GB2331702A - Tablets containing a bitter excipient and/or a dye - Google Patents
Tablets containing a bitter excipient and/or a dye Download PDFInfo
- Publication number
- GB2331702A GB2331702A GB9826000A GB9826000A GB2331702A GB 2331702 A GB2331702 A GB 2331702A GB 9826000 A GB9826000 A GB 9826000A GB 9826000 A GB9826000 A GB 9826000A GB 2331702 A GB2331702 A GB 2331702A
- Authority
- GB
- United Kingdom
- Prior art keywords
- bitter
- dye
- excipient
- tablet
- tablets
- 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.)
- Withdrawn
Links
- 239000000546 pharmaceutical excipient Substances 0.000 title claims abstract description 18
- 239000011248 coating agent Substances 0.000 claims abstract description 11
- 238000000576 coating method Methods 0.000 claims abstract description 11
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract description 5
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract description 5
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract description 5
- RBTBFTRPCNLSDE-UHFFFAOYSA-N 3,7-bis(dimethylamino)phenothiazin-5-ium Chemical group C1=CC(N(C)C)=CC2=[S+]C3=CC(N(C)C)=CC=C3N=C21 RBTBFTRPCNLSDE-UHFFFAOYSA-N 0.000 claims abstract description 4
- IOSXSVZRTUWBHC-LBTVDEKVSA-N Quassin Chemical group CC([C@@H]1CC(=O)O[C@@H]([C@]21C)C1)=C(OC)C(=O)[C@@H]2[C@]2(C)[C@@H]1[C@H](C)C=C(OC)C2=O IOSXSVZRTUWBHC-LBTVDEKVSA-N 0.000 claims abstract description 4
- 229960000907 methylthioninium chloride Drugs 0.000 claims abstract description 4
- IOSXSVZRTUWBHC-UHFFFAOYSA-N quassin Natural products C1C(C23C)OC(=O)CC3C(C)=C(OC)C(=O)C2C2(C)C1C(C)C=C(OC)C2=O IOSXSVZRTUWBHC-UHFFFAOYSA-N 0.000 claims abstract description 4
- 235000019658 bitter taste Nutrition 0.000 claims abstract description 3
- 229940079593 drug Drugs 0.000 abstract description 12
- 239000003814 drug Substances 0.000 abstract description 12
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 abstract description 4
- 229960001797 methadone Drugs 0.000 abstract description 4
- 235000009508 confectionery Nutrition 0.000 abstract description 2
- 230000009747 swallowing Effects 0.000 description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 210000003296 saliva Anatomy 0.000 description 2
- 230000003248 secreting effect Effects 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- MPBRYMWMMKKRGC-UHFFFAOYSA-M carbocyanin DBTC Chemical compound [Br-].C1=CC=CC2=C([N+](=C(C=C(C)C=C3N(C4=C5C=CC=CC5=CC=C4S3)CC)S3)CC)C3=CC=C21 MPBRYMWMMKKRGC-UHFFFAOYSA-M 0.000 description 1
- 239000000599 controlled substance Substances 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 229960005189 methadone hydrochloride Drugs 0.000 description 1
- FJQXCDYVZAHXNS-UHFFFAOYSA-N methadone hydrochloride Chemical compound Cl.C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 FJQXCDYVZAHXNS-UHFFFAOYSA-N 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 201000009032 substance abuse Diseases 0.000 description 1
- 210000004243 sweat Anatomy 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- 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
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Emergency Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
Abstract
A pharmaceutical tablet contains a bitter excipient and/or a dye and has a soluble coating. When placed in the mouth the soluble coating dissolves rapidly releasing the bitter excipient and/or the dye into the mouth. The bitter taste will prompt a child who has incorrectly mistaken the tablet for a sweet to spit it out, thus avoiding harm. The dye colour will confirm that the tablet has been placed in the mouth and so allow someone to confirm that the tablet has been swallowed. This is important with medication to control anti-social or self-harming conditions or to ensure that drugs such as methadone have not been hidden for later sale by a drug addict. The presence of a very bitter excipient would also encourage the tablet to be swallowed. The preferred bitter excipient is quassin, the preferred dye is methylene blue which is clearly visible even at very low concentrations and polyvinylpyrrolidone is the soluble coating of choice.
Description
1 TITLE: Tablets.
DESCRIPT ON 2331702 This invention relates to tablets.
There is a very great danger in tablets falling into the wrong hands. Most at risk are children mistaking tablets for sweets and becoming ill or even dying as a result of taking someone else's tablets.
Another area of difficulty is in the administration of drugs by tablet to addicts, who can be skilled at secreting tablets in the mouth, so as to be able to recover the tablets later for sale to others.
An object of this invention is to provide a tablet that can mitigate against the above-identified problems.
According to the present invention it is proposed that tablets include one or both of a bitter excipient and a dye and that the tablets have a soluble coating.
The soluble coating is preferably one that will dissolve rapidly in order to release the bitter excipient and/or dye in the mouth before the tablet is swallowed. A suitable coating may be PVP (polyvinylpyrrolidone) The bitter excipient is preferably one that is in excess of a bitterness threshold of 1:60,000. Quassin is an example of a suitable bitter excipient for use in the invention.
An aim of including a bitter excipient in tablets is to reduce the risk of children swallowing a tablet that could be harmful to them. Young children usually 2 do not swallow tablets immediately but lick, suck or chew medication tablets prior to swallowing. As the tablets of the invention are coated with a soluble film, the bitter excipient will be released into the mouth quite quickly on contact of the tablet with saliva in the mouth and cause the child to spit the tablet out.
Thus, according to one preferred aspect the present invention has application to medication tablets for adult administration to reduce the risk of children swallowing such tablets.
A suitable dye for use in tablets of the invention is one that will show up clearly from even a small amount being present. Methylene blue is an example of a suitable dye for use in tablets of the invention.
An aim of including a dye in tablets is to reduce the likelihood of drug addicts secreting tablets of, for example, methadone, in the mouth. The soluble coating will dissolve on contact with saliva in the mouth and release the dye quickly into the mouth. Thus, it will be very readily apparent when a drug addict has not swallowed the tablet. The same principle applies to those who are on medication to control antisocial or self-harming conditions, so that those administering the medication can ascertain whether or not the medication has been swallowed.
Another benefit of incorporation of a dye into tablets in accordance with the invention is that handling of such tablets by addicts would be quickly noticeable. Normal sweat on the hands would cause the soluble coating to dissolve and the dye would be released onto the hands.
A further advantage of the tablets of the invention containing a dye is that they will be less attractive for converting into injectable form. It is known to crush such 3 tablets, boil the crushed tablets with water and then inject the resulting solution. The dye will be released and will stain all utensils used.
A yet further advantage of tablets of the invention is an increase in the complexity of extracting the base drug from a tablet, especially one incorporating both the bitter excipient and dye, in a home chemistry set.
Thus, the present invention has particular application to controlled drug tablets, such as containing methadone, to reduce risk of abuse.
This invention will now be further described by means of the following Example.
Example
A methadone tablet was prepared by mixing normal tablet excipients, such as silicon dioxide, magnesium stearate and lactose, with methadone hydrochloride, methylene blue in amounts of 10mg and quassin as a bitter excipient. After pressing the mixture to form tablets, the tablets were coated with a rapidly soluble film coat of PVP such that if the tablet is held in the mouth or the hand for a certain period of time, the film dissolves to release the dye and bitter excipient.
4
Claims (1)
- ClaimsA pharmaceutical tablet including one or both of a bitter excipient and a dye and having soluble coating.2. A pharmaceutical tablet as claimed in claim 1, wherein the soluble coating dissolves in the mouth.3. A pharmaceutical tablet as claimed in claim 1 or 2, wherein the soluble coating is polyvinylpyrrolidone.4. A pharmaceutical tablet as claimed in claim 1, 2 or 3, wherein the bitter excipient has a bitterness threshold in excess of 1:60,000.5. A pharmaceutical tablet as claimed in claim any one of claims 1 to 4, wherein the bitter excipient is quassin.6. A pharmaceutical tablet as claimed in any one of claims 1 to 5, wherein the dye is noticeable even when a small amount is present. A pharmaceutical tablet as claimed in any one of claims 1 to 6, wherein the dye is methylene blue.8. A pharmaceutical tablet substantially as hereinbefore described with reference to the foregoing Example.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9725219.1A GB9725219D0 (en) | 1997-11-29 | 1997-11-29 | Tablets |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB9826000D0 GB9826000D0 (en) | 1999-01-20 |
| GB2331702A true GB2331702A (en) | 1999-06-02 |
Family
ID=10822807
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GBGB9725219.1A Ceased GB9725219D0 (en) | 1997-11-29 | 1997-11-29 | Tablets |
| GB9826000A Withdrawn GB2331702A (en) | 1997-11-29 | 1998-11-27 | Tablets containing a bitter excipient and/or a dye |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GBGB9725219.1A Ceased GB9725219D0 (en) | 1997-11-29 | 1997-11-29 | Tablets |
Country Status (1)
| Country | Link |
|---|---|
| GB (2) | GB9725219D0 (en) |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1293195A1 (en) * | 2001-09-17 | 2003-03-19 | Rohm And Haas Company | Oral pharmaceutical dosage forms with reduced potential for drug abuse, comprising respiratory irritants or bitter substances |
| FR2829932A1 (en) * | 2001-09-21 | 2003-03-28 | Ellipse Pharmaceuticals | Orally administered pharmaceutical product, containing agents with recognizable taste, color and appearance to prevent administration of active agent, e.g. hypnotic or sedative, to unsuspecting subject |
| WO2003026621A3 (en) * | 2001-09-21 | 2003-10-09 | Ellipse Pharmaceuticals | Method for making an oral pharmaceutical product with tell-tale agents, in particular of taste and resulting product |
| FR2949062A1 (en) * | 2009-08-12 | 2011-02-18 | Debregeas Et Associes Pharma | NEW PHARMACEUTICAL FORMULATIONS AGAINST MEASURING MEDICINES |
| US20120244409A1 (en) * | 2010-09-21 | 2012-09-27 | Victoria Link Limited | Battery safety systems, methods and compositions |
| US20130104796A1 (en) * | 2011-11-01 | 2013-05-02 | Nikhil BHAT | Swallowing indicator for solid objects |
| US8529954B2 (en) | 2008-11-14 | 2013-09-10 | Debregeas Et Associes Pharma | Composition based on gamma-hydroxybutyric acid |
| US20180207375A1 (en) * | 2014-02-13 | 2018-07-26 | Cardiff Scintigraphics Limited | Pressurized metered dose inhalers and method of manufacture |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108887455B (en) * | 2018-06-17 | 2021-07-30 | 西宝生物科技（上海）股份有限公司 | A kind of product for preventing excessive chewing and preparation method thereof |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB762229A (en) * | 1953-11-09 | 1956-11-28 | Abbott Lab | Improvements in or relating to coated tablets and to compositions adapted for application to tablets |
| GB764342A (en) * | 1953-12-03 | 1956-12-28 | Abbott Lab | Improvements in or relating to coated water soluble tablets |
| US4551512A (en) * | 1983-04-08 | 1985-11-05 | Basf Aktiengesellschaft | Water-soluble polymers having a low hygroscopicity |
| WO1992011002A1 (en) * | 1990-12-20 | 1992-07-09 | Warner-Jenkinson Company | Wet powder film-forming compositions |
| WO1993001712A1 (en) * | 1991-07-16 | 1993-02-04 | Zeneca Limited | Rodent bait package |
| EP0582396A1 (en) * | 1992-07-30 | 1994-02-09 | Pfizer Inc. | Taste-masking composition of bitter pharmaceutical agents |
| WO1994018953A1 (en) * | 1993-02-24 | 1994-09-01 | Warner-Jenkinson Company, Inc. | Dye compositions and methods for film coating tablets and the like |
-
1997
- 1997-11-29 GB GBGB9725219.1A patent/GB9725219D0/en not_active Ceased
-
1998
- 1998-11-27 GB GB9826000A patent/GB2331702A/en not_active Withdrawn
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB762229A (en) * | 1953-11-09 | 1956-11-28 | Abbott Lab | Improvements in or relating to coated tablets and to compositions adapted for application to tablets |
| GB764342A (en) * | 1953-12-03 | 1956-12-28 | Abbott Lab | Improvements in or relating to coated water soluble tablets |
| US4551512A (en) * | 1983-04-08 | 1985-11-05 | Basf Aktiengesellschaft | Water-soluble polymers having a low hygroscopicity |
| WO1992011002A1 (en) * | 1990-12-20 | 1992-07-09 | Warner-Jenkinson Company | Wet powder film-forming compositions |
| WO1993001712A1 (en) * | 1991-07-16 | 1993-02-04 | Zeneca Limited | Rodent bait package |
| EP0582396A1 (en) * | 1992-07-30 | 1994-02-09 | Pfizer Inc. | Taste-masking composition of bitter pharmaceutical agents |
| WO1994018953A1 (en) * | 1993-02-24 | 1994-09-01 | Warner-Jenkinson Company, Inc. | Dye compositions and methods for film coating tablets and the like |
Cited By (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1293195A1 (en) * | 2001-09-17 | 2003-03-19 | Rohm And Haas Company | Oral pharmaceutical dosage forms with reduced potential for drug abuse, comprising respiratory irritants or bitter substances |
| US7655256B2 (en) | 2001-09-17 | 2010-02-02 | Rohm And Haas Company | Pharmaceutical formulation including a resinate and an aversive agent |
| FR2829932A1 (en) * | 2001-09-21 | 2003-03-28 | Ellipse Pharmaceuticals | Orally administered pharmaceutical product, containing agents with recognizable taste, color and appearance to prevent administration of active agent, e.g. hypnotic or sedative, to unsuspecting subject |
| WO2003026621A3 (en) * | 2001-09-21 | 2003-10-09 | Ellipse Pharmaceuticals | Method for making an oral pharmaceutical product with tell-tale agents, in particular of taste and resulting product |
| US8529954B2 (en) | 2008-11-14 | 2013-09-10 | Debregeas Et Associes Pharma | Composition based on gamma-hydroxybutyric acid |
| FR2949062A1 (en) * | 2009-08-12 | 2011-02-18 | Debregeas Et Associes Pharma | NEW PHARMACEUTICAL FORMULATIONS AGAINST MEASURING MEDICINES |
| WO2011018583A3 (en) * | 2009-08-12 | 2011-04-07 | Debregeas Et Associes Pharma | Novel pharmaceutical formulations against drug misuse |
| CN102573801A (en) * | 2009-08-12 | 2012-07-11 | D&A制药 | New pharmaceutical formulations to prevent drug abuse |
| EA021856B1 (en) * | 2009-08-12 | 2015-09-30 | Дебрежа Э Ассосье Фарма | PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION OF THE ABUSE OF MEDICINAL PREPARATIONS |
| US8999392B2 (en) | 2009-08-12 | 2015-04-07 | Debregeas Et Associes Pharma | Pharmaceutical formulations to prevent the misuse of medicinal drugs |
| CN102573801B (en) * | 2009-08-12 | 2013-08-21 | D&A制药 | Novel pharmaceutical formulations for preventing drug abuse |
| TWI465261B (en) * | 2009-08-12 | 2014-12-21 | Debregeas Et Associes Pharma | Novel pharmaceutical formulations for the prevention of drug abuse |
| EP2619826A4 (en) * | 2010-09-21 | 2015-01-21 | Victoria Link Ltd | SAFETY MATERIAL AND SYSTEM |
| US20120244409A1 (en) * | 2010-09-21 | 2012-09-27 | Victoria Link Limited | Battery safety systems, methods and compositions |
| US9865862B2 (en) | 2010-09-21 | 2018-01-09 | Victoria Link Limited | Safety material and system |
| US20130104796A1 (en) * | 2011-11-01 | 2013-05-02 | Nikhil BHAT | Swallowing indicator for solid objects |
| US20180207375A1 (en) * | 2014-02-13 | 2018-07-26 | Cardiff Scintigraphics Limited | Pressurized metered dose inhalers and method of manufacture |
| US11260185B2 (en) * | 2014-02-13 | 2022-03-01 | Cardiff Scintigraphics Limited | Pressurized metered dose inhalers and method of manufacture |
Also Published As
| Publication number | Publication date |
|---|---|
| GB9725219D0 (en) | 1998-01-28 |
| GB9826000D0 (en) | 1999-01-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2031572C (en) | Non-alcoholic delivery system for orally ingestible active ingredients | |
| DK1648421T3 (en) | ORAL SOLUBLE MOVIES | |
| CA2704929C (en) | Compositions and methods for procedural sedation and analgesia using oral transmucosal dosage forms | |
| US6406717B2 (en) | Rapid-melt semi-solid compositions, methods of making same and methods of using same | |
| AU668004B2 (en) | Compositions and methods of manufacture of oral dissolvable medicaments | |
| AU2003267268B2 (en) | Modified release oral dosage form | |
| US7011843B2 (en) | Method for protecting a human being against health impairment by ingestion of a transdermal therapeutic system | |
| HUP0203451A2 (en) | Pharmaceutical compositions of anti-tubercular drugs and process for their preparation | |
| CA2387705A1 (en) | Stable pharmaceutical composition for oral use | |
| SG108230A1 (en) | Flash-melt oral dosage formulation | |
| HUT74920A (en) | Improved nicotine lozenge and therapeutic method for smoking cessation | |
| GB2331702A (en) | Tablets containing a bitter excipient and/or a dye | |
| RS52374B (en) | FORMS OF MEDICINES WITH IMPROVED PHARMACOKINETIC CHARACTERISTICS | |
| KR20230044355A (en) | Orally disintegrating tablet containing mirogabalin besylate | |
| JP2013530206A (en) | Methods and agents for detecting drugs in beverages | |
| D'Orlando et al. | Tolerability and pharmacokinetics of single and repeated doses of nicotine with The Straw, a novel nicotine replacement product | |
| US4454142A (en) | Hyperkinetic child treatment agent | |
| US4511570A (en) | Senile dementia treatment | |
| AU759609B2 (en) | Method for preventing the misuse of a transdermal therapeutic system | |
| Stenson et al. | Ingestion of caustic cosmetic products | |
| ES2733732T3 (en) | Pharmaceutical form to fight the chemical submission of a drug | |
| Breitkreutz et al. | Pediatric and geriatric pharmaceutics and formulation | |
| RU2125878C1 (en) | Analgetic agent | |
| JPH11171767A (en) | Hypnoticum | |
| MXPA00002933A (en) | Method for preventing the misuse of a transdermal therapeutic system |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |