WO2009150514A1 - Process for making gastroretentive dosage forms - Google Patents

Process for making gastroretentive dosage forms Download PDF

Info

Publication number
WO2009150514A1
WO2009150514A1 PCT/IB2009/005889 IB2009005889W WO2009150514A1 WO 2009150514 A1 WO2009150514 A1 WO 2009150514A1 IB 2009005889 W IB2009005889 W IB 2009005889W WO 2009150514 A1 WO2009150514 A1 WO 2009150514A1
Authority
WO
WIPO (PCT)
Prior art keywords
agents
hydrochloride
dosage form
anyone
powder
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/IB2009/005889
Other languages
English (en)
French (fr)
Inventor
Pascal Prinderre
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.)
Aix Marseille Universite
Original Assignee
Universite de la Mediterranee Aix Marseille II
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 Universite de la Mediterranee Aix Marseille II filed Critical Universite de la Mediterranee Aix Marseille II
Priority to ES09762044.7T priority Critical patent/ES2561478T3/es
Priority to CA2727206A priority patent/CA2727206A1/en
Priority to EP09762044.7A priority patent/EP2303241B1/en
Priority to CN200980128984.9A priority patent/CN102105139B/zh
Priority to JP2011513066A priority patent/JP5675598B2/ja
Priority to US12/997,092 priority patent/US9060930B2/en
Publication of WO2009150514A1 publication Critical patent/WO2009150514A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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
    • A61K9/0012—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

Definitions

  • (2002) 241 :279-292 which provides examples of such matrix forming polymers: hydroxypropyl methylcellulose, polyacrylates, sodium alginates, corn starch, carrageenan, gum guar, gum arabic, Eudragit®RS, ethyl cellulose, or poly methyl methacrylate.
  • the resulting overgranulated material provided with high porosity and low density may be used to manufacture either the solid dosage form in its whole, or the core. Indeed, according to these different embodiments, any oral dosage form comprising this material will have the required floating properties.
  • Bioadhesive agents may also be incorporated on the outer layer of the solid form, allowing the pharmaceutical form positioning and adhesion to the mucosa of the stomach or the upper gastrointestinal tract.
  • the invention provides an oral solid dosage form having an enhanced solubility in acidic medium such as the gastric juice.
  • the composition exhibits a dissolution profile in hydrochloric acid 0.1 N buffer at pH 1.2, using the US Pharmacopoeia type II method at 150 rpm and using a sinker instead of a mesh, of no more than 80% after 2 hours, preferably no more than 70% after 2 hours and more preferably no more than 60%.
  • the sinker is used in order to conform the USP standards to the case of the present floating forms and ensure the immersion of the form into the liquid. Thus, this characteristic allows an improved bioavailability of the drug to be released.
  • the wetting solution can comprise (albeit this is not preferred) part or, all of the binder and/or part or all of the API, if it is water soluble and/or part or all of a surfactant if any.
  • the weight ratio of solution: powder to reach is strongly dependant of the global solubility of the powder mixture and is generally higher than 0.3, and typically comprised in the range of about 0.3:1 to about 3:1, preferably of about 0.7:1 to about 2:1. It is worth to remind that traditional granulation is performed with a rather low liquid: powder ratio, typically of from 0.1 :1 to 0.3:1. Such a low ratio is used to avoid overgranulation in a typical granulation method, where overgranulation is exactly what is looked for in the instant process.
  • the solid dosage forms of the invention can be prepared by techniques which are easily operated at an industrial scale.

Landscapes

  • Health & Medical Sciences (AREA)
  • Nutrition Science (AREA)
  • Physiology (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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
PCT/IB2009/005889 2008-06-09 2009-06-08 Process for making gastroretentive dosage forms Ceased WO2009150514A1 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
ES09762044.7T ES2561478T3 (es) 2008-06-09 2009-06-08 Proceso de fabricación de formas de dosificación de retención gástrica
CA2727206A CA2727206A1 (en) 2008-06-09 2009-06-08 Process for making gastroretentive dosage forms
EP09762044.7A EP2303241B1 (en) 2008-06-09 2009-06-08 Process for making gastroretentive dosage forms
CN200980128984.9A CN102105139B (zh) 2008-06-09 2009-06-08 制备胃滞留剂型的方法
JP2011513066A JP5675598B2 (ja) 2008-06-09 2009-06-08 胃保持型製剤の製造法
US12/997,092 US9060930B2 (en) 2008-06-09 2009-06-08 Process for making gastroretentive dosage forms

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08290529.0 2008-06-09
EP08290529A EP2133071A1 (en) 2008-06-09 2008-06-09 Process for making gastroretentive dosage forms

Publications (1)

Publication Number Publication Date
WO2009150514A1 true WO2009150514A1 (en) 2009-12-17

Family

ID=40219495

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2009/005889 Ceased WO2009150514A1 (en) 2008-06-09 2009-06-08 Process for making gastroretentive dosage forms

Country Status (7)

Country Link
US (1) US9060930B2 (https=)
EP (2) EP2133071A1 (https=)
JP (2) JP5675598B2 (https=)
CN (1) CN102105139B (https=)
CA (1) CA2727206A1 (https=)
ES (1) ES2561478T3 (https=)
WO (1) WO2009150514A1 (https=)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013540148A (ja) * 2010-10-22 2013-10-31 メリアティ 多粒子状の胃保持型製剤の製造方法
US8580302B2 (en) 2000-11-20 2013-11-12 Warner Chilcott Company, Llc Pharmaceutical dosage form with multiple coatings for reduced impact of coating fractures
US9119793B1 (en) 2011-06-28 2015-09-01 Medicis Pharmaceutical Corporation Gastroretentive dosage forms for doxycycline
US10835495B2 (en) 2012-11-14 2020-11-17 W. R. Grace & Co.-Conn. Compositions containing a biologically active material and a non-ordered inorganic oxide material and methods of making and using the same
US10842802B2 (en) 2013-03-15 2020-11-24 Medicis Pharmaceutical Corporation Controlled release pharmaceutical dosage forms
CN118526484A (zh) * 2024-07-26 2024-08-23 中国中医科学院中药研究所 青蒿琥酯或双氢青蒿素在制备改善罗格列酮不良反应制剂中的应用

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013114390A1 (en) * 2012-01-02 2013-08-08 Medreich Limited Gastro retentive drug delivery system of calcium supplements
CN103462917A (zh) * 2013-09-12 2013-12-25 南京正宽医药科技有限公司 一种用于抗病毒的阿昔洛韦片剂及其制备方法
CN103462926B (zh) * 2013-09-23 2015-09-16 淄博齐鼎立专利信息咨询有限公司 一种泛昔洛韦片剂及其制备方法
EP3148514B1 (en) 2014-06-02 2024-04-17 Clexio Biosciences Ltd. Expandable gastroretentive dosage form
US10076494B2 (en) 2016-06-16 2018-09-18 Dexcel Pharma Technologies Ltd. Stable orally disintegrating pharmaceutical compositions
EP3547974B1 (en) 2016-12-02 2023-11-15 Clexio Biosciences Ltd. Gastric residence system
JP7296084B2 (ja) 2017-12-04 2023-06-22 クレキシオ バイオサイエンシーズ エルティーディー． 長時間作用型胃滞留システム
US11337919B2 (en) * 2017-12-18 2022-05-24 Tris Pharma, Inc. Modified release drug powder composition comprising gastro-retentive RAFT forming systems having trigger pulse drug release
CN116459226B (zh) * 2023-04-26 2025-04-18 重庆康刻尔制药股份有限公司 一种铝碳酸镁双层片及其制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0235718A2 (en) * 1986-02-24 1987-09-09 Eisai Co., Ltd. Granule remaining in stomach
US5626876A (en) * 1988-02-05 1997-05-06 Lts Lohmann Therapie-Systeme Gmbh & Co., Kg Floating system for oral therapy
WO2001058424A1 (en) * 2000-02-09 2001-08-16 West Pharmaceutical Services Drug Delivery & Clinical Research Centre Limited Floating drug delivery composition

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL149493B1 (en) 1985-04-12 1990-02-28 Method of obtaining a tablet capable to buoy over surface of gastric juice
US4814178A (en) 1987-07-01 1989-03-21 Sanford Bolton Floating sustained release therapeutic compositions
US5169638A (en) 1991-10-23 1992-12-08 E. R. Squibb & Sons, Inc. Buoyant controlled release powder formulation
ATE260646T1 (de) * 1996-04-16 2004-03-15 Novartis Consumer Health Sa Schnell zerfallende orale dosierungsform
JP2001270827A (ja) 2000-03-23 2001-10-02 Eisai Co Ltd ベンズイミダゾール系化合物含有錠剤
JP2002154948A (ja) * 2000-11-22 2002-05-28 Eisai Co Ltd 崩壊性に優れた錠剤
EP1478345A4 (en) * 2002-01-03 2010-11-17 Glaxosmithkline Llc NOVEL PHARMACEUTICAL DOSAGE FORMS AND PROCESS FOR PRODUCTION OF SAID DOSAGE FORMS
WO2004002445A2 (en) * 2002-06-26 2004-01-08 Cadila Healthcare Limited Novel floating dosage form
WO2007137216A2 (en) * 2006-05-22 2007-11-29 Janssen Pharmaceutica, N.V. Gastroretentive sustained release formulations
ES2368356T3 (es) * 2007-07-06 2011-11-16 Basf Corporation Composición de retención gástrica basada en un producto de reacción hidrosoluble procedente de un precursor que contiene un grupo vinilo.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0235718A2 (en) * 1986-02-24 1987-09-09 Eisai Co., Ltd. Granule remaining in stomach
US5626876A (en) * 1988-02-05 1997-05-06 Lts Lohmann Therapie-Systeme Gmbh & Co., Kg Floating system for oral therapy
WO2001058424A1 (en) * 2000-02-09 2001-08-16 West Pharmaceutical Services Drug Delivery & Clinical Research Centre Limited Floating drug delivery composition

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8580302B2 (en) 2000-11-20 2013-11-12 Warner Chilcott Company, Llc Pharmaceutical dosage form with multiple coatings for reduced impact of coating fractures
US9089492B2 (en) 2000-11-20 2015-07-28 Warner Chilcott Company, Llc Pharmaceutical dosage form with multiple coatings for reduced impact of coating fractures
JP2013540148A (ja) * 2010-10-22 2013-10-31 メリアティ 多粒子状の胃保持型製剤の製造方法
US9119793B1 (en) 2011-06-28 2015-09-01 Medicis Pharmaceutical Corporation Gastroretentive dosage forms for doxycycline
US10835495B2 (en) 2012-11-14 2020-11-17 W. R. Grace & Co.-Conn. Compositions containing a biologically active material and a non-ordered inorganic oxide material and methods of making and using the same
US10842802B2 (en) 2013-03-15 2020-11-24 Medicis Pharmaceutical Corporation Controlled release pharmaceutical dosage forms
CN118526484A (zh) * 2024-07-26 2024-08-23 中国中医科学院中药研究所 青蒿琥酯或双氢青蒿素在制备改善罗格列酮不良反应制剂中的应用

Also Published As

Publication number Publication date
ES2561478T3 (es) 2016-02-26
US9060930B2 (en) 2015-06-23
JP2015007131A (ja) 2015-01-15
JP5675598B2 (ja) 2015-02-25
EP2133071A1 (en) 2009-12-16
CN102105139A (zh) 2011-06-22
US20120021009A1 (en) 2012-01-26
JP6054931B2 (ja) 2016-12-27
JP2011522873A (ja) 2011-08-04
EP2303241B1 (en) 2015-11-04
EP2303241A1 (en) 2011-04-06
CN102105139B (zh) 2014-12-31
CA2727206A1 (en) 2009-12-17

Similar Documents

Publication Publication Date Title
US9060930B2 (en) Process for making gastroretentive dosage forms
JP5871939B2 (ja) 多粒子状の胃保持型製剤の製造方法
US11839684B2 (en) Mucoadhesive pharmaceutical composition and preparation method therefor
US20090317465A1 (en) Composition and method of preparation of release systems for constant (zero-order) release of active agents
CA2631492A1 (en) Processes for making particle-based pharmaceutical formulations for oral administration
US20100112054A1 (en) Tablets and discs with compartments with two or more drugs for release at certain intervals and with specific rates
CN101073573A (zh) 可口服β－内酰胺抗生素的缓释组合物
WO2012006963A1 (zh) 在控释制剂中的聚合物增强剂
JP5433295B2 (ja) キサンタンガム被覆水溶性糖類及び圧縮成形製剤
JP2011184378A (ja) 口腔内崩壊製剤
Kumar et al. A review on floating drug delivery systems
HK1189505A (en) Process for making multiparticulate gastroretentive dosage forms
TW201609193A (zh) 含有碳酸鹽之口腔內崩解錠劑用組成物及口腔內崩解錠劑
Korbely Preparation and investigation of polymethacrylate-based matrix systems

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 200980128984.9

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 09762044

Country of ref document: EP

Kind code of ref document: A1

WWE Wipo information: entry into national phase

Ref document number: 2727206

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 2011513066

Country of ref document: JP

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 139/CHENP/2011

Country of ref document: IN

Ref document number: 2009762044

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 12997092

Country of ref document: US