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WO2004062647A1 - Simple tablet compression using gelatin - Google Patents

Simple tablet compression using gelatin Download PDF

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Publication number
WO2004062647A1
WO2004062647A1 PCT/US2003/002945 US0302945W WO2004062647A1 WO 2004062647 A1 WO2004062647 A1 WO 2004062647A1 US 0302945 W US0302945 W US 0302945W WO 2004062647 A1 WO2004062647 A1 WO 2004062647A1
Authority
WO
WIPO (PCT)
Prior art keywords
tablet
gelatin
powder
disintegrator
diluent
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.)
Ceased
Application number
PCT/US2003/002945
Other languages
French (fr)
Inventor
Minh Nguyen
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to PCT/US2003/002945 priority Critical patent/WO2004062647A1/en
Priority to CA002477221A priority patent/CA2477221A1/en
Priority to AU2003208918A priority patent/AU2003208918A1/en
Priority to EP03707641A priority patent/EP1587501A4/en
Publication of WO2004062647A1 publication Critical patent/WO2004062647A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2063—Proteins, e.g. gelatin

Definitions

  • This invention relates to tablet preparations.
  • a tablet basically contains: (1) diluent, (2) binder, (3) disintegrator, and (4) lubricant.
  • Diluent is a substance or a mixture of substances added to a tablet to increase the bulk in order to make the tablet a practical size for compression.
  • Binder is a substance or a mixture of substances added to a tablet to impart a cohesiveness to the tablet formulation which insures the tablet remaining intact after compression.
  • Disintegrator is a substance or a mixture of substances added to a tablet to facilitate its breakup or disintegration after administration.
  • Lubricant is a substance or a mixture of substances added to a tablet to improve the flowability and to prevent adhesion of the tablet material to the surface of the dies and punches, reduce interparticle friction, and facilitate the ejection of the tablets from the die cavity.
  • wet-granulation method is the most widely used method. Its popularity is due to the greater probability that the granulation will meet all the physical requirements for the compression of good tablets. Its chief disadvantages are the number of separate steps involved and the time and labor necessary to carry out the procedure.
  • the steps involved in the wet-granulation method are: (1) weighing, (2) mixing, (3) granulation, (4) screening the damp mass after granulation, (5) drying (6) dry screening (7) lubrication, and (8) compression.
  • Dry-granulation method is generally used when tablet ingredients are sensitive to moisture or are unable to withstand elevated temperatures during drying. This method eliminates a number of steps but still includes (1) weighing, (2) mixing, (3) dry granulation, (4) dry screening, (5) lubrication, and (6) compression. However, this method requires that the tablet ingredients must have sufficient inherent binding or cohesive properties for dry granulation.
  • Direct compression consists of compressing tablets directly from ingredients without wet or dry granulation. This method comprises only three steps: (1) weighing, (2) mixing, and (3) compression.
  • the active ingredients must possess inherent binding and cohesive properties, and/or (2) the diluents and/or binders must be capable of imparting the compressible characteristics.
  • the ingredients must be subjected to preprocessing step such as wet granulation, dry granulation, or other granulation processes such as spheronization, spray drying, and crystallization.
  • the present invention discloses a new method of tablet preparation which is very simple and cost effective.
  • the method of the present invention consists of compressing tablets directly from powdered materials without modifying the physical nature of the materials using gelatin. All ingredients used in this method do not have to undergo preprocessing step such as wet granulation, dry granulation, or other granulation processes such as spheronization, spray drying, and crystallization.
  • aqueous solution of gelatin has often been used in wet granulation. However, its dry form, powder or granules, has never been directly used in tablet compression .
  • the method of tablet preparation in this invention comprises only three simple steps: (1) weighing, (2) mixing, and (3) compression.
  • Gelatin used in this invention can be powder or granules and in concentrations from 0.1% to 99.9% of the tablet weight.
  • STEP 1- WEIGHING Active ingredient(s), gelatin, and other ingredient(s) are accurately weighed.
  • STEP 2- MIXING Active ingredient(s), gelatin, and other ingredient(s) are added, one item at a time, into a suitable blender and mix for an appropriate length of time.
  • STEP 3- COMPRESSION The mixture from STEP 2 is compressed into tablets.
  • the following examples of method of preparing tablets using gelatin at different concentrations are given. It is understood that these examples are considered as illustrative only and are not to be construed as limitations on the present invention.
  • EXAMPLFi I Gelatin is used as diluent, binder, and disintegrator
  • Vitamin B 12 powder (active ingredient) 0.006 mg/tablet
  • methenamine naturally possesses cohesive property which makes compression without binders possible. However, if gelatin is absent, the disintegration would take longer than 30 minutes.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention comprises a method of tablet preparation. The invention provides a simple and cost effective method to compress good tablets.

Description

SIMPLE TABLET COMPRESSION USING GELATIN
FIELD OF THE INVENTION
This invention relates to tablet preparations.
BACKGROUND OF THE INVENTION
In addition to the active ingredient(s), a tablet basically contains: (1) diluent, (2) binder, (3) disintegrator, and (4) lubricant.
Diluent is a substance or a mixture of substances added to a tablet to increase the bulk in order to make the tablet a practical size for compression.
Binder is a substance or a mixture of substances added to a tablet to impart a cohesiveness to the tablet formulation which insures the tablet remaining intact after compression.
Disintegrator is a substance or a mixture of substances added to a tablet to facilitate its breakup or disintegration after administration.
Lubricant is a substance or a mixture of substances added to a tablet to improve the flowability and to prevent adhesion of the tablet material to the surface of the dies and punches, reduce interparticle friction, and facilitate the ejection of the tablets from the die cavity.
There are currently three general methods of tablet preparation: (1) wet-granulation method, (2) dry-granulation method, and (3) direct compression. All three methods have disadvantages. Wet-granulation method is the most widely used method. Its popularity is due to the greater probability that the granulation will meet all the physical requirements for the compression of good tablets. Its chief disadvantages are the number of separate steps involved and the time and labor necessary to carry out the procedure. The steps involved in the wet-granulation method are: (1) weighing, (2) mixing, (3) granulation, (4) screening the damp mass after granulation, (5) drying (6) dry screening (7) lubrication, and (8) compression.
Dry-granulation method is generally used when tablet ingredients are sensitive to moisture or are unable to withstand elevated temperatures during drying. This method eliminates a number of steps but still includes (1) weighing, (2) mixing, (3) dry granulation, (4) dry screening, (5) lubrication, and (6) compression. However, this method requires that the tablet ingredients must have sufficient inherent binding or cohesive properties for dry granulation.
Direct compression consists of compressing tablets directly from ingredients without wet or dry granulation. This method comprises only three steps: (1) weighing, (2) mixing, and (3) compression. However, it has two major disadvantages: (1) the active ingredients must possess inherent binding and cohesive properties, and/or (2) the diluents and/or binders must be capable of imparting the compressible characteristics. To acquire these properties, the ingredients must be subjected to preprocessing step such as wet granulation, dry granulation, or other granulation processes such as spheronization, spray drying, and crystallization.
SUMMARY OF INVENTION
The present invention discloses a new method of tablet preparation which is very simple and cost effective.
The method of the present invention consists of compressing tablets directly from powdered materials without modifying the physical nature of the materials using gelatin. All ingredients used in this method do not have to undergo preprocessing step such as wet granulation, dry granulation, or other granulation processes such as spheronization, spray drying, and crystallization.
An aqueous solution of gelatin has often been used in wet granulation. However, its dry form, powder or granules, has never been directly used in tablet compression .
It is an object of this invention to provide a simple method of preparing tablets in which gelatin, in its dry form, with its strong binding, cohesive, and liydrophiUic properties, can be utilized as tablet diluent, and/or binder, and/or disintegrator.
The method of tablet preparation in this invention comprises only three simple steps: (1) weighing, (2) mixing, and (3) compression.
DETAIL DESCRIPTION OF THE INVENTION
The following discussion details procedure of the tablet preparation using gelatin.
Gelatin used in this invention can be powder or granules and in concentrations from 0.1% to 99.9% of the tablet weight.
STEP 1- WEIGHING: Active ingredient(s), gelatin, and other ingredient(s) are accurately weighed.
STEP 2- MIXING: Active ingredient(s), gelatin, and other ingredient(s) are added, one item at a time, into a suitable blender and mix for an appropriate length of time.
STEP 3- COMPRESSION: The mixture from STEP 2 is compressed into tablets. In order to more clearly define the invention, the following examples of method of preparing tablets using gelatin at different concentrations are given. It is understood that these examples are considered as illustrative only and are not to be construed as limitations on the present invention.
EXAMPLFi I: Gelatin is used as diluent, binder, and disintegrator
Vitamin Bι2 6 meg tablets
Vitamin B12, powder (active ingredient) 0.006 mg/tablet
Gelatine, powder 199.804 mg/tablet
Magnesium stearate, powder (lubricant) 0.190 mg/tablet
Total Weight 200.000 mg/tablet
Procedure
1. Accurately weigh vitamin Bι2, gelatin, and magnesium stearate.
2. Mix vitamin B)2 and gelatin in a suitable blender for 15 minutes. Add magnesium stearate and mix for additional 5 minutes.
3. Compress.
Tablet properties
Size/Form: 0.291" round tablet
Weight: 200.0 mg
Hardness: 5.0 Kg
Friability: Less than 1.0%
Disintegration: 1 minute EXAMPLE II: Gelatin is used as diluent, binder, and disintegrator
Vitamins-minerals-herbs tablets
Thiamin HCl, powder (active ingredient) 10.00 mg/tablet Niacinamide, powder (active ingredient) 20.00 mg/tablet Pyridoxine HCl, powder (active ingredient) 10.00 mg/tablet Calcium carbonate, powder (active ingredient) 525.00 mg/tablet Magnesium oxide, powder (active ingredient) 335.00 mg/tablet Green tea, powder (active ingredient) 10.00 mg/tablet Korean ginseng, powder (active ingredient) 20.00 mg/tablet Gelatine, powder 100.00 mg/tablet
Magnesium stearate, powder (lubricant) 20.00 mg/tablet Silicon dioxide, powder (lubricant) 10.00 mg/tablet
Total Weight 1060.00 mg/tablet
Procedure
1. Accurately weigh thiamin HCl, niacinamide, pyridoxine HCl, calcium carbonate, magnesium oxide, green tea, Korean ginseng, gelatin, magnesium stearate, and silicon dioxide.
2. Add thiamin HCl, niacinamide, pyridoxine HCl, calcium carbonate, magnesium oxide, green tea, Korean ginseng, gelatin, one item at a time, in a suitable blender and mix for 15 minutes. Add magnesium stearate and silicon dioxide and mix for additional 5 minutes.
3. Compress. Tablet properties
Size/Form: 5/8" round tablet
Weight: 1060.0 mg
Hardness: 8.0 Kg
Friability: Less than 1.0%
Disintegration: 10 minutes
EXAMPLE III: Gelatin is used as diluent and binder
Potassium chloride 30 mg tablets
Potassium chloride, powder (active ingredient) 30.0 mg/tablet
Gelatin, powder 160.0 mg/tablet
Croscarmelose sodium, powder (disintegrator) 2.0 mg/tablet
Talc, powder (lubricant) 5.0 mg/tablet
Magnesium stearate, powder (lubricant) 3.0 mg/tablet
Total Weight 200.0 mg/tablet
Procedure
1. Accurately weigh potassium chloride, gelatin, croscarmelose sodium, talc, and magnesium stearate.
2. Add potassium chloride, gelatin, and croscarmelose sodium, one item at a time, in a suitable blender and mix for 15 minutes. Add talc and magnesium stearate and mix for additional 5 minutes.
3. Compress. Tablet properties
Size/Form: 0.291" round tablet
Weight: 200.0 mg
Hardness: 7.0 Kg
Friability: Less than 1.0%
Disintegration: 2 minutes
EXAMPLE TV: Gelatin is used as binder
Calcium carbonate 1250 mg tablets
Calcium carbonate, powder (active ingredient) 1250.0 mg/tablet Gelatine, powder 80.0 mg/tablet Stearic acid, powder (diluent) 40.0 mg/tablet Microcrystalline cellulose, powder (diluent) 35.0 mg/tablet Croscannelose sodium, powder (disintegrator) 35.0 mg/tablet Magnesium stearate, powder (lubricant) 30.0 mg/tablet Silicon dioxide, powder (lubricant) 15.0 mg/tablet
Total Weight 1485.0 mg/tablet
Procedure
1. Accurately weigh calcium carbonate, gelatin, stearic acid, microcrystalline cellulose, croscarmelose sodium, magnesium stearate, and silicon dioxide.
2. Add calcium carbonate, gelatin, stearic acid, microcrystalline cellulose, croscarmelose sodium, one item at a time, in a suitable blender and mix for 15 minutes. Add magnesium stearate and silicon dioxide and mix for additional 5 minutes. 3. Compress.
Tablet properties
Size/Form: 0.750 x 0.312" caplet
Weight: 1485.0 mg
Hardness: 8.0 Kg
Friability: Less than 1.0%
Disintegration: 5 minutes
EXAMPLE V : Gelatin is used as disintegrator
Methenamine 500 mg tablets
Methenamine, powder (active ingredient) 500.0 mg/tablet
Gelatine, powder 0.5 mg/tablet
Magnesium stearate, powder (lubricant) 4.5 mg/tablet
Total Weight 505.0 mg/tablet
Procedure
1. Accurately weigh methenamine, gelatin, and magnesium stearate.
2. Mix methenamine and gelatin in a suitable blender for 15 minutes. Add magnesium stearate and mix for additional 5 minutes.
3. Compress. Tablet properties
Size/Form: 3/8" round tablet
Weight: 505.0 mg
Hardness: 5.0 Kg
Friability: Less than 1.0%
Disintegration: 5 minutes
Note: In this example, methenamine naturally possesses cohesive property which makes compression without binders possible. However, if gelatin is absent, the disintegration would take longer than 30 minutes.

Claims

ClaimsI claim:
1. A simple method for directly compressing tablets, consisting of compressing tablets directly from powdered materials without modifying the physical nature of the materials using gelatin wherein said powdered materials do not undergo a preprocessing step.
2. The method of claim 1, wherein said gelatin can be powder or granules.
3. The method of claim 1, wherein said gelatin is used in concentrations from 0.1 % to 99.9% of the tablet weight.
4. The method of claim 1, wherein said gelatin is used as diluent, binder, and disintegrator.
5. The method of claim 1. wherein said gelatin is used as diluent and binder.
6. The method of claim 1, wherein said gelatin is used as diluent and disintegrator.
7. The method of claim 1, wherein said gelatin is used as binder and disintegrator.
8. The method of claim 1 , wherein said gelatin is used as diluent.
9. The method of claim 1, wherein said gelatin is used as binder.
10. The method of claim 1, wherein said gelatin is used as disintegrator.
PCT/US2003/002945 2003-01-03 2003-01-03 Simple tablet compression using gelatin Ceased WO2004062647A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
PCT/US2003/002945 WO2004062647A1 (en) 2003-01-03 2003-01-03 Simple tablet compression using gelatin
CA002477221A CA2477221A1 (en) 2003-01-03 2003-01-03 Simple tablet compression using gelatin
AU2003208918A AU2003208918A1 (en) 2003-01-03 2003-01-03 Simple tablet compression using gelatin
EP03707641A EP1587501A4 (en) 2003-01-03 2003-01-03 Simple tablet compression using gelatin

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2003/002945 WO2004062647A1 (en) 2003-01-03 2003-01-03 Simple tablet compression using gelatin

Publications (1)

Publication Number Publication Date
WO2004062647A1 true WO2004062647A1 (en) 2004-07-29

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PCT/US2003/002945 Ceased WO2004062647A1 (en) 2003-01-03 2003-01-03 Simple tablet compression using gelatin

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EP (1) EP1587501A4 (en)
AU (1) AU2003208918A1 (en)
CA (1) CA2477221A1 (en)
WO (1) WO2004062647A1 (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5738872A (en) * 1995-02-28 1998-04-14 Hoechst Marion Roussel, Inc. Pharmaceutical composition for piperidinoalkanol compounds
US6068854A (en) * 1991-12-05 2000-05-30 Alfatec-Pharma Gmbh Sol-controlled thermocolloid matrix based on gelatin for oral sustained-release form

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5958455A (en) * 1996-02-09 1999-09-28 Quadrant Holdings Cambridge Ltd Oral solid dosage forms, methods of making same and compositions thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6068854A (en) * 1991-12-05 2000-05-30 Alfatec-Pharma Gmbh Sol-controlled thermocolloid matrix based on gelatin for oral sustained-release form
US5738872A (en) * 1995-02-28 1998-04-14 Hoechst Marion Roussel, Inc. Pharmaceutical composition for piperidinoalkanol compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP1587501A4 *

Also Published As

Publication number Publication date
AU2003208918A1 (en) 2004-08-10
EP1587501A1 (en) 2005-10-26
EP1587501A4 (en) 2007-04-11
CA2477221A1 (en) 2004-07-29

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