WO2004014341A1 - Composition pharmaceutique pour administration orale contenant du florfenicol en tant que principe actif - Google Patents

Composition pharmaceutique pour administration orale contenant du florfenicol en tant que principe actif Download PDF

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Publication number
WO2004014341A1
WO2004014341A1 PCT/KR2003/001266 KR0301266W WO2004014341A1 WO 2004014341 A1 WO2004014341 A1 WO 2004014341A1 KR 0301266 W KR0301266 W KR 0301266W WO 2004014341 A1 WO2004014341 A1 WO 2004014341A1
Authority
WO
WIPO (PCT)
Prior art keywords
florfenicol
pharmaceutical composition
oral administration
surfactant
administration according
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/KR2003/001266
Other languages
English (en)
Inventor
Si-Young Chang
Jae-Seung Choi
Sung-Bae Park
Jong-Myung Park
Byeung-Gie Kim
Ji-Hoon Park
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.)
DAE HAN NEW PHARM Co Ltd
Original Assignee
DAE HAN NEW 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 DAE HAN NEW PHARM Co Ltd filed Critical DAE HAN NEW PHARM Co Ltd
Priority to AU2003244259A priority Critical patent/AU2003244259A1/en
Publication of WO2004014341A1 publication Critical patent/WO2004014341A1/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
    • A61K9/10—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
    • A61K9/10—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
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide

Definitions

  • the present invention relates to a pharmaceutical composition comprising florfenicol as an active ingredient, and more particularly to a pharmaceutical composition for oral administration comprising a florfenicol-containing microemulsion as an effective ingredient which is obtained by adding an oil and a surfactant to a solution of florfenicol in a hydrophilic or amphiphilic dispersion medium.
  • a pharmaceutical composition for oral administration comprising a florfenicol- containing microemulsion as an effective ingredient wherein the microemulsion is obtained by adding an oil and a surfactant to a solution of florfenicol in a hydrophilic or amphiphilic dispersion medium.
  • microemulsion containing florfenicol as an active ingredient enables the provision of the pharmaceutical composition comprising the active ingredient in the high concentration with excellent bioavailability in which the concentration of the active ingredient can be easily controlled by drinking water upon oral administration.
  • the hydrophilic or amphiphilic solvent as a dispersion medium is at least one solvent selected from the group consisting of diethyleneglycol monoethylether,
  • the weight ratio of the florfenicol to the hydrophilic or amphiphilic solvent is preferably within the range of 1: 0.5 ⁇ 5, and more preferably 1: 1 ⁇ 3.
  • the surfactant preferably has a hydrophilic lipophlic balance (HLB) of 1 ⁇ 20.
  • the surfactant usable in the present invention is at least one compound selected from the group consisting of reaction products between vegetable hardened oils and ethylene glycol (e.g., Cremophor RH40, Cremophor RH60); polyethylene sorbitan fatty acid esters (e.g., Tween 20, Tween 40); polyoxyethylene fatty acid esters; polyoxyethylene-polyoxypropylene copolymers; and ester group transfer reaction products between vegetable oil triglycerides and polyalkylenepolyols (e.g., Labrafil, Labrasol).
  • the surfactant includes polyethyleneglycol 40 castor hardened oil and polyethyleneglycol 35 castor hardened oil.
  • the oil used in the present invention is at least one compound selected from the group consisting of vegetable oils, esterification products of vegetable oils and highly unsaturated fatty acids.
  • the weight ratio of the florfenicol to the oil is preferably within the range of 1: 0.1 ⁇ 10, and more preferably 1: 0.5 ⁇ 3. When the ratio is less than 1: 0.1, addition effect of the oil is none or little. When the ratio exceeds 1 : 10, there is a risk of phase separation.
  • this range is given only for the purpose of illustration, and is not to be construed as limiting the scope ofthe invention.
  • the pharmaceutical composition for oral administration of the present invention comprising the florfenicol-containing microemulsion may further comprise various medically acceptable additives.
  • these additives include antioxidants (butylparahydroxy benzoic acid, butylhydroquinone, tocopherol, etc.), viscosity enhancing agents (sodium alginate, carboxymethylcellulose, methylcellulose, tragacanth, agar, polyvinylpyrrolidone, etc.), aromatics (orange oil, peppermint, vanilla, cocoa, etc.), preservative agents (methyl paraoxybenzoate, propyl paraoxybenzoate, sodium benzoylbenzoate, benzalkonium chloride, etc), colorants (Red #40, Yellow #4, Green #3, Blue #1), and the like.
  • antioxidants butylparahydroxy benzoic acid, butylhydroquinone, tocopherol, etc.
  • viscosity enhancing agents sodium alginate, carboxymethylcellulose, methylcellulose, trag
  • Fig. 1 is a graph showing the concentration of an active ingredient in blood, measured at predetermined time intervals after a pharmaceutical composition of the present invention is orally administered into male rats.
  • the pharmaceutical composition for oral administration according to the present invention comprises a high concentration active ingredient with excellent bioavailability in which the concentration of the active ingredient can be easily controlled by drinking water upon oral administration.

Landscapes

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

Abstract

Composition pharmaceutique pour administration orale contenant une micro-émulsion à base de florfénicol en tant que principe actif, ladite micro-émulsion étant obtenue par ajout d'une huile et d'un tensioactif à une solution de florfénicol dans un milieu de dispersion hydrophile ou amphiphile. Ladite composition pharmaceutique pour administration orale possède une forte concentration de principe actif présentant une excellente biodisponibilité, la concentration du principe actif pouvant être facilement régulée par absorption d'eau lors de la prise orale du médicament.
PCT/KR2003/001266 2002-08-13 2003-06-27 Composition pharmaceutique pour administration orale contenant du florfenicol en tant que principe actif Ceased WO2004014341A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003244259A AU2003244259A1 (en) 2002-08-13 2003-06-27 Oral injectable pharmaceutical composition comprising florfenicol as an active ingredient

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2002-0047910 2002-08-13
KR1020020047910A KR20040015624A (ko) 2002-08-13 2002-08-13 플로르페니콜을 활성성분으로 함유하는 경구투여용약제학적 조성물

Publications (1)

Publication Number Publication Date
WO2004014341A1 true WO2004014341A1 (fr) 2004-02-19

Family

ID=31713128

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2003/001266 Ceased WO2004014341A1 (fr) 2002-08-13 2003-06-27 Composition pharmaceutique pour administration orale contenant du florfenicol en tant que principe actif

Country Status (3)

Country Link
KR (1) KR20040015624A (fr)
AU (1) AU2003244259A1 (fr)
WO (1) WO2004014341A1 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2451811A (en) * 2007-08-09 2009-02-18 Ems Sa Delivery composition for solubilising water-insoluble pharmaceutical active ingredients
FR2925335A1 (fr) * 2007-12-21 2009-06-26 Ceva Sante Animale Sa Compositions orales liquides de florfenicol diluables dans l'eau de boisson
FR2925855A1 (fr) * 2007-12-26 2009-07-03 Virbac Sa Sa Composition liquide autoemulsionnable de florfenicol destinee a etre incorporee a l'eau de boisson des animaux d'elevage.
AU2005318187B2 (en) * 2004-12-21 2010-12-16 Intervet International B.V. Injectable veterinary composition
CN106236705A (zh) * 2016-08-30 2016-12-21 瑞普（天津）生物药业有限公司 一种可用于饮水给药的氟苯尼考溶液剂及其制备方法
CN109125262A (zh) * 2018-09-11 2019-01-04 江苏农牧科技职业学院 氟苯尼考纳米乳及其制备方法
US10905759B2 (en) 2016-08-19 2021-02-02 Sementis Limited Vector-based attenuated poxvirus vaccines

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992004016A1 (fr) * 1990-08-29 1992-03-19 Schering Corporation Composition pharmaceutique de florfenicol
US5932243A (en) * 1993-05-27 1999-08-03 Novartis Ag Galenical formulations

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992004016A1 (fr) * 1990-08-29 1992-03-19 Schering Corporation Composition pharmaceutique de florfenicol
US5932243A (en) * 1993-05-27 1999-08-03 Novartis Ag Galenical formulations

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005318187B2 (en) * 2004-12-21 2010-12-16 Intervet International B.V. Injectable veterinary composition
US9278065B2 (en) 2007-08-09 2016-03-08 Ems S/A Delivery systems for solubilising water-insoluble pharmaceutical active ingredients
WO2009019604A3 (fr) * 2007-08-09 2009-07-23 Ems Sa Systèmes d'administration pour solubiliser des principes actifs pharmaceutiques insolubles dans l'eau.
US20120177692A1 (en) * 2007-08-09 2012-07-12 Ems S/A Delivery systems for solubilising water-insoluble pharmaceutical active ingredients
GB2451811A (en) * 2007-08-09 2009-02-18 Ems Sa Delivery composition for solubilising water-insoluble pharmaceutical active ingredients
FR2925335A1 (fr) * 2007-12-21 2009-06-26 Ceva Sante Animale Sa Compositions orales liquides de florfenicol diluables dans l'eau de boisson
WO2009083520A3 (fr) * 2007-12-21 2009-12-03 Ceva Sante Animale Compositions orales liquides de florfenicol diluables dans l'eau de boisson
US20110028560A1 (en) * 2007-12-26 2011-02-03 Virbac Sa Self-emulsifiable liquid florfenicol composition intended to be incorporated into the drinking water of livestock
WO2009106714A3 (fr) * 2007-12-26 2009-12-17 Virbac Sa Composition liquide autoemuls ionnable de florfeni col destinee a etre incorporee a l'eau de boisson des animaux d'elevage
WO2009106714A2 (fr) 2007-12-26 2009-09-03 Virbac Sa Composition liquide autoemuls ionnable de florfeni col destinee a etre incorporee a l'eau de boisson des animaux d'elevage
FR2925855A1 (fr) * 2007-12-26 2009-07-03 Virbac Sa Sa Composition liquide autoemulsionnable de florfenicol destinee a etre incorporee a l'eau de boisson des animaux d'elevage.
US9339460B2 (en) 2007-12-26 2016-05-17 Virbac Sa Self-emulsifiable liquid florfenicol composition intended to be incorporated into the drinking water of livestock
US10905759B2 (en) 2016-08-19 2021-02-02 Sementis Limited Vector-based attenuated poxvirus vaccines
CN106236705A (zh) * 2016-08-30 2016-12-21 瑞普（天津）生物药业有限公司 一种可用于饮水给药的氟苯尼考溶液剂及其制备方法
CN109125262A (zh) * 2018-09-11 2019-01-04 江苏农牧科技职业学院 氟苯尼考纳米乳及其制备方法
CN109125262B (zh) * 2018-09-11 2020-12-25 江苏农牧科技职业学院 氟苯尼考纳米乳及其制备方法

Also Published As

Publication number Publication date
KR20040015624A (ko) 2004-02-19
AU2003244259A1 (en) 2004-02-25

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