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US4766012A Expired / Lapsed US ⏱️ 0.0 years remaining

Microencapsulation of a medicament

Assignee: FARMACUTICI FORMENTI SpA
•
Filing: 1986-08-22
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Granted: 1988-08-23
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Expires: 2006-08-22
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Abstract

Abstract The present invention relates to a process for the microencapsulation of a medicament by means of at least one coating agent, characterized in that is comprises the following steps: (a) Dissolution of the coating agent in water, by salification; (b) Dispersion of the particles of medicament to be microencapsulated, first in water, and then into the solution of the salified coating agent according to (a); (c) Addition to the so-obtained suspension of an acidifying substance, which causes the precipitation of the coating agent onto the particles of medicament while these are being kept in suspension by stirring, thus microcapsules being formed. (d) Recovery of microcapsules.

Inventors

  • 👤 Mauro Valenti

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 12:26
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5026; A61K9/5036; A61K9/5042; A61K9/5089; Y; Y10; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2989

Claims Analysis

Total Claims: 20
Claim 1
Independent Claim 101 words
A process for the microencapsulation of a medicament by at least one coating agent consisting essentially of the steps of: (a) dissolving the coating agent in water by salification, whereby a solution is formed; (b) dispersing particles of the medicament to be microencapsulated first in water and then in the solution of salified coating agent obtained in step (a), whereby a suspension is formed; (c) adding an acidifyig substance to the suspension obtained in step (b) so that the coating agent precipitates onto the particles of medicament kept in suspension by stirring, whereby microcapsules are formed; and (d) recovering the microcapsules.
Claim 2
Dependent Claim 101 words
A process for the microencapsulation of a medicament by at least one coating agent consisting essentially of the steps of: (a) dissolving the coating agent in water by salification, whereby a solution is formed; (b) dispersing particles of the medicament to be microencapsulated first in water and then in the solution of salified coating agent obtained in step (a), whereby a suspension is formed; (c) adding an acidifyig substance to the suspension obtained in step (b) so that the coating agent precipitates onto the particles of medicament kept in suspension by stirring, whereby microcapsules are formed; and (d) recovering the microcapsules.
Claim 3
Dependent Claim 160 words
The process as claimed in claim 1, wherein the coating agent is selected from the group consisting of a carboxyalkyl-alkylcellulose; a hemiester of an organic dicarboxy acid of an alkyl cellulose or of a hydroxyalkyl-alkyl cellulose or of cellulose acetate; a copolymer of an alkenylcarboxy acid and an alkyl ester of an alkenyl carboxy acid; a copolymer of an alkenyl carboxy acid and two alkyl esters of an alkenyl carboxy acid; a phthalic or succinic hemiester of an alkyl cellulose or of a hydroxyalkyl-alkyl cellulose or of cellulose acetate; a copolymer formed by an acrylic or methacrylic acid and an alkyl ester of an acrylic or methacrylic acid; a copolymer composed by an acrylic and methacrylic acid and by an alkyl acrylate or by an alkyl methacrylate; a copolymer of methacrylic acid and of an alkyl acrylate; a copolymer of methacrylic acid and alkyl methacrylate; a copolymer of methacrylic acid-alkyl acrylate-alkyl methacrylate; and a copolymer of methacrylic acid-alkyl methacrylate-alkyl methacrylate.
Claim 4
Dependent Claim 16 words
The process according to claim 2, wherein the alkyl group has one to four carbon atoms.
Claim 5
Dependent Claim 16 words
The process according to claim 2, wherein the alkenyl group has 3 or 4 carbon atoms.
Claim 6
Dependent Claim 31 words
The process according to claim 1, wherein the coating agent is selected from the group consisting of a carboxymethylethyl cellulose; cellulose aceto-phthalate; hydroxypropyl methylcellulose phthalate; and a copolymer of methacrylic acid.
Claim 7
Dependent Claim 19 words
The process according to claim 1, wherein in step (a), the coating agent is dissolved in previously alkalified water.
Claim 8
Dependent Claim 25 words
The process according to claim 1, wherein the concentration of the coating agent in solution is within the range of from 0.05% to 43% weight/weight.
Claim 9
Dependent Claim 25 words
The process according to claim 7, wherein the concentration of the coating agent in solution is within the range of from 0.1% to 27% weight/weight.
Claim 10
Dependent Claim 25 words
The process according to claim 1, wherein the amount of coating agent/gram of medicament used is within the range of from 0.01 to 5 g.
Claim 11
Dependent Claim 25 words
The process according to claim 9, wherein the amount of coating agent/gram of medicament used is within the range of from 0.05 to 2.5 g.
Claim 12
Dependent Claim 23 words
The process according to claim 1, wherein the particles of medicament are within the range of from 5 to 1000 microns in size.
Claim 13
Dependent Claim 23 words
The process according to claim 11, wherein the particles of medicament are within the range of from 5 to 500 microns in size.
Claim 14
Dependent Claim 15 words
The process according to claim 1, wherein the medicament has the form of a solid.
Claim 15
Dependent Claim 23 words
The process according to claim 1, wherein the medicament is insoluble in water or in aqueous solutions at pH values lower, than 5.
Claim 16
Dependent Claim 29 words
The process according to claim 1, wherein the solubilization of the coating agent is obtained by salification with an inorganic base or with the salt of an inorganic base.
Claim 17
Dependent Claim 21 words
The process according to claim 15, wherein the solubilization of the coating agent is obtained by salification with an inorganic base.
Claim 18
Dependent Claim 25 words
The process according to claim 1, wherein the precipitation of the coating agent on the medicament particles is obtained by acidification with an inorganic acid.
Claim 19
Dependent Claim 34 words
The process according to claim 17, wherein the precipitation of the coating agent is obtained by acidification with a solution of hydrochloric acid having a concentration within the range of from 0.1N to 1N.
Claim 20
Dependent Claim 34 words
The process according to claim 17, wherein the precipitation of the coating agent is obtained by acidification with a solution of hydrochloric acid having a concentration within the range of from 1N to 5N.

References Cited (Backward Citations)

US28779A Cited
USRE28779E Cited
US3943063A Cited
GB1483542A Cited
GB1573361A Cited
US4460563A Cited
EP0130162A2 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-08-23 1992-02-22 1992-08-23 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-08-23 1996-02-22 1996-08-23 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-08-23 2000-02-22 2000-08-23 $7700.00 Window Closed / Lapsed

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