 words
A composition according to claim 42 wherein the anti-microbial agents are selected from the group consisting of dehydroacetic acid, methylparaben, ethylparaben, phenol, phenylethyl alcohol, propylparaben, sodium benzoate, sorbic acid, thymol, thimersal, sodium dehydroacetate, benzyl alcohol and butylparaben.
Claim 51
Dependent Claim
13 words
A composition according to claim 30 wherein the composition further includes enzyme inhibitors.
Claim 52
Dependent Claim
36 words
A composition according to claim 44 wherein the enzyme inhibitors are selected from the group consisting of stearylamine, stearyl alcohol, triethylamine HCl, citric acid, lactic acid, pyrophosphate, triethanolamine, ethylamine tetraacetate, iodoacetamide, phenylhydrazine, hydroxylamine 3 and 8-hydroquinoline.
Claim 53
Dependent Claim
13 words
A composition according to claim 30 wherein the composition further includes antifoaming agents.
Claim 54
Dependent Claim
16 words
The composition according to claim 30 wherein the lipoprotein includes a lipid and an amino acid.
Claim 55
Dependent Claim
36 words
The composition of claim 47 where in the lipid is selected from the group consisting of cholesterol, oleic acid, stearic acid, sodium lauryl sulfate, lecithin, phosphatides, sodium lauryl sulfate and lecithin, palmitic and phosphatide phosphate choline.
Claim 56
Dependent Claim
22 words
The composition of claim 47 wherein the amino acid is selected from the group consisting of arginine, lysine, histidine, and aspartic acid.
Claim 57
Dependent Claim
21 words
A composition according to claim 46 wherein the antifoaming agents are selected from the group consisting of stearyl alcohol and silicones.
Claim 58
Dependent Claim
77 words
A composition adapted for the oral administration of insulin in biologically active form, said composition comprising: (a) particles having an average diameter of from about 1 micron to about 1/2 millimeter and including a low density of lipoprotein composition; (b) insulin bound to the surface of said particles with a binder; (c) a water soluble coating layer, for coating the particles and insulin; and (d) a lipid coating for coating the water soluble layer, particles and insulin.
Claim 59
Dependent Claim
77 words
A composition adapted for the oral administration of insulin in biologically active form, said composition comprising: (a) particles having an average diameter of from about 1 micron to about 1/2 millimeter and including a low density of lipoprotein composition; (b) insulin bound to the surface of said particles with a binder; (c) a water soluble coating layer, for coating the particles and insulin; and (d) a lipid coating for coating the water soluble layer, particles and insulin.
Claim 60
Dependent Claim
9 words
The composition of claim 51 including a lipolytic enzyme.
Claim 61
Dependent Claim
15 words
The composition of claim 51 including an enteric coating layer for coating the lipid layer.
Claim 62
Independent Claim
101 words
A method for the preparation of compositions adapted for the oral administration of selected proteinaceous material in biologically active form comprising the steps of: (a) forming low density lipoprotein particles having an average diameter of from about 1 micron to 1/2 millimeter; (b) binding a selected biologically active proteinaceous material to the surfaces of said particles with a binder agent; (c) coating the particles and proteinaceous material with a water soluble coating; and (d) coating the water soluble coated particles having said proteinaceous material bound to their surfaces with a lipid coating layer having a thickness of 0.05 to 1.0 microns.
Claim 63
Independent Claim
101 words
A method for the preparation of compositions adapted for the oral administration of selected proteinaceous material in biologically active form comprising the steps of: (a) forming low density lipoprotein particles having an average diameter of from about 1 micron to 1/2 millimeter; (b) binding a selected biologically active proteinaceous material to the surfaces of said particles with a binder agent; (c) coating the particles and proteinaceous material with a water soluble coating; and (d) coating the water soluble coated particles having said proteinaceous material bound to their surfaces with a lipid coating layer having a thickness of 0.05 to 1.0 microns.
Claim 64
Dependent Claim
24 words
A method according to claim 54 further including the step (e) coating said particles with an enteric coating layer surrounding said lipid coating layer.
Claim 65
Dependent Claim
8 words
The product of the process of claim 54.
Claim 66
Dependent Claim
8 words
The product of the process of claim 55.
Claim 67
Dependent Claim
68 words
A composition adapted for the oral administration of insulin in biologically active form comprising: low density lipoprotein particles; insulin bound to the surface of the particles; a water soluble coating surrounding the particles and insulin; a lipid coating surrounding the water soluble coating and particles having insulin bound to their surfaces; a gel capsule for surrounding the lipid coating; and an enteric coating layer surrounding the gel capsule.
Claim 68
Dependent Claim
68 words
A composition adapted for the oral administration of insulin in biologically active form comprising: low density lipoprotein particles; insulin bound to the surface of the particles; a water soluble coating surrounding the particles and insulin; a lipid coating surrounding the water soluble coating and particles having insulin bound to their surfaces; a gel capsule for surrounding the lipid coating; and an enteric coating layer surrounding the gel capsule.
Claim 69
Independent Claim
62 words
A method of treating diabetes comprising the steps of: administering orally at least one capsule having a composition including a low density lipoprotein, insulin bound to the lipoprotein, a water soluble coating over the insulin and lipoprotein, and a lipid coating over the water soluble coating; and administering orally at least one capsule having a composition icluding lipolytic enzymes and bile salts.
Claim 70
Independent Claim
62 words
A method of treating diabetes comprising the steps of: administering orally at least one capsule having a composition including a low density lipoprotein, insulin bound to the lipoprotein, a water soluble coating over the insulin and lipoprotein, and a lipid coating over the water soluble coating; and administering orally at least one capsule having a composition icluding lipolytic enzymes and bile salts.
Claim 71
Independent Claim
46 words
The method of treating diabetes comprising the steps of: administering orally at least one capsule having a composition including emulsifier/solubilizer particles, insulin bound to the particles, and a lipid coating over the particles; and administering orally at least one capsule having a composition including lipolytic enzymes.
Claim 72
Independent Claim
46 words
The method of treating diabetes comprising the steps of: administering orally at least one capsule having a composition including emulsifier/solubilizer particles, insulin bound to the particles, and a lipid coating over the particles; and administering orally at least one capsule having a composition including lipolytic enzymes.
Claim 73
Dependent Claim
26 words
A composition useful for the oral administration of a proteinaceous compound comprising lipolytic enzymes selected from the group including, pancreatic lipase, amylase, protease, and bile salts.
Claim 74
Dependent Claim
26 words
A composition useful for the oral administration of a proteinaceous compound comprising lipolytic enzymes selected from the group including, pancreatic lipase, amylase, protease, and bile salts.
Claim 75
Dependent Claim
16 words
The composition of claim 61 wherein the lipolytic enzymes selected are pancreatic lipase and bile salts.
Claim 76
Dependent Claim
37 words
A composition adapted for the oral administration of insulin comprising the following components: (a) particles of pancreatic lipase; (b) particles of bile salt; (c) lipid coated insulin bound lipid particles; (d) sodium bicarbonate; and (e) citric acid.
Claim 77
Dependent Claim
37 words
A composition adapted for the oral administration of insulin comprising the following components: (a) particles of pancreatic lipase; (b) particles of bile salt; (c) lipid coated insulin bound lipid particles; (d) sodium bicarbonate; and (e) citric acid.
Claim 78
Dependent Claim
14 words
The composition of claim 63 wherein the components are placed in hard gel capsules.
Claim 79
Dependent Claim
12 words
The composition of claim 63 wherein the components are pressed into tablets.
Claim 80
Dependent Claim
21 words
The composition of claim 63 wherein the weight percent ratio of sodium bicarbonate to citric acid is between 3:1 to 1:1.
Claim 81
Dependent Claim
19 words
The composition of claim 63 wherein the insulin bound particle has a spherical size of less than 1.5 millimeters.
Claim 82
Dependent Claim
16 words
The composition of claim 63 wherein the pancreatic lipase and bile salt particles are enteric coated.
Claim 83
Dependent Claim
53 words
A composition adapted for the oral administration of insulin comprising a sodium bicarbonate and citric acid mixture in a ratio of approximately 3:1 to about 1:1, the mixture forming a seed that is coated with a layer of an insulin lipid mixture, and a resultant particle is then coated with an enteric coating.
Claim 84
Dependent Claim
53 words
A composition adapted for the oral administration of insulin comprising a sodium bicarbonate and citric acid mixture in a ratio of approximately 3:1 to about 1:1, the mixture forming a seed that is coated with a layer of an insulin lipid mixture, and a resultant particle is then coated with an enteric coating.
References Cited (Backward Citations)
GB285091A
Cited
GB461317A
Cited
US2474729A
Cited
US2574889A
Cited
US3656997A
Cited
US3991180A
Cited
US3922339A
Cited
US3965260A
Cited
US4173629A
Cited
US4356167A
Cited
GB2013087A
Cited
US4448765A
Cited
US4250163A
Cited
US4454317A
Cited
GB2050287A
Cited
US4529589A
Cited
EP0071433A1
Cited
US4452775A
Cited
US4447412A
Cited
EP0127535A2
Cited
US4579730A
Cited
EP0130779A2
Cited
EP0140085A2
Cited
EP0143949A1
Cited
EP0142085A2
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-07-17 | 1993-01-16 | 1993-07-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-17 | 1997-01-16 | 1997-07-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-17 | 2001-01-16 | 2001-07-18 | $7700.00 | Window Closed / Lapsed |