PL423041A1 - New crystalline form of anhydrous 17-ß-estradiol, method for obtaining it and pharmaceutical composition that contains new crystalline form of anhydrous 17-ß-estradiol and its application - Google Patents

New crystalline form of anhydrous 17-ß-estradiol, method for obtaining it and pharmaceutical composition that contains new crystalline form of anhydrous 17-ß-estradiol and its application

Info

Publication number
PL423041A1
PL423041A1 PL423041A PL42304117A PL423041A1 PL 423041 A1 PL423041 A1 PL 423041A1 PL 423041 A PL423041 A PL 423041A PL 42304117 A PL42304117 A PL 42304117A PL 423041 A1 PL423041 A1 PL 423041A1
Authority
PL
Poland
Prior art keywords
estradiol
anhydrous
crystalline form
application
new crystalline
Prior art date
Application number
PL423041A
Other languages
Polish (pl)
Other versions
PL236889B1 (en
Inventor
Łukasz SZELESZCZUK
Ewa JURCZAK
Dariusz Maciej PISKLAK
Monika ZIELIŃSKA-PISKLAK
Original Assignee
Warszawski Univ Medyczny
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 Warszawski Univ Medyczny filed Critical Warszawski Univ Medyczny
Priority to PL423041A priority Critical patent/PL236889B1/en
Priority to PCT/PL2018/050050 priority patent/WO2019070139A1/en
Priority to EP18864585.7A priority patent/EP3692050A4/en
Publication of PL423041A1 publication Critical patent/PL423041A1/en
Publication of PL236889B1 publication Critical patent/PL236889B1/en

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Classifications

    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • 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
    • A61P15/18—Feminine contraceptives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Endocrinology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Przedmiotem zgłoszenia jest forma krystaliczna bezwodnego 17-ß-estradiolu charakteryzująca się tym, że na zarejestrowanym dla niej rentgenowskim dyfraktogramie proszkowym występują refleksy przy następujących wartościach kąta 2? zmierzone stosując promieniowanie CuK?: 4,506, 4,687, 11,813, 11,898, 13,915, 15,351, 15,675, 16,237, 16,427, 17,979, 18,584, 18,712, 27,494, oraz że jej widmo wykonane techniką jądrowego rezonansu magnetycznego 13C dla postaci ciała stałego charakteryzowane jest przez sygnały o następujących przesunięciach chemicznych wyrażonych w częściach na milion: 154,4, 153,2, 138,6, 137,2, 132,7, 131,7, 129,8, 126,0, 115,8, 115,1, 114,1, 81,6, 50,0, 45,4, 44,4, 43,5, 40,8, 38,3, 33,5, 31,3, 30,0, 27,5, 23,9, 22,8, 14,2, 11,0. Przedmiotem zgłoszenia jest też sposób otrzymywania formy krystalicznej bezwodnego 17-ß-estradiolu z hemihydratu 17-ß-estradiolu, oraz zastosowanie formy krystalicznej SPJ 17-ß-estradiolu. Zgłoszenie obejmuje też kompozycję farmaceutyczną zawierającą substancję czynną i farmaceutycznie dopuszczalny nośnik, charakteryzującą się tym, że jako substancję czynną zawiera formę krystaliczną bezwodnego 17-ß-estradiolu określoną w zastrzeżeniu 1 i 2.The subject of the application is the crystalline form of anhydrous 17-ß-estradiol characterized by the fact that on the registered X-ray powder diffraction pattern there are reflections at the following values of the angle 2? measured using CuK? radiation: 4.506, 4.687, 11.813, 11.898, 13.915, 15.31, 15.675, 16.237, 16.427, 17.979, 18.584, 18.712, 27.494, and that its spectrum made by 13C nuclear magnetic resonance imaging is characterized by signals with the following chemical shifts expressed in parts per million: 154.4, 153.2, 138.6, 137.2, 132.7, 131.7, 129.8, 126.0, 115.8, 115.1, 114.1, 81.6, 50.0, 45.4, 44.4, 43.5, 40.8, 38.3, 33.5, 31.3, 30.0, 27.5, 23, 9, 22.8, 14.2, 11.0. The subject of the application is also the method of obtaining anhydrous 17-ß-estradiol anhydrous form from 17-ß-estradiol hemihydrate, and the use of SPJ 17-ß-estradiol crystal form. The application also includes a pharmaceutical composition comprising the active substance and a pharmaceutically acceptable carrier, characterized in that as the active substance it contains the crystalline form of anhydrous 17-ß-estradiol as defined in claims 1 and 2.

PL423041A 2017-10-03 2017-10-03 New crystalline form of anhydrous 17-β-estradiol, method for obtaining it and pharmaceutical composition that contains new crystalline form of anhydrous 17-β-estradiol and its application PL236889B1 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
PL423041A PL236889B1 (en) 2017-10-03 2017-10-03 New crystalline form of anhydrous 17-β-estradiol, method for obtaining it and pharmaceutical composition that contains new crystalline form of anhydrous 17-β-estradiol and its application
PCT/PL2018/050050 WO2019070139A1 (en) 2017-10-03 2018-10-03 A NEW CRYSTALLINE FORM OF ANHYDROUS 17-β-ESTRADIOL, A METHOD FOR ITS PREPARATION AND A PHARMACEUTICAL COMPOSITION CONTAINING A NEW CRYSTALLINE FORM OF ANHYDROUS 17-β-ESTRADIOL AND ITS APPLICATION
EP18864585.7A EP3692050A4 (en) 2017-10-03 2018-10-03 NEW CRYSTALLINE SHAPE OF 17-

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PL423041A PL236889B1 (en) 2017-10-03 2017-10-03 New crystalline form of anhydrous 17-β-estradiol, method for obtaining it and pharmaceutical composition that contains new crystalline form of anhydrous 17-β-estradiol and its application

Publications (2)

Publication Number Publication Date
PL423041A1 true PL423041A1 (en) 2019-04-08
PL236889B1 PL236889B1 (en) 2021-02-22

Family

ID=65992083

Family Applications (1)

Application Number Title Priority Date Filing Date
PL423041A PL236889B1 (en) 2017-10-03 2017-10-03 New crystalline form of anhydrous 17-β-estradiol, method for obtaining it and pharmaceutical composition that contains new crystalline form of anhydrous 17-β-estradiol and its application

Country Status (3)

Country Link
EP (1) EP3692050A4 (en)
PL (1) PL236889B1 (en)
WO (1) WO2019070139A1 (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA935107B (en) * 1992-07-16 1994-02-04 Lohmann Therapie Syst Lts Transdermal therapeutic system comprising the active substance 17-BETA-estradiol (anhydrous)
WO2002034741A2 (en) * 2000-10-20 2002-05-02 Eli Lilly And Company A NOVEL CRYSTALLINE FORM OF 6-HYDROXY-3-(4-[2-(PIPERIDIN-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5827245A (en) * 1992-07-16 1998-10-27 Lts Lohmann Therapie-Systeme Gmbh & Co. Kg Transdermal therapeutic system comprising the active subtance 17-β-Estradiol (Anhydrous)
US5928666A (en) * 1996-11-12 1999-07-27 Cygnus Inc. Crystalline form of estradiol and pharmaceutical formulations comprising same
US6287693B1 (en) * 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA935107B (en) * 1992-07-16 1994-02-04 Lohmann Therapie Syst Lts Transdermal therapeutic system comprising the active substance 17-BETA-estradiol (anhydrous)
WO2002034741A2 (en) * 2000-10-20 2002-05-02 Eli Lilly And Company A NOVEL CRYSTALLINE FORM OF 6-HYDROXY-3-(4-[2-(PIPERIDIN-1-YL)ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SILWIA LATSCH, CRYSTALLISATION OF ESTRADIOL CONTAINING TDDS DETERMINED BY ISOTHERMAL MICROCALORIMETRY, X-RAY DIFFRACTION, AND OPTICAL MICROSCOPY, July 2003 (2003-07-01) *

Also Published As

Publication number Publication date
EP3692050A1 (en) 2020-08-12
PL236889B1 (en) 2021-02-22
EP3692050A4 (en) 2021-06-16
WO2019070139A1 (en) 2019-04-11

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