US3506756A - Use of adipic acid as a tableting lubricant - Google Patents
Use of adipic acid as a tableting lubricant Download PDFInfo
- Publication number
- US3506756A US3506756A US839714A US3506756DA US3506756A US 3506756 A US3506756 A US 3506756A US 839714 A US839714 A US 839714A US 3506756D A US3506756D A US 3506756DA US 3506756 A US3506756 A US 3506756A
- Authority
- US
- United States
- Prior art keywords
- adipic acid
- tableting
- tablet
- lubricant
- composition
- 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
Links
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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
Definitions
- Tableting lubricants perform the general functions of providing (1) surface lubrication for the punch and die surfaces which come into contact with one another and with the compressed composition and (2) internal compression lubrication in order to lend pliability to the composition being compressed. Both of these lubrication functions must be satisfied if the powdered tabletable composition of interest is to be tableted commercially on tableting machines operated at high speeds. Some prior lubricants have provided only one of these two necessary lubrication functions and hence have necessitated joint use with another lubricant. A general problem with these prior lubricants has been their insolubility. This causes a tablet formed from an otherwise soluble composition to exhibit the appearance of a clouded suspension rather than a clear solution when dissolved in water.
- lubricants are examples of such lubricants.
- Other lubricants are precluded in one or more marketing areas because of their toxicity.
- examples of such lubricants are boric acid, benzoic acid and polyethylene glycol.
- Some tableting lubricants such as sodium benzoate have therapeutic action and therefore alter the pharmacological acceptability of tablets in which they are included.
- the adipic acid tableting lubricant can be used with a wide range of powdered tabletable compositions to allow high speed tableting thereof. While various amounts of adipic acid can be mixed with such compositions depending upon the presence therein of ingredients which impart some lubrication and upon the tableting speed desired, it is usually sufiicient to use about at least adipic acid based on the total weight of the composition being tableted when no other lubricants are used. If desired, adipic acid may be used in larger amounts, approaching the total tablet weight, since it is cohesive when compressed.
- Adipic acid exists naturally as minute, colorless, monoclinic prisms which permit use according to the present invention without further modification. If desired, these small prisms can be comminuted to any desired fineness. Mesh sizes of 40 and finer are particularly preferred for 3,506,756 Patented Apr. 14, 1970 use with most powdered compositions. Adipic acid is characterized by its low toxicity and hence it may be used for tablets which are intended to be taken internally.
- the tabletable compositions which can be lubricated for tableting with adipic acid can, for example, be any compositions which are cohesive enough when compressed to form and retain a tablet shape.
- Such compositions can be composed of powdered detergents, disinfectants, germicides and/or abrasives which disintegrate when placed in water to form cleaning solutions of various types. Inclusion of quarternary compounds, such as cetyl pyridinium chloride, is particularly useful when cleaning tab lets are to be produced.
- compositions are effervescent mixtures comprised of an alkali metal carbonate or bicarbonate and an acid such as malic, citric or tartaric acids which are capable of rapidly releasing carbon dioxide upon addition of water thereto.
- an acid such as malic, citric or tartaric acids which are capable of rapidly releasing carbon dioxide upon addition of water thereto.
- the solution formed is useful for its alkalizing properties when taken orally.
- compositions can also include at least one therapeutic agent, water-soluble excipients, and any necessary coloring or flavoring agents, diluents, binders, or disintegrators.
- the therapeutic agent may be acetylsalicylic acid, acetyl p-aminophenol or other suitable analgesic.
- binders may be added to the base composition to promote cohesion. All of such compositions are tabletable in that they are cohesive when compressed. However, without a lubricant most of such compositions can be tableted only by hand, since they cause binding and scoring of the punches and dies of power driven tableting machines. In order to attain commercial production speeds a tableting lubricant must be employed to reduce surface friction and internal compression friction.
- the adipic acid of the present invention may be used as the sole lubricant or may be employed in conjunction with another lubricant included in the tabletable composition. More particularly the adipic acid lubricant can be substituted for various materials which function as tablet lubricants during compression.
- adipic acid provides the additional effect of taking part in the effervescent action.
- the adipic acid does form part of the effervescent couple it is neutralized to a metal salt, if a sufiicient amount of an alkaline material is employed, and in such form is even more highly soluble than is the free adipic acid.
- a source of alkali metal ions may be included in the pharmaceutical composition, whereby upon dissolution of the composition in water the alkali metal salt of adipic acid is formed and any solubility limitations of adipic acid are obviated.
- this is not necessary due to the fact that the adipic acid is used in amounts low enough so that the volume of water normally used for dissolution of the tablets is suflicient to dissolve all of the adipic acid employed.
- Amounts of at least about 5% adipic acid based on the total weight of the lubricated tabletable composition are generally sufiicient to allow high speed tableting when adipic acid is used as the sole lubricant. When it is used as one of at least two tableting lubricants a proportionately smaller amount may be used. Amounts of about from 5% to 15% adipic acid allow tableting of effervescent mixtures at rates up to about 5000 tablets per minute on rotary tablet machines containing 47 punch and die sets. Each punch and die set produces approximately 106 tablets per minute in such machines. On a rotary machine containing 33 punch and die sets, tablets may be compressed at a rate of 76 tablets per minute per set for a total production of about 2500 tablets per minute.
- the resulting mixture was placed in a hopper of a hand-operated punch rotary tableting machine from which the mixture was fed to the dies of the punch and die sets of the machine.
- the compression pressure was 11 kg.
- the tablets produced were 0.158 in. thick and Weighed approximately 3.2 g. each.
- a tablet producing a clear aqueous solution and being free from insoluble tablet lubricants or other tablet excipients or components which cause a tablet formed from an otherwise soluble composition to produce a clouded suspension having undesirable surface scum rather than a uniform solution when dissolved in'water consisting essentially of a compressed, essentially freeflowing mixture of a powdered, Water-soluble, tabletable essential active ingredient and, as the essential tablet lubricant, a dry-mixable tableting lubricant comprising adipic acid.
- powdered, watersoluble, tabletable essential active ingredient is an internal use oral therapeutic agent, effervescent couple alkalizer, quaternary ammonium disinfectant or solution-forming, external use, solid surface general cleansing germicide.
- said effervescent couple alkalizer is an adipic acid-free effervescent mixture of a base and an acid.
- the tablet of claim 3 including an additional therapeutic agent.
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Detergent Compositions (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US83971469A | 1969-07-07 | 1969-07-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
US3506756A true US3506756A (en) | 1970-04-14 |
Family
ID=25280462
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US839714A Expired - Lifetime US3506756A (en) | 1969-07-07 | 1969-07-07 | Use of adipic acid as a tableting lubricant |
Country Status (7)
Country | Link |
---|---|
US (1) | US3506756A (it) |
BR (1) | BR7018850D0 (it) |
CA (1) | CA936097A (it) |
DE (1) | DE2033411A1 (it) |
FR (1) | FR2104730B1 (it) |
GB (1) | GB1316622A (it) |
IT (1) | IT972026B (it) |
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4557926A (en) * | 1983-09-06 | 1985-12-10 | Monsanto Company | Method and tablet for sanitizing toilets |
US4650667A (en) * | 1982-10-15 | 1987-03-17 | Kao Corporation | Gas-emitting bath additive composition |
US4717503A (en) * | 1982-08-18 | 1988-01-05 | Mitsubishi Mining & Co., Ltd. | Demolition agent for brittle materials |
WO1998024874A1 (en) * | 1996-12-06 | 1998-06-11 | The Procter & Gamble Company | Coated detergent tablet |
US5922351A (en) * | 1991-03-27 | 1999-07-13 | Bayer Corporation | Lubricants for use in tabletting |
US6087311A (en) * | 1996-12-06 | 2000-07-11 | The Proctor & Gamble Company | Coated detergent tablet |
US20080063713A1 (en) * | 2006-09-07 | 2008-03-13 | Peter Gruber | Particulate form of a pharmaceutical composition which is easy to swallow |
US10053653B2 (en) | 2016-10-18 | 2018-08-21 | Sterilex, Llc | Ambient moisture-activated hard surface treatment powder |
Citations (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2448524A (en) * | 1947-11-07 | 1948-09-07 | Du Pont | Coated granular resin and process of making same |
DE1074958B (de) * | 1960-02-04 | General Foods Corporation, White Plains, N. Y. (V. St. A.) | Verfahren zum künstlichen Süßen eines Nahrungsmittels | |
DE1075255B (de) * | 1957-12-16 | 1960-02-11 | N. V. De Bataafsche Petroleum Maatschappij, Den Haag | Schmieröl |
US2971848A (en) * | 1958-05-12 | 1961-02-14 | Gen Foods Corp | Artificial sweetening product |
US2977300A (en) * | 1958-08-21 | 1961-03-28 | Continental Oil Co | Method of producing heat-stable greases |
US2977301A (en) * | 1958-08-21 | 1961-03-28 | Continental Oil Co | Wide-temperature range greases |
US3105792A (en) * | 1960-11-29 | 1963-10-01 | Warner Lambert Pharmaceutical | Stable effervescent compositions and method of preparing same |
US3136692A (en) * | 1961-06-30 | 1964-06-09 | Strong Cobb Arner Inc | Effervescent composition containing polyvinylpyrrolidone |
US3355392A (en) * | 1963-10-18 | 1967-11-28 | West Laboratories Inc | Alkaline germicidal cleaner with color indicator |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2918404A (en) * | 1956-07-30 | 1959-12-22 | Ortho Pharma Corp | Solid compressed amino acid spermicidal vehicle |
GB1178294A (en) * | 1967-02-17 | 1970-01-21 | Miles Lab | Improvements in or relating to Tableting Lubricants. |
-
1969
- 1969-07-07 US US839714A patent/US3506756A/en not_active Expired - Lifetime
-
1970
- 1970-03-06 CA CA076682A patent/CA936097A/en not_active Expired
- 1970-04-01 IT IT49689/70A patent/IT972026B/it active
- 1970-05-07 BR BR218850/70A patent/BR7018850D0/pt unknown
- 1970-05-20 GB GB2450070A patent/GB1316622A/en not_active Expired
- 1970-06-23 FR FR7023168A patent/FR2104730B1/fr not_active Expired
- 1970-07-06 DE DE19702033411 patent/DE2033411A1/de active Pending
Patent Citations (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE1074958B (de) * | 1960-02-04 | General Foods Corporation, White Plains, N. Y. (V. St. A.) | Verfahren zum künstlichen Süßen eines Nahrungsmittels | |
US2448524A (en) * | 1947-11-07 | 1948-09-07 | Du Pont | Coated granular resin and process of making same |
DE1075255B (de) * | 1957-12-16 | 1960-02-11 | N. V. De Bataafsche Petroleum Maatschappij, Den Haag | Schmieröl |
GB845628A (en) * | 1957-12-16 | 1960-08-24 | Bataafsche Petroleum | Lubricating oil compositions |
US2971848A (en) * | 1958-05-12 | 1961-02-14 | Gen Foods Corp | Artificial sweetening product |
US2977300A (en) * | 1958-08-21 | 1961-03-28 | Continental Oil Co | Method of producing heat-stable greases |
US2977301A (en) * | 1958-08-21 | 1961-03-28 | Continental Oil Co | Wide-temperature range greases |
US3105792A (en) * | 1960-11-29 | 1963-10-01 | Warner Lambert Pharmaceutical | Stable effervescent compositions and method of preparing same |
US3136692A (en) * | 1961-06-30 | 1964-06-09 | Strong Cobb Arner Inc | Effervescent composition containing polyvinylpyrrolidone |
US3355392A (en) * | 1963-10-18 | 1967-11-28 | West Laboratories Inc | Alkaline germicidal cleaner with color indicator |
Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4717503A (en) * | 1982-08-18 | 1988-01-05 | Mitsubishi Mining & Co., Ltd. | Demolition agent for brittle materials |
US4650667A (en) * | 1982-10-15 | 1987-03-17 | Kao Corporation | Gas-emitting bath additive composition |
US4557926A (en) * | 1983-09-06 | 1985-12-10 | Monsanto Company | Method and tablet for sanitizing toilets |
US5922351A (en) * | 1991-03-27 | 1999-07-13 | Bayer Corporation | Lubricants for use in tabletting |
WO1998024874A1 (en) * | 1996-12-06 | 1998-06-11 | The Procter & Gamble Company | Coated detergent tablet |
US6087311A (en) * | 1996-12-06 | 2000-07-11 | The Proctor & Gamble Company | Coated detergent tablet |
US20080063713A1 (en) * | 2006-09-07 | 2008-03-13 | Peter Gruber | Particulate form of a pharmaceutical composition which is easy to swallow |
US8889184B2 (en) * | 2006-09-07 | 2014-11-18 | Losan Pharma Gmbh | Particulate form of a pharmaceutical composition which is easy to swallow |
US10053653B2 (en) | 2016-10-18 | 2018-08-21 | Sterilex, Llc | Ambient moisture-activated hard surface treatment powder |
US10851328B2 (en) | 2016-10-18 | 2020-12-01 | Sterilex, Llc | Ambient moisture-activated hard surface treatment powder |
Also Published As
Publication number | Publication date |
---|---|
CA936097A (en) | 1973-10-30 |
GB1316622A (en) | 1973-05-09 |
IT972026B (it) | 1974-05-20 |
DE2033411A1 (de) | 1971-01-14 |
FR2104730A1 (it) | 1972-04-21 |
BR7018850D0 (pt) | 1973-02-08 |
FR2104730B1 (it) | 1975-01-10 |
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