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Patent US3890433A successfully refreshed from Google Patents.
US3890433A
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Method for manufacturing pharmaceutical preparation
Assignee: Individual
•
Filing: 1972-10-04
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Granted: 1975-06-17
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Expires: 1992-10-04
Abstract
Abstract A method for manufacturing a pharmaceutical preparation which comprises melting an amide compound of the formula: WHEREIN R is a straight or branched, saturated or unsaturated hydrocarbon group having 17 to 25 carbon atoms substituted or not with hydroxyl and R1, R2, R3 and R4 are each a hydrogen atom, a haolgen atom, a lower alkyl group or a lower alkoxy group but all of them are not simultaneously hydrogen atoms in the form of a paste or wax-like solid at an ordinary temperature in the presence of oil-soluble anti-oxidizing agents, emulsifying the resulting melted mixture with a gellating agent in the presence of water-soluble anti-oxidizing agents and saccharides and/or sugar alcohols, spraying the resultant emulsion onto fine particles of a water-absorptive material and separating the gelled fine beads of the amide compound from the fine particles of the water-absorptive material, followed by drying. The thus manufactured preparation of the amide compound is highly stable to air oxidation, easily administrable through an intestinal route and exhibits a highly pharmacological activity.
Inventors
- 👤 Ryota Oishi
- 👤 Yotaka Mito
- 👤 Kenji Yamauchi
- 👤 Katsuyuki Takahashi
- 👤 Kazushi Hirata
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 20:09
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K31/00; A61K31/16
Claims Analysis
Total Claims: 50
Claim 1
Independent Claim
15 words
A METHOD FOR MANUFACTURING A PHARMACEUTICAL PREPARATION OF AN AMIDE COMPOUND OF THE FOLLOWING FORMULA:
Claim 2
Independent Claim
15 words
A METHOD FOR MANUFACTURING A PHARMACEUTICAL PREPARATION OF AN AMIDE COMPOUND OF THE FOLLOWING FORMULA:
Claim 3
Dependent Claim
35 words
MELTING SAID AMIDE COMPOUND AT 110*C. TO 120*C. IN THE PRESENCE OF ABOUT 0.2 TO 0.5 PPERCENT BY WEIGHT, ON THE BASIS OF THE AMOUNT OF AMIDE COMPOUND, OF AT LEAST ONE OIL-SOLUBLE ANTIOXIDIZING AGENT:
Claim 4
Dependent Claim
35 words
MELTING SAID AMIDE COMPOUND AT 110*C. TO 120*C. IN THE PRESENCE OF ABOUT 0.2 TO 0.5 PPERCENT BY WEIGHT, ON THE BASIS OF THE AMOUNT OF AMIDE COMPOUND, OF AT LEAST ONE OIL-SOLUBLE ANTIOXIDIZING AGENT:
Claim 5
Dependent Claim
41 words
ADDING TO AND MELTING INTO THE MELTED MIXTURE MAINTAINED AT SAID TEMPERATURE OF 110*C. TO 120*C ABOUT 1.0 TO 3.0 PERCENT BY WEIGHT, ON THE BASIS OF THE AMOUNT OF AMIDE COMPOUND, OF AT LEAST ONE OF SAID OIL-SOLUBLE ANTIOXIDIZING AGENTS;
Claim 6
Dependent Claim
41 words
ADDING TO AND MELTING INTO THE MELTED MIXTURE MAINTAINED AT SAID TEMPERATURE OF 110*C. TO 120*C ABOUT 1.0 TO 3.0 PERCENT BY WEIGHT, ON THE BASIS OF THE AMOUNT OF AMIDE COMPOUND, OF AT LEAST ONE OF SAID OIL-SOLUBLE ANTIOXIDIZING AGENTS;
Claim 7
Dependent Claim
41 words
adding to and melting into the melted mixture maintained at said temperature of 110*C. to 120*C. about 1.0 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one of said oil-soluble anti-oxidizing agents;
Claim 8
Dependent Claim
41 words
adding to and melting into the melted mixture maintained at said temperature of 110*C. to 120*C. about 1.0 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one of said oil-soluble anti-oxidizing agents;
Claim 9
Dependent Claim
54 words
adding to and melting into the melted mixture maintained at said temperature of 110*to 120*C. about 1.0 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one of said oil-soluble anti-oxidizing agents and an antioxidizing agent selected from the group consisting of butyl hydroxytoluene and butyhydroxyanisole;
Claim 10
Dependent Claim
54 words
adding to and melting into the melted mixture maintained at said temperature of 110*to 120*C. about 1.0 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one of said oil-soluble anti-oxidizing agents and an antioxidizing agent selected from the group consisting of butyl hydroxytoluene and butyhydroxyanisole;
Claim 11
Dependent Claim
56 words
The method according to claim 1, wherein the melted mixture is dispersed in step (3 ) in an aqueous solution of a gellating agent, about 0.1 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one water-soluble anti oxidizing agent and at least one saccharide or sugar alcohol.
Claim 12
Dependent Claim
24 words
The method according to claim 1, wherein the content of the amide compound in the produced beads is 30 to 60 percent by weight.
Claim 13
Dependent Claim
51 words
dispersing the resulting melted mixture in an aqueous solution of a gellating agent and about 0.1 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one water-soluble anti-oxidizing agent by stirring said mixture at 70*C. to 85*C. until a uniform emulsion is obtained;
Claim 14
Dependent Claim
51 words
dispersing the resulting melted mixture in an aqueous solution of a gellating agent and about 0.1 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one water-soluble anti-oxidizing agent by stirring said mixture at 70*C. to 85*C. until a uniform emulsion is obtained;
Claim 15
Dependent Claim
100 words
dispersing the resulting melted mixture in an aqueous solution of a gellating agent, about 0.1 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one water-soluble anti-oxidizing agent selected from the group consisting of erythorbic acid, ascorbic acid, citric acid, the sodium salts thereof and sodium hydrogen sulfite, and at least one saccharide selected from the group consisting of sucrose, glucose and fructose or at least one sugar alcohol selected from the group consisting of sorbitol and mannitol by stirring said mixture at 70* to 85*C. until a uniform emulsion is obtained;
Claim 16
Dependent Claim
100 words
dispersing the resulting melted mixture in an aqueous solution of a gellating agent, about 0.1 to 3.0 percent by weight, on the basis of the amount of amide compound, of at least one water-soluble anti-oxidizing agent selected from the group consisting of erythorbic acid, ascorbic acid, citric acid, the sodium salts thereof and sodium hydrogen sulfite, and at least one saccharide selected from the group consisting of sucrose, glucose and fructose or at least one sugar alcohol selected from the group consisting of sorbitol and mannitol by stirring said mixture at 70* to 85*C. until a uniform emulsion is obtained;
Claim 17
Dependent Claim
51 words
DISPERSING THE RESULTING METLED MIXTURE IN AN AQUEOUS SOLUTION OF A GELLATING AGENT AND ABOUT 0.1 TO 3.0 PERCENT BY WEIGHT, ON THE BASIS OF THE AMOUNT OF AMIDE COMPOUND, OF AT LEAST ONE WATER-SOLUBLE ANTI-OXIDIZING AGENT BY STIRRING SAID MIXTURE AT 70*C. TO 85*C. UNTIL A UNIFORM EMULSION IS OBTAINED;
Claim 18
Dependent Claim
51 words
DISPERSING THE RESULTING METLED MIXTURE IN AN AQUEOUS SOLUTION OF A GELLATING AGENT AND ABOUT 0.1 TO 3.0 PERCENT BY WEIGHT, ON THE BASIS OF THE AMOUNT OF AMIDE COMPOUND, OF AT LEAST ONE WATER-SOLUBLE ANTI-OXIDIZING AGENT BY STIRRING SAID MIXTURE AT 70*C. TO 85*C. UNTIL A UNIFORM EMULSION IS OBTAINED;
Claim 19
Dependent Claim
39 words
SPRAYING THE RESULTANT EMULSION, WHILE MAINTAINED AT A TEMPERATURE OF FROM 70* TO 80*C. ONTO FINE PARTICLES OF A WATER-ABSORPTIVE MATERIAL WHICH IS INERT AND INSOLUBLE IN WATER AND HAS A PARTICLE SIZE OF NOT MORE THAN 74 MICRONS;
Claim 20
Dependent Claim
39 words
SPRAYING THE RESULTANT EMULSION, WHILE MAINTAINED AT A TEMPERATURE OF FROM 70* TO 80*C. ONTO FINE PARTICLES OF A WATER-ABSORPTIVE MATERIAL WHICH IS INERT AND INSOLUBLE IN WATER AND HAS A PARTICLE SIZE OF NOT MORE THAN 74 MICRONS;
Claim 21
Dependent Claim
39 words
spraying the resultant emulsion, while maintained at a temperature of from 70* to 80*C., onto fine particles of a water-absorptive material which is inert and insoluble in waTer and has a particle size of not more than 74 microns;
Claim 22
Dependent Claim
39 words
spraying the resultant emulsion, while maintained at a temperature of from 70* to 80*C., onto fine particles of a water-absorptive material which is inert and insoluble in waTer and has a particle size of not more than 74 microns;
Claim 23
Dependent Claim
39 words
spraying the resultant emulsion, while maintained at a temperature of from 70* to 80*C., onto fine particles of a water-absorptive material which is inert and insoluble in water and has a particle size of not more than 74 microns;
Claim 24
Dependent Claim
39 words
spraying the resultant emulsion, while maintained at a temperature of from 70* to 80*C., onto fine particles of a water-absorptive material which is inert and insoluble in water and has a particle size of not more than 74 microns;
Claim 25
Dependent Claim
24 words
The method according to claim 1, wherein the oil-soluble anti-oxidizing agent is selected from the group consisting of tocopherol, stearyl ascorbate, butylhydroxyanisole and butylhydroxytoluene.
Claim 26
Dependent Claim
32 words
The method according to claim 1, wherein the water-soluble anti-oxidizing agent is selected from the group consisting of erythorbic acid, ascorbic acid, citric acid, the sodium salts thereof and sodium hydrogen sulfite.
Claim 27
Dependent Claim
12 words
separating the gelled beads from the fine particles of water-absorptive material, and;
Claim 28
Dependent Claim
12 words
separating the gelled beads from the fine particles of water-absorptive material, and;
Claim 29
Dependent Claim
12 words
separating the gelled beads from the fine particles of water-absorptive material, and;
Claim 30
Dependent Claim
12 words
separating the gelled beads from the fine particles of water-absorptive material, and;
Claim 31
Dependent Claim
12 words
SPEARATING THE GELLED BEADS FROM THE FINE PARTICLES OF WATER-ABSORPTIVE MATERIAL, AND;
Claim 32
Dependent Claim
12 words
SPEARATING THE GELLED BEADS FROM THE FINE PARTICLES OF WATER-ABSORPTIVE MATERIAL, AND;
Claim 33
Dependent Claim
4 words
DRYING THE GELLED BEADS.
Claim 34
Dependent Claim
4 words
DRYING THE GELLED BEADS.
Claim 35
Dependent Claim
4 words
drying the gelled beads.
Claim 36
Dependent Claim
4 words
drying the gelled beads.
Claim 37
Dependent Claim
19 words
The method according to claim 1, wherein the viscosity of the emulsion is 250 to 750 cps at 70*C.
Claim 38
Dependent Claim
4 words
drying the gelled beads.
Claim 39
Dependent Claim
4 words
drying the gelled beads.
Claim 40
Dependent Claim
18 words
The method according to claim 1, wherein the spraying is effected at a temperature of 60 to 80*C.
Claim 41
Dependent Claim
26 words
The method according to claim 1 wherein the weight ratio of the water absorptive material to the water in the emulsion is not less than 8.
Claim 42
Dependent Claim
21 words
The method according to claim 1, wherein the particle size of the produced beads is from 100 to 1000 Mu .
Claim 43
Dependent Claim
29 words
The method according to claim 1, wherein the amount of gellating agent is about 30 to 80 percent by weight, on the basis of the amount of amide compound.
Claim 44
Dependent Claim
23 words
The method according to claim 1, wherein said water-absorptive material is selected from the group consisting of starch, talc and aluminum hydroxy gel.
Claim 45
Dependent Claim
30 words
The method according to claim 11, wherein the amount of water-absorptive material is 8 parts by weight or more to 1 part by weight of the water in the emulsion.
Claim 46
Dependent Claim
31 words
The method according to claim 2, wherein the amount of saccharide or sugar alcohol is about 20 to 70 percent by weight, on the basis of the amount of amide compound.
Claim 47
Independent Claim
14 words
A method for manufacturing a pharmaceutical preparation of an amide compound of the formula:
Claim 48
Independent Claim
14 words
A method for manufacturing a pharmaceutical preparation of an amide compound of the formula:
Claim 49
Dependent Claim
38 words
The method according to claim 14, wherein the amount of butylhydroxytoluene or butylhydroxyanisole added to the melted mixture in step (2) is about 0.1 to 0.3 percent by weight, on the basis of the amount of amide compound.
Claim 50
Dependent Claim
17 words
A pharmaceutical preparation in the form of beads prepared by the method as claimed in claim 12.
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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) | 1978-06-16 | 1978-12-16 | 1979-06-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1982-06-16 | 1982-12-16 | 1983-06-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1986-06-16 | 1986-12-16 | 1987-06-17 | $7700.00 | Window Closed / Lapsed |