WO2000016744A1 - Solution pharmaceutique du type sedds pour le traitement des troubles de l'erection - Google Patents

Solution pharmaceutique du type sedds pour le traitement des troubles de l'erection Download PDF

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Publication number
WO2000016744A1
WO2000016744A1 PCT/KR1999/000568 KR9900568W WO0016744A1 WO 2000016744 A1 WO2000016744 A1 WO 2000016744A1 KR 9900568 W KR9900568 W KR 9900568W WO 0016744 A1 WO0016744 A1 WO 0016744A1
Authority
WO
WIPO (PCT)
Prior art keywords
component
acid
composition
oil
value
Prior art date
Application number
PCT/KR1999/000568
Other languages
English (en)
Inventor
Sang Soon Lee
Young Wook Choi
Sang Kil Lee
Gee Bae Park
Original Assignee
Guju Pharm. Co., Ltd.
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 Guju Pharm. Co., Ltd. filed Critical Guju Pharm. Co., Ltd.
Publication of WO2000016744A1 publication Critical patent/WO2000016744A1/fr

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Classifications

    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/5575—Eicosanoids, e.g. leukotrienes or prostaglandins having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • 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
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers

Definitions

  • the present invention relates to a new pharmaceutical
  • composition for the treatment of erectile dysfunction More
  • composition containing prostaglandins, or prostan landin E ⁇ PGE ⁇ composition containing prostaglandins, or prostan landin E ⁇ PGE ⁇
  • Prostaglandin Ei is a bioactive compound chemically designated as
  • pH 3—4 range in the form of an aqueous solution preparation
  • composition comprising a biologically active prostaglandin of
  • prostaglandin being present in the amount of from about 0.005 to
  • US Patent No.3, 952, 04 discloses a
  • lyophilized pharmaceutical composition comprising a biologically
  • pellet-type suppository that enables the drug to be absorbed
  • prostaglandin based on the concept of self-emulsi ying drug
  • An object of the present invention is to provide a new urethral
  • This preparation has a property, upon administration to a human
  • the characteristic features of the preparation include such facts that it is capable to overcome instability of the drug to
  • Figure la is a diagram of phase equilibria for systems
  • Figure lb is a diagram of phase equilibria for systems
  • Figure lc is a diagram of phase equilibria for systems containing Labrafil M1944CS and represents Examples 3-1 through
  • Figure Id is a diagram of phase equilibria for systems
  • Figure le is a diagram of phase equilibria, for systems
  • Figures 2aa and 2ab show the distribution patterns of particle
  • microemulsion prepared according to the present invention While
  • the ratio of surfactant to cosurfactant is controlled at 2.5.
  • microemulsion prepared according to the present invention While
  • the ratio of surfactant to cosurfactant is controlled at 2.
  • Figure 3 represents changes in the viscosity in relation to the
  • Figure 4a is a graph showing stabilities of the drug in Example
  • prostaglandins such as PGEi as the active ingredient
  • the skin consisting of ethanol, isopropyl alcohol and benzyl
  • HLB hydrophile-lipophile balance
  • composition consisting of ingredients or components which are
  • composition of the present invention can be any prostaglandin
  • the present invention can include a mixture of monoglycerides
  • the fatty acid portion can include both saturated
  • fatty acid portion will include saturated fatty acid residues
  • composition of the present invention Component (2)
  • suitable for the present invention include the followings.
  • esters of glycerol contains five major fatty acids(58.9* of 1 linoleic acid, 25.8* of oleic acid, 11.0* of palmitic acid, 1.7*
  • capric acid as the principal components and monoglycerides
  • palmitic acid 4 20*.
  • stearic acid 1 6*, oleic
  • invention will preferably be a hydrophilic surfactant having an
  • Cremophor EL Cremophor ELP
  • Cremophor RH 40 Cremophor RH 60, etc. and, in particular,
  • Cremophor EL having a molecular weight of about 1,630, a
  • oleic acid and palmitic acid less than 1*. respectively but
  • Cremophor ELP is more preferable.
  • microemulsion preconcentrate The pharmaceutical composition of
  • the present invention should preferably be of SEDDS, or.
  • composition of the present invention contains
  • Component (2) will be any amount of 5—35*. preferably 10—25*.
  • Component (2) will be any amount of 5—35*. preferably 10—25*.
  • Component (3) will preferably exist in an amount of
  • single-use urethral solution is in the range from 0.1 to 1.0 ml
  • prostaglandin Ei is between 250
  • microemulsions of the preparations according to the SEDDS method are microemulsions of the preparations according to the SEDDS method.
  • Figures 2b and 2c represent changes of the particle sizes in
  • the average particle size is in the range of 20—300 nm and it is
  • microemulsion preconcentrate was determined to be about 688
  • Figure 4b represents an Arrhenius plot demonstrating a
  • the ratio of surfactant over cosurfactant(hereinafter to be abbreviated as "km") is 3 and for Examples from 1.-1 to 1-4 and from 1-16 to
  • km is 2.5. Further, for Examples from 1-5 to 1-7 and from 1-20 to 1-22, km is 2 and for Examples from 1-8 to 1-9 and from
  • Cremophor EL or Cremophor ELP and Labrafil M1944CS are the Cremophor ELP and Labrafil M1944CS.
  • Cremophor EL or Cremophor ELP and WL2609BS are added
  • the ratio of surfactant over cosurfactant is 2.5.
  • Cremophor RH40 or Cremophor ELP and Maisine are added

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Dispersion Chemistry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention porte sur une nouvelle solution pharmaceutique pour le traitement des troubles de l'érection à base de prostanglandine E1, se présentant sous la forme d'un préconcentré d'une microémulsion. Ladite préparation, administrée à l'homme s'émulsionne facilement ou se disperse elle-même d'ou son appellation de 'SEDDS' (système autoémulsifiant d'administration de médicaments) obtenu par dispersion ou dissolution du médicament dans un mélange liquide d'huile, d'un tensio-actif et d'un co-tensio-actif.
PCT/KR1999/000568 1998-09-23 1999-09-21 Solution pharmaceutique du type sedds pour le traitement des troubles de l'erection WO2000016744A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR19980039462 1998-09-23
KR1998/39462 1998-09-23
KR1019990034157A KR100350179B1 (ko) 1998-09-23 1999-08-18 Ｓｅｄｄｓ로 제제화한 발기부전치료용 주입액제
KR1999/34157 1999-08-18

Publications (1)

Publication Number Publication Date
WO2000016744A1 true WO2000016744A1 (fr) 2000-03-30

Family

ID=26634145

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR1999/000568 WO2000016744A1 (fr) 1998-09-23 1999-09-21 Solution pharmaceutique du type sedds pour le traitement des troubles de l'erection

Country Status (2)

Country Link
KR (1) KR100350179B1 (fr)
WO (1) WO2000016744A1 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009084021A3 (fr) * 2007-10-16 2009-12-03 Sun Pharma Advanced Research Company Limited Nouvelles compositions ophtalmologiques
EP2377577A1 (fr) * 2010-04-06 2011-10-19 Panaxia Ltd Mélange d'alcool benzylique pour traiter l'éjaculation précoce
US8802095B2 (en) 2007-01-26 2014-08-12 Durect Corporation Injectable, non-aqueous suspension with high concentration of therapeutic agent
WO2015071841A1 (fr) 2013-11-12 2015-05-21 Druggability Technologies Holdings Limited Complexes de dabigatran et ses dérivés, procédé de préparation de ceux-ci et compositions pharmaceutiques contenant ceux-ci
CN104706591A (zh) * 2013-12-16 2015-06-17 天津迈迪瑞康生物医药科技有限公司 一种前列地尔药物组合物、其制备方法及用途
WO2015165373A1 (fr) * 2014-04-29 2015-11-05 北京蓝丹医药科技有限公司 Émulsion lipidique d'alprostadil pour injection et son procédé de préparation

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5154930A (en) * 1987-03-05 1992-10-13 The Liposome Company, Inc. Pharmacological agent-lipid solution preparation
WO1996003113A1 (fr) * 1994-07-22 1996-02-08 G.D. Searle & Co. Systeme d'apport de medicaments auto-emulsifiant
WO1996028142A1 (fr) * 1995-03-14 1996-09-19 Vivus, Incorporated Procede de prevention de la dyserection et kit correspondant
WO1997022334A1 (fr) * 1995-12-15 1997-06-26 Harvard Scientific Corporation Liposomes lyophilises contenant de la pge-1 pour le traitement des troubles de l'erection

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5154930A (en) * 1987-03-05 1992-10-13 The Liposome Company, Inc. Pharmacological agent-lipid solution preparation
WO1996003113A1 (fr) * 1994-07-22 1996-02-08 G.D. Searle & Co. Systeme d'apport de medicaments auto-emulsifiant
WO1996028142A1 (fr) * 1995-03-14 1996-09-19 Vivus, Incorporated Procede de prevention de la dyserection et kit correspondant
WO1997022334A1 (fr) * 1995-12-15 1997-06-26 Harvard Scientific Corporation Liposomes lyophilises contenant de la pge-1 pour le traitement des troubles de l'erection

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8802095B2 (en) 2007-01-26 2014-08-12 Durect Corporation Injectable, non-aqueous suspension with high concentration of therapeutic agent
WO2009084021A3 (fr) * 2007-10-16 2009-12-03 Sun Pharma Advanced Research Company Limited Nouvelles compositions ophtalmologiques
US9539262B2 (en) 2007-10-16 2017-01-10 Sun Pharma Advanced Research Company Ltd. Ophthalmic composition comprising a prostaglandin
US9629852B2 (en) 2007-10-16 2017-04-25 Sun Pharma Advanced Research Company Ltd. Ophthalmic composition comprising a prostaglandin
EP2377577A1 (fr) * 2010-04-06 2011-10-19 Panaxia Ltd Mélange d'alcool benzylique pour traiter l'éjaculation précoce
WO2015071841A1 (fr) 2013-11-12 2015-05-21 Druggability Technologies Holdings Limited Complexes de dabigatran et ses dérivés, procédé de préparation de ceux-ci et compositions pharmaceutiques contenant ceux-ci
CN104706591A (zh) * 2013-12-16 2015-06-17 天津迈迪瑞康生物医药科技有限公司 一种前列地尔药物组合物、其制备方法及用途
CN104706591B (zh) * 2013-12-16 2018-09-04 天津迈迪瑞康生物医药科技有限公司 一种前列地尔药物组合物、其制备方法及用途
WO2015165373A1 (fr) * 2014-04-29 2015-11-05 北京蓝丹医药科技有限公司 Émulsion lipidique d'alprostadil pour injection et son procédé de préparation

Also Published As

Publication number Publication date
KR20000022734A (ko) 2000-04-25
KR100350179B1 (ko) 2002-08-27

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