GB1116670A - Process for the manufacture of pharmaceutical preparations in bead form - Google Patents

Process for the manufacture of pharmaceutical preparations in bead form

Info

Publication number
GB1116670A
GB1116670A GB25691/65A GB2569165A GB1116670A GB 1116670 A GB1116670 A GB 1116670A GB 25691/65 A GB25691/65 A GB 25691/65A GB 2569165 A GB2569165 A GB 2569165A GB 1116670 A GB1116670 A GB 1116670A
Authority
GB
United Kingdom
Prior art keywords
acid
mixture
medicament
bead
methyl methacrylate
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
GB25691/65A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
BASF Schweiz AG
Original Assignee
Ciba AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ciba AG filed Critical Ciba AG
Publication of GB1116670A publication Critical patent/GB1116670A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F2/00—Processes of polymerisation
    • C08F2/44—Polymerisation in the presence of compounding ingredients, e.g. plasticisers, dyestuffs, fillers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/06—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of pills, lozenges or dragees
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Polymers & Plastics (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)

Abstract

A process for the manufacture of a pharmaceutical preparation in bead form comprises subjecting a mixture of a synthetic monomer and an organic medicament to bead polymerization, the mixture being capable when polymerized of yielding a physiologically tolerable polymeric material that is capable of being dissolved in or swollen by stomach and/or intestinal juices. Preferred monomers comprise methyl methacrylate and mixtures of methacrylic acid and methyl methacrylate, methacrylic acid and divinylbenzene with or without methyl methacrylate, acrylic acid and methyl acrylate, vinyl acetate and crotonic acid, styrene and acrylic acid and/or maleic anhydride, vinyl methyl ether and maleic anhydride and/or fumaric acid and/or itaconic acid. The polymerization mixture may contain conventional fillers, swelling agents, electrolytes, and surface active agents. The medicament may be coated in wax or fat, and synthetic resins that are insoluble in and not swollen by the stomach and/or intestinal juices may be included in the polymerization mixture. Bead polymerization may be effected by dispersing the synthetic monomer-medicament mixture in a dispersion medium with which it is immiscible, e.g. water, in such a manner that beads having the desired degree of fineness are obtained, polymerization being carried out at room temperature or above generally with the aid of a catalyst, e.g. benzoyl peroxide, t-butyl hydroperoxide or azodiisobutyronitrile, and, optionally, an accelerator, e.g. a tertiary amine, an iron, manganese or cobalt compound, a sulphinic acid or a sulphite, and a dispersing agent, e.g. sodium polyacrylate or polyethylene glycol. A preformed polymer may also be present, e.g. a vinylacetate/crotonic acid copolymer or an ethyl acrylate/t-butyl-acrylamide/acrylic acid copolymer.ALSO:A process for the manufacture of a pharmaceutical preparation in bead form comprises subjecting a mixture of a synthetic monomer and an organic medicament to bead polymerisation, the mixture being capable when polymerised of yielding a physiologically tolerable polymeric material that is capable of being dissolved in or swollen by stomach and/or intestinal juices. Preferred monomers comprise methyl methacrylate and mixtures of methacrylic acid and methyl methacrylate, methyl methacrylate and divinyl benzene, acrylic acid and methyl acrylate, vinyl acetate and crotonic acid, styrene and acrylic acid and/or maleic anhydride, vinyl methyl ether and maleic acid anhydride and/or fumaric acid and/or itaconic acid. Exemplified medicaments comprise 5 - (1-cyclohexenyl) - 5 - ethyl calcium barbiturate, acetyl para - phenetidine, 2 - ethyl - 2 - phenylglutarimide, papaverine, 4 - dimethylamino - 1 - phenyl - 2, 3 - dimethyl pyrozolone - 5, hydrocortisone, N - [6 - methoxy - 2 (methoxy - methyl) - 4 - pyrimidinyl] - sulphanilamide, and the sodium salt of 3 - acetylamino - 2,4,6 - triiodobenzoic acid. The preparations may contain conventional fillers, swelling agents, electrolytes, and surface active agents. The medicament may be coated in wax or fat, and synthetic resins that are insoluble in and not swollen by the stomach and/or intestinal juices may be included in the preparations. Bead polymerisation may be effected by dispersing the medicament - synthetic monomer mixture in a dispersion medium with which it is imiscible in such a manner that beads having the desired degree of fineness are obtained, polymerisation being carried out at room temperature or above generally with the aid of a catalyst and an accelerator. The preparations may be used in the form of granules, in capsules, in a liquid suspension medium, or in tablet form together with suitable adjuvants.
GB25691/65A 1964-06-19 1965-06-17 Process for the manufacture of pharmaceutical preparations in bead form Expired GB1116670A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH806264A CH468192A (en) 1964-06-19 1964-06-19 Process for the manufacture of medicaments in pearl form
CH705065 1965-05-20

Publications (1)

Publication Number Publication Date
GB1116670A true GB1116670A (en) 1968-06-12

Family

ID=25700654

Family Applications (1)

Application Number Title Priority Date Filing Date
GB25691/65A Expired GB1116670A (en) 1964-06-19 1965-06-17 Process for the manufacture of pharmaceutical preparations in bead form

Country Status (6)

Country Link
US (1) US3390050A (en)
BE (1) BE665607A (en)
CH (1) CH468192A (en)
DE (1) DE1467843A1 (en)
FR (1) FR1468716A (en)
GB (1) GB1116670A (en)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA927282A (en) * 1968-09-03 1973-05-29 S. Banker Gilbert Entrapment compositions and processes
CA935092A (en) * 1968-09-03 1973-10-09 S. Banker Gilbert Molecular drug entrapment process and compositions
USRE28316E (en) * 1968-09-03 1975-01-21 Entrapment compositions and processes
DE2037947C3 (en) * 1969-08-01 1983-01-13 Bush Boake Allen Ltd., London Encapsulated preparations
FR2407720A1 (en) * 1977-11-08 1979-06-01 Lipha Lyonnaise Indle Pharmace Oral sustained-action capsule formulations - of drug and excipient which swells in contact with digestive juices
US4539199A (en) * 1981-01-14 1985-09-03 Egyt Gyogyszervegyeszeti Gyar Sustained release pharmaceutical compositions
ES259491Y (en) * 1981-07-15 1982-07-01 GARDENING
EP0076158B1 (en) * 1981-09-30 1989-10-25 National Research Development Corporation Compositions comprising encapsulated particles
US4649043A (en) * 1982-03-22 1987-03-10 Alza Corporation Drug delivery system for delivering a plurality of tiny pills in the gastrointestinal tract
US4764380A (en) * 1982-03-22 1988-08-16 Alza Corporation Drug delivery system comprising a volume increasing matrix containing a plurality of tiny pills
US4642233A (en) * 1982-03-22 1987-02-10 Alza Corporation Gastrointestinal drug delivery system comprising a hydrogel reservoir containing a plurality of tiny pills
US4659558A (en) * 1982-03-22 1987-04-21 Alza Corporation Oral delivery system comprising a plurality of tiny pills for delivering drug in the stomach and intestine
JPS5965009A (en) * 1982-10-05 1984-04-13 Chisso Corp Prolonged release type vasodilator
DE3314003A1 (en) * 1983-04-18 1984-10-18 Boehringer Ingelheim KG, 6507 Ingelheim DIVISIBLE TABLET WITH DELAYED ACTIVE SUBSTANCE RELEASE AND METHOD FOR THE PRODUCTION THEREOF
US4548990A (en) * 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US4795436A (en) * 1983-11-14 1989-01-03 Bio-Mimetics, Inc. Bioadhesive composition and method of treatment therewith
US4983392A (en) * 1983-11-14 1991-01-08 Bio-Mimetics, Inc. Bioadhesive compositions and methods of treatment therewith
GB8331546D0 (en) * 1983-11-25 1984-01-04 Exxon Research Engineering Co Polymeric compositions
EP0143608B1 (en) * 1983-11-25 1992-07-22 Ciba Specialty Chemicals Water Treatments Limited Manufacture and use of polymeric beads
US4749576A (en) * 1984-05-10 1988-06-07 Ciba-Geigy Corporation Active agent containing hydrogel devices wherein the active agent concentration profile contains a sigmoidal concentration gradient for improved constant release, their manufacture and use
US4624848A (en) * 1984-05-10 1986-11-25 Ciba-Geigy Corporation Active agent containing hydrogel devices wherein the active agent concentration profile contains a sigmoidal concentration gradient for improved constant release, their manufacture and use
DE3524337A1 (en) * 1985-07-08 1987-01-08 Roehm Gmbh MEDICINAL PACKAGING
US4690825A (en) * 1985-10-04 1987-09-01 Advanced Polymer Systems, Inc. Method for delivering an active ingredient by controlled time release utilizing a novel delivery vehicle which can be prepared by a process utilizing the active ingredient as a porogen
US5246714A (en) * 1985-10-11 1993-09-21 Aktiebolaget Hassle Drug preparation
US4940556A (en) * 1986-01-30 1990-07-10 Syntex (U.S.A.) Inc. Method of preparing long acting formulation
US5198226A (en) * 1986-01-30 1993-03-30 Syntex (U.S.A.) Inc. Long acting nicardipine hydrochloride formulation
DE3608721A1 (en) * 1986-03-15 1987-09-17 Hoelter Heinz Method for improving the service life of chemisorption compositions
NZ220599A (en) * 1986-06-16 1990-10-26 Merck & Co Inc Controlled release oral dosage formulation of carbidopa and levodopa
US4851232A (en) * 1987-02-13 1989-07-25 Alza Corporation Drug delivery system with means for obtaining desirable in vivo release rate pattern
US5030454A (en) * 1987-10-26 1991-07-09 Alza Corporation Method for delivering drug in tiny pills in liquid carrier
US4853229A (en) * 1987-10-26 1989-08-01 Alza Corporation Method for adminstering tiny pills
US4961932A (en) * 1987-10-26 1990-10-09 Alza Corporation Plurality of tiny pills in liquid dosage form
US5055300A (en) * 1988-06-17 1991-10-08 Basic Bio Systems, Inc. Time release protein
US5023080A (en) * 1988-06-17 1991-06-11 Basic Bio Systems, Inc. Time release protein
US5079005A (en) * 1988-06-17 1992-01-07 Gupta Kashmiri L Time release protein
US5139787A (en) * 1989-01-19 1992-08-18 Wm. Wrigley Jr. Company Gum composition containing dispersed porous beads containing active chewing gum ingredients and method
US4963369A (en) * 1989-01-19 1990-10-16 Wm. Wrigley Jr. Co. Gum composition containing dispersed porous beads containing active chewing gum ingredients and method
US5154927A (en) * 1989-01-19 1992-10-13 Wm. Wrigley Jr. Company Gum composition containing dispersed porous beads containing active chewing gum ingredients and method
US5126174A (en) * 1989-02-16 1992-06-30 Wm. Wrigley Jr. Company Food packaging improvements
US5064698A (en) * 1989-02-16 1991-11-12 Wm. Wrigley, Jr. Company Food packaging improvements
US5007790A (en) * 1989-04-11 1991-04-16 Depomed Systems, Inc. Sustained-release oral drug dosage form
ES2050096T3 (en) 1989-10-31 1995-01-16 Columbia Lab Inc HUMIDIFYING COMPOSITION OF THE VAGINAL TISSUE.
DE4029591C2 (en) * 1990-09-19 1995-01-26 Stockhausen Chem Fab Gmbh Process for the preparation of polymer-based absorption material with the addition of water-soluble substances and use of this absorption material for the absorption and / or subsequent release of water or aqueous solutions
US5154938A (en) * 1990-12-20 1992-10-13 Wm. Wrigley Jr. Company Gum composition having dispersed porous beads containing plasticizers

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2846057A (en) * 1954-02-09 1958-08-05 Polin Herbert Spencer Devices for dosage control
US2810716A (en) * 1954-06-28 1957-10-22 White Lab Inc Batchwise copolymerization technique
US3092553A (en) * 1959-01-30 1963-06-04 Jr Carl E Fisher Pharmaceutical preparations and method and apparatus for making same
US3162573A (en) * 1959-10-14 1964-12-22 Plants Products Corp Internal treatment of animals with resin biocidal compositions
US3074795A (en) * 1959-11-12 1963-01-22 Pfizer & Co C Production of bacitracin adsorbate and process of administration to animals for promoting growth
US3121043A (en) * 1960-05-11 1964-02-11 Scient Associates Inc Sustained release pharmaceutical preparation and methods for making same
US3158538A (en) * 1961-02-23 1964-11-24 White Lab Inc Antidiarrheal compositions and method of using
US3202577A (en) * 1962-05-25 1965-08-24 White Lab Inc Process of treating diarrhea with resins
US3247066A (en) * 1962-09-12 1966-04-19 Parke Davis & Co Controlled release dosage form containing water-swellable beadlet
US3328256A (en) * 1963-05-27 1967-06-27 William E Gaunt Spherical beads and their production

Also Published As

Publication number Publication date
BE665607A (en) 1965-12-20
DE1467843A1 (en) 1968-12-12
US3390050A (en) 1968-06-25
CH468192A (en) 1969-02-15
FR1468716A (en) 1967-02-10

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