KR970704472A - 수성 리스페리돈 제제(aqueous risperidone formulations) - Google Patents

수성 리스페리돈 제제(aqueous risperidone formulations) Download PDF

Info

Publication number
KR970704472A
KR970704472A KR1019970700039A KR19970700039A KR970704472A KR 970704472 A KR970704472 A KR 970704472A KR 1019970700039 A KR1019970700039 A KR 1019970700039A KR 19970700039 A KR19970700039 A KR 19970700039A KR 970704472 A KR970704472 A KR 970704472A
Authority
KR
South Korea
Prior art keywords
solution
amount
water
range
risperidone
Prior art date
Application number
KR1019970700039A
Other languages
English (en)
Other versions
KR100212942B1 (ko
Inventor
마르크 카렐 조제프 프랑소와즈
윌리 마리아 알버트 카를로 드리스
Original Assignee
디르크 반테
얀센 파마슈티카 엔. 브이.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26955530&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR970704472(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 디르크 반테, 얀센 파마슈티카 엔. 브이. filed Critical 디르크 반테
Publication of KR970704472A publication Critical patent/KR970704472A/ko
Application granted granted Critical
Publication of KR100212942B1 publication Critical patent/KR100212942B1/ko

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

본 발명은 물리화학적으로 안정한 경구 및 비경구 투여용 수성 리스페리돈 용액; 그 제제의 제조 방법에 관한 것이다.

Description

수성 리스페리돈 제제(AQUEOUS RISPERIDONE FORMULATIONS)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (13)

  1. pH를 2 내지 6의 범위로 유지시키기 위한 완충제를 함유하며 필수적으로 솔비톨을 함유하지 않음을 특징으로 하는 물, 리스페리돈 또는 약제학적으로 허용되는 그의 산 부가염을 함유하는 경구 및 비경구 투여에 적합한 수성 용액.
  2. 제1항에 있어서, pH범위가 타르타르산/수산화 나트륨 완충제에 의해 얻어지는 용액.
  3. 제1항에 있어서, 피스페리돈의 양이 용액의 총 부피 기준으로 0.01 내지 1중량% 범위인 용액.
  4. 제1항에 있어서 경구 투여에 적합한 3 내지 4의 pH 범위를 가지는 용액.
  5. 제4항에 있어서, 추가로 벤조산을 방부제로서 함유하는 용액.
  6. 제5항에 있어서, (a) 1mg/ml의 리스페리돈; (b) 2mg/ml의 벤조산; (c) 7.5mg/ml의 타르타르산 및 pH를 3 내지 4의 범위로 조정하기에 충분한 양의 수산화 나트륨: 및 (d) 총량을 1ml로 맞추기 위한 잔여량의 물을 함유하는 용액.
  7. 제6항에 있어서, 추가로 하나 또는 그 이상의 감미제 및/또는 향료를 함유하는 용액.
  8. 제1항에 있어서, 비경구 투여에 적합한 5 내지 6의 pH 범위를 가진 용액.
  9. 제4항에 있어서, 추가로 염화 나트륨을 등장화제로서 함유한 용액.
  10. 제9항에 있어서, (a) 1mg/ml의 리스페리돈; (b) 5mg/ml의 염화 나트륨; (c) 7.5mg/ml의 타르타르산 및 pH를 5 내지 6의 범위로 조정하기에 충분한 양의 수산화 나트륨: 및 (d) 1ml로 맞추기 위한 잔여량의 물을 함유하는 용액.
  11. (a)완충제의 산 성분 및 활성 성분인 리스페리돈을 일정량의 물에 가한 후, (b) 혼합물을 완전히 용해될 때까지 교반하고 용액을 실온으로 냉각시키고, (c)완충제의 염기 성분으로 pH를 조정한 후, (d) 생성된 용액을 추가로 목적하는 최종 부피까지 물로 희석하는 단계를 포함하여 제1항에 따르는 용액을 제조하는 방법.
  12. 제11항에 있어서, (a) 일정량의 가열된 물에 방부제를 용해시키고, (b)생성된 용액을 대략 동량의 물로 희석하는 단계를 수행한 후에 단계(a)를 수행하여 제5항의 경구용 용액을 제조하는 방법.
  13. 제11항에 있어서, 적절한 양의 등장화제를 첨가하여 용액을 대략 등장성으로 조절한 후에 단계 (d)를 수행하고, 이어서 고온 멸균시키는 단계를 수행하여 제9항의 비경구 용액을 제조하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019970700039A 1994-07-11 1995-07-04 수성 리스페리돈 제제 KR100212942B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US272462 1994-07-11
US08/272,462 US5453425A (en) 1994-07-11 1994-07-11 Risperidone oral formulation
US08/429,435 US5616587A (en) 1994-07-11 1995-04-26 Aqueous risperidone formulations
PCT/EP1995/002615 WO1996001652A1 (en) 1994-07-11 1995-07-04 Aqueous risperidone formulations

Publications (2)

Publication Number Publication Date
KR970704472A true KR970704472A (ko) 1997-09-06
KR100212942B1 KR100212942B1 (ko) 1999-08-02

Family

ID=26955530

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019970700039A KR100212942B1 (ko) 1994-07-11 1995-07-04 수성 리스페리돈 제제

Country Status (37)

Country Link
US (3) US5453425A (ko)
EP (1) EP0769965B1 (ko)
JP (1) JP2872412B2 (ko)
KR (1) KR100212942B1 (ko)
CN (1) CN1148226C (ko)
AP (1) AP774A (ko)
AT (1) ATE206931T1 (ko)
AU (1) AU684193B2 (ko)
BG (1) BG63070B1 (ko)
BR (1) BR9508253A (ko)
CA (1) CA2194564C (ko)
CY (1) CY2268B1 (ko)
CZ (1) CZ285204B6 (ko)
DE (1) DE69523313T2 (ko)
DK (1) DK0769965T3 (ko)
EE (1) EE03426B1 (ko)
ES (1) ES2165918T3 (ko)
FI (1) FI116510B (ko)
HK (1) HK1010691A1 (ko)
HR (1) HRP950397B1 (ko)
HU (1) HU222352B1 (ko)
IL (1) IL114525A (ko)
MX (1) MX9700374A (ko)
MY (1) MY114389A (ko)
NO (1) NO320366B1 (ko)
NZ (1) NZ289432A (ko)
PH (1) PH31626A (ko)
PL (1) PL179972B1 (ko)
PT (1) PT769965E (ko)
RO (1) RO116778B1 (ko)
RU (1) RU2161965C2 (ko)
SI (1) SI9500220B (ko)
SK (1) SK282159B6 (ko)
TR (1) TR199500778A1 (ko)
TW (1) TW420615B (ko)
WO (1) WO1996001652A1 (ko)
ZA (1) ZA955720B (ko)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ276088A (en) 1993-11-19 1999-07-29 Janssen Pharmaceutica Nv [(1,2-benzisoxazol-3-yl)-1-piperidinyl-alkyl-6,7,8,9-tetrahydro-4h- pyrido[1,2-a]-pyrimidin-4-one derivatives (ie risperidone)
US5453425A (en) * 1994-07-11 1995-09-26 Janssen Pharmaceutica N.V. Risperidone oral formulation
UA72189C2 (uk) * 1997-11-17 2005-02-15 Янссен Фармацевтика Н.В. Фармацевтична композиція, що містить водну суспензію субмікронних ефірів 9-гідроксирисперидон жирних кислот
US6682758B1 (en) 1998-12-22 2004-01-27 The United States Of America As Represented By The Department Of Health And Human Services Water-insoluble drug delivery system
US6495164B1 (en) * 2000-05-25 2002-12-17 Alkermes Controlled Therapeutics, Inc. I Preparation of injectable suspensions having improved injectability
US20050232995A1 (en) 2002-07-29 2005-10-20 Yam Nyomi V Methods and dosage forms for controlled delivery of paliperidone and risperidone
AU2003250472A1 (en) * 2002-08-23 2004-03-11 Ranbaxy Laboratories Limited Stable aqueous solutions of risperidone and methods for their preparation
WO2004094414A1 (en) * 2003-04-22 2004-11-04 Synthon B.V. Water soluble salts of risperidone
AR044852A1 (es) 2003-06-24 2005-10-05 Novartis Ag Una composicion farmaceutica para la administracion parenteral que comprende un analogo de somatostatina
US20050036977A1 (en) * 2003-08-11 2005-02-17 Dilip Gole Taste-masked resinate and preparation thereof
ES2245252B1 (es) * 2004-06-15 2007-03-01 Farmalider, S.A. Solucion acuosa de risperidona para administracion oral.
ES2245891B1 (es) * 2004-07-09 2006-11-16 Clinmet S.L. "metodo para la obtencion de un excipiente universal para la administracion oral de principios activos farmaceuticos y composiciones de excipientes resultantes del metodo".
WO2006129160A2 (en) * 2005-06-01 2006-12-07 Aurobindo Pharma Limited Stable aqueous oral solution of risperidone
DE602006005423D1 (de) * 2005-06-29 2009-04-16 Verisfield Uk Ltd Pharmazeutische Zusammensetzungen von Risperidon in wässriger Lösung
US8852638B2 (en) 2005-09-30 2014-10-07 Durect Corporation Sustained release small molecule drug formulation
JP4922657B2 (ja) * 2006-05-09 2012-04-25 高田製薬株式会社 リスペリドン経口用液剤
WO2007138462A2 (en) * 2006-06-01 2007-12-06 Wockhardt Ltd Aqueous oral formulations of risperidone
CA2687979C (en) 2007-05-25 2017-07-04 Tolmar Therapeutics, Inc. Sustained delivery formulations of risperidone compounds
US7776866B2 (en) * 2007-09-15 2010-08-17 Protia, Llc Deuterium-enriched risperidone
CN101932327A (zh) * 2007-12-19 2010-12-29 詹森药业有限公司 与长效注射用帕潘立酮酯相关的给药方案
CA3037010A1 (en) 2009-01-20 2010-07-29 Los Angeles Biomedical Research Institute At Harbor-Ucla Medical Cente Sorbic and benzoic acid and derivatives thereof enhance the activity of a neuropharmaceutical
US9272044B2 (en) 2010-06-08 2016-03-01 Indivior Uk Limited Injectable flowable composition buprenorphine
GB2513060B (en) 2010-06-08 2015-01-07 Rb Pharmaceuticals Ltd Microparticle buprenorphine suspension
EP2763676B1 (en) * 2011-10-03 2019-12-25 The University of Utah Research Foundation Application of 5-ht6 receptor antagonists for the alleviation of cognitive deficits of down syndrome
GB201404139D0 (en) 2014-03-10 2014-04-23 Rb Pharmaceuticals Ltd Sustained release buprenorphine solution formulations
NZ731309A (en) 2014-11-07 2022-02-25 Indivior Uk Ltd Buprenorphine dosing regimens
CA3027300C (en) 2016-06-13 2023-08-08 Syneurx International (Taiwan) Corp. Co-crystals of lithium benzoate and uses thereof
US11008277B2 (en) 2016-06-13 2021-05-18 Syneurx International (Taiwan) Corp. Co-crystals of sodium benzoate and uses thereof
BR112019005542A2 (pt) * 2016-09-23 2019-06-18 Delpor Inc composições para compostos de agente terapêutico de pequenas moléculas
RU2646812C1 (ru) * 2016-10-24 2018-03-07 Общество с ограниченной ответственностью "Трейдсервис" Жидкая лекарственная форма рисперидона и способ ее получения
US11369579B2 (en) 2016-10-24 2022-06-28 Syneurx International (Taiwan) Corp. Polymorphic forms of sodium benzoate and uses thereof
US10336679B2 (en) 2016-10-24 2019-07-02 Syneurx International (Taiwan) Corp. Polymorphic forms of sodium benzoate and uses thereof
US10646484B2 (en) 2017-06-16 2020-05-12 Indivior Uk Limited Methods to treat opioid use disorder
CN107260662A (zh) * 2017-06-21 2017-10-20 南京正科医药股份有限公司 一种利培酮口服溶液及其制备方法
CN107441037A (zh) * 2017-08-16 2017-12-08 南京正科医药股份有限公司 一种利培酮口服溶液
CN109589304A (zh) * 2017-10-01 2019-04-09 万特制药(海南)有限公司 利培酮口服溶液及其制备方法
US10098861B1 (en) 2017-10-24 2018-10-16 Syneurx International (Taiwan) Corp. Pharmaceutical composition comprising sodium benzoate compound and clozapine, and uses thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4337261A (en) * 1980-07-28 1982-06-29 Hoechst-Roussel Pharmaceuticals Inc. (1,2-Benzisoxazol)phenoxyacetic acids as diuretics
IL88233A (en) * 1987-11-03 1993-08-18 Genentech Inc Gamma interferon formulation
FR2641278B1 (fr) * 1989-01-05 1991-03-22 Lipha Piperidines, procedes de preparation et medicaments les contenant
DK203990D0 (da) * 1990-08-24 1990-08-24 Novo Nordisk As Piperazinylderivater
TW376319B (en) * 1993-04-28 1999-12-11 Janssen Pharmaceutica Nv Pharmaceutical composition containing risperidone pamoate and having a long acting activity for treating psychoses induced by the release of dopamine
US5453425A (en) * 1994-07-11 1995-09-26 Janssen Pharmaceutica N.V. Risperidone oral formulation
FR2796273B1 (fr) * 1999-07-15 2003-09-12 Oreal Composition a phase grasse liquide gelifiee par un polyamide a groupements ester terminaux

Also Published As

Publication number Publication date
ATE206931T1 (de) 2001-11-15
NZ289432A (en) 1998-05-27
CA2194564A1 (en) 1996-01-25
US5616587A (en) 1997-04-01
HRP950397A2 (en) 1997-10-31
CZ2797A3 (en) 1997-07-16
DE69523313T2 (de) 2002-06-27
CZ285204B6 (cs) 1999-06-16
NO320366B1 (no) 2005-11-28
PL179972B1 (pl) 2000-11-30
EP0769965A1 (en) 1997-05-02
EP0769965B1 (en) 2001-10-17
RU2161965C2 (ru) 2001-01-20
TR199500778A1 (tr) 1996-10-21
AP774A (en) 1999-10-28
SK2297A3 (en) 1997-09-10
EE03426B1 (et) 2001-06-15
HK1010691A1 (en) 1999-06-25
FI116510B (fi) 2005-12-15
HU222352B1 (hu) 2003-06-28
KR100212942B1 (ko) 1999-08-02
SK282159B6 (sk) 2001-11-06
HRP950397B1 (en) 2002-04-30
AU2927595A (en) 1996-02-09
CN1148226C (zh) 2004-05-05
HUT76826A (en) 1997-11-28
PH31626A (en) 1999-01-12
ZA955720B (en) 1997-01-10
AU684193B2 (en) 1997-12-04
SI9500220A (en) 1996-02-29
CA2194564C (en) 1997-12-16
RO116778B1 (ro) 2001-06-29
NO970051D0 (no) 1997-01-07
FI970109A0 (fi) 1997-01-10
DE69523313D1 (de) 2001-11-22
HU9700082D0 (en) 1997-02-28
BG101106A (en) 1997-08-29
BR9508253A (pt) 1997-12-23
JPH09511751A (ja) 1997-11-25
FI970109A (fi) 1997-01-10
PL318132A1 (en) 1997-05-12
ES2165918T3 (es) 2002-04-01
TW420615B (en) 2001-02-01
USRE39181E1 (en) 2006-07-11
NO970051L (no) 1997-01-07
EE9700009A (et) 1997-08-15
JP2872412B2 (ja) 1999-03-17
PT769965E (pt) 2002-04-29
AP9700910A0 (en) 1997-01-31
WO1996001652A1 (en) 1996-01-25
DK0769965T3 (da) 2002-02-04
US5453425A (en) 1995-09-26
MX9700374A (es) 1997-04-30
MY114389A (en) 2002-10-31
CY2268B1 (en) 2003-07-04
BG63070B1 (bg) 2001-03-30
IL114525A0 (en) 1995-11-27
SI9500220B (sl) 2004-12-31
CN1155247A (zh) 1997-07-23
IL114525A (en) 1999-06-20

Similar Documents

Publication Publication Date Title
KR970704472A (ko) 수성 리스페리돈 제제(aqueous risperidone formulations)
RU97102139A (ru) Водные композиции рисперидона
US11116724B2 (en) Methotrexate composition
FI95773C (fi) Menetelmä vesipitoisen, N-(3,4-dimetoksikinnamoyyli)antraniilihappoa sisältävän farmaseuttisen koostumuksen valmistamiseksi
HUP0105173A2 (hu) Adagolási módszer és készítmény sürgősségi fogamzásgátlásra
JP2002528404A (ja) 脂肪酸／アミノ酸セッケンを含む局所投与可能薬学的組成物のための保存系
JPH1160505A (ja) 防腐組成物
US5422102A (en) Antiinflammatory and analgesic gel preparation
JP2003505419A (ja) ケトチフェンを含む眼用組成物
JP5314014B2 (ja) テルビブジンを含む医薬内用液
JPS605567B2 (ja) オキシテトラサイクリンの調合液
JP2002114711A (ja) 外用剤組成物
JPH0536412B2 (ko)
JP2000204036A (ja) グルタミン酸塩含有液剤
JP2004182719A (ja) ラタノプロストを有効成分とする安定な点眼液
MXPA06014386A (es) Solucion acuosa de risperidona para administracion oral.
TH20763A (th) สูตรผสมเอเควียสริสเพอริโดน
TH14760B (th) สูตรผสมเอเควียสริสเพอริโดน
JP2004196671A (ja) 水溶性アズレン含有点眼剤
JPH10139666A (ja) 液剤およびその製造方法
KR0159730B1 (ko) 케토코나졸 수성 제제
JPH085784B2 (ja) シロツプ剤
JP4134358B2 (ja) ビオチンの溶解方法及び内服液剤
JPH1149698A (ja) 安定性を向上させたラクトフェリンの水性製剤
RU2276982C2 (ru) Средство, обладающее противовоспалительным, анальгетическим, жаропонижающим действием в форме таблетки

Legal Events

Date Code Title Description
A201 Request for examination
E701 Decision to grant or registration of patent right
GRNT Written decision to grant
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid
FPAY Annual fee payment
FPAY Annual fee payment
FPAY Annual fee payment

Payment date: 20150417

Year of fee payment: 17

EXPY Expiration of term