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WO2008147169A2 - Microémulsion contenant de la pirfénidone - Google Patents

Microémulsion contenant de la pirfénidone Download PDF

Info

Publication number
WO2008147169A2
WO2008147169A2 PCT/MX2008/000068 MX2008000068W WO2008147169A2 WO 2008147169 A2 WO2008147169 A2 WO 2008147169A2 MX 2008000068 W MX2008000068 W MX 2008000068W WO 2008147169 A2 WO2008147169 A2 WO 2008147169A2
Authority
WO
WIPO (PCT)
Prior art keywords
composition
weight
unit dose
pirfenidone
soft gelatin
Prior art date
Application number
PCT/MX2008/000068
Other languages
English (en)
Spanish (es)
Other versions
WO2008147169A8 (fr
WO2008147169A3 (fr
Inventor
Laura Vásquez Cervantes
Original Assignee
Cell Therapy Technology, S.A. De C.V.
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 Cell Therapy Technology, S.A. De C.V. filed Critical Cell Therapy Technology, S.A. De C.V.
Publication of WO2008147169A2 publication Critical patent/WO2008147169A2/fr
Publication of WO2008147169A3 publication Critical patent/WO2008147169A3/fr
Publication of WO2008147169A8 publication Critical patent/WO2008147169A8/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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • 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 formulation containing pirfenidone, which is prepared in a microemulsion that offers advantages over other oral administration pharmaceutical forms known in the state of the art, such as tablets, capsules, suspensions and solutions.
  • Pirfenidone is itself a known compound and its pharmacological effects have been described in, for example, Japanese applications KOKAI Nos. 87677/1974 and 1284338/1976, as an anti ⁇ inflammatory agent that includes anti -Pyretic and analgesic, United States patents Nos. 3,839,346, published on October 1, 1974, 3,974,281, published on August 10, 1976, 4,042,699, published on August 16, 1977, and 4,052,509, published on October 4, 1911, describe methods for obtaining Pirfenidone, thus as its use as an anti ⁇ inflammatory agent.
  • Mexican patent 182,266 describes the anti-fibrotic activity of 5-methyl-l-phenyl- (IH) -pyridone.
  • Pirfenidone has demonstrated its effectiveness as an anti-fibrotic agent, in different pathologies and organs, as it has been shown in previous studies, where we have observed an effect on fibroblasts and collagen produced by them, both in experimental models and in clinical trials
  • Soft gelatin capsules are used in the pharmaceutical, cosmetic, nutritional and veterinary industry. This diversity demonstrates the versatility of the soft gelatin capsule, the content within a soft gelatin capsule can be a liquid, semi-solid mixtures, non-aqueous solutions or suspensions, all this due to the water-soluble nature of the gelatin.
  • Soft gelatin capsules are containers or unit packages, consisting of two soft gelatin films, which contain the active ingredient among them. The soft gelatin capsule can Prepare in various shapes and sizes depending on the design needs of the medication. The advantages offered by soft gelatin capsules over other oral administration pharmaceutical forms are:
  • - can be used as a means of oral, rectal, vaginal and ophthalmic administration
  • the accuracy of filling is 1 to 2.5% depending on the asset to be filled; - they have elegant, bright and striking appearance of the finished product;
  • - can be manufactured in different colors and sizes, thus responding to the administration needs of the medicament or design, being able to be manufactured transparent or colorful, with solid colors, natural transparency, solid colors in combination of two tones, transparent in two tones, polished or matte finishes.
  • microemulsions differ from the emulsions by the fact that the former spontaneously forms r whereby a minimum free energy state of a single phase corresponds to them.
  • Emulsions require the addition of energy (mechanical and / or heat) for their formulation. It follows that the interfacial tension between the continuous and dispersed phases in the microemulsion is low.
  • micro droplet emulsions also called mini emulsions
  • Micro emulsions are always stable to these changes.
  • the easiest way to differentiate between micro emulsions and emulsions with micro droplets is to use repeated cycles of freezing and heating in both systems.
  • the micro emulsion will return to its original state of stability, - since its restoration is controlled by diffusion while the emulsion is separated into the original components that gave rise to it.
  • Soft gelatin capsules are made from the following components: gelatin between 38% and 42% preferably between 39% and 40% and more preferably between 39.9 and 40% by weight of the composition, purified water between 38% and 42% preferably between 39% and 40% and more preferably between 39.9 and 40% by weight of the composition, glycerin between 18% and 22% preferably between 19% and 20% and more preferably between 19.5 and 20% in weight of the composition, at least one conservative between 0.15% and 0.20% preferably between 0.16% and 0.19% and more preferably between 17 and 18% by weight of the composition, titanium dioxide between 0.25% and 0.30% preferably between 0.27% and 0.29% and more preferably between 0.28 and 0.29% by weight of the composition and a dye ⁇ yellow color No. 10 FDC) between 0.0095% and 0.015% preferably between 0.0097 and 0.013% and more preferably between 0.0099 and 0.011% by weight of the composition .
  • An example of bark composition of jelly is shown in table 1:
  • a second composition can be prepared from the components shown in Table 2:
  • compositions are shown by way of examples, but are not limited in any way to the scope of the description of the present invention.
  • the microemulsifiable composition of Pirfenidone object of the present invention further comprises; alcohol absolute ethyl, dl-alpha tocophexol acetate, Pluracol E-400, Cremophor RH-40 and Amaranth Oil.
  • pirfenidone is present in an amount between 8.58% and 10.38% by weight of the composition, absolute ethyl alcohol in an amount between 6.92% and 15.57%, di-alpha tocopherol acetate in an amount between 12.58% and 28.30%, pluracol E-400 in an amount between 9.43% and 21.23%, Cremophor RH-40 in an amount between 25.16% and 56.60% and Amaranth Oil in an amount between 6.29% and 14.15%.
  • compositions are shown by way of examples but are not limited in any way to the scope of the description of the present invention.

Landscapes

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

Abstract

La présente invention concerne une composition microémulsionnable de Pirfénidone, qui présente des avantages par rapport à d'autres formes pharmaceutiques à administrer par voie orale connues dans l'état de la technique, comme des comprimés, capsules, suspensions et solutions.
PCT/MX2008/000068 2007-05-29 2008-05-29 Microémulsion contenant de la pirfénidone WO2008147169A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
MX2007006438 2007-05-29
MXMX/A/2007/006348 2007-05-29

Publications (3)

Publication Number Publication Date
WO2008147169A2 true WO2008147169A2 (fr) 2008-12-04
WO2008147169A3 WO2008147169A3 (fr) 2009-01-22
WO2008147169A8 WO2008147169A8 (fr) 2009-07-30

Family

ID=40075678

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/MX2008/000068 WO2008147169A2 (fr) 2007-05-29 2008-05-29 Microémulsion contenant de la pirfénidone

Country Status (1)

Country Link
WO (1) WO2008147169A2 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102846555A (zh) * 2012-04-09 2013-01-02 珠海亿邦制药股份有限公司 一种以吡非尼酮为活性成分的固体制剂及其应用
US8969347B2 (en) 2008-06-03 2015-03-03 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
US9675593B2 (en) 2012-10-02 2017-06-13 Intermune, Inc. Anti-fibrotic pyridinones
US10233195B2 (en) 2014-04-02 2019-03-19 Intermune, Inc. Anti-fibrotic pyridinones

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000016775A1 (fr) * 1998-09-18 2000-03-30 Mepha Ag Formulation topique a base d'alkyl-, phenyl-pyridone
WO2004058256A1 (fr) * 2002-12-26 2004-07-15 Kdl, Inc. Composition pharmaceutique liquide contenant un derive de pyridone
US20060039931A1 (en) * 2002-09-13 2006-02-23 Mepha Ag Stable cream preparations of phenyl-pyridone compounds for topical application
WO2007038315A2 (fr) * 2005-09-22 2007-04-05 Intermune, Inc. Formule de capsules de pirfenidone et excipients pharmacocompatibles

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000016775A1 (fr) * 1998-09-18 2000-03-30 Mepha Ag Formulation topique a base d'alkyl-, phenyl-pyridone
US20060039931A1 (en) * 2002-09-13 2006-02-23 Mepha Ag Stable cream preparations of phenyl-pyridone compounds for topical application
WO2004058256A1 (fr) * 2002-12-26 2004-07-15 Kdl, Inc. Composition pharmaceutique liquide contenant un derive de pyridone
WO2007038315A2 (fr) * 2005-09-22 2007-04-05 Intermune, Inc. Formule de capsules de pirfenidone et excipients pharmacocompatibles

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
GARCIA SANCHEZ M.J. ET AL.: 'Monografias Galenicas, Formas orales solidas (I)' LABORATORIOS GLAXO 1993, pages 22 - 30 *

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8969347B2 (en) 2008-06-03 2015-03-03 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
USRE47142E1 (en) 2008-06-03 2018-11-27 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
CN102846555A (zh) * 2012-04-09 2013-01-02 珠海亿邦制药股份有限公司 一种以吡非尼酮为活性成分的固体制剂及其应用
US9675593B2 (en) 2012-10-02 2017-06-13 Intermune, Inc. Anti-fibrotic pyridinones
US10376497B2 (en) 2012-10-02 2019-08-13 Intermune, Inc. Anti-fibrotic pyridinones
US10898474B2 (en) 2012-10-02 2021-01-26 Intermune, Inc. Anti-fibrotic pyridinones
US10233195B2 (en) 2014-04-02 2019-03-19 Intermune, Inc. Anti-fibrotic pyridinones
US10544161B2 (en) 2014-04-02 2020-01-28 Intermune, Inc. Anti-fibrotic pyridinones

Also Published As

Publication number Publication date
WO2008147169A8 (fr) 2009-07-30
WO2008147169A3 (fr) 2009-01-22

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