KR960706353A - Long-acting injection suspensions and a process for their preparation - Google Patents

Long-acting injection suspensions and a process for their preparation Download PDF

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KR960706353A
KR960706353A KR1019960702947A KR19960702947A KR960706353A KR 960706353 A KR960706353 A KR 960706353A KR 1019960702947 A KR1019960702947 A KR 1019960702947A KR 19960702947 A KR19960702947 A KR 19960702947A KR 960706353 A KR960706353 A KR 960706353A
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South Korea
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salt according
salt
particle diameter
lhrh
medicament
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KR1019960702947A
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Korean (ko)
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KR100344330B1 (en
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엔겔 위르겐
클록커스베트케 카린
라이쓰만 토마스
힐가르트 페터
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볼프강 메르크, 후베르트 보프
아스타 메디카 아크티엔게젤샤프트
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Priority claimed from DE4342092A external-priority patent/DE4342092B4/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/10—Peptides having 12 to 20 amino acids
    • A61K38/105—Bombesin; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/31—Somatostatins
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Zoology (AREA)
  • Urology & Nephrology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 입자 크기 5 내지 200㎛에서 내재적 서방성 효과를 나타내는, 세트로렐릭스 엠보네이트와 같은 LHRH 유사체의 용해성이 불량한 염에 관한 것이다.The present invention relates to salts with poor solubility of LHRH analogs, such as Setrorelix embonate, which exhibit intrinsic sustained release effects at particle sizes of 5 to 200 μm.

Description

장기 활성 주사 현탁제 및 이의 제조 방법(Long-acting injection suspensions and a process for their preparation)Long-acting injection suspensions and a process for their preparation

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (30)

입자 크기가 주로 5 내지 200㎛임을 특징으로 하는, LHRH 유사체의 용해성이 불량한 염.Salts with poor solubility of LHRH analogues, characterized in that the particle size is mainly between 5 and 200 μm. 입자 직경이 주로 10 내지 150㎛임을 특징으로 하는, LHRH 유사체의 용해성이 불량한 염.Salts with poor solubility of LHRH analogues, characterized in that the particle diameter is predominantly 10 to 150 μm. 입자 직경이 주로 20 내지 125㎛임을 특징으로 하는, LHRH 유사체의 용해성이 불량한 염.Salts with poor solubility of LHRH analogues, characterized in that the particle diameter is predominantly 20 to 125 μm. 제1항 내지 제3항 중의 어느 한 항에 있어서, 엠본산이 염 형성제로 상용됨을 특징으로 하는 용해성이 불량한 염.The poorly soluble salt according to any one of claims 1 to 3, wherein embonic acid is compatible as a salt forming agent. 약제를 제조하기 위한 제1항 내지 제4항 중의 어느 한 항에 따르는 용해성이 불량한 염의 용도.Use of a poorly soluble salt according to any one of claims 1 to 4 for the manufacture of a medicament. 제1항 내지 제5항 중의 어느 한 항에 있어서, 세트로렐릭스가 LHRH 유사체로 사용됨을 특징으로 하는 염.The salt according to any one of claims 1 to 5, characterized in that Setlorellix is used as the LHRH analogue. 제1항 내지 제5항 중의 어느 한 항에 있어서, 안타렉릭스가 LHRH 유사체로 사용됨을 특징으로 하는 염.6. The salt according to claim 1, wherein antarexix is used as the LHRH analog. 7. 제1항 내지 제5항 중의 어느 한 항에 있어서, 가니렐릭스가 LHRH 유사체로 사용됨을 특징으로 하는 염.The salt according to any one of claims 1 to 5, wherein Ganirelix is used as an LHRH analog. 제1항 내지 제5항 중의 어느 한 항에 있어서, 앤타이드가 LHRH 유사체로 사용됨을 특징으로 하는 염.The salt according to any one of claims 1 to 5, wherein the antide is used as an LHRH analog. 제1항 내지 제5항 중의 어느 한 항에 있어서, A-75988이 LHRH 유사체로 사용됨을 특징으로 하는 염.The salt according to any one of claims 1 to 5, wherein A-75988 is used as an LHRH analog. 제6항 내지 제10항 중의 어느 한 항에 있어서, 엠본산이염 형성제로 사용됨을 특징으로 하는 염.The salt according to any one of claims 6 to 10, characterized in that it is used as an embon dichloride forming agent. 입자 직경이 10 내지 125㎛임을 특징으로 하는 앤타이드 엠보네이트.An amide emidenate, characterized in that the particle diameter is 10 to 125 μm. 입자 직경이 10 내지 124㎛임을 특징으로 하는 가니렐릭스 엠보네이트.Ganirelix emonate, characterized in that the particle diameter is 10 to 124㎛. 입자 직경이 10 내지 125㎛임을 특징으로 하는 A-75998 엠보네이트.A-75998 emonate, characterized in that the particle diameter is 10 to 125 μm. 입자 직경이 5 내지 200㎛임을 특징으로 하는 세트로렐릭스 엠보네이트.Setlorellix emonate, characterized in that the particle diameter is 5 to 200㎛. 입자 직경이 10 내지 125㎛임을 특징으로 하는 세트로렐릭스 엠보네이트.Setlorellix emonate, characterized in that the particle diameter is 10 to 125㎛. 입자 직경이 20 내지 125㎛임을 특징으로 하는 세트로렐릭스 엠보네이트.Setlorellix emonate, characterized in that the particle diameter is 20 to 125㎛. 약제를 제조하기 위한 제6항 내지 제17항 중 어느 한 항에 따르는 염의 용도.Use of a salt according to any one of claims 6 to 17 for the manufacture of a medicament. 입자 직경이 5 내지 200㎛임을 특징으로 하는, 펩타이드의 용해성이 불량한 염.Salt having poor solubility of the peptide, characterized in that the particle diameter is 5 to 200㎛. 제19항에 있어서, 엠본산이 염 형성제로 사용됨을 특징으로 하는 염.20. The salt according to claim 19, wherein embonic acid is used as the salt former. 약제를 제조하기 위한 제20항에 따르는 염의 용도.Use of a salt according to claim 20 for the manufacture of a medicament. 입자 직경이 5 내지 200㎛임을 특징으로 하는, 소마토스타틴 유사체의 용해성이 불량한 염.A poorly soluble salt of somatostatin analog, characterized in that the particle diameter is 5 to 200 mu m. 제22항에 있어서, 엠본산이 염 형성제로 사용됨을 특징으로 하는 염.23. A salt according to claim 22, wherein embonic acid is used as the salt former. 약제를 제조하기 위한 제23항에 따르는 염의 용도.Use of a salt according to claim 23 for the manufacture of a medicament. 입자의 직경이 5 내지 200㎛임을 특징으로 하는, GHRH 유사체의 용해성이 불량한 염.Salts with poor solubility of GHRH analogues, characterized in that the particles have a diameter of 5 to 200 μm. 제25항에 있어서, 엠본산이 염 형성제로 사용됨을 특징으로 하는 염.26. The salt of claim 25, wherein embonic acid is used as the salt former. 약제를 제조하기 위한 제26항에 따르는 염의 용도.Use of a salt according to claim 26 for the manufacture of a medicament. 입자 직경이 5 내지 200㎛임을 특징으로 하는, 봄베신 유사체의 용해성이 불량한 염.Salts with poor solubility of bombesin analogues, characterized in that the particle diameter is between 5 and 200 μm. 제28항에 있어서, 엠본산이 염 형성제로 사용됨을 특징으로 하는 염.29. A salt according to claim 28, wherein embonic acid is used as the salt former. 약제를 제조하기 위한 제29항에 따르는 염의 용도.Use of a salt according to claim 29 for the manufacture of a medicament. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019960702947A 1993-12-09 1994-11-25 Long-acting injection suspensions and a process for their preparation KR100344330B1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE4342092A DE4342092B4 (en) 1993-12-09 1993-12-09 Long-acting suspension for injection and method of preparation
DEP4342092.3 1993-12-09
PCT/EP1994/003904 WO1995015767A1 (en) 1993-12-09 1994-11-25 Long-acting injection suspensions and a process for their preparation

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Publication Number Publication Date
KR960706353A true KR960706353A (en) 1996-12-09
KR100344330B1 KR100344330B1 (en) 2002-11-30

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KR (1) KR100344330B1 (en)
DE (1) DE69434553T2 (en)
MY (1) MY119896A (en)
SI (1) SI0732934T1 (en)
TW (1) TW327176B (en)
UA (1) UA44722C2 (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4342092B4 (en) * 1993-12-09 2007-01-11 Zentaris Gmbh Long-acting suspension for injection and method of preparation

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MY119896A (en) 2005-08-30
SI0732934T1 (en) 2006-02-28
TW327176B (en) 1998-02-21
DE69434553D1 (en) 2005-12-29
KR100344330B1 (en) 2002-11-30
DE69434553T2 (en) 2006-08-10
UA44722C2 (en) 2002-03-15

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