WO2007032643A1 - Materiau solubilise comprenant de l’ubidecarenone, solution aqueuse et son procede de fabrication - Google Patents

Materiau solubilise comprenant de l’ubidecarenone, solution aqueuse et son procede de fabrication Download PDF

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Publication number
WO2007032643A1
WO2007032643A1 PCT/KR2006/003649 KR2006003649W WO2007032643A1 WO 2007032643 A1 WO2007032643 A1 WO 2007032643A1 KR 2006003649 W KR2006003649 W KR 2006003649W WO 2007032643 A1 WO2007032643 A1 WO 2007032643A1
Authority
WO
WIPO (PCT)
Prior art keywords
ubidecarenone
solubilized
coqlo
hydroxystearate
macrogol
Prior art date
Application number
PCT/KR2006/003649
Other languages
English (en)
Inventor
Ji Sun Kim
Dong Hyun Cho
Hyoung Goo Shin
Tae Wan Kim
Min Suk Lee
Jeong Hwa Park
Original Assignee
Daewoong 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 Daewoong Co., Ltd. filed Critical Daewoong Co., Ltd.
Publication of WO2007032643A1 publication Critical patent/WO2007032643A1/fr

Links

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
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/18—Antioxidants, e.g. antiradicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

  • the present invention relates to insoluble ubidecarenone compound, particularly
  • diseases comprising chronic hypertension, ischemic heart disease, congestion due to heart
  • CoQlO is included mainly in
  • CoQlO is conventionally marketed as a solid formulation for oral administration.
  • CoQlO exists in solid state at normal temperature (the melting point of CoQlO: 48 "C-
  • 1994-0021054 disclosed a method using non-ionic surfactant such as hydrogenated or
  • the surfactants in the solution may cause side
  • Korean Patent No. 28370 also disclosed a method for solubilizing lipid active
  • Such liquid formulation is administered to patients via oral route, the taste and taking
  • the present invention provides a solubilized
  • the present invention also provides an aqueous solution
  • the present invention provides an ubidecarenone-containing solubilized material
  • the present invention provides a solubilized aqueous solution
  • CoQlO is prepared by heating a solubilizer to its melting temperature or more to melt the
  • solubilizer to a liquid state, adding CoQlO as an active agent to the molten solubilizer, and
  • Macrogol 15 Hydroxystearate, non-ionic surfactant.
  • Hydroxystearate is preferably molten by heating it to a temperature of 50 ° C or more, and
  • Macrogol 15 Hydroxystearate can be heated to a melting point or more, and so the upper limit of the
  • temperature is not restricted. However, heating and mixing are carried out at the
  • active agent CoQlO may be chemically denatured.
  • weight ratio of CoQlO to Macrogol 15 Hydroxystearate is preferably 1:1 ⁇ 1:20, more
  • solubilized aqueous solution may stimulate the gastrointestinal tract and make the taste
  • the present invention is prepared by mixing the solubilized material with water or liquid
  • Liquid agent may comprise additional known additives used for oral liquid
  • the additives may comprise solubilizing aids, sweeteners, acidifiers,
  • solution may be optionally selected within the range of dosage known to be effective for oral administration in the art.
  • amount of CoQlO may be varied depending on age,
  • the amount of CoQlO is administered via oral route in the form of liquid formulation.
  • solubilizer for aqueous solutions, 2g of solubilizer was molten to a liquid form by heating the
  • solubilized material was cooled, and then the state was observed (A). Also, to said solubilized material was added IL of water to obtain a solubilized aqueous solution, and
  • Example 1 and Comparative Examples 3 and 4 showed good transparency and solubility.
  • Example 2 and Comparative Examples 10 and 11 showed good transparency and solubility.
  • solubilizer of Comparative Example 4 were molten to obtain liquid forms by heating
  • solubilized materials corresponding to lOmg of CoQlO were mixed with 100ml of
  • vitamin C content 700mg/100ml
  • solubilized aqueous solutions were determined.
  • solubilized aqueous solutions were evaluated by sensory test after taking them in oral
  • CoQlO was O.lg and the amount of Macrogol 15 Hydroxystearate was 0.4g or more
  • the present invention provides a solubilized material comprising the insoluble
  • ubidecarenone which has high transparency, and good taste and taking feeling. Also, the
  • present invention provides an aqueous solution comprising the same, and a process for

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La présente invention concerne un matériau solubilisé, ainsi qu’une solution aqueuse et son procédé de fabrication. La présente invention a plus particulièrement pour objet un matériau solubilisé contenant de l’ubidécarénone et de l’hydroxystéarate de macrogol 15 en tant que solubilisant ; une solution aqueuse comprenant un mélange dudit matériau, et d’eau ou d'un agent aqueux ; et un procédé de préparation dudit matériau comprenant les étapes suivantes : chauffage de 1 à 20 parties en poids d'hydroxystéarate de macrogol 15 à une température de 50 °C ou plus, et formation du matériau solubilisé par addition d’1 partie en poids d’ubidécarénone à l'hydroxystéarate de macrogol 15.
PCT/KR2006/003649 2005-09-14 2006-09-14 Materiau solubilise comprenant de l’ubidecarenone, solution aqueuse et son procede de fabrication WO2007032643A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2005-0085718 2005-09-14
KR1020050085718A KR100754953B1 (ko) 2005-09-14 2005-09-14 유비데카레논을 함유한 가용화물, 액상 제제 및 그 제조 방법

Publications (1)

Publication Number Publication Date
WO2007032643A1 true WO2007032643A1 (fr) 2007-03-22

Family

ID=37865185

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2006/003649 WO2007032643A1 (fr) 2005-09-14 2006-09-14 Materiau solubilise comprenant de l’ubidecarenone, solution aqueuse et son procede de fabrication

Country Status (2)

Country Link
KR (1) KR100754953B1 (fr)
WO (1) WO2007032643A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113440483B (zh) * 2021-06-30 2023-04-07 佛山市南海东方澳龙制药有限公司 一种犬用盐酸特比萘芬喷剂及其制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002024184A2 (fr) * 2000-09-19 2002-03-28 Abbott Gmbh & Co. Kg Formes galeniques stables contenant des ubiquinones
WO2004050072A1 (fr) * 2002-12-04 2004-06-17 Nisshin Pharma Inc. Composition soluble dans l'eau contenant une coenzyme q10
WO2004064543A1 (fr) * 2003-01-17 2004-08-05 Taiyo Kagaku Co., Ltd. Compositions contenant une coenzyme q10

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1191608B (it) 1985-02-01 1988-03-23 Zambon Spa Composizione farmaceutica e forme farmaceutiche che la contengono
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
WO2002043704A1 (fr) 2000-12-01 2002-06-06 Kyowa Hakko Kogyo Co., Ltd. Composition a solubilite ou absorbabilite orale amelioree

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002024184A2 (fr) * 2000-09-19 2002-03-28 Abbott Gmbh & Co. Kg Formes galeniques stables contenant des ubiquinones
WO2004050072A1 (fr) * 2002-12-04 2004-06-17 Nisshin Pharma Inc. Composition soluble dans l'eau contenant une coenzyme q10
WO2004064543A1 (fr) * 2003-01-17 2004-08-05 Taiyo Kagaku Co., Ltd. Compositions contenant une coenzyme q10

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WEIS M. ET AL.: "Bioavailability of four oral coenzyme Q10 formulations in healthy volunteers", MOL. ASPECTS MED., vol. 15, no. SUPPL., 1994, pages 273 - 280, XP003010244 *

Also Published As

Publication number Publication date
KR20070031065A (ko) 2007-03-19
KR100754953B1 (ko) 2007-09-04

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