WO2016020936A2 - Nouvelle forme posologique pharmaceutique orale de rétention gastrique - Google Patents

Nouvelle forme posologique pharmaceutique orale de rétention gastrique Download PDF

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Publication number
WO2016020936A2
WO2016020936A2 PCT/IN2015/050070 IN2015050070W WO2016020936A2 WO 2016020936 A2 WO2016020936 A2 WO 2016020936A2 IN 2015050070 W IN2015050070 W IN 2015050070W WO 2016020936 A2 WO2016020936 A2 WO 2016020936A2
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WO
WIPO (PCT)
Prior art keywords
core
insoluble
dosage form
container
composition layer
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PCT/IN2015/050070
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English (en)
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WO2016020936A3 (fr
Inventor
Jayendrakumar Dasharathlal PATEL
Shwetaben Dasharathlal PATEL
Original Assignee
Patel Jayendrakumar Dasharathlal
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Application filed by Patel Jayendrakumar Dasharathlal filed Critical Patel Jayendrakumar Dasharathlal
Publication of WO2016020936A2 publication Critical patent/WO2016020936A2/fr
Publication of WO2016020936A3 publication Critical patent/WO2016020936A3/fr

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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
    • A61K9/4891—Coated capsules; Multilayered drug free capsule shells
    • 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
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2886—Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer
    • 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
    • A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release

Definitions

  • U.S. Patent No. 7,485,322 discloses a floating capsule dosage form having prolonged
  • a NOVEL ORAL GASTRORETENTIVE gastric residence time wherein the capsule body and PHARMACEUTICAL DOSAGE FORM cap are assembled such as to encapsulate at least a
  • a present invention is relates to a novel oral is coated with a coating which is substantially gastroretentive pharmaceutical dosage form and insoluble or poorly soluble in an acidic medium.
  • the tablet and granulate comprise pharmaceutical dosage form.
  • active and hydrophihc or lipophilic substances which BACKGROUND OF THE INVENTION helps in controlling the release.
  • the active -release is [0002]
  • Oral delivery of drugs is by far the most controlled by a dual mechanism, one with the help of preferable route of drug delivery due to the ease of hydrophihc or lipophilic substances in the matrix of administration, patient compliance and flexibility in tablet and granulates, and second with the help of an formulation, etc. Controlled drug therapy may reduce outer coating layer.
  • WO2013054285A1 disclose a gastroretentive dosage resulting in improved patient compliance.
  • the main system comprising: (a) a shell filled with the active target is the improved efficiency in treatment. ingredient in powder form; (b) an extended-release However, conventional controlled-release drug layer over the shell; and (c) an immediate -release delivery systems are of only limited use for (1) drugs layer comprising the active ingredient over the acting locally in the stomach, (2) drugs that are extended -release layer.
  • U.S. Pat. No. 5,198,229 discloses a fluid- poorly soluble at alkaline pH, (4) drugs with a narrow imbibing drug delivery device having a first, low window of absorption, (5) drugs rapidly absorbed density such that it floats in the stomach contents for from the GI tract and (6) drugs that degrade in the a predetermined prolonged period of time, during colon. which prolonged period of time it dispenses a drug or
  • Controlled-release drug delivery systems other active agent to the stomach, and having a intended for prolonged gastric retention in the second, higher density such that the device exits the stomach are known in the art.
  • Several systems are stomach at the end of the predetermined prolonged described in the art, implementing various period of time.
  • U.S. Patent No. 3,976,764 discloses solid feasible manner. Moreover, it is desired to obtain a therapeutic preparations floatable in the gastric juice novel gastroretentive technology that deliver one or wherein the active ingredient is impregnated into a more active substances at same or different release body of empty globular shell or a small granular rate by same or different release mechanism for same lump of a material having high buoyancy.
  • outer surface of half-piece of capsule is of gastrointestinal tract from single drug delivery separately coated with enteric coating material.
  • Each system i.e. a dosage form that is relatively flexible of the openings of said coated half pieces are tamped with respect to how to obtain a desired release pattern with flat tablets and the gap between the contact area of the same or different active substances.
  • a novel oral gastroretentive pharmaceutical dosage of the piece of capsule and the tamped tablet with a form comprises single layer or multilayer core, sealant of water insoluble material. wherein at least one layer of core is floatable in the gastric fluid of the stomach while releasing drug or drugs contained therein into the gastric fluid of the into two or more segment, wherein each segment has stomach. a predetermined quantity of drug or drugs.
  • a novel oral gastroretentive pharmaceutical dosage form comprises multilayer core, wherein at least one form which provide different release pattern.
  • layer of core is floatable in the gastric fluid of the Example of such release pattern include, but are not stomach while releasing drug or drugs contained limited to be, zero order release, release other than therein into the gastric fluid of the stomach and at zero order, ascending order release, descending order least another layer of core is either gastroretentive release, conventional order release, release in specific layer or non gastroretentive layer releasing drug or location of gastrointestinal tract, release in two drugs contained therein into stomach or other than different location of gastrointestinal tract, etc.
  • a novel oral gastroretentive pharmaceutical dosage a novel oral gastroretentive pharmaceutical dosage form, wherein size or dimension of oral form comprises multilayer core, wherein at least one gastroretentive pharmaceutical dosage form may be layer of core is active ingredient composition layer smaller compare to conventional dosage form to and at least another layer of core is functional obtain such release pattern.
  • composition layer wherein particular function is [0021] It is an object of present invention to design assign to each functional composition layer. a novel oral gastroretentive pharmaceutical dosage [0013] It is an object of present invention to provide form which delivers the drug or drugs in controlled the aforesaid a novel oral gastroretentive manner from predefined surface area.
  • composition layer of core that are optimized with [0014] It is an object of present invention to provide respect to therapeutic effect.
  • an oral a novel oral gastroretentive pharmaceutical dosage gastroretentive pharmaceutical dosage form form that comprises multi-layer core, wherein said comprising:
  • dosage form is being able to release each layer a) at least one container (S) having one or more independently of same or different active substances aperture and a wall having an inside and an into the aqueous fluid with which it comes into outside;
  • container (S) is form which is divisible from specific region of capsule shell.
  • a drug delivery compromising with functionality of coating film. system comprises a core, a said core comprising one [0018] It is an object of present invention to provide or more composition layer, wherein at least one afore-said a novel oral gastroretentive pharmaceutical composition layer is active ingredient composition dosage form comprising predetermined quantity of layer (L) comprises an active ingredients (A) and drug or drugs is administrable in part after dividing it optionally other pharmaceutically acceptable excipients (X).
  • dosage form BRIEF DESCRIPTION OF THE DRAWINGS additionally comprising one or more inner coat on [0035]
  • Figure 1 is a diagrammatic representation of outer surface of core.
  • inner coat an embodiment of novel oral gastroretentive dosage is swellable coat.
  • inner coat form of the present invention which comprises is non- swellable coat or insoluble coat. container (S).
  • Figure 1A is a diagrammatic representation least one preselected external surface of core within of an embodiment of novel oral gastroretentive container (S) in such a way that it entrap air or create dosage form of the present invention comprising at void between at least one inner surface of container least one container (S) (4) having one or more (S) and at least one outer surface of core which is at aperture and a wall having an inside and an outside, a least sufficient to float the whole dosage form in core (5) comprising an active ingredients (A) and gastric fluid of stomach for sufficient period of time.
  • S novel oral gastroretentive container
  • drug delivery excipients encapsulate at least one preselected system comprises a water insoluble coating in full or external surface of core (3) within container (S) (4) in in part on outer surface of step (c) composition. such a way that it entrap air or create void (2)
  • Figure IB is a diagrammatic representation inside and an outside; of an embodiment of novel oral gastroretentive b) a core comprising an active ingredients (A) dosage form of the present invention comprising at and optionally other pharmaceutically least one container (S) (4) having one or more acceptable excipients (X); and aperture and a wall having an inside and an outside, a c) encapsulate at least one preselected external core (5) comprising an active ingredients (A) and surface of core within insoluble container (C) optionally other pharmaceutically acceptable in such a way that it entrap air or create void excipients, inner coat (8) surrounding core, between at least one inner surface of encapsulate at least one preselected external surface insoluble container (C) and at least one outer of inner coated core (3) within container (S) (4) in surface of core. such a way that it entrap air or create void (2)
  • insoluble container between at least one inner surface of container (S) (1) (C) is capsule shell. and at least one outer surface of inner coated core (3);
  • insoluble and water insoluble coating (7) surrounding step (c) container (C) is made insoluble by chemical composition comprising pore forming agent (6). treatment, by high temperature, by high humidity, by [0038]
  • Figure 1C is a diagrammatic representation ultraviolet (UV) and visible rays, by dyes, by making of an embodiment of novel oral gastroretentive it from material which is either slowly soluble or dosage form of the present invention comprising at soluble in aqueous environment after certain period least one container (S) (4) having one or more of lag time or pH dependent soluble material, or by aperture and a wall having an inside and an outside, a any other novel techniques for which the amount of multilayer core (5) comprising three composition information is limited. layer, wherein two composition layer is active
  • a drug delivery ingredient composition layer (L) and another system comprises a core, a said core comprising one composition layer is functional composition layer (F), or more composition layer, wherein at least one inner coat (8) surrounding multilayer core, composition layer is active ingredient composition encapsulate at least one preselected external surface layer (L) comprises an active ingredients (A) and of inner coated multilayer core (3) within container optionally other pharmaceutically acceptable (S) (4) in such a way that it entrap air or create void excipients (X). (2) between at least one inner surface of container (S)
  • Figure 2 is a diagrammatic representation of of core which is at least sufficient to float the whole an embodiment of novel oral gastroretentive dosage dosage form in gastric fluid of stomach for sufficient form of the present invention which comprises period of time. insoluble container (C).
  • FIG. 2A is a diagrammatic representation
  • the gastroretentive drug delivery system not of an embodiment of novel oral gastroretentive only reduce the number of administrations of active dosage form of the present invention comprising at substance but also improve therapeutic efficacy of (1) least one insoluble container (C) (4) having one or drugs acting locally in the stomach, (2) drugs that are more aperture and a wall having an inside and an primarily absorbed in the stomach or at upper part of outside, a core (5) comprising an active ingredients intestinal tract, (3) drugs that is poorly soluble at (A) and optionally other pharmaceutically acceptable alkaline pH, (4) drugs with a narrow window of excipients, encapsulate at least one preselected absorption, (5) drugs that degrade in the colon, and external surface of core (3) within insoluble container (6) Drugs that disturb normal colonic microbes.
  • C insoluble container
  • water container (C) (1) and at least one outer surface of insoluble excipient is used to refer excipient which inner coated core (3). is insoluble in water at all pH or insoluble as such but
  • Figure 2B is a diagrammatic representation soluble in presence of other excipients or insoluble in of an embodiment of novel oral gastroretentive at least one region of gastrointestinal tract or dosage form of the present invention comprising at insoluble in water at certain pH such as e.g. eudragit least one insoluble container (C) (4) having one or L100 55 is insoluble at pH below 5.5.
  • pH such as e.g. eudragit least one insoluble container (C) (4) having one or L100 55 is insoluble at pH below 5.5.
  • a core (5) comprising an active ingredients be understood as it is insoluble in water at all pH or (A) and optionally other pharmaceutically acceptable insoluble in water at certain pH or insoluble as such excipients, inner coat (6) surrounding core, but soluble in presence of other excipients.
  • water soluble of inner coated core (3) within insoluble container excipient is used to refer excipients which are (C) (4) in such a way that it entrap air or create void soluble in water at all pH or soluble in at least one (2) between at least one inner surface of insoluble region of gastrointestinal tract or soluble in water at container (C) (1) and at least one outer surface of certain pH such as e.g. Eudragit L100 55 is soluble at inner coated core (3). pH 5.5 or it above. So when the term "water soluble of inner coated core (3) within insoluble container excipient” is used to refer excipients which are (C) (4) in such a way that it entrap air or create void soluble in water at all pH or soluble in at least one (2) between at least one inner surface of insoluble region of gastrointestinal tract or soluble in water at container (C) (1) and at least one outer surface of certain pH such as e.g. Eudragit L100 55 is soluble at inner coated core (3). pH 5.5 or it above. So when
  • Figure 2C is a diagrammatic representation excipient" is specified, it is to be understood as it is of an embodiment of novel oral gastroretentive soluble in water at all pH or soluble in water at dosage form of the present invention comprising at certain pH.
  • the term "water more aperture and a wall having an inside and an insoluble coating” is used to refer coating which is outside, a multilayer core (5) comprising three insoluble in water at all pH or insoluble as such but composition layer, wherein two composition layer is soluble in presence of other excipients or insoluble in active ingredient composition layer (L) and another at least one region of gastrointestinal tract or composition layer is functional composition layer (F), insoluble in water at certain pH such as e.g. coating inner coat (8) surrounding a multilayer core, of eudragit LI 00 55 is insoluble at pH below 5.5.
  • FIG. 3 is a diagrammatic representation of floatable in the gastric fluid of the stomach while container (3) having one or more aperture (4) and a releasing drug or drugs contained therein into the wall having an inside (1) and an outside (2). gastric fluid of the stomach.
  • Figure 4 is a diagrammatic representation of provide a novel gastroretentive pharmaceutical core (1) having outer/external surface (2). dosage form, wherein whole dosage form is floatable DETAILED DESCRIPTION OF THE in the gastric fluid of the stomach or part of dosage INVENTION form is floatable in the gastric fluid of the stomach.
  • a novel gastroretentive pharmaceutical medicament but also on whether its formulation is dosage form which is floatable in the gastric fluid of optimum from the technical and biopharmaceutical the stomach is being capable to release drug or drugs viewpoint. contained therein for prolong period of time into at least one region of GI tract, wherein at least one region of GI tract is stomach.
  • a novel surface for specific period of time is provided.
  • the term "active floatable in the gastric fluid of the stomach is being ingredient composition layer” is used herein to refer capable to release drug or drugs contained therein composition layer that release the drug contained into two or more region of GI tract, wherein at least therein into immediate release or controlled release one region of GI tract is stomach and another region manner.
  • the letter “L” is used in present invention to of GI tract is other than stomach. refer active ingredient composition layer.
  • controlled release includes “delayed release", invention, a novel gastroretentive pharmaceutical "extended release”, “prolong release”, “long-acting”, dosage form is divisible from specific region of “modified release”, “slow release”, “sustained dosage form into two or more segments without release”, “time release”, “pulsatile release” and the altering the release of drug or drugs from dosage like, all of which are understood to refer to a release form.
  • a novel gastroretentive pharmaceutical release after certain period of time is later or slower than "immediate release or invention.
  • an oral dosage form into two or more segment without gastroretentive pharmaceutical dosage form altering the release of drug or drugs from dosage comprising:
  • “segment” is used to refer divided part of b) a core comprising an active ingredients (A) and gastroretentive pharmaceutical dosage form. optionally other pharmaceutically acceptable [0053] According to an embodiment of present excipients (X);
  • a novel gastroretentive pharmaceutical c) encapsulate at least one preselected external dosage form is being capable to release drug or drugs surface of core within container (S) in such a contained therein in pulsatile manner or after specific way that it entrap air or create void between at period of time.
  • the present least one outer surface of core; and invention provides a novel gastroretentive d) water insoluble coating surrounding step (c) pharmaceutical dosage form, wherein it is a possible composition.
  • Example of such release pattern include, but system comprising one or more containers (S), a said are not limited to be, zero order release, release other container (S) has one or more aperture and a wall than zero order, ascending order release, descending having an inside and an outside surface.
  • container (S) is period of time, conventional release, release in soluble in gastrointestinal fluid.
  • container (S) is two different location of gastrointestinal tract, etc. capsule shell.
  • dosage form desired release pattern of the same or different active additionally comprising one or more inner coat on substances from single drug delivery system. outer surface of core.
  • inner coat [0056]
  • the present invention is swellable coat comprising at least one swellable provide a novel gastroretentive pharmaceutical excipient.
  • inner coat is non- dosage form, wherein size or dimension of dosage swellable coat or insoluble coat comprising at least form may be smaller compare to conventional dosage one excipients selected from group consisting of form to obtain such release pattern.
  • a gastroretentive pH dependent soluble material, enzyme degradable pharmaceutical dosage form is able to release drug or material or mixture thereof.
  • inner coat is either insoluble or soluble. In some and/or film coating surrounding outer surface of embodiment, inner coat is water insoluble coating water insoluble coating.
  • part of inner coat is gastroretentive pharmaceutical dosage form being sandwich between inner surface of container comprising:
  • core is utilized in present invention, it is to be b) a core comprising an active ingredients (A) understood as it is either coated with inner coat or and optionally other pharmaceutically without inner coat. acceptable excipients (X); and
  • encapsulate at c) encapsulate at least one preselected external least one preselected external surface of core within surface of core within insoluble container (C) one or more container (S) in such a way that it entrap in such a way that it entrap air or create void air or create void between at least one inner surface between at least one inner surface of of container (S) and at least one outer surface of core.
  • insoluble container (C) and at least one outer In one embodiment, encapsulate at least one surface of core.
  • drug delivery composition layer of core within container (S) in system comprising one or more insoluble container such a way that it entrap air or create void between at (C), a said insoluble container (C) has one or more least one inner surface of container (S) and at least aperture and a wall having an inside and an outside one outer surface of said composition layers of core. surface.
  • insoluble container (C) created between at least one inner surface of is insoluble in at least one region of gastrointestinal container (S) and at least one outer surface of core is tract.
  • insoluble container (C) is permeable or stomach for sufficient period of time. In some impermeable to gastrointestinal fluid. So when the embodiment, container is being sandwich between term “insoluble container” is utilized, it is to be outer surface of core and water insoluble coating.
  • container is insoluble and some embodiment, container is being sandwich impermeable, insoluble but permeable, insoluble in between inner insoluble coat and water insoluble one region of gastrointestinal tract but soluble in coating, resulting into outer and inner surface of another region of gastrointestinal tract or insoluble container may not be available for direct contact with for specific period of time.
  • insoluble container which help in maintaining floating of dosage form for (C) is capsule shell.
  • insoluble insoluble
  • drug delivery container (C) is made insoluble by chemical system comprises a water insoluble coating in full or treatment, by high temperature, by high humidity, by in part on outer surface of step (c) composition.
  • water insoluble coating comprises it from material which is either slowly soluble or water insoluble excipients or mixture of water soluble in aqueous environment after certain period insoluble excipients and water soluble excipients in of lag time or pH dependent soluble material, or by appropriate ratio.
  • coating is any other novel techniques for which the amount of impermeable or permeable to active ingredients. In information is limited.
  • coating is impermeable or [0072]
  • a drug delivery semipermeable to aqueous fluid comprises a core, a said core comprising one coating is insoluble throughout drug release profile. or more composition layer, wherein at least one
  • coating is insoluble for composition layer is active ingredient composition specific period of time or soluble after specific period layer (L) comprises an active ingredients (A) and of time.
  • coating is insoluble optionally other pharmaceutically acceptable in one region of gastrointestinal tract but it may be excipients (X).
  • coating further comprises one least one preselected external surface of core within or more aperture.
  • drug one or more insoluble container (C) in such a way delivery system further comprises drug coating that it entrap air or create void between at least one inner surface of insoluble container (C) and at least specific embodiment, a functional composition layer one outer surface of core.
  • (F) is being sandwich between two composition encapsulate at least one preselected external surface layers.
  • a said functional of at least one composition layer of core within composition layer (F) comprises at least one insoluble container (C) in such a way that it entrap air pharmaceutically acceptable excipients (X) selected or create void between at least one inner surface of from group consisting of release rate controlling insoluble container (C) and at least one outer surface agent or gelling agent, swellable excipients, pH of said composition layers of core.
  • X pharmaceutically acceptable excipients
  • water embodiment, entrapped air or void created between at insoluble excipients, gas generating agent, agent least one inner surface of insoluble container (C) and thereby mechanism of gastric retention of core is at least one outer surface of core is at least sufficient attained or mixture thereof.
  • to float the whole dosage form or at least one functional composition layer may optionally composition layer in gastric fluid of stomach for comprise a drug.
  • particular function drug delivery system further comprises drug coating is assign to each functional composition layer (F) and/or film coating surrounding outer surface of such as, but not to be limited:
  • drug delivery system release layer in core composition comprising a core, a said core comprises one or more b) Functional composition layer act as time composition layers as describes below. release or delay release composition layer for [0075]
  • layer in core composition i.e. functional as it is active ingredient composition layer (L) or composition layer allow the release of drug or functional composition layer (F) or both.
  • the term “container” is layer after specific period of time or in utilized, it is to be understood as it is either container specific location of gastrointestinal tract (S) or insoluble container (C).
  • Functional composition layer as barrier
  • drug delivery composition layer to separate composition system comprises a core, a said core comprising one layer
  • composition layer wherein at least one d) Functional composition layer as composition layer is active ingredient composition additional/supportive gastroretentive layer in layer (L).
  • composition layer as divisible active ingredient composition layers (L), wherein at composition layer in core composition to least one active ingredient composition layer (L) divide dosage form into two or more release the drug or drugs contained therein in gastric segments without compromise with fluid of stomach.
  • active functionality of coating intended for ingredient composition layer (L) comprising one or particular function.
  • core comprises two or more pharmaceutically acceptable excipients (X) more functional composition layer (F), wherein selected from group consisting of release rate particular function assign to each functional controlling agent, swellable excipients, pH modifying composition layer (F) is similar or different.
  • agent water soluble excipients, water insoluble specific embodiment, component of functional excipients, gas generating agent, agent thereby composition layer is selected based on function mechanism of gastric retention of core is attained or assign to each functional composition layer (F) in mixture thereof. dosage form.
  • functional system comprises a core, a said core comprising two composition layer act as immediate release layer, or more composition layer, wherein at least one wherein said functional composition layer comprises composition layer is active ingredient composition drug or drugs and one or more swellable excipients layer (L) and at least another composition layer is and/or pH modifying agent.
  • a functional composition layer (F) is composition layer act as time release or delay release located at one end of core such as forming top or composition layer for one or more drug composition bottom part of core or at two opposite end of core layer in core composition, wherein said functional such as forming top and bottom part of core.
  • composition layer comprises at least one excipients selected from group consisting of pH modifying encapsulation are either gastroretentive or non- agent, water soluble excipients, water insoluble gastroretentive in gastric fluid of stomach.
  • composition Container ком ⁇ онентs of Gastroretentive Pharmaceutical functional composition layers (F) allow the release of Dosage Form - drug or drugs form active ingredients composition Container:
  • the container is capsule shell.
  • composition layer act as barrier composition layer to "capsule shell”
  • capsule shell when used, it is to be understood as it is separate two composition layer, wherein said part of capsule or whole capsule.
  • Part of capsule functional composition layer comprises at least one means either body part or cap part of capsule.
  • Whole excipients selected from group consisting of capsule shell means capsule having both cap and swellable excipients, pH modifying agent, water body part.
  • the capsule shell is mixture thereof. typically a hollow shell of generally cylindrical shape
  • composition layer having a diameter and length sufficient so that the composition layer act as additional/supportive composition layers of core fits appropriately in the gastroretentive layer in core composition, wherein empty capsule.
  • the clearance between the capsule said functional composition layer comprises at least shell and the composition layers of core is preferably one agent thereby mechanism of gastric retention is from about +1.0 mm to about 0 mm. According to a attained. specifically preferred embodiment of the present
  • the clearance between the capsule shell composition layer act as divisible composition layer and the composition layers of core is in the range of in core composition, wherein said functional from about +0.5 mm to about -0.5 mm.
  • composition layer is placebo composition layer, i.e.
  • the capsule shell comprising a material, drug free composition layer.
  • said material is selected from group divisible composition layer comprises at least one consisting of, but are not to be limited, gelatin, starch, excipients selected from group consisting of casein, chitosan, soya bean protein, gum Arabic, swellable excipients, pH modifying agent, water safflower protein, alginates, gellan gum, carrageenan, soluble excipients, water insoluble excipients or xanthan gum, phtalated gelatin, succinated gelatin, mixture thereof.
  • a drug cellulosephtalate-acetate, polyvinylacetate, cellulose delivery system is divisible at functional composition derivatives include, but not to be limited, layers (F) into two or more segments without hydroxypropyl methylcellulose, hypromellose compromise with functionality of coating film phthalate, carboxy-methyl cellulose, intended for particular purpose.
  • polyvinylacetate-phthalate polymerisates of acrylic embodiment, divided segment yields a predetermined or methacrylic esters, sodium alginate, carrageenan, quantity of drug or drugs.
  • a polyvinylpyrrolidone, natural or synthetic materials drug delivery system can be administered in part after or mixtures thereof.
  • releases of drug or drugs from divided consisting of gelatin and its derivative, cellulose and segments are similar or not similar to release profile its derivatives and starch and its derivatives.
  • container (S) is
  • an oral soluble in gastrointestinal fluid is provided.
  • gastroretentive pharmaceutical dosage form can be [0092]
  • drug release occurs through porous gastrointestinal tract.
  • capsule polymeric membrane while in matrix system, drug shell materials may be made insoluble by chemical release by dissolution, diffusion or erosion process. treatment, by high temperature, by high humidity, by
  • a dosage form release the drug ultraviolet (UV) and visible irradiation, by dyes, by or drugs in sustained manner from predefined making it from material which is either slowly surface.
  • UV ultraviolet
  • dyes by or drugs in sustained manner from predefined making it from material which is either slowly surface.
  • composition layers of certain period of lag time or pH dependent soluble core encapsulate within container are gastroretentive material, or by any other novel techniques for which in the gastric fluid of the stomach. In another the amount of information is limited.
  • Radiation embodiment, composition layer of core without crosslinking includes crosslinking by electron beams, ultraviolet, ⁇ -irradiation, x-rays, and other means.
  • Chemical crosslinking is carried out by exposing the disorders, CNS stimulants, contraceptives, cystic polymers to the crosslinking composition or molecule fibrosis management, antipsychotics, dopamine that contains a plurality of functional groups that are receptor agonists, endometriosis management, reactive with functional groups on the polymer such anxiolytics, antidiarrheals, erectile dysfunction as e.g. cross linking with cross linking agent, e.g therapy, fertility agents, corticosteroid, glutr aldehyde. gastrointestinal agents, Decongestant, cough Active Substance: suppressant, immunomodulators and
  • the core comprises one or more active preparations, muscle relaxants, anaesthetics, ingredient composition layers (L), wherein active nucleoside analogues, opioids, osteoporosis ingredient (A) in any of one composition layers may management, adrenergics, parasympathomimetics, be the same or different from the active ingredient expectorants, antinauseants, prostaglandins, active (A) in any of the other composition layers.
  • drugs used for "pharmacologically active agent”, “therapeutically skin ailments, steroids and hormones and drugs used active substance”, “physiologically active agent” or to treat narcolepsy and attention deficit hyperactivity "drug substance in physiologically active form” are disorder.
  • drugs that may be used interchangeably herein to refer to a chemical used in the pharmaceutical composition of the present compound that induces a desired pharmacological or invention may be selected from active substance physiological effect.
  • opioids include opioids, pharmaceutically acceptable derivatives of those CNS depressants, CNS stimulants, cannabinoids, active agents specifically mentioned herein, nicotine-like compounds, glutamate antagonists and including, but not to be limited, salts, solvates, N-methyl-D-aspartate (NMDA) antagonists.
  • NMDA N-methyl-D-aspartate
  • the active substance can be in various molecules, prodrug, active metabolites, analogs, and forms, such as uncharged or charged molecules, the like.
  • the letter “A” is used herein to denote molecular complexes, crystalline forms, amorphous "Active substance”.
  • drug active form, polyamorphous form, polymorphous form, substance
  • active ingredient active agent
  • drug complexes solvates, anhydrates, if relevant isomers, substance", “pharmacologically active agent”, enantiomers, racemic mixtures and “therapeutically active substance", “physiologically pharmacologically acceptable salts.
  • Derivatives of active agent or “drug substance in physiologically active substances such as esters, ethers and amides active form” are used, or when a particular drug, for which have solubility characteristics suitable for use example Sertraline, is identified, it is to be herein can be used alone or mixed with other drugs.
  • active agent or “drug substance in physiologically active substances such as esters, ethers and amides active form”
  • it is to be herein can be used alone or mixed with other drugs.
  • the active agent as well as
  • a pharmaceutically acceptable salts, solvates, system it may be converted by enzymes, hydrolysed polymorphs, hydrates, complexes with one or more
  • drugs that may be composition of the invention may in addition be used in the pharmaceutical composition of the present suitable for the delivery of peptides, polypeptides, invention may be selected from the group consisting, hormones, proteins, antibodies and microorganisms, but are not limited to be, of Alzheimer's disease, either living, attenuated or dead.
  • the drug substance (A) may also include appetite suppressants, anti-inflammatory, nonnew chemical entity for which the amount of steroids anti-inflammatory, anticancer agents, information is limited.
  • the dosage form anticoagulants and antithrombotic agents, regimen needs to evaluate based on preclinical and anticonvulsants, antidiabetics antiemetics, clinical trials.
  • a suitable water soluble or water insoluble antiparkinsons, antiplatelet agents, antirheumatic release rate controlling excipient is selected from agents, antispasmodics and anticholinergic agents, group consisting of cellulose derivatives include, but antitussives, carbonic anhydrase inhibitors, are not limited to be, methyl cellulose, ethyl cardiovascular agents, antiobesity, lipid modifying cellulose, hydroxypropyl methylcellulose, agents, cholinesterase inhibitors, treatment of CNS hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxyethyl methylcellulose, cellulose acetate may be used may be a moderately swellable excipient phthalate, microcrystalline cellulose, and may be used in an amount ranging from about ethylhydroxyethylcellulose, ethylmethylcellulose, 4% to about 80% by weight of composition or layer,
  • composition layers may also comprise carboxymethylcellulose, ethyl cellulose; glycerol gas generating agent in an amount ranging from palmitostearate, beeswax, glycowax, castor wax, about 0.5% to about 60% by weight of composition carnauba wax, glycerol monostearate, hydrogenated or layer.
  • Gas generating agents may helps in release vegetable oils, vegetable oils, stearyl alcohol, of insoluble or poorly soluble drug or drugs, acetylated hydrogenated soybean oil glycerides, disintegration of composition layer and may act as a castor oil, glycerol behenic acid ester, glyceryl agent thereby mechanism of gastric retention is monooleate, glyceryl monostearate, propylene glycol achieved.
  • Gas generating agents that may be used in monostearate, cetyl alcohol, natural and synthetic the present invention include carbonates such as glycerides, waxes, fatty acids, fatty alcohol, lipid, calcium carbonate, bicarbonates such as sodium or steryl alcohol, sorbitan monolaurate, sorbitan potassium bicarbonate, sulfites such as sodium monooleate, sorbitan monopalmitate, sorbitan sulfite, sodium bisulfite, or sodium metabisulfite, and monostearate, sorbitan sesquioleate, sorbitan the like.
  • carbonates such as glycerides, waxes, fatty acids, fatty alcohol, lipid, calcium carbonate
  • bicarbonates such as sodium or steryl alcohol
  • sorbitan monolaurate such as sodium or steryl alcohol
  • sorbitan potassium bicarbonate such as sodium or steryl alcohol
  • sorbitan monolaurate such as sodium or steryl alcohol
  • salts may be used alone or in trioleate, sorbitan tristearate, polyacrylamide combination with an acid source as a gas generating derivatives, methacrylic acid derivatives; vinyl couple.
  • the acid source may be an edible organic pyrrolidone polymers such as polyvinylpyrrolidone acid, a salt of an edible organic acid, acidic and copolymers of vinyl pyrrolidone and vinyl components such as acrylate polymers, or mixtures acetate; Polyalkylene oxide and copolymer thereof, thereof.
  • organic acids that may be used alkylene oxide homopolymers; gums of plant, include citric acid, malic acid, succinic acid, tartaric animal, mineral or synthetic origin, polylactic acid or acid, fumaric acid, maleic acid, ascorbic acid, polyglycolic acid and copolymers thereof, glutamic acid, and their salts, and mixtures thereof.
  • a co-polymer of methacrylate-galactomannan [0102]
  • pH etc., Polyvinyl alcohols, glycerinated gelatin, cocoa modifying agents are acidic agent or alkalizing agent.
  • phosphate pH modifying alkalizing agent include, but are not to esters, amides, phthalate esters, glyceryl cocoate be limited, magnesium oxide, meglumine, sodium oleyl alcohol, myristyl alcohol, sucrose octaacetate, oxide, sodium hydroxide, sodium bicarbonate, diacetylated monoglycerides, diethylene glycol potassium citrate, sodium citrate, sodium carbonate, monostearate, ethylene, polyoxyethylene 50 stearate, potassium bicarbonate, potassium carbonate, calcium macrogol ethers, cetomacrogol 1000, lauromacrogols, carbonate, magnesium hydroxide, magnesium poloxamers; and mixtures thereof.
  • an active ingredient composition layer aluminum hydroxide, ammonium Carbonate, (L) may comprise one or more release rate monoethanolamine, diethanolamine, triethanolamine, controlling excipients mentioned above in an amount Potassium Hydroxide, Sodium Phosphate Dibasic ranging from about 2% to about 90%, by weight of and Trolamine.
  • pH modifying acidic agent include, the composition or layer. but are not to be limited, ascorbic acid, benzoic acid, Swellable Excipients: boric acid, citric acid, EDTA and derivative thereof
  • the swelling agent is generally used in an like disodium edetate, trisodium edetate, tetrasodium amount ranging from about 0.5% to about 95% by edetate, disodium calcium edetate and like, edetic weight of composition or layer.
  • the swellable acid, erythrobic acid, fumaric acid, lactic acid, lauric excipient that may be used may be a highly swellable acid, linoleic acid, malic acid, myristic acid, oleic excipient selected from vinylpyrrolidone polymers acid, palmitic acid, sorbic acid, succinic acid and such as crospovidone; cellulose and cellulose tartaric acid.
  • pH modifying agent can be added as derivatives such as carboxyalkyl celluloses, acidic agent alone or alkalizing agent alone or crosslinked carboxyalkylcelluloses and their alkali mixture thereof in dosage form composition.
  • water swellable excipient is preferably used in an amount soluble excipients include natural, synthetic or semi ranging from about 1% to about 40% by weight of synthetic water soluble material.
  • the swellable excipient that material are selected from group consisting of polymer, sugar, salts, salts of organic acid, acid and Wax include microcrystalline wax, beeswax, polysaccharide.
  • Water soluble polymer include, but glycowax, castor wax, carnauba wax; glycerol are not to be limited, cellulose derivatives include, monostearate, hydrogenated vegetable oils, vegetable but are not limited to be, methyl cellulose, oils, stearyl alcohol, acetylated hydrogenated soybean hydroxypropyl methylcellulose, hydroxyethyl oil glycerides, castor oil, glycerol behenic acid ester, cellulose, hydroxypropyl cellulose, hydroxyethyl glyceryl monooleate, glyceryl monostearate, methylcellulose, ethylhydroxyethylcellulose, propylene glycol monostearate, cetyl alcohol, natural ethylmethylcellulose, hydroxymethylcellulose, and synthetic glycerides, fatty acids, fatty alcohol, hydroxymethylpropylcellulose, sodium lipid, steryl alcohol, sorbitan monolaurate, sorbitan carboxymethylcellulose, polyacrylamide
  • Preferred sugars starch polylactic acid or polyglycolic acid and include dextrose, glucose, arabinose, ribose, copolymers thereof, methacrylates, Polyacrylic acid arabinose, xylose, lyxose, xylol, allose, altrose, and copolymer thereof, a co-polymer of inositol, glucose, sorbitol, mannose, gulose, Glycerol, methacrylate-galactomannan etc., cocoa butter, idose, galactose, talose, trehalose, mannitol, macrogol Stearate, diethylene glycol monostearate, erythritol, ribitol, xylitol, maltitol, isomalt, lactitol, polyoxyethylene 50 stearate, dibasic calcium sucrose, raffinose, maltose, fructose, lactose
  • Water soluble salts Agent thereby mechanism of gastric retention is include sodium chloride, potassium chloride, calcium attained:
  • Agent thereby mechanism of gastric lithium, sodium or potassium hydrogen phosphate, retention comprises at least one material lithium, sodium or potassium dihydrogen phosphate, selected from group consisting of gas generating salts of organic acids such as sodium or potassium agent, low density material, high density material, acetate, magnesium succinate, sodium benzoate, partially or completely hollow or porous material or sodium citrate or sodium ascorbate. Preferred acids mixture thereof.
  • List of gas generating agent is include ascorbic acid, 2-benzene carboxylic acid, already discuss above.
  • Partially or completely hollow benzoic acid, fumaric acid, citric acid, maleic acid, or porous materials include cellulosic polymers, serbacic acid, sorbic acid, edipic acid, edetic acid, cellulose ether polymers, methacrylate polymers, glutamic acid, toluene sulfonic acid, water-soluble waxes or combinations thereof.
  • Suitable low density amino acids such as glycine, leucine, alanine, or materials include, but are not to be limited, polyvinyl methionine and tartaric acid; and like.
  • Alcohol-polyethylene glycol graft copolymers acrylic Polysaccharides are polymeric carbohydrate acid polymers, Wax, methacrylic acid copolymers, molecules composed of long chains of polyvinyl alcohol, polyvinyl acetate, polysaccharides, monosaccharide units bound together by glycosidic cellulose based polymers or combinations thereof. linkages and on hydrolysis give the constituent High density materials include, but are not to be monosaccharides or oligosaccharides. They range in limited, barium sulphate, zinc oxide, iron powder, structure from linear to highly branched. Examples titanium dioxide etc.
  • insoluble excipients include natural, synthetic or semi c) Encapsulate at least one preselected outer synthetic water insoluble material.
  • Natural, synthetic surface of step (b) inner coated tablet within or semi synthetic water insoluble material include, container in such a way that it entrap air or but are not to be limited, cellulose derivatives include create a void between at least one inner surface cellulose acetate phthalate, microcrystalline cellulose, of container and at least one outer surface of cellulose acetate, HPMC phthalate, microcrystalline inner coated tablet
  • Core Tablet Sertraline HC1, lactose, examples, which are meant by way of illustration and microcrystalline cellulose and magnesium not limitation. stearate were mixed in polybag and tablets were

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Abstract

L'invention concerne une nouvelle forme posologique pharmaceutique orale de rétention gastrique et des procédés de préparation d'une nouvelle forme posologique pharmaceutique orale de rétention gastrique. La présente invention concerne également une nouvelle forme posologique de rétention gastrique qui administre une ou plusieurs substances actives à la même vitesse de libération ou à une vitesse différente par des mécanismes de libération identiques ou différents pendant des périodes de temps identiques ou différentes dans des régions du tractus gastro-intestinal identiques ou différentes à partir d'un seul système d'administration de médicament, c'est-à-dire une forme posologique qui est relativement souple quant au mode d'obtention d'un modèle de libération désiré de substances actives identiques ou différentes.
PCT/IN2015/050070 2014-07-21 2015-07-21 Nouvelle forme posologique pharmaceutique orale de rétention gastrique WO2016020936A2 (fr)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106309404A (zh) * 2016-10-27 2017-01-11 四川省百草生物药业有限公司 一种高稳定性的盐酸舍曲林胶囊及其制备方法

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KR100371730B1 (ko) * 1997-07-01 2003-02-07 화이자 프로덕츠 인코포레이티드 세르트랄린의 젤라틴 캡슐화된 용액 투여형
IL152330A0 (en) * 1997-07-01 2003-05-29 Pfizer Sertraline salts and sustained-release dosage forms of sertraline
EP1239839A2 (fr) * 1999-12-23 2002-09-18 Pfizer Products Inc. Forme de dosage d'un medicament stratifie entraine par un hydrogel
WO2006072878A1 (fr) * 2005-01-07 2006-07-13 Ranbaxy Laboratories Limited Formes posologiques orales de sertraline possedant une taille de particule controlee, et leurs procedes de preparation
US20060257475A1 (en) * 2006-08-17 2006-11-16 Boehringer Ingelheim International Gmbh Stable Sertraline Hydrochloride Formulation and Method

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106309404A (zh) * 2016-10-27 2017-01-11 四川省百草生物药业有限公司 一种高稳定性的盐酸舍曲林胶囊及其制备方法
CN106309404B (zh) * 2016-10-27 2019-10-25 四川省百草生物药业有限公司 一种高稳定性的盐酸舍曲林胶囊及其制备方法

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