WO2021126099A1 - Pastille à enrobage entérique comprenant du chlorhydrate de duloxétine avec des degrés de neutralisation optimisés - Google Patents

Pastille à enrobage entérique comprenant du chlorhydrate de duloxétine avec des degrés de neutralisation optimisés Download PDF

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Publication number
WO2021126099A1
WO2021126099A1 PCT/TR2019/051106 TR2019051106W WO2021126099A1 WO 2021126099 A1 WO2021126099 A1 WO 2021126099A1 TR 2019051106 W TR2019051106 W TR 2019051106W WO 2021126099 A1 WO2021126099 A1 WO 2021126099A1
Authority
WO
WIPO (PCT)
Prior art keywords
layer
enteric
enteric coated
duloxetine
coated pellet
Prior art date
Application number
PCT/TR2019/051106
Other languages
English (en)
Inventor
Ersin Yildirim
Bayram Kanik
Fatma ÖZTÜRK
Original Assignee
Santa Farma İlaç Sanayi̇ A.Ş.
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 Santa Farma İlaç Sanayi̇ A.Ş. filed Critical Santa Farma İlaç Sanayi̇ A.Ş.
Priority to PCT/TR2019/051106 priority Critical patent/WO2021126099A1/fr
Publication of WO2021126099A1 publication Critical patent/WO2021126099A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K9/5073—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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/24—Antidepressants

Definitions

  • duloxetine As being a member of selective serotonin reuptake inhibitors (SNRI) which inhibits specifically the reuptake of both serotonin and norepinephrine, duloxetine is used to treat depression particularly major depressive disorder.
  • SNRI selective serotonin reuptake inhibitors
  • the present invention provides an enteric coated pellet comprises a pellet core, a drug layer with duloxetine hydrochloride, a separating layer, an enteric layer comprising hydroxypropyl methylcellulose acetate succinate, and optionally a finishing layer, wherein the hydroxypropyl methylcellulose acetate succinate is partially neutralized with at least one alkaline material to the degree from 25% to 75% of the succinic acid groups with a pH range from 5.0 to 5.5.
  • the present invention also provides an enteric coated pellet according to the invention or a pharmaceutical composition compises the pellet described in the invention, for use in the treatment of major depressive disorder, peripheral diabetic neuropathy, generalized anxiety disorders and moderate to severe stress urinary incontinence in women.
  • HPMCAS solubility of HPMCAS is a pH-dependent polymer in aqueous liquids due to its succinate groups. In the acidic environments, HPMCAS is protonated and insoluble. But, in the higher pH environments, it undergoes deprotonation and becomes soluble. The onset of aqueous solubility of HPMCAS is in a pH range of 5.5 - 6.8.
  • hydroxypropyl methylcellulose acetate succinate is partially neutralized with at least one alkaline material to the degree from 25% to 75%, preferably 50% of the succinic acid groups.

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une pastille à enrobage entérique comprenant un noyau de pastille, une couche de médicament contenant du chlorhydrate de duloxétine, une couche de séparation, une couche entérique comprenant de l'acétate succinate d'hydroxypropylméthylcellulose, et éventuellement une couche de finition, le succinate d'acétate d'hydroxypropylméthylcellulose étant partiellement neutralisé avec au moins un matériau alcalin à raison de 25 % à 75 % des groupes acide succinique avec une plage de pH de 5,0 à 5,5.
PCT/TR2019/051106 2019-12-18 2019-12-18 Pastille à enrobage entérique comprenant du chlorhydrate de duloxétine avec des degrés de neutralisation optimisés WO2021126099A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/TR2019/051106 WO2021126099A1 (fr) 2019-12-18 2019-12-18 Pastille à enrobage entérique comprenant du chlorhydrate de duloxétine avec des degrés de neutralisation optimisés

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/TR2019/051106 WO2021126099A1 (fr) 2019-12-18 2019-12-18 Pastille à enrobage entérique comprenant du chlorhydrate de duloxétine avec des degrés de neutralisation optimisés

Publications (1)

Publication Number Publication Date
WO2021126099A1 true WO2021126099A1 (fr) 2021-06-24

Family

ID=76478505

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/TR2019/051106 WO2021126099A1 (fr) 2019-12-18 2019-12-18 Pastille à enrobage entérique comprenant du chlorhydrate de duloxétine avec des degrés de neutralisation optimisés

Country Status (1)

Country Link
WO (1) WO2021126099A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024117996A1 (fr) * 2022-11-30 2024-06-06 Santa Farma Ilac Sanayii A.S. Composition pharmaceutique orale bioéquivalente comprenant du chlorhydrate de duloxétine

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0693282A2 (fr) * 1994-07-18 1996-01-24 Eli Lilly And Company Pilules entériques contenant de la duloxétine
EP1867326A2 (fr) * 2006-06-16 2007-12-19 Shin-Etsu Chemical Co., Ltd. Granule entérique enrobé et son procédé de préparation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0693282A2 (fr) * 1994-07-18 1996-01-24 Eli Lilly And Company Pilules entériques contenant de la duloxétine
EP1867326A2 (fr) * 2006-06-16 2007-12-19 Shin-Etsu Chemical Co., Ltd. Granule entérique enrobé et son procédé de préparation

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KIM, I. H. ET AL.: "Swelling and drug release behavior of tablets coated with aqueous hydroxypropyl methylcellulose phthalate (HPMCP) nanoparticles", JOURNAL OF CONTROLLED RELEASE, vol. 89, no. 2, pages 225 - 233, XP004421358, DOI: 10.1016/S0168-3659(03)00089-0 *
KUANG CHEN, SUN YINGHUA, LI BING, FAN RUI, ZHANG JING, YAO YUMIN, HE ZHONGGUI: "Preparation and evaluation of duloxetine hydrochloride enteric-coated pellets with different enteric polymers", ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES, ELSEVIER BV, NL, vol. 12, no. 3, 1 May 2017 (2017-05-01), NL, pages 216 - 226, XP055836952, ISSN: 1818-0876, DOI: 10.1016/j.ajps.2016.08.007 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024117996A1 (fr) * 2022-11-30 2024-06-06 Santa Farma Ilac Sanayii A.S. Composition pharmaceutique orale bioéquivalente comprenant du chlorhydrate de duloxétine

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