WO1998002141A1 - Dispositif osmotique a emboitement - Google Patents

Dispositif osmotique a emboitement Download PDF

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Publication number
WO1998002141A1
WO1998002141A1 PCT/US1997/011525 US9711525W WO9802141A1 WO 1998002141 A1 WO1998002141 A1 WO 1998002141A1 US 9711525 W US9711525 W US 9711525W WO 9802141 A1 WO9802141 A1 WO 9802141A1
Authority
WO
WIPO (PCT)
Prior art keywords
housing
active agent
formulation
agent
fluid
Prior art date
Application number
PCT/US1997/011525
Other languages
English (en)
Inventor
Patrick S.-L. Wong
Felix Theeuwes
Liang C. Dong
Vincent J. Ferrari
Original Assignee
Alza Corporation
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 Alza Corporation filed Critical Alza Corporation
Priority to AU35904/97A priority Critical patent/AU3590497A/en
Publication of WO1998002141A1 publication Critical patent/WO1998002141A1/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
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

Definitions

  • the present invention is related to the delayed delivery of an active agent. More particularly, it is related to interlocking osmotically-activated devices for dispensing active agents to a biological environment of use following an initial period of delay.
  • Osmotic dispensing devices for delivery of therapeutically active agents are well known in the art. Such devices use an expansion agent to deliver an active agent formulation to an environment of use over a period of hours, days or months.
  • the expansion agent absorbs liquid, expands, and acts to drive out the active agent formulation from the interior of the device in a controlled, constant or other preprogrammed manner.
  • the osmotic expansion agent is used to controllably, usually relatively slowly, and over a period of time, deliver the agent.
  • Osmotic devices have also been described for protonged and controlled delivery of one or more active agents where an initial delay of delivery is desired. US Patent No.
  • 5,198,229 which is incorporated herein by reference, is directed to an osmotic device for delivery of an active agent to the upper gastrointestinal tract.
  • the dispensing device comprises concentric housings that are in slidabiy telescoping arrangement with each other.
  • a first expansion means imbibes fluid when placed in the stomach environment. This expansion means expands and pushes against a partition layer that in turn pushes against an active agent formulation.
  • the active agent is delivered to the stomach environment through a small exit port in a controlled and continuous manner. After all the active agent has been delivered, the ⁇ housings separate, the buoyancy chamber is exposed to the stomach
  • the invention is directed to a fluid-imbibing o delivery device comprising a first housing and a second semipermeable 1 housing that are in reversibly sliding telescoping interlocking arrangement 2 with each other
  • the first housing contains an active agent formulation and 3 the second housing contains an expansion agent 4
  • the invention is directed to a fluid-imbibing device s for dispensing an active agent formulation following an initial preset delay 6 of startup of delivery
  • the device comprises male and female housings 7 ireversibly sliding telescoping relationship with each other One of the s housings is semipermeable and the other contains an active agent 9 formulation
  • the outer surface of the male housing and the inner surface 0 of the female housing are in interlocking arrangement with each other 1 2 DESCRIPTION OF THE DRAWINGS 3
  • the drawings are not drawn to scale, but are set forth to illustrate 5 various embodiments of the invention
  • Like numbers refer to like structures 6
  • FIG 1 is a cross-sectional view of one embodiment of the delivery 7 device of the present invention, the device
  • FIG. 3 is a side cross-sectional view of another embodiment of the
  • FIG. 4 shows the device of FIG.3 in operation after placement in the
  • the present invention provides a device which is useful for the delivery
  • the active agent is preferably
  • the dose of agent in the device is released in a short period of
  • active agent refers to an agent, drug,
  • mice 17 dogs, sheep, goats, cattle, horses and pigs, laboratory animals such as is mice, rats and guinea pigs, fish, reptiles, zoo and wild animals, and the like
  • the active agent that can be delivered includes inorganic and organic
  • histamine system and the central nervous system Suitable agents may be
  • nucleoproteins 28 nucleoproteins, polysacchandes, glycoproteins, lipoproteins, polypeptides,
  • prochlorperazine edisylate ferrous sulfate, aminocaproic acid, mecaxylamine ⁇ o hydrochlo ⁇ de, procainamide hydrochlonde, amphetamine sulfate, ⁇ methamphetamine hydrochlonde, benzphetamine hydrochlonde,
  • prochlorperazine maleate is anisindione, diphenadione, erythrityl tetranitrate, digoxin, isofiurophate,
  • proteins and peptides which include, but are not limited to, insulin, ⁇ o colchicine, glucagon, thyroid stimulating hormone, parathyroid and pituitary ⁇ hormones, calcitonin, renin, prolactin, corticotrophin, thyrotropic hormone,
  • interferons such as human growth hormone
  • active agent formulation intends active agent optionally in
  • the agents can be in various forms, such as uncharged
  • the environment of use is a fluid environment
  • 5 devices can be administered to a subject during a therapeutic program.
  • FIG. 1 depicts, in cross-sectional view, a first embodiment of the
  • the device is shown in ⁇ closed or prepared form prior to placement in the environment of use.
  • Dispensing device 1 comprises a first housing 12 and a second housing 14. ⁇ o First housing 12 and second housing 14 are in slidabiy telescoping ⁇ interlocking arrangement with each other. First housing 12 contains an active
  • Second housing 14 contains an expansion agent 20 and an
  • First housing 12 and second housing 14 are shown to be ovoloid
  • First housing 12 is shown to be a male housing and second is housing 14 is shown to be a female housing.
  • first housing 12 is adapted to fit within
  • dispensing device 1 is placed in the fluid environment of
  • first housing 12 and second housing 14 separate apart
  • FIG. 2 shows the dispensing device 1 of FIG. 1 in operation.
  • FIG. 3 depicts, in side cross-sectional view, a second embodiment ⁇ o of the delivery device according to the present invention.
  • the device 50 ⁇ is similar to the device described above with regard to FIGS. 1 and 2,
  • the interlocking arrangement comprises
  • the first housing protuberance is 52 interlocks with the second housing protuberance 54 until there is sufficient
  • first expansion agent 20 dosage form, or it may be semipermeable. Because first expansion agent 20
  • 26 may be a microporous membrane or a screen, or may be of a composition
  • Housings 12 and 14 may optionally comprise additional ingredients
  • Impermeable and semipermeable resin 29 such as, for example, plasticizers. Impermeable and semipermeable resin
  • compositions suitable for use in housings 12 and 14, as well as suitable ⁇ additives are known in the art, examples of which are disclosed in US Patent
  • the housings are designed so they will not come apart until there is
  • the delivery device of the present invention is nontoxic, biologically ⁇ inert, nonallergenic and nonir tating to body tissue, and it maintains its
  • the device be insoluble only during the period of intended is use and can thereafter dissolve away in the environment of use.
  • the expansion agent or expandable driving agent 20 is nontoxic,
  • agent 20 comprises
  • Osmopolymers interact with water and aqueous biological
  • Osmagents are also known as
  • the expansion agent 20 in yet another embodiment is an ⁇ osmagent dispersed within an osmopolymer.
  • the expansion agent can be a
  • the osmagent or osmopolymer can be in any suitable form such as particles, crystals, pellets,
  • expansion agent 20 is an effervescent couple.
  • Effervescent ⁇ o couples are comprised of a dry compound or an anhydrous mixture of ⁇ compounds that, when intimately contacted by an external fluid, generate a
  • the couple often comprises a
  • Partition 32 is substantially impermeable to the passage of fluid
  • 21 agent 20 is applied directly against first housing 12 to effect the separation
  • partition 32 must be of sufficient
  • the active agent formulation comprises the active agent to be
  • the active agent formulation may additionally include dosage
  • the pharmaceutically acceptable carrier useful herein may include
  • the carrier may contain more than one active agent.
  • the active agent may contain more than one active agent.
  • formulation can erode or disintegrate and can be in the form of a wax is formulation, a solid core or a tablet, for example.
  • the formulation can
  • the active agent formulation can be designed in a multitude of ways
  • One embodiment may comprise
  • the formulation may contain a fluid-insoluble wax and a
  • the formulation may be effervescent and provide
  • the formulation may include an osmotic
  • the agent formulation can be comprised of an agent and a thermoresponsive
  • the formulation would exhibit solid-like ⁇ properties at room temperature of 21°C and within a few degrees Celsius
  • thermoresponsive as used herein denotes the physical-chemical property
  • additional elements are included in the device, or the device is ⁇ designed in such a way to provide for such particular delivery.
  • the device is ⁇ designed in such a way to provide for such particular delivery.
  • 3 element may be included in the dispensing device so that the device is
  • the device 7 environment of use is the human stomach, it may be desirable for the device s to, for example, have a low initial density or to include air in that portion of the 9 internal compartment of the device that also contains the agent formulation. ⁇ o In this manner, the device will float on the surface of the stomach contents ⁇ and remain in the stomach until the device opens to release the formulation.
  • an enteric coating can be applied over at least
  • compositions with a viscosity Compositions with a viscosity
  • control means may be used.
  • Such control means are known in the art ⁇ and can be determined without undue experimentation.
  • the delivery device of the present invention can be manufactured ⁇ o by standard manufacturing techniques.
  • first housing 12 the vessel
  • second housing 12 the vessel
  • water flux enhanced Hytrel® polyester elastomers is (Du Pont), cellulose esters, water flux enhanced ethylene-vinyl acetate
  • the device can be assembled as follows. Active agent formulation 22
  • the formulation may be in the form of a liquid, solid, semi-solid, 2 ⁇ powder or shaped tablet or tablets, for example.
  • the partition 32 and expansion ⁇ agent 20 are compressed into a tablet on a rotary bilayer tablet press.
  • the first housing with one closed end and one open end and ridges
  • the second housing is made by injection molding a composition
  • An expanding layer is formed from the following dry components:
  • NaCMC sodium carboxymethyl cellulose
  • Magnesium stearate (0.25 wt%) is
  • An impermeable partition is formed by screening 5 wt%
  • the opening time of the device of Example 1 is measured as follows.
  • the device is placed in artificial intestinal fluid (USPXIX, intestinal fluid, simulated, TS; modified by not including enzymes).
  • a plastic rod is glued onto the first housing of the device.
  • the opening time is determined to be the time interval at which the second housing separates from the first housing.
  • the opening time is about 6.5 hours after placement in the intestinal fluid.

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

Abstract

L'invention concerne un dispositif d'apport de médicament imbibant un fluide, qui est utile pour l'apport initial différé d'une formulation d'agent actif à un milieu fluide d'emploi, la période de retard initial précédant le début de l'activation étant d'une durée prédéterminée. Ce dispositif d'apport est formé d'un premier et d'un deuxième boîtier qui s'emboîtent de manière téléscopique et réversible.
PCT/US1997/011525 1996-07-15 1997-07-01 Dispositif osmotique a emboitement WO1998002141A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU35904/97A AU3590497A (en) 1996-07-15 1997-07-01 Interlocking osmotic device

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US2172696P 1996-07-15 1996-07-15
US60/021,726 1996-07-15

Publications (1)

Publication Number Publication Date
WO1998002141A1 true WO1998002141A1 (fr) 1998-01-22

Family

ID=21805802

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1997/011525 WO1998002141A1 (fr) 1996-07-15 1997-07-01 Dispositif osmotique a emboitement

Country Status (2)

Country Link
AU (1) AU3590497A (fr)
WO (1) WO1998002141A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10985437B2 (en) 2016-07-12 2021-04-20 Stmicroelectronics Sa Integrated coupling device, in particular of the 90° hybrid type

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5198229A (en) * 1991-06-05 1993-03-30 Alza Corporation Self-retaining gastrointestinal delivery device
US5223265A (en) * 1992-01-10 1993-06-29 Alza Corporation Osmotic device with delayed activation of drug delivery

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5198229A (en) * 1991-06-05 1993-03-30 Alza Corporation Self-retaining gastrointestinal delivery device
US5223265A (en) * 1992-01-10 1993-06-29 Alza Corporation Osmotic device with delayed activation of drug delivery
US5312390A (en) * 1992-01-10 1994-05-17 Alza Corporation Osmotic device with delayed activation of drug delivery

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10985437B2 (en) 2016-07-12 2021-04-20 Stmicroelectronics Sa Integrated coupling device, in particular of the 90° hybrid type

Also Published As

Publication number Publication date
AU3590497A (en) 1998-02-09

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