WO2007102714A1 - Composition pour preparation a liberation controlee sure contenant du zolpidem ou un de ses sels - Google Patents

Composition pour preparation a liberation controlee sure contenant du zolpidem ou un de ses sels Download PDF

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Publication number
WO2007102714A1
WO2007102714A1 PCT/KR2007/001146 KR2007001146W WO2007102714A1 WO 2007102714 A1 WO2007102714 A1 WO 2007102714A1 KR 2007001146 W KR2007001146 W KR 2007001146W WO 2007102714 A1 WO2007102714 A1 WO 2007102714A1
Authority
WO
WIPO (PCT)
Prior art keywords
release
polymer
composition according
layer
water
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/KR2007/001146
Other languages
English (en)
Inventor
Jong Lae Lim
Byoung Moo Lee
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.)
Chong Kun Dang Corp
Original Assignee
Chong Kun Dang Corp
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 Chong Kun Dang Corp filed Critical Chong Kun Dang Corp
Publication of WO2007102714A1 publication Critical patent/WO2007102714A1/fr
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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
    • H—ELECTRICITY
    • H04—ELECTRIC COMMUNICATION TECHNIQUE
    • H04N—PICTORIAL COMMUNICATION, e.g. TELEVISION
    • H04N7/00—Television systems
    • H04N7/18—Closed-circuit television [CCTV] systems, i.e. systems in which the video signal is not broadcast
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • G—PHYSICS
    • G06—COMPUTING OR CALCULATING; COUNTING
    • G06V—IMAGE OR VIDEO RECOGNITION OR UNDERSTANDING
    • G06V20/00—Scenes; Scene-specific elements
    • G06V20/50—Context or environment of the image
    • G06V20/52—Surveillance or monitoring of activities, e.g. for recognising suspicious objects
    • H—ELECTRICITY
    • H03—ELECTRONIC CIRCUITRY
    • H03M—CODING; DECODING; CODE CONVERSION IN GENERAL
    • H03M1/00—Analogue/digital conversion; Digital/analogue conversion
    • H03M1/12—Analogue/digital converters
    • H—ELECTRICITY
    • H04—ELECTRIC COMMUNICATION TECHNIQUE
    • H04N—PICTORIAL COMMUNICATION, e.g. TELEVISION
    • H04N19/00—Methods or arrangements for coding, decoding, compressing or decompressing digital video signals
    • H04N19/42—Methods or arrangements for coding, decoding, compressing or decompressing digital video signals characterised by implementation details or hardware specially adapted for video compression or decompression, e.g. dedicated software implementation
    • H—ELECTRICITY
    • H04—ELECTRIC COMMUNICATION TECHNIQUE
    • H04N—PICTORIAL COMMUNICATION, e.g. TELEVISION
    • H04N23/00—Cameras or camera modules comprising electronic image sensors; Control thereof
    • H04N23/60—Control of cameras or camera modules
    • H—ELECTRICITY
    • H04—ELECTRIC COMMUNICATION TECHNIQUE
    • H04N—PICTORIAL COMMUNICATION, e.g. TELEVISION
    • H04N5/00—Details of television systems
    • H04N5/76—Television signal recording
    • H04N5/765—Interface circuits between an apparatus for recording and another apparatus
    • H04N5/77—Interface circuits between an apparatus for recording and another apparatus between a recording apparatus and a television camera

Definitions

  • the present invention relates to a safe controlled release preparation
  • Zolpidem is a sedative-hypnotic drug, which has a bioavailability of about 70%
  • Stilnox ® commercially available, has defects in that it cannot maintain sleep for a
  • EP 1194132 discloses a sustained-release preparation for
  • the sustained-release tablet in the matrix form the sustained-release tablet in the matrix form
  • sustained-release preparation prepared by forming a coating onto pellets comprising an
  • pellets affect perfection of the coating as well as the thickness of the coating applied on
  • sustained-release coating can be damaged.
  • the designed drug release mode can be damaged.
  • such protection coating comprises mainly pH-independent polymer that does
  • the Zolpidem and its salt are psychotropic medicines and it is very important to
  • the present invention relates to a controlled release preparation composition
  • a controlled release preparation composition comprising:
  • the drug of present invention comprises Zolpidem or its pharmaceutically
  • the most preferable salt is in the hemitartrate form, which is
  • part may be in the forms of granule, pellet or coating.
  • coating for example,
  • the drug may be applied on the surface of the delayed sustained-release pellet.
  • immediately-acting part may be prepared using spherical seeds, and it can be
  • pellets having a layer containing the drug formed on the surface of the
  • the method for preparing the immediately-acting part may employ the
  • a pH-independent polymer may be added to form a
  • a binding agent or a disintegrant may be used.
  • a binding agent or a disintegrant those commonly used
  • composition and the preparation method of the immediately-acting part are not
  • the immediately-acting part is defined as having a
  • composition according to the present invention preferably, the delayed
  • sustained-release pellet has a dissolution rate of 10% or less, as measured in 900 mL of
  • composition according to the present invention the drug content of
  • immediately-acting part is preferably 0.3 to 4 times of the drug content of the delayed
  • the delayed sustained-release pellet may have the following configurations.
  • the delayed sustained-release pellet comprises:
  • the active ingredient formed on the surface of the first layer
  • the second layer may further comprise a layer comprising a water-insoluble polymer between the core and the first
  • the delayed sustained-release pellet includes:
  • it may further comprise a layer
  • water-soluble or water-swellable in the "core of a water-soluble or
  • water-swellable inactive material means that the material is substantially soluble
  • polymer for controlling release of the active ingredient means a
  • controlling the release of the active ingredient can accomplish the control of drug
  • compositional ratios of the polymers are compositional ratios of the polymers.
  • polymer for controlling the release of the active ingredient and polymer for protecting the pellet under an acidic condition means that two or more
  • polymers are mixed to protect the pellet under an acidic condition while controlling the
  • composition according to the present invention is not limited to the above-
  • compositional ratio of the components preferably, the active
  • polystyrene resin are used in a weight ratio of 1 :0.3 to 1 :5.0.
  • sucrose/starch spheres sucrose/starch spheres
  • sucrose crystals or spheres prepared using typical excipient, for example,
  • microcrystalline cellulose and lactose by exclusion and drying. Any seeds known and
  • the seeds have a particle size of 300 to 1,000 ⁇ m.
  • the active ingredient contained in the pellet comprises Zolpidem or its
  • the layer comprising the active ingredient may be formed of the active
  • polyalkylene glycol for example, polyethylene glycol; gelatin; polyvinyl alcohol; starch
  • cellulose derivative for example,
  • HPMC hydroxypropylmethylcellulose
  • methacrylic acid polymer or methacrylate polymer(Eudragits) methacrylic acid polymer or methacrylate polymer(Eudragits)
  • hydroxypropylmethylcellulose phthalate and pharmaceutically acceptable polymer.
  • composition of the present invention a water-insoluble polymer can be used alone, or in
  • the usable examples of the water-insoluble polymer include ethylcellulose,
  • water-soluble polymer added for release control examples include polyethylene glycol, polyethylene oxide, gelatin, starch, dextran
  • polyacrylic acid polyvinylpyrrolidone, arabia gum and sodium alginate, but are not
  • the polymer for protecting the pellet under an acidic condition includes enteric
  • coating materials that is enteric polymers, known and commonly used in the
  • HPMCP hydroxypropylmethyl cellulose phthalate
  • HPMCAS cellulose acetate phthalate
  • CAP cellulose acetate phthalate
  • plasticizer may be added.
  • water-insoluble polymer include ethylcellulose, copolymers of metachrylic acid and
  • the capsule filling process is performed by mixing the immediately-acting part
  • a lubricant such as talc or talc
  • magnesium stearate may be added.
  • composition of the present invention has
  • the delayed sustained-release pellet is protected by the enteric coating. That is, the delayed sustained-release pellet is protected by the enteric coating.
  • Example 1 Preparation of immediately-acting pellet 600 g of sugar spheres of 500 to 710 ⁇ m was placed in a fluid bed coating
  • Example 1 except using 355 to 500 ⁇ m sugar spheres, was placed in a fluid bed coating
  • Example 1 78.6 g and 86.5 g of the pellets prepared in Example 1 and Example 3 were
  • Example 2 83.3 g and 86.5 g of the pellets prepared in Example 2 and Example 4 were
  • Example 1 except using 355 to 500 ⁇ m sugar spheres, was placed in a fluid bed coating
  • delayed sustained-release pellets were prepared.
  • Example 1 78.6 g and 81.3 g of pellets prepared in Example 1 and Example 7 were mixed
  • Dissolution test 1 Dissolution test of immediately-acting pellet The pellets corresponding to 12.5 mg of Zolpidem hemitartrate were precisely
  • Dissolution test 2 Acid resistant test of delayed sustained-release pellet
  • Dissolution test 3 Dissolution test of delayed sustained-release pellet
  • Dissolution test 4 dissolution test of capsules
  • capsules were taken from each group of capsules prepared in Examples 5, 6
  • dissolution sample was taken from the solution of 900 mL and after 2 hours and 8 hours, the dissolution sample was taken from 900 mL of the solution of pH 6.8 phosphate
  • Dissolution rate [At/As] x [9/10] x [reference weight (mg)/20] x reference
  • the present invention relates to a safe controlled release preparation comprising
  • sustained-release pellets it is possible to rapidly induce sleep, stably control drug

Landscapes

  • Engineering & Computer Science (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Multimedia (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Signal Processing (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Theoretical Computer Science (AREA)
  • Physics & Mathematics (AREA)
  • General Physics & Mathematics (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une préparation à libération contrôlée contenant du Zolpidem ou un de ses sels. L'invention concerne plus particulièrement une composition pharmaceutique contenant une partie à action immédiate libérant rapidement un médicament, et des pastilles à libération soutenue retardant la libération de médicament le temps que le revêtement gastro-résistant traverse l'estomac. La composition selon l'invention se caractérise par une libération double chrono-contrôlée et elle permet d'éviter les effets secondaires causés par une libération subite de médicament des pastilles à libération soutenue.
PCT/KR2007/001146 2006-03-08 2007-03-08 Composition pour preparation a liberation controlee sure contenant du zolpidem ou un de ses sels Ceased WO2007102714A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020060021792A KR20070091960A (ko) 2006-03-08 2006-03-08 졸피뎀 또는 그의 염을 포함하는 안전한 제어방출형 제제조성물
KR10-2006-0021792 2006-03-08

Publications (1)

Publication Number Publication Date
WO2007102714A1 true WO2007102714A1 (fr) 2007-09-13

Family

ID=38475107

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2007/001146 Ceased WO2007102714A1 (fr) 2006-03-08 2007-03-08 Composition pour preparation a liberation controlee sure contenant du zolpidem ou un de ses sels

Country Status (2)

Country Link
KR (1) KR20070091960A (fr)
WO (1) WO2007102714A1 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009085310A1 (fr) * 2007-12-26 2009-07-09 Teva Pharmaceutical Industries Ltd. Compositions pharmaceutiques à libération prolongée contenant du zolpidem
EP1980244A3 (fr) * 2007-04-12 2010-11-17 Nipro Corporation Particules de base et comprimé se délitant en bouche les contenant
EP2829267A4 (fr) * 2012-03-23 2015-09-30 Inst Pharm & Toxicology Amms Composition pharmaceutique à libération prolongée à base de topiramate, son procédé de préparation et son utilisation
US9421188B2 (en) 2012-03-23 2016-08-23 Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China Combination product comprising phentermine and topiramate, and preparation method thereof
US9457008B2 (en) 2012-03-23 2016-10-04 Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China Joint product comprising synephrine and topiramate
JPWO2017146053A1 (ja) * 2016-02-23 2018-12-20 ニプロ株式会社 医薬組成物粒子とそれを含む口腔内崩壊製剤

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101579254B1 (ko) 2015-04-29 2015-12-21 김희수 금속바

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000033835A1 (fr) * 1998-12-04 2000-06-15 Sanofi-Synthelabo Formes posologiques a liberation regulee contenant du zolpidem ou un sel de celui-ci
US6228398B1 (en) * 1998-11-02 2001-05-08 Elan Corporation, Plc Multiparticulate modified release composition
WO2004045589A1 (fr) * 2002-11-15 2004-06-03 Elan Pharmaceuticals, Inc. Composition a liberation modifiee comprenant un hypnotique a action breve, destinee au traitement des troubles du sommeil
EP1194132B1 (fr) * 1999-06-28 2004-06-16 Sanofi-Synthelabo Formes de dosage a double liberation dans le temps comprenant un hypnotique, ou un de ses sels, a action breve

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6228398B1 (en) * 1998-11-02 2001-05-08 Elan Corporation, Plc Multiparticulate modified release composition
WO2000033835A1 (fr) * 1998-12-04 2000-06-15 Sanofi-Synthelabo Formes posologiques a liberation regulee contenant du zolpidem ou un sel de celui-ci
EP1194132B1 (fr) * 1999-06-28 2004-06-16 Sanofi-Synthelabo Formes de dosage a double liberation dans le temps comprenant un hypnotique, ou un de ses sels, a action breve
WO2004045589A1 (fr) * 2002-11-15 2004-06-03 Elan Pharmaceuticals, Inc. Composition a liberation modifiee comprenant un hypnotique a action breve, destinee au traitement des troubles du sommeil

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1980244A3 (fr) * 2007-04-12 2010-11-17 Nipro Corporation Particules de base et comprimé se délitant en bouche les contenant
WO2009085310A1 (fr) * 2007-12-26 2009-07-09 Teva Pharmaceutical Industries Ltd. Compositions pharmaceutiques à libération prolongée contenant du zolpidem
EP2829267A4 (fr) * 2012-03-23 2015-09-30 Inst Pharm & Toxicology Amms Composition pharmaceutique à libération prolongée à base de topiramate, son procédé de préparation et son utilisation
US9421188B2 (en) 2012-03-23 2016-08-23 Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China Combination product comprising phentermine and topiramate, and preparation method thereof
US9457008B2 (en) 2012-03-23 2016-10-04 Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China Joint product comprising synephrine and topiramate
JPWO2017146053A1 (ja) * 2016-02-23 2018-12-20 ニプロ株式会社 医薬組成物粒子とそれを含む口腔内崩壊製剤
EP3431107A4 (fr) * 2016-02-23 2019-11-13 Nipro Corporation Particules de composition pharmaceutique et préparation se délitant par voie orale comprenant celles-ci

Also Published As

Publication number Publication date
KR20070091960A (ko) 2007-09-12

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