CA2441123A1 - A pharmaceutical tablet system that floats on gastric fluid for multipulse release of active substance, and respective processes of producing same and a cup-shaped envelope of same - Google Patents
A pharmaceutical tablet system that floats on gastric fluid for multipulse release of active substance, and respective processes of producing same and a cup-shaped envelope of same Download PDFInfo
- Publication number
- CA2441123A1 CA2441123A1 CA002441123A CA2441123A CA2441123A1 CA 2441123 A1 CA2441123 A1 CA 2441123A1 CA 002441123 A CA002441123 A CA 002441123A CA 2441123 A CA2441123 A CA 2441123A CA 2441123 A1 CA2441123 A1 CA 2441123A1
- Authority
- CA
- Canada
- Prior art keywords
- cup
- release
- core
- tablet system
- shaped envelope
- 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.)
- Granted
Links
- 239000012530 fluid Substances 0.000 title claims abstract 8
- 230000002496 gastric effect Effects 0.000 title claims abstract 8
- 239000013543 active substance Substances 0.000 title claims abstract 7
- 238000000034 method Methods 0.000 title claims 5
- 239000000463 material Substances 0.000 claims abstract 11
- 230000002209 hydrophobic effect Effects 0.000 claims abstract 9
- 239000000945 filler Substances 0.000 claims abstract 8
- 239000000126 substance Substances 0.000 claims abstract 4
- 230000006835 compression Effects 0.000 claims abstract 3
- 238000007906 compression Methods 0.000 claims abstract 3
- 239000000203 mixture Substances 0.000 claims abstract 3
- 239000000843 powder Substances 0.000 claims abstract 2
- 230000002035 prolonged effect Effects 0.000 claims abstract 2
- 239000008187 granular material Substances 0.000 claims 6
- 239000011248 coating agent Substances 0.000 claims 3
- 238000000576 coating method Methods 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 238000005507 spraying Methods 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
Abstract
A tablet system for prolonged floating in or on gastric fluid for releasing therein pharmaceutically active substances in an alternate succession of substance release and no-release periods is made up of a multilayered core placed in a cup-shaped envelope. The core is made up of release layers and n o- release layers devoid of pharmaceutically active substance, superposed in alternate succession. The cup-shaped envelope covers bottom and side surface s of the core while leaving exposed an upper surface of the core. The cup-shap ed envelope provides for buoyancy by being formed of a compression-sintered mixture comprising hydrophobic material and inert powdered filler. The hydrophobic material is composed of fatty and/or waxy material capable of being sintered by compression and whose bulk density is lower than gastric fluid density. The powdered filler has a loose powder density that is lower than gastric fluid density.
Claims (9)
1. A pharmaceutical tablet system capable of prolonged floating in or on gastric fluid for releasing therein one or more pharmaceutically active substances in the course of an alternate succession of periods of substance release and no-release, said alternate succession including at least two periods of substance release separated by one period of no-release, whereby the tablet system is made up of a multilayered core placed in a cup-shaped envelope, the core is made up of release and no-release layers superposed in alternate succession to form a pile of layers that includes at least two release layers flanking an in-termediate no-release layer, each release layer being com-posed of pharmaceutically acceptable excipient and/or carrier having admixed thereto at least one of said pharmaceutically active substances, each no-release layer being composed of pharmaceutically acceptable excipient and/or carrier devoid of said pharmaceutically active substance, the cup-shaped envelope covers a bottom surface and side surfaces of the core placed therein while leaving exposed an upper surface of the core, characterized in that the cup-shaped envelope provides for buoyancy of the pharmaceutical tablet system with respect to gastric fluid by being formed of a compression-sintered mixture that comprises pharmaceutically acceptable hydrophobic material and pharma-ceutically acceptable inert powdered filler, the hydrophobic material being composed of fatty and/or waxy material capable of being sintered by compression and whose bulk density is lower than gastric fluid density, and the powdered filler having a loose powder density that is lower than gastric fluid density.
2. A pharmaceutical tablet system according to claim 1, in which the voids are interstices between grains of the pow-dered filler.
3. A pharmaceutical tablet system according to claim 2, in which the voids generally are sealed off from each other by virtue of the hydrophobic material.
4. A pharmaceutical tablet system according to claim 1, in which the voids are micropores included within the hydropho-bic material.
5. A pharmaceutical tablet system according to claim 1, in which the mixture which the cup-shaped envelope is made of also includes at least one or more pharmaceutically active agent different from said substances contained in one or more release layers.
6. A process of producing a pharmaceutical tablet system according to claim 1, involving the following steps:
coating the powdered filler with the hydrophobic materi-al;
granulating the resulting coated material;
placing a layer of the resulting granulated material into a die;
placing a core according to claim 1 onto the layer of granulated material within the die;
forcing the core into the layer of granulated material within the die; and removing the resulting tablet system from the die.
coating the powdered filler with the hydrophobic materi-al;
granulating the resulting coated material;
placing a layer of the resulting granulated material into a die;
placing a core according to claim 1 onto the layer of granulated material within the die;
forcing the core into the layer of granulated material within the die; and removing the resulting tablet system from the die.
7. A process according to claim 6, in which the step of forcing the core into the layer of granulated material within the die involves a compression of the tablet system made up of the cup-shaped envelope having the core inserted therein to provide a snug fit between mutually facing bottom and side surfaces of the core and surface portions of the cup-shaped envelope.
8. A process of producing a cup-shaped envelope of a phar-maceutical tablet system according to claim 1, involving the following steps:
coating the powdered filler with the hydrophobic materi-al;
granulating the resulting coated material;
placing a layer of the resulting granulated material into a die;
forming a cup-shaped recess into the layer of granulated material by forcing a correspondingly shaped body into it within the die; and removing the resulting cup-shaped envelope from the die.
coating the powdered filler with the hydrophobic materi-al;
granulating the resulting coated material;
placing a layer of the resulting granulated material into a die;
forming a cup-shaped recess into the layer of granulated material by forcing a correspondingly shaped body into it within the die; and removing the resulting cup-shaped envelope from the die.
9. A process according to any of claims 6 to 8, in which the step of coating the powdered filler with the hydrophobic material is a step of spray-coating performed under vigorous stirring.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01108252.6 | 2001-03-31 | ||
| EP01108252A EP1245227A1 (en) | 2001-03-31 | 2001-03-31 | A pharmaceutical tablet system that floats in the stomach for programmed release of active substance and process of producing buoyant material contained in same |
| PCT/IB2002/000959 WO2002085332A1 (en) | 2001-03-31 | 2002-03-18 | A pharmaceutical tablet system that floats on gastric fluid for multipulse release of active substance and respective processes of producing same and a cup-shaped envelope of same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2441123A1 true CA2441123A1 (en) | 2002-10-31 |
| CA2441123C CA2441123C (en) | 2011-05-24 |
Family
ID=8177016
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2441123A Expired - Fee Related CA2441123C (en) | 2001-03-31 | 2002-03-18 | A pharmaceutical tablet system that floats on gastric fluid for multipulse release of active substance, and respective processes of producing same and a cup-shaped envelope of same |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7838028B2 (en) |
| EP (2) | EP1245227A1 (en) |
| JP (1) | JP4276437B2 (en) |
| CN (1) | CN100589793C (en) |
| CA (1) | CA2441123C (en) |
| WO (1) | WO2002085332A1 (en) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602004023597D1 (en) * | 2003-04-24 | 2009-11-26 | Jagotec Ag | TABLET WITH DYED CORE |
| KR20130115401A (en) | 2004-11-19 | 2013-10-21 | 글락소스미스클라인 엘엘씨 | Pharmaceutical product |
| EA012998B1 (en) | 2005-11-18 | 2010-02-26 | Глэксо Груп Лимитед | Machine and method for pharmaceutical and pharmaceutical-like product assembly |
| US20070178155A1 (en) * | 2006-01-31 | 2007-08-02 | Jiang David Yihai | Preparation for gastric buoyant sustained drug release dosage form |
| DE102007026037A1 (en) | 2007-06-04 | 2008-12-11 | Lts Lohmann Therapie-Systeme Ag | Gastroretentive system with alginate body |
| US20160244459A1 (en) | 2013-05-24 | 2016-08-25 | Rhodes Technologies | Opioid ketal compounds and uses thereof |
| DE102014003744A1 (en) | 2014-03-10 | 2015-09-10 | Laboratorium für Lebensmittelwissenschaft (FPE) - Eidgenössische Technische Hochschule Zürich (ETH) | Product for oral administration to humans or animals with microstructured encapsulated ingredients, and apparatus for making such a product, and method of making the same |
| CN109985016B (en) * | 2017-12-29 | 2021-07-27 | 江苏恒瑞医药股份有限公司 | Controlled release composition of febuxostat and preparation method thereof |
| EP3755704A1 (en) | 2018-02-23 | 2020-12-30 | Rhodes Technologies Inc. | Novel opioid compounds and uses thereof |
| WO2021176361A1 (en) * | 2020-03-02 | 2021-09-10 | Craft Health Pte Ltd | Method of manufacturing oral dosage forms for extended drug release |
Family Cites Families (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5512411B2 (en) * | 1974-03-12 | 1980-04-02 | ||
| CH630257A5 (en) * | 1975-03-17 | 1982-06-15 | Hoffmann La Roche | Sustained release formulation |
| US4126672A (en) * | 1976-02-04 | 1978-11-21 | Hoffmann-La Roche Inc. | Sustained release pharmaceutical capsules |
| US4140755A (en) * | 1976-02-13 | 1979-02-20 | Hoffmann-La Roche Inc. | Sustained release tablet formulations |
| US4167558A (en) * | 1976-02-13 | 1979-09-11 | Hoffmann-La Roche Inc. | Novel sustained release tablet formulations |
| GB1576376A (en) * | 1977-03-30 | 1980-10-08 | Benzon As Alfred | Multiple-unit drug dose |
| US4101650A (en) * | 1977-04-06 | 1978-07-18 | Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai | Pepstatin floating minicapsules |
| US4434153A (en) * | 1982-03-22 | 1984-02-28 | Alza Corporation | Drug delivery system comprising a reservoir containing a plurality of tiny pills |
| JPS6143108A (en) * | 1984-08-03 | 1986-03-01 | Nippon Shinyaku Co Ltd | Medicinal drug and its preparation |
| PL149493B1 (en) * | 1985-04-12 | 1990-02-28 | Method of obtaining a tablet capable to buoy over surface of gastric juice | |
| US4735804A (en) * | 1985-05-10 | 1988-04-05 | Merck & Co., Inc. | Drug delivery device which can be retained in the stomach for a controlled period of time |
| EP0202159B1 (en) | 1985-05-10 | 1991-07-03 | Merck & Co. Inc. | Drug delivery device which can be retained in the stomach for a controlled period of time |
| US4767627A (en) * | 1985-05-29 | 1988-08-30 | Merck & Co., Inc. | Drug delivery device which can be retained in the stomach for a controlled period of time |
| US4758436A (en) * | 1985-05-29 | 1988-07-19 | Merck & Co., Inc. | Drug delivery device which can be retained in the stomach for a controlled period of time |
| JPS62195323A (en) * | 1986-02-24 | 1987-08-28 | Eisai Co Ltd | Gastric resident particle |
| US5374430A (en) * | 1986-09-18 | 1994-12-20 | London School Of Pharmacy | Pharmaceutical formulation |
| US4814178A (en) * | 1987-07-01 | 1989-03-21 | Sanford Bolton | Floating sustained release therapeutic compositions |
| JPS6416715A (en) | 1987-07-10 | 1989-01-20 | Kyoto Pharma Ind | Intragastric floating pharmaceutical |
| IL87710A (en) * | 1987-09-18 | 1992-06-21 | Ciba Geigy Ag | Covered floating retard form for controlled release in gastric juice |
| DE3803482A1 (en) * | 1988-02-05 | 1989-08-17 | Lohmann Therapie Syst Lts | FLOATING ORAL THERAPEUTIC SYSTEM |
| GB8809421D0 (en) * | 1988-04-21 | 1988-05-25 | Fordonal Sa | Antacid compositions with prolonged gastric residence time |
| US5002772A (en) * | 1988-05-31 | 1991-03-26 | Pfizer Inc. | Gastric retention system for controlled drug release |
| US5169639A (en) * | 1988-09-19 | 1992-12-08 | Edward Mendell Co., Inc. | Controlled release verapamil tablets |
| JPH0795889B2 (en) | 1989-06-07 | 1995-10-18 | 松山株式会社 | Mining machine |
| DK469989D0 (en) * | 1989-09-22 | 1989-09-22 | Bukh Meditec | PHARMACEUTICAL PREPARATION |
| DE4036757A1 (en) * | 1990-11-17 | 1992-05-21 | Bayer Ag | ANTAZIDA PREPARATION WITH EXTENDED STOMACH TEMPERING |
| US5232704A (en) * | 1990-12-19 | 1993-08-03 | G. D. Searle & Co. | Sustained release, bilayer buoyant dosage form |
| US5198229A (en) * | 1991-06-05 | 1993-03-30 | Alza Corporation | Self-retaining gastrointestinal delivery device |
| IT1249980B (en) | 1991-08-07 | 1995-03-30 | Comau Spa | DEVICE FOR THE WELDING OF STRUCTURES, SUCH AS BODIES OF MOTOR VEHICLES OR PARTS OF THEM, MADE UP OF ELEMENTS OF PRINTED SHEET METAL ASSEMBLED PRELIMINARILY AMONG THEM IN A LABULAR WAY. |
| JPH0624959A (en) | 1991-10-04 | 1994-02-01 | Bayer Yakuhin Kk | Medice release solid pharmaceutical preparation of gastric suspending type sustained |
| US5571533A (en) * | 1992-02-07 | 1996-11-05 | Recordati, S.A., Chemical And Pharmaceutical Company | Controlled-release mucoadhesive pharmaceutical composition for the oral administration of furosemide |
| GB9211148D0 (en) | 1992-05-26 | 1992-07-08 | Smithkline Beecham Plc | Novel treatment |
| US5360793A (en) * | 1993-05-24 | 1994-11-01 | Sterling Winthrop Inc. | Rafting antacid formulation |
| IT1264517B1 (en) | 1993-05-31 | 1996-09-24 | Ekita Investments Nv | PHARMACEUTICAL TABLET SUITABLE FOR THE RELEASE IN SUBSEQUENT TIMES OF THE ACTIVE PRINCIPLES CARRIED THEREIN |
| DE4406424A1 (en) * | 1994-02-28 | 1995-08-31 | Bayer Ag | Expandable dosage forms |
| DE69613966T2 (en) | 1995-03-17 | 2002-04-04 | Boots Co Ltd | PHARMACEUTICAL COMPOSITIONS WITH PECTIN |
| IT1282576B1 (en) * | 1996-02-06 | 1998-03-31 | Jagotec Ag | PHARMACEUTICAL TABLET SUITABLE TO GIVE THE ACTIVE SUBSTANCE IN SUBSEQUENT AND PREDETERMINABLE TIMES |
| WO1997047285A1 (en) | 1996-06-10 | 1997-12-18 | Depomed, Inc. | Gastric-retentive oral controlled drug delivery system with enhanced retention properties |
| PL193282B1 (en) | 1997-01-14 | 2007-01-31 | Lohmann Therapie Syst Lts | Expandable therapeutic system of controllable active substance release in the gastrointestinal tract |
| KR20000076329A (en) | 1997-03-25 | 2000-12-26 | 다케다 야쿠힌 고교 가부시키가이샤 | Gastrointestinal mucosa-adherent pharmaceutical composition |
| FR2762213B1 (en) | 1997-04-18 | 1999-05-14 | Synthelabo | PHARMACEUTICAL COMPOSITION WITH GASTRIC RETENTION |
| GB9710699D0 (en) | 1997-05-24 | 1997-07-16 | Danbiosyst Uk | Gastro-retentive controlled release system |
| US6342249B1 (en) * | 1998-12-23 | 2002-01-29 | Alza Corporation | Controlled release liquid active agent formulation dosage forms |
| EP1074249A1 (en) | 1999-07-27 | 2001-02-07 | Jagotec Ag | A pharmaceutical tablet system for releasing at least one active substance during a release period subsequent to a no-release period |
-
2001
- 2001-03-31 EP EP01108252A patent/EP1245227A1/en not_active Withdrawn
-
2002
- 2002-03-18 US US10/473,055 patent/US7838028B2/en not_active Expired - Fee Related
- 2002-03-18 WO PCT/IB2002/000959 patent/WO2002085332A1/en not_active Application Discontinuation
- 2002-03-18 CN CN02807431A patent/CN100589793C/en not_active Expired - Fee Related
- 2002-03-18 EP EP02716969A patent/EP1372612A1/en not_active Withdrawn
- 2002-03-18 JP JP2002582906A patent/JP4276437B2/en not_active Expired - Fee Related
- 2002-03-18 CA CA2441123A patent/CA2441123C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP2004532222A (en) | 2004-10-21 |
| CN1499961A (en) | 2004-05-26 |
| EP1372612A1 (en) | 2004-01-02 |
| WO2002085332A1 (en) | 2002-10-31 |
| JP4276437B2 (en) | 2009-06-10 |
| CN100589793C (en) | 2010-02-17 |
| US7838028B2 (en) | 2010-11-23 |
| CA2441123C (en) | 2011-05-24 |
| US20040166161A1 (en) | 2004-08-26 |
| EP1245227A1 (en) | 2002-10-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20180319 |