Microcapsule-sustained Or Differential Release Patents (Class 514/963)
  • Patent number: 4749620
    Abstract: Capsules are formed herein a liquified core while avoiding capsule core gelation by adding drops of a solution of either an anionic polymer composition or a cationic polymer composition to a solution of an ionic polymer of opposite charge. The drops contain an active ingredient such as a cell or microorganism capable of producing a biologically active product or can contain a biological or chemical composition. The interface of the ionic polymers form a permeable membrane surrounding the liquid drops.
    Type: Grant
    Filed: September 18, 1985
    Date of Patent: June 7, 1988
    Assignee: Massachusetts Institute of Technology
    Inventors: ChoKyun Rha, Dolores Rodriguez-Sanchez
  • Patent number: 4744933
    Abstract: Capsules are formed herein a liquified core while avoiding capsule core gelation by adding drops of a solution of either an anionic polymer composition or a cationic polymer composition to a solution of an ionic polymer of opposite charge. The drops contain an active ingredient such as a cell or microorganism capable of producing a biologically active product or can contain a biological or chemical composition. The interface of the ionic polymers form a permeable membrane surrounding the liquid drops.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: May 17, 1988
    Assignee: Massachusetts Institute of Technology
    Inventors: ChoKyun Rha, Dolores Rodriguez-Sanchez
  • Patent number: 4741872
    Abstract: A method for preparing biodegradable microspheres having a three-dimensional network in which biologically active macromolecular agents are physically entrapped therein. The microsphere is able to degrade and release the macromolecular agent at a controlled rate. The method involves emulsifying a vinyl derivative of a biodegradable hydrophilic polymer, a water-soluble monovinyl monomer and a biologically active macromolecule in water, and copolymerizing the biodegradable hydrophilic polymer and the water-soluble monovinyl monomer such that the biologically active macromolecule is entrapped therein.
    Type: Grant
    Filed: May 16, 1986
    Date of Patent: May 3, 1988
    Assignee: The University of Kentucky Research Foundation
    Inventors: Patrick P. De Luca, Frantisek Rypacek
  • Patent number: 4740375
    Abstract: This disclosure recognizes the fact that the technology of making vesicles from lecithin and lecithin-like molecules, although well known and highly developed, is associated with problems of instability. It is known that vesicles coalesce, rupture and spill their contents long before the vesicle is used for its intended purpose.It has been discovered and disclosed herein that the deterioration of the vesicle delivery system is due in part to the rupture of the bipolar lipid vesicle membrane by the contents of the core volume or by an external agent. For example, the more detergent-like the properties of the pharmacological agent within the vesicle core volume, the more pronounced will be the attack on the vesicle wall interior. These events in turn will lead to vesicle membrane rupture.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: April 26, 1988
    Assignee: Technology Unlimited, Inc.
    Inventors: W. Blair Geho, John R. Lau
  • Patent number: 4732763
    Abstract: Antibody or antigen containing microparticles for the active or passive immunization of the internal female reproductive organs, comprising: microparticles of an antigen or antibody incorporated in a matrix material which is biocompatible and biologically degradable, said microparticles capable of being transported after deposition in the vagina by the natural transport mechanism of the internal female reproductive organs across the cervix into the uterus.
    Type: Grant
    Filed: September 28, 1984
    Date of Patent: March 22, 1988
    Assignee: Stolle Research and Development Corporation
    Inventors: Lee R. Beck, Charles F. Flowers, Donald R. Cowsar, Albert C. Tanquary
  • Patent number: 4726966
    Abstract: This invention provides a simple method for preparing granular ibuprofen microsphere whose surface is coated with acrylic acid resin. By this method granulation of ibuprofen and coating of its surface can be simultaneously accomplished. Namely, the method of preparation includes the steps of: (a) dissolving ibuprofen with acrylic acid resin into lower aliphatic alcohol, acetone, methylene chloride or N,N-dimethylformamide; and (b) depositing coated granular ibuprofen microsphere by mixing the solution of step (a) with water and by stirring the mixed solution.
    Type: Grant
    Filed: November 25, 1986
    Date of Patent: February 23, 1988
    Assignee: Showa Shinyaku Co., Ltd.
    Inventors: Yoshiaki Kawashima, Hirofumi Takeuchi, Toshiyuki Niwa, Tetsurou Handa
  • Patent number: 4722838
    Abstract: This invention relates to a self-microencapsulating pesticidal composition consisting essentially of a solution of a polymeric barrier material in an organic solvent system, a dissolved or dispersed pesticidal agent and a surfactant.
    Type: Grant
    Filed: May 9, 1986
    Date of Patent: February 2, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Stan Tocker
  • Patent number: 4719112
    Abstract: Foam capsules with telescopically engaged body and cap portions, also known as hard shell capsules, having a special wall structure, obtained by a microdispersion of a gas in a gelatin solution.The capsule body and cap portions are formed by dipmolding the film-forming mixture obtained by a microdispersion of the gas in a gelatin solution; optionally with the inclusion of a plasticizer and/or coloring agent, and/or flavoring agent, and/or foam stabilizer, and/or gelatin extender.By a suitable choice of the gas proportion in the capsule wall and its micronization level, it is possible, within certain limits, to control the capsule wall disintegration speed and its opacity. In addition, inclusion of gas bubbles into the capsule wall lowers the gelatin content for a foam capsule and provides energy saving during the process due to a faster drying of the wall, thereby providing lower cost prices for the production of pharmaceutically acceptable capsules.
    Type: Grant
    Filed: August 19, 1985
    Date of Patent: January 12, 1988
    Assignee: Warner-Lambert Company
    Inventors: Jean P. Mayer, Fritz Wittwer
  • Patent number: 4711782
    Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.
    Type: Grant
    Filed: December 11, 1986
    Date of Patent: December 8, 1987
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Okada, Yasuaki Ogawa, Takatsuka Yashiki
  • Patent number: 4698264
    Abstract: A solid, water-dispersible, delayed-release particulate composition comprising: a matrix composition, a relatively small amount of an active ingredient insoluble in and uniformly distributed through the matrix composition, the matrix composition comprising: a normally solid, slowly water soluble or slightly water soluble salt selected from the group consisting of alkali metal and calcium phosphates, citrates, tartrates and carbonates, and hydrates thereof, and readily cold water soluble bulking agent.
    Type: Grant
    Filed: May 3, 1985
    Date of Patent: October 6, 1987
    Assignee: Durkee Industrial Foods, Corp.
    Inventor: James A. Steinke
  • Patent number: 4690825
    Abstract: Delivery vehicles comprised of a polymeric bead having a network of pores with an active ingredient held within the network are provided for use in a method to provide controlled release of the active ingredient. The network of pores is substantially non-collapsible upon removal of the active ingredient and the delivery vehicles are polymerized by a process in which the active ingredient also comprises the porogen during formation of the network of pores.
    Type: Grant
    Filed: October 4, 1985
    Date of Patent: September 1, 1987
    Assignee: Advanced Polymer Systems, Inc.
    Inventor: Richard Won
  • Patent number: 4690786
    Abstract: A process for producing a microcapsule containing a liquid active material is described, comprising the steps of:(1) dissolving in an organic solvent a polymer, esp. a polysulfone and an active material which has a limited solubility of about 0.01 to about 2 parts by weight in 100 parts by weight of said polymer and which is liquid at room temperature, the amount of said liquid active material added being more than the limited solubility and being about 2 to about 250 parts by weight per 100 parts by weight of the polymer and said organic solvent being capable of dissolving the respective components and being more volatile than said active material;(2) atomizing the resulting solution through a nozzle into a gaseous atmosphere to form a mist of tiny liquid droplets; and(3) removing the solvent from the droplets by evaporation so as to provide a microcapsule having the liquid active material confined by the wall of said microcapsule made of the polymer.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: September 1, 1987
    Assignee: Nitto Electric Industrial Co., Ltd.
    Inventors: Yasuo Ninomiya, Chiaki Komamura, Yoshikazu Musa
  • Patent number: 4677003
    Abstract: The present invention relates to a sequential polymerization process for preparing a water-insoluble dispersion of core/shell particles. In one embodiment the process may be employed to produce a particulate dispersion useful in making water-based coating compositions wherein on drying the particulate dispersion serves as an opacifying agent. In another embodiment the process may be employed to microencapsulate a hydrophobic target material, such as a biocide or herbicide.
    Type: Grant
    Filed: April 30, 1985
    Date of Patent: June 30, 1987
    Assignee: Rohm and Haas Company
    Inventors: George H. Redlich, Ronald W. Novak
  • Patent number: 4675189
    Abstract: This invention concerns novel sustained release microcapsule compositions comprising water-soluble, hormonally active polypeptides and, optionally, a polymer hydrolysis modifying agent encapsulated in a biocompatible, biodegradable polymer.
    Type: Grant
    Filed: February 8, 1985
    Date of Patent: June 23, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John S. Kent, Danny H. Lewis, Lynda M. Sanders, Thomas R. Tice
  • Patent number: 4671954
    Abstract: Novel hydrophilic protein or polypeptide microspheres prepared by dispersing an aqueous solution or dispersion of protein or polypeptide in an organic solvent solution of a high molecular weight polymer to form a stabilized dispersion of microspheres and cross-linking said microspheres with a polyfunctional cross-linking agent.
    Type: Grant
    Filed: February 4, 1986
    Date of Patent: June 9, 1987
    Assignee: University of Florida
    Inventors: Eugene P. Goldberg, William E. Longo, Hiroo Iwata
  • Patent number: 4670246
    Abstract: A sprayable insecticidal composition of low fish toxicity of a mixture in water of microcapsules comprised of a pyrethroid (synthetic pyrethrin) contained within an encapsulating wall of a cross-linked polymeric material, and methods of preparation and method of use of the composition on a wide variety of crops and aquatic sites infested with a broad spectrum of undesirable insects.
    Type: Grant
    Filed: April 24, 1985
    Date of Patent: June 2, 1987
    Assignee: Pennwalt Corporation
    Inventors: Gerd H. Dahl, Joseph Simkin
  • Patent number: 4670250
    Abstract: Impact-resistant microcapsules for the sustained and controlled release of biologically active ingredients through a surrounding permeable polymeric wall are disclosed wherein the ratio by weight of active ingredient to polymer is from about 4:1 to about 1:4, the polymeric walls having high tensile yield and tensile impact strengths and low nitrogen permeabilities.
    Type: Grant
    Filed: October 21, 1983
    Date of Patent: June 2, 1987
    Assignee: Bend Research, Inc.
    Inventor: Richard W. Baker
  • Patent number: 4666641
    Abstract: The present invention relates to biodegradable microcapsules based on serum albumin, the preparation thereof and the application thereof to the release of drugs in situ.A feature of the microcapsules according to the present invention is that their wall consists of serum albumin, a portion of which is crosslinked by interfacial polymerization with the aid of an acylating bifunctional reagent, and the other, non-crosslinked portion of which is denatured by means of an alcohol.
    Type: Grant
    Filed: June 4, 1985
    Date of Patent: May 19, 1987
    Assignee: Universite Paris-Sud (Paris XI)
    Inventors: Rene Fickat, Simon Benita, Francis Puisieux
  • Patent number: 4663308
    Abstract: Polymers from ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene are useful as carriers or capsules for medicaments, which are degraded by the enzymes of the upper gastrointestinal tract or which must be transferred intact past the upper gastrointestinal tract, to deliver the medicament to the large intestine.Polymers containing monomeric units of the formulaH.sub.2 C.dbd.CH--C.sub.6 H.sub.4 --N.dbd.N--M,wherein M is the residue of an amino-containing medicament, are useful as carriers for therapeutic agents or as therapeutic agents per se.
    Type: Grant
    Filed: July 18, 1984
    Date of Patent: May 5, 1987
    Assignees: Medical College of Ohio, Bowling Green State University
    Inventors: Murray Saffran, Douglas C. Neckers
  • Patent number: 4652441
    Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.
    Type: Grant
    Filed: November 1, 1984
    Date of Patent: March 24, 1987
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Okada, Yasuaki Ogawa, Takatsuka Yashiki
  • Patent number: 4643764
    Abstract: In a process of encapsulating water-immiscible material within discrete capsules of polyurea without addition of a second reactant, whereby hydrolysis of an isocyanate monomer to form an amine takes place which in turn reacts with another isocyanate monomer to form polyurea, which comprises the steps(a) providing at room temperature a dispersion of(i) a water-immiscible phase comprising the water-immiscible material to be encapsulated and organic polyisocyanates in(ii) an aqueous phase comprising a solution of water, a surfactant and a protective colloid; and(b) heating and maintaining said dispersion in a temperature range of about 40.degree. C. to about 90.degree. C.
    Type: Grant
    Filed: January 31, 1985
    Date of Patent: February 17, 1987
    Assignee: Stauffer Chemical Company
    Inventor: Herbert B. Scher
  • Patent number: 4637905
    Abstract: A process for preparing polylactide (PLA) microcapsules is described and involves dissolving PLA in a mixture of two miscible organic liquids, the higher vapor pressure liquid having solvent power for PLA and the second having little or no solvent power for PLA. The solution is prepared such that it is near its saturation point for PLA. Encapsulation of dispersed core material is achieved by vaporizing the liquid having solvent power for PLA causing phase separation of the PLA, then transferring the separated dispersion to an organic liquid having no solvent power for the PLA in order to harden the encapsulating coating. The disclosed process enables forming true microcapsules or reservoir-type devices encapsulating liquid core material particularly aqueous liquid core material and oil in water emulsion or suspensions.
    Type: Grant
    Filed: April 11, 1985
    Date of Patent: January 20, 1987
    Assignee: Batelle Development Corporation
    Inventor: David L. Gardner
  • Patent number: 4632843
    Abstract: A process for the preparation of solid pharmaceutical products, wherein, in a first step, spherical single crystals of a pharmaceutical active compound or assistant are prepared by agitating a saturated aqueous, organic or organic-aqueous solution in high speed stirred crystallizers or draft-tube crystallizers at 50-500 revolutions per minute and seeding the solution with finely ground seed crystals of particle size less than 100 .mu.m, while ensuring that at the time of addition of the seed crystals and during the growth thereof the solution is at all times only minimally supersaturated, this being achieved by slow cooling at a rate of not more than 50 K/h or corresponding slow evaporation of the solution, and in a second step the resulting spherical single crystals with diameters of 0.1-3 mm, preferably 0.5-2 mm, are separated from the solution, dried at 40.degree.-200.degree. C.
    Type: Grant
    Filed: February 21, 1984
    Date of Patent: December 30, 1986
    Assignee: BASF Aktiengesellschaft
    Inventors: Claus H. Pich, Thomas Moest
  • Patent number: 4622244
    Abstract: Microcapsules particularly those less than 300 microns in size are provided which are adapted for injection by conventional means to afford controlled release of the encapsulated drug material, such as a narcotic antagonist, an antibiotic or the like, over a prolonged period. The microcapsules are characterized by a solid core material of a solid, injectable drug material and a wall material engulfing the core material and composed of a polymer material such as a bioabsorbable polymer material. The microcapsules are made by providing a system containing a mixture of particles of a solid, injectable drug material and a solution of a bioabsorbable polymer material in a solvent in which the drug material is substantially insoluble. The system is treated to induce phase separation of the bioabsorbable polymer material from the solution by the addition to the system of a phase separation agent at a temperature at least as low as -30.degree. C.
    Type: Grant
    Filed: August 23, 1984
    Date of Patent: November 11, 1986
    Assignee: The Washington University
    Inventors: Galen G. Lapka, Norbert S. Mason, Curt Thies
  • Patent number: 4590065
    Abstract: A dentifrice composition that reduces the migration/absorption of flavor into plastic packaging materials, containing a flavor oil in combination with about 5.0%-50.0% and preferably 12.0% by weight of the total flavor oils of polyvinyl pyrrolidone (PVP), dispersed in a dental vehicle. The dentifrice composition may be in the form of a paste, cream or gel. It is essential that the flavor oil and PVP be premixed prior to its addition to the dentifrice composition, preferably as a final step in its formulation.
    Type: Grant
    Filed: April 18, 1985
    Date of Patent: May 20, 1986
    Assignee: Colgate-Palmolive Company
    Inventors: Stanley E. Piechota, Jr., Dorinda A. Sparacio
  • Patent number: 4590063
    Abstract: Compounds of the formula ##STR1## where R is a methyl, ethyl or propyl group and n is 1 or 2 and their nontoxic salts are useful as anticonvulsants.
    Type: Grant
    Filed: April 25, 1985
    Date of Patent: May 20, 1986
    Assignee: Adria Laboratories, Inc.
    Inventors: John P. Carter, Jr., Richard L. Wolgemuth
  • Patent number: 4585651
    Abstract: Antibody or antigen containing microparticles for the active or passive immunization of the internal female reproductive organs, comprising: microparticles of an antigen or antibody incorporated in a matrix material which is biocompatible and biologically degradable, said microparticles capable of being transported after deposition in the vagina by the natural transport mechanism of the internal female reproductive organs across the cervix into the uterus.
    Type: Grant
    Filed: December 18, 1980
    Date of Patent: April 29, 1986
    Assignee: Stolle Research & Development Corporation
    Inventors: Lee R. Beck, Charles F. Flowers, Jr., Donald R. Cowsar, Albert C. Tanquary