US3395211A - Tableting process - Google Patents

Tableting process Download PDF

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Publication number
US3395211A
US3395211A US513094A US51309465A US3395211A US 3395211 A US3395211 A US 3395211A US 513094 A US513094 A US 513094A US 51309465 A US51309465 A US 51309465A US 3395211 A US3395211 A US 3395211A
Authority
US
United States
Prior art keywords
tablets
tablet
granulation
abrasive
die
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 - Lifetime
Application number
US513094A
Other languages
English (en)
Inventor
Wielich Kurt Hans
Henry B Zimmerman
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.)
Meda Pharmaceuticals Inc
Original Assignee
Carter Wallace Inc
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 Carter Wallace Inc filed Critical Carter Wallace Inc
Priority to US513094A priority Critical patent/US3395211A/en
Priority to GB49515/66A priority patent/GB1113299A/en
Priority to FR83129A priority patent/FR1499681A/fr
Priority to DE19661617389 priority patent/DE1617389A1/de
Priority to JP7621666A priority patent/JPS4522959B1/ja
Priority to SE16043/66A priority patent/SE305509B/xx
Priority to DK611766AA priority patent/DK118420B/da
Priority to NO165942A priority patent/NO122269B/no
Application granted granted Critical
Publication of US3395211A publication Critical patent/US3395211A/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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
    • A61J3/10—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
    • 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
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing

Definitions

  • ABSTRACT OF THE DISCLOSURE A two-cycle tableting process for producing compressed tablets containing a low-melting or adhesive active medicinal material which comprises introducing into the tablet die a first granulation containing an abrasive material, compressing :and ejecting the resulting tablet, introducing into the same die a second granulation containing the lowmelting or adhesive material, compressing and ejecting the resulting tablet. The cycle can be repeated until the desired number of tablets is obtained.
  • the present invention relates to a tableting process. More particularly, the invention rel-ates to a novel tableting process which makes it possible to produce acceptable tablets from materials or combinations which, under standard operating conditions, would normally tend to adhere to the dies and punches of a tableting machine.
  • the invention relates to a method of producing acceptable compressed tablets from a tablet granulation containing a low-melting or adhesive material, said method comprising the steps of:
  • tybamate chemically, Z-methyl 2 propyltrimethylene butylcarbamate carbamate
  • mephenesin guaianesin
  • theophylline meprobamate-aluminum hydroxide combinations, and the like.
  • the terms low and high as applied to the compression forces used during the tableting of, respectively, the production tablets and the abrasive tablets, signify compression forces which are lower or higher than those commonly used during standard tableting operations.
  • suitable tablets can be prepared from low melting or adhesive materials by employing a compression force, as measured at the punch face, in the range of from about 2 to about 8 tons per square inch and preferably about 4 tons per square inch.
  • Said forces which are unusually low by pharmaceutical tableting standards, would normally yield tablets which would adhere to the dies and punch faces of the tableting machine and which consequently, would be physically deformed.
  • Such low compression forces are utilized in the process of the invention, there are produced elegant tablets which have suitable disintegration and dissolution rates.
  • the high compression forces used in the preparation of the abrasive tablets are in the range of from about 15 to about 25 tons per square inch and higher.
  • the upper limit is generally determined by the physical capabilities of the tableting machine employed in the process since it has been found that, the higher the compression force, the better the cleaning effect will be on the punch and die walls.
  • the abrasive materials which are used in the present process are materials which are sufficiently abrasive as to effectively clean the die walls and punch faces without damaging same. In addition, for the sake of avoiding contamination, it is preferred that said materials be non-toxic. Furthermore, for efficiency and economy, preferred materials should be easily compressible into coherent tablets, preferably without the need of complicated granulation stages.
  • Suitable abrasive materials useful in the practice of the invention include, for example, lactose, wood cellulose, magnesium hydroxide, tricalcium phosphate, dicalcium phosphate, and mixtures thereof.
  • compositions I-IV can be tableted directly after the components thereof are intimately admixed whereas composition V should be subjected to a stagewise granulation prior to tableting in a manner known in the art.
  • the percentages in parenthesis indicate the most preferred compositions.
  • Composition I Components: Weight percent Anhydrous lactose (75) 65-90 Wood cellulose (24.5) 10-35 Magnesium stearate (0.5) 0.5-1.0
  • Composition II Components: Weight percent Anhydrous lactose (75) 65-90 Magnesium hydroxide (24.5) 10-35 Magnesium stearate (0.5) 0.5-1.0
  • Composition III Components: Weight percent Anhydrous lactose (75 65-90 Wood cellulose (12.5) 5-18 Magnesium hydroxide (12.0) 5-18 Magnesium stearate (0.5) 0.5-1.0
  • composition IV The low melting or adhesive materials are prepared for tableting in accordance with the present invention in manners well known to those skilled in the art by combining the active material with conventional excipients.
  • a suitable granulation to be compressed into acceptable tablets according to the present teachings would contain at least 50 percent by weight of the low melting or adhesive material, from about to about 30 percent by weight of a suitable filler, from about 5 to about percent by weight of a disintegrating agent, from about 2 to about 15 percent by weight of a binding agent, and from about 1 to about 5 percent by weight of a lubricant.
  • a preferred granulation for compounding tybamate granules into tablets has the following composition:
  • the process of the invention is conveniently carried out in a standard double rotary tablet press, with a plurality of dies arranged to compress and eject two tablets per die per revolution of the head.
  • Two feed hoppers are provided, one filled with the abrasive composition and the other with the production granulation.
  • the press is adjusted so that, during the first half revolution of the head, each successive die is filled with the abrasive material which is then compressed into a tablet at a pressure of from about 15 to tons per square inch and at a punch penetration of about inch or more.
  • the tablets thus formed are then ejected and collected into a suitable container.
  • the cycle is then repeated during the second half revolution of the head, using the production granulation and compressing same into tablets at a pressure of from about 2 to about 8 tons per square inch and with a punch penetration of about A: inch or less.
  • abrasive tablets produced can, of course, be crushed by any suitable means and the resulting material reused in the practice of the invention.
  • Tybamate tablets were produced according to the practice of the invention.
  • the tybamate granulation was prepared by coating 67.0 parts of tybamate powder with 3.5 parts of gelatin (applied as a 10% solution). After the resulting granules were dried, they were admixed with 13 parts of Wood cellulose and again coated with 1.5 parts of starch (applied as a paste having a 5% starch concentration). The final granulation was obtained by admixing the dried double-coated granules with 3.0 parts of Wood cellulose, 10.5 parts of starch and 1.5 parts of stearic acid.
  • the granulation was compressed into tablets using a standard double rotary tablet press equipped with dies of inch diameter.
  • the abrasive material used had the following composition.
  • Tablets were compressed from the tybamate granulation and from the abrasive material according to the present invention.
  • the punch penetration for the production tablets was maintained at inch while the compression force was varied as indicated below. In tableting the abrasive material, the punch penetration and the compression force were maintained at inch and 22 tons per square inch respectively.
  • tybamate tablets thus produced were examined visually and samples thereof were then tested for disintegration using the U.S.P. XVI method for disintegration.
  • the tablets produced in accordance with the present invention also possess excellent disintegration rates.
  • the present process will also permit the compression of other soft materials used in the pharmaceutical industry, such as suppositories.
  • a suitable granulation made of suppository medicaments and excipients may be compressed according to the claimed method by using suitable dies and punches to produce the conventional suppository shapes.
  • Suppository granulations to be compressed may contain, for example, a bismuth salt as an astringent, benzocain as a local anesthetic, and meprobamate as a tranquillizer.
  • the medicaments may be granulated with a CarboWax-4000 to 6000 and suitable fillers as excipients.
  • Effervescent laxative suppository compositions containing CarboWax-6000, sodium bicarbonate and sodium biphosphate have been compressed according to the method of the present invention.
  • a method of producing compressed tablets from a tablet granulation containing a low-melting or adhesive active medicinal material comprising the steps of:
  • a method of producing compressed tablets from a tablet granulation containing tybamate comprising the steps of:

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Medicinal Preparation (AREA)
  • Medical Preparation Storing Or Oral Administration Devices (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
US513094A 1965-12-10 1965-12-10 Tableting process Expired - Lifetime US3395211A (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
US513094A US3395211A (en) 1965-12-10 1965-12-10 Tableting process
GB49515/66A GB1113299A (en) 1965-12-10 1966-11-04 Tablets
FR83129A FR1499681A (fr) 1965-12-10 1966-11-09 Procédé de production de comprimés
DE19661617389 DE1617389A1 (de) 1965-12-10 1966-11-12 Tablettenherstellungsverfahren
JP7621666A JPS4522959B1 (enrdf_load_stackoverflow) 1965-12-10 1966-11-21
SE16043/66A SE305509B (enrdf_load_stackoverflow) 1965-12-10 1966-11-23
DK611766AA DK118420B (da) 1965-12-10 1966-11-25 Fremgangsmåde til fremstilling af pressede tabletter.
NO165942A NO122269B (enrdf_load_stackoverflow) 1965-12-10 1966-12-09

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US513094A US3395211A (en) 1965-12-10 1965-12-10 Tableting process

Publications (1)

Publication Number Publication Date
US3395211A true US3395211A (en) 1968-07-30

Family

ID=24041866

Family Applications (1)

Application Number Title Priority Date Filing Date
US513094A Expired - Lifetime US3395211A (en) 1965-12-10 1965-12-10 Tableting process

Country Status (8)

Country Link
US (1) US3395211A (enrdf_load_stackoverflow)
JP (1) JPS4522959B1 (enrdf_load_stackoverflow)
DE (1) DE1617389A1 (enrdf_load_stackoverflow)
DK (1) DK118420B (enrdf_load_stackoverflow)
FR (1) FR1499681A (enrdf_load_stackoverflow)
GB (1) GB1113299A (enrdf_load_stackoverflow)
NO (1) NO122269B (enrdf_load_stackoverflow)
SE (1) SE305509B (enrdf_load_stackoverflow)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040105896A1 (en) * 1997-09-19 2004-06-03 Crosfield Limited Metal compunds, mixed or sulphated, as phosphate binders
US20090317459A1 (en) * 2006-01-31 2009-12-24 Ineos Healthcare Limited Material
US20100203152A1 (en) * 2007-07-27 2010-08-12 Ineos Healthcare Kimited Mixed metal compounds used as antacids
US20100215770A1 (en) * 2007-10-16 2010-08-26 Maurice Sydney Newton Mixed metal compounds for treatment of hyperphosphataemia
US9066917B2 (en) 2009-08-03 2015-06-30 Cytochroma Development Inc. Mixed metal compound
US9566302B2 (en) 2010-02-04 2017-02-14 Opko Ireland Global Holdings, Ltd. Composition comprising mixed metal compounds and xanthan gum

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2327655C (en) * 1998-04-08 2010-03-09 Kyowa Hakko Kogyo Co., Ltd. Tablet production method and tablet

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3042531A (en) * 1959-12-09 1962-07-03 Leslie Salt Company Method of making a compressed tablet
US3096248A (en) * 1959-04-06 1963-07-02 Rexall Drug & Chemical Company Method of making an encapsulated tablet
US3116204A (en) * 1961-11-09 1963-12-31 Merck & Co Inc Pharmaceutical compositions and method of preparing the same
US3134719A (en) * 1962-04-05 1964-05-26 American Cyanamid Co Calcium phosphates in tablet compressing
US3175948A (en) * 1963-01-10 1965-03-30 Hoffmann La Roche Multivitamin tablets and premixes
US3293132A (en) * 1963-03-25 1966-12-20 Merck & Co Inc Spray dried vitamin compositions and method of preparation
US3332848A (en) * 1963-07-10 1967-07-25 Hoffmann La Roche Microcrystalline cellulose with starch in niacinamide ascorbic acid tablet granulations
US3344030A (en) * 1964-06-15 1967-09-26 American Home Prod Reinforced directly compressed nongranulated pharmaceutical crystalline lactose tables

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3096248A (en) * 1959-04-06 1963-07-02 Rexall Drug & Chemical Company Method of making an encapsulated tablet
US3042531A (en) * 1959-12-09 1962-07-03 Leslie Salt Company Method of making a compressed tablet
US3116204A (en) * 1961-11-09 1963-12-31 Merck & Co Inc Pharmaceutical compositions and method of preparing the same
US3134719A (en) * 1962-04-05 1964-05-26 American Cyanamid Co Calcium phosphates in tablet compressing
US3175948A (en) * 1963-01-10 1965-03-30 Hoffmann La Roche Multivitamin tablets and premixes
US3293132A (en) * 1963-03-25 1966-12-20 Merck & Co Inc Spray dried vitamin compositions and method of preparation
US3332848A (en) * 1963-07-10 1967-07-25 Hoffmann La Roche Microcrystalline cellulose with starch in niacinamide ascorbic acid tablet granulations
US3344030A (en) * 1964-06-15 1967-09-26 American Home Prod Reinforced directly compressed nongranulated pharmaceutical crystalline lactose tables

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9242869B2 (en) 1997-09-19 2016-01-26 Opko Ireland Global Holdings, Ltd. Metal compounds mixed or sulphated, as phosphate binders
US7799351B2 (en) 1997-09-19 2010-09-21 Ineos Healthcare Limited Metal compounds, mixed or sulphated, as phosphate binders
US20110014301A1 (en) * 1997-09-19 2011-01-20 Ineos Healthcare Limited Metal compounds, mixed or sulphated, as phosphate binders
US8568792B2 (en) 1997-09-19 2013-10-29 Cytochroma Development Inc. Metal compounds, mixed or sulphated, as phosphate binders
US20040105896A1 (en) * 1997-09-19 2004-06-03 Crosfield Limited Metal compunds, mixed or sulphated, as phosphate binders
US9907816B2 (en) 2006-01-31 2018-03-06 Opko Ireland Global Holdings, Ltd. Water-insoluble, iron-containing mixed metal, granular material
US20090317459A1 (en) * 2006-01-31 2009-12-24 Ineos Healthcare Limited Material
US9168270B2 (en) 2006-01-31 2015-10-27 Opko Ireland Global Holdings, Ltd. Water-insoluble, iron-containing mixed metal, granular material
US20100203152A1 (en) * 2007-07-27 2010-08-12 Ineos Healthcare Kimited Mixed metal compounds used as antacids
US10201501B2 (en) 2007-07-27 2019-02-12 Opko Ireland Global Holdings, Ltd. Mixed metal compounds used as antacids
US20100215770A1 (en) * 2007-10-16 2010-08-26 Maurice Sydney Newton Mixed metal compounds for treatment of hyperphosphataemia
US10155040B2 (en) 2007-10-16 2018-12-18 Opko Ireland Global Holdings, Ltd. Mixed metal compounds for treatment of hyperphosphataemia
US9314481B2 (en) 2009-08-03 2016-04-19 Opko Ireland Global Holdings, Ltd. Method
US9066917B2 (en) 2009-08-03 2015-06-30 Cytochroma Development Inc. Mixed metal compound
US9566302B2 (en) 2010-02-04 2017-02-14 Opko Ireland Global Holdings, Ltd. Composition comprising mixed metal compounds and xanthan gum

Also Published As

Publication number Publication date
JPS4522959B1 (enrdf_load_stackoverflow) 1970-08-03
DE1617389A1 (de) 1970-06-25
FR1499681A (fr) 1967-10-27
GB1113299A (en) 1968-05-08
NO122269B (enrdf_load_stackoverflow) 1971-06-07
SE305509B (enrdf_load_stackoverflow) 1968-10-28
DK118420B (da) 1970-08-17

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