EP1242088A1 - Formes posologiques d'apomorphine administree oralement par voie muqueuse - Google Patents

Formes posologiques d'apomorphine administree oralement par voie muqueuse

Info

Publication number
EP1242088A1
EP1242088A1 EP00988174A EP00988174A EP1242088A1 EP 1242088 A1 EP1242088 A1 EP 1242088A1 EP 00988174 A EP00988174 A EP 00988174A EP 00988174 A EP00988174 A EP 00988174A EP 1242088 A1 EP1242088 A1 EP 1242088A1
Authority
EP
European Patent Office
Prior art keywords
weight
dextran
apomorphine
percent
tablet
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.)
Withdrawn
Application number
EP00988174A
Other languages
German (de)
English (en)
Inventor
Paul E. Stach
Craig W. Davis
Raymundo A. Sison
Robert K. Mansfield
John D. Bollinger
Pramod K. Gupta
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.)
TAP Holding Inc
Original Assignee
TAP Holding Inc
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 TAP Holding Inc filed Critical TAP Holding Inc
Publication of EP1242088A1 publication Critical patent/EP1242088A1/fr
Withdrawn legal-status Critical Current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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • 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
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the present invention relates to pharmaceutical formulations suitable for the administration of a therapeutic agent via oral mucosal tissue. More particularly, the present invention concerns tablet dosage forms containing dextran which are particularly suited for prolonged release delivery of apomorphine through oral mucosal tissue.
  • United States Patents 5,624,677 and 5,888,534 describe a controlled- release tablet formulation for the sublingual or buccal administration of apomorphine (cf. Prior Art Example below) .
  • the formulation comprises a mixture of a water-insoluble carrier forming a porous structure which is filled, coated, or covered by the active ingredient, an osmotic agent, and a water dispersible polymer, with the mixture being compressed into tablets.
  • biological fluids such as saliva
  • the release of apomorphine is controlled by the competing actions of the water-insoluble carrier and the water-dispersible polymer. Both components undergo changes, with swelling of the water-insoluble carrier providing additional surface area with attendant channeling and fluid penetration.
  • Examples 1 -3 illustrate tablet formulations of apomorphine in which reduced amounts of microcrystalline cellulose are combined with dextrans of varying molecular weights.
  • Examples 4 and 5 illustrate formulations in which dextrans of different molecular weights are employed as the sole polymeric component for prolonging the release of the active drug component.
  • prior art and control formulations are also presente
  • Hydroxypropyl methylcellulose 1 0.00 1 0.00
  • Control Example B illustrates a formulation which was devoid of any polymer ingredient which would function to prolong the release of apomorphine. As a consequence, the drug was essentially completely released within the first ten minutes. In the case of apomorphine such a formulation would administer a "bolus" dose of the drug causing, in some patients, serum levels of the dug to rise above the threshold required to induce nausea. This is, of course, undesirable and a slower release is needed. Such prolonged release formulations are presented in Examples 1 -5. The data for Examples 1 -3 show, for example, complete or almost complete release of apomorphine over a period of 45 minutes.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Zoology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

L'invention concerne une formulation pharmaceutique destinée à l'administration orale par voie muqueuse à libération prolongée d'apomorphine. Cette formulation contient une dose efficace d'apomorphine ou un sel ou un promédicament pharmaceutiquement acceptable dudit composé en combinaison avec un support comprenant entre environ 10 % en poids et environ 95 % en poids de dextrane, sur la base du poids total de cette formulation. Dans un mode de réalisation de l'invention, le dextrane présentant un poids moléculaire variant entre 5000 Daltons et 100 000 Daltons est le seul composant de cette formulation qui permet de prolonger la libération du composant médicamenteux actif. Dans un autre mode de réalisation, un mélange de cellulose microcristalline et de dextrane tient lieu de composant prolongeant la libération d'apomorphine.
EP00988174A 1999-12-30 2000-12-19 Formes posologiques d'apomorphine administree oralement par voie muqueuse Withdrawn EP1242088A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US47584499A 1999-12-30 1999-12-30
US475844 1999-12-30
PCT/US2000/034548 WO2001049292A1 (fr) 1999-12-30 2000-12-19 Formes posologiques d'apomorphine administree oralement par voie muqueuse

Publications (1)

Publication Number Publication Date
EP1242088A1 true EP1242088A1 (fr) 2002-09-25

Family

ID=23889387

Family Applications (1)

Application Number Title Priority Date Filing Date
EP00988174A Withdrawn EP1242088A1 (fr) 1999-12-30 2000-12-19 Formes posologiques d'apomorphine administree oralement par voie muqueuse

Country Status (14)

Country Link
EP (1) EP1242088A1 (fr)
JP (1) JP2004501065A (fr)
CN (1) CN1414853A (fr)
AU (1) AU2440901A (fr)
BR (1) BR0012822A (fr)
CA (1) CA2394297A1 (fr)
CZ (1) CZ20022245A3 (fr)
HK (1) HK1051315A1 (fr)
HU (1) HUP0400495A3 (fr)
IL (1) IL150034A0 (fr)
MX (1) MXPA02006034A (fr)
NO (1) NO20023190L (fr)
PL (1) PL366204A1 (fr)
WO (1) WO2001049292A1 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0202365D0 (sv) 2002-08-05 2002-08-05 Pharmacia Ab New formulation and use thereof
EP1617823B1 (fr) * 2003-01-24 2019-01-09 Nicachet AB Sachet contenant une composition de nicotine pour administration par voie transmuqueuse
SE0302947D0 (sv) 2003-01-24 2003-11-07 Magle Ab A composition material for transmucosal delivery
EP1738754B1 (fr) * 2004-04-14 2015-07-15 Takeda Pharmaceutical Company Limited Preparation pharmaceutique solide
GB0509317D0 (en) * 2005-05-06 2005-06-15 Clarke Anthony Pharmaceutical formulation of apomorphine
US9044475B2 (en) * 2009-06-12 2015-06-02 Cynapsus Therapeutics, Inc. Sublingual apomorphine
US20220249465A1 (en) * 2019-05-31 2022-08-11 Primo Pharmatech Llc Unit dosage form for transmucosal drug delivery of an active pharmaceutical ingredient

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0689438T3 (da) * 1993-03-26 2003-09-29 Franciscus Wilhelmus He Merkus Farmaceutiske præparater til intranasal administration af apomorfin
GB9517062D0 (en) * 1995-08-18 1995-10-25 Scherer Ltd R P Pharmaceutical compositions

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0149292A1 *

Also Published As

Publication number Publication date
BR0012822A (pt) 2004-03-09
CN1414853A (zh) 2003-04-30
JP2004501065A (ja) 2004-01-15
HK1051315A1 (zh) 2003-08-01
AU2440901A (en) 2001-07-16
MXPA02006034A (es) 2004-08-23
CZ20022245A3 (cs) 2002-10-16
NO20023190D0 (no) 2002-07-01
NO20023190L (no) 2002-08-29
IL150034A0 (en) 2002-12-01
PL366204A1 (en) 2005-01-24
HUP0400495A2 (hu) 2004-06-28
WO2001049292A1 (fr) 2001-07-12
CA2394297A1 (fr) 2001-07-12
HUP0400495A3 (en) 2007-05-02

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