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WO2017105090A1 - Polymorphe cristallin de l-carnitine orotate, son procédé de production, ou son utilisation - Google Patents

Polymorphe cristallin de l-carnitine orotate, son procédé de production, ou son utilisation Download PDF

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Publication number
WO2017105090A1
WO2017105090A1 PCT/KR2016/014672 KR2016014672W WO2017105090A1 WO 2017105090 A1 WO2017105090 A1 WO 2017105090A1 KR 2016014672 W KR2016014672 W KR 2016014672W WO 2017105090 A1 WO2017105090 A1 WO 2017105090A1
Authority
WO
WIPO (PCT)
Prior art keywords
carnitine
orotic acid
present
orotate
weight
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/KR2016/014672
Other languages
English (en)
Korean (ko)
Inventor
김재선
유형철
정중근
김혁민
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
J2H Biotech Inc
Original Assignee
J2H Biotech Inc
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
Priority claimed from KR1020160169508A external-priority patent/KR20170071431A/ko
Application filed by J2H Biotech Inc filed Critical J2H Biotech Inc
Publication of WO2017105090A1 publication Critical patent/WO2017105090A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/22—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated the carbon skeleton being further substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals

Definitions

  • Crystalline polymorph 1 of orot acid L-carnitine orotate of the present invention has the differential scanning calorimetry (DSC) characteristic of FIG.
  • the present invention provides a pharmaceutical composition for preventing or treating liver disease comprising the above-described L-carnitine orotate polymorph type 1 of the present invention as an active ingredient. do.
  • Suitable dosages of the pharmaceutical compositions of the present invention may vary depending on factors such as the formulation method, mode of administration, age, weight, sex, morbidity, condition of food, time of administration, route of administration, rate of excretion and response to response of the patient. Can be.
  • the daily dose of the pharmaceutical composition of the present invention is, for example, 0.001-100 mg / kg.
  • L-carnitine in place of orotic acid D, L-carnitine was confirmed that there is no problem in the formulation, and a stable hard capsule was prepared without problems due to changes in carnitine isomeric components.
  • the protection scope of the present invention is not limited by these.
  • L-carnitine in place of orotic acid D, L-carnitine was confirmed that there was no problem in the formulation, and a stable tablet was prepared without problems due to changes in the carnitine isomeric component.
  • the protection scope of the present invention is not limited by these.
  • L-carnitine orotic acid crystalline form 1 of the present invention has very low hygroscopicity compared to L-carnitine intramolecular salt under a temperature of 40 ° C. and a relative humidity of 75%, and does not increase water content over time. Because of its saturation properties, it is useful for pharmaceutical use as a pharmaceutical ingredient.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne le polymorphe cristallin de forme 1 de L-carnitine orotate, son procédé de production, et son utilisation. Le polymorphe cristallin de forme 1 de L-carnitine orotate de la présente invention peut être utilisé en tant que composition pharmaceutique pour la prévention ou le traitement de maladies du foie.
PCT/KR2016/014672 2015-12-14 2016-12-14 Polymorphe cristallin de l-carnitine orotate, son procédé de production, ou son utilisation Ceased WO2017105090A1 (fr)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
KR20150178236 2015-12-14
KR10-2015-0178236 2015-12-14
KR20160013105 2016-02-02
KR10-2016-0013105 2016-02-02
KR10-2016-0169508 2016-12-13
KR1020160169508A KR20170071431A (ko) 2015-12-14 2016-12-13 오로트산 l-카르니틴의 결정질 다형체, 이의 제조방법 또는 용도

Publications (1)

Publication Number Publication Date
WO2017105090A1 true WO2017105090A1 (fr) 2017-06-22

Family

ID=59057030

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2016/014672 Ceased WO2017105090A1 (fr) 2015-12-14 2016-12-14 Polymorphe cristallin de l-carnitine orotate, son procédé de production, ou son utilisation

Country Status (1)

Country Link
WO (1) WO2017105090A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019031898A3 (fr) * 2017-08-10 2019-04-25 주식회사 셀트리온화학연구소 Composition pharmaceutique et sa méthode de préparation
WO2022019578A1 (fr) * 2020-07-22 2022-01-27 주식회사 셀트리온제약 Comprimé pelliculé pour la prévention et le traitement d'une hépatopathie

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4602039A (en) * 1983-12-28 1986-07-22 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Salts of-carnitine and alkanoyl L-carnitines and process for preparing same
US4883786A (en) * 1984-06-29 1989-11-28 Magis Farmaceutici Srl Derivatives of L-carnitine
WO2001017525A1 (fr) * 1999-09-03 2001-03-15 Sigma-Tau Healthscuience S.P.A L-carnitine ultrafine, procedes de preparation associes, compositions contenant cette derniere et procedes d'utilisation associes
KR100294329B1 (ko) * 1999-11-08 2001-06-15 권철 간질환 치료 및 예방용 의약 조성물
KR20140019769A (ko) * 2010-09-06 2014-02-17 론자 아게 (론자 엘티디.) L-카르니틴 타르트레이트의 제조방법

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4602039A (en) * 1983-12-28 1986-07-22 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Salts of-carnitine and alkanoyl L-carnitines and process for preparing same
US4883786A (en) * 1984-06-29 1989-11-28 Magis Farmaceutici Srl Derivatives of L-carnitine
WO2001017525A1 (fr) * 1999-09-03 2001-03-15 Sigma-Tau Healthscuience S.P.A L-carnitine ultrafine, procedes de preparation associes, compositions contenant cette derniere et procedes d'utilisation associes
KR100294329B1 (ko) * 1999-11-08 2001-06-15 권철 간질환 치료 및 예방용 의약 조성물
KR20140019769A (ko) * 2010-09-06 2014-02-17 론자 아게 (론자 엘티디.) L-카르니틴 타르트레이트의 제조방법

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019031898A3 (fr) * 2017-08-10 2019-04-25 주식회사 셀트리온화학연구소 Composition pharmaceutique et sa méthode de préparation
CN111132665A (zh) * 2017-08-10 2020-05-08 赛特瑞恩制药股份有限公司 药物组合物及其制备方法
CN111132665B (zh) * 2017-08-10 2022-06-14 赛特瑞恩制药股份有限公司 药物组合物及其制备方法
WO2022019578A1 (fr) * 2020-07-22 2022-01-27 주식회사 셀트리온제약 Comprimé pelliculé pour la prévention et le traitement d'une hépatopathie

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