WO2010058349A1 - Composition pharmaceutique pour application topique - Google Patents

Composition pharmaceutique pour application topique Download PDF

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Publication number
WO2010058349A1
WO2010058349A1 PCT/IB2009/055140 IB2009055140W WO2010058349A1 WO 2010058349 A1 WO2010058349 A1 WO 2010058349A1 IB 2009055140 W IB2009055140 W IB 2009055140W WO 2010058349 A1 WO2010058349 A1 WO 2010058349A1
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
solution
topical application
present
composition
Prior art date
Application number
PCT/IB2009/055140
Other languages
English (en)
Inventor
Todor Alexandrov Popov
Christo Tzachev Tzachev
Ivan Nedialkov Denev
Original Assignee
Fortune Apex Development Limited
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 Fortune Apex Development Limited filed Critical Fortune Apex Development Limited
Priority to US13/578,425 priority Critical patent/US9993468B2/en
Publication of WO2010058349A1 publication Critical patent/WO2010058349A1/fr
Priority to US16/005,149 priority patent/US20180289688A1/en

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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
    • 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
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants

Definitions

  • composition for topical application is provided.
  • the present invention concerns a pharmaceutical composition for topical application.
  • the present invention concerns a pharmaceutical composition which is suitable for nasal mucosa administration.
  • Aqueous pharmaceutical compositions for nasal administration comprising solutions of loratadine are disclosed in WO-A-04082589 and solutions of loratadine and desloratadineare disclosed in WO-A-03101434.
  • the nasal pharmaceutical compositions disclosed in these prior art references comprise relatively low levels of antihistamine in solution.
  • nasal pharmaceutical compositions which may comprise relatively higher amounts of antihistamine in solution than the prior art solutions but which do not demonstrate increased mucosa irritation.
  • a pharmaceutical composition comprising an aqueous solution having a pH of from 5 to 7.5, preferably from 5 to 7, comprising:
  • Lutrol is a trademark of BASF SE.
  • the pharmaceutical composition comprises an aqueous solution having a pH from 5 to 7.5 comprising:
  • a particularly preferred pharmaceutical composition of this embodiment comprises an aqueous solution having a pH from 5 to 7 comprising:
  • the pharmaceutical composition comprises an aqueous solution having a pH from 5 to 7.5 comprising:
  • a particularly preferred pharmaceutical composition of this embodiment comprises an aqueous solution having a pH from 5 to 7 comprising:
  • compositions of the present invention contain higher dosage levels of antihistamine in solution but overall lower dosages of potential irritants.
  • component b) was eliminated, higher levels of component c) would be required to solubilise the antihistamine, and visa- versa: higher levels of b) or c) on their own in the composition causes irritation on the nasal mucosa, which in turn leads to a reduction the time the composition may be effective.
  • component d) was eliminated, higher levels of component e) would be required to solubilise the antihistamine, and visa- versa: higher levels of d) or e) on their own in the composition causes irritation on the nasal mucosa, which in turn leads to a reduction the time the composition may be effective.
  • the pharmaceutical composition of the present invention may contain, in addition to co- solvents b) and c), one or more other co-solvents, such as sorbitol and glycerine, but such co-solvents should be used at non- irritating levels.
  • the pharmaceutical composition of the present invention may contain, in addition to co- solubilizers b) and c), one or more other co-solubilizers, but such co-solubilizers should be used at non-irritating levels.
  • the stabilizer is preferably a chelator for the antihistamine.
  • the aqueous solution may require pH adjustment to the range 5 to 7.5, preferably 5 to 7. This can be achieved readily by a person skilled in the art. For example, if the pH of the solution is lower than 5, then the pH may be raised by the incorporation of an appropriate amount of alkali, such as NaOH solution.
  • the pharmaceutical composition is especially suitable for nasal administration, for example for the treatment of allergic rhinitis, though it may also be suitable for ocular administration, for example for the relief of allergic conjunctivitis.
  • the invention in its various embodiments shall now be further described by way of exemplification only:
  • a pharmaceutical composition according to the present invention was prepared as follows:
  • Solution C is adjusted as necessary to pH 5,5 with IM solution of Sodium Hydroxide and is complemented to a total of 100 parts w/w with purified water to obtain the final composition.
  • composition is as shown in Table 1.
  • the pharmaceutical composition has the characteristics shown in Table 2:

Landscapes

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

Abstract

Une composition pharmaceutique inclut une solution de pH compris entre 5 et 7,5, qui comprend de la loratadine et/ou de la desloratadine. La composition est adaptée au traitement de, par exemple, la rhinite allergique ou la conjonctivite allergique.
PCT/IB2009/055140 2008-11-21 2009-11-18 Composition pharmaceutique pour application topique WO2010058349A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US13/578,425 US9993468B2 (en) 2008-11-21 2009-11-18 Pharmaceutical composition for topical application
US16/005,149 US20180289688A1 (en) 2008-11-21 2018-06-11 Pharmaceutical composition for topical application

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0821298A GB2465746B (en) 2008-11-21 2008-11-21 Pharmaceutical composition for topical application
GB0821298.7 2008-11-21

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/578,425 A-371-Of-International US9993468B2 (en) 2008-11-21 2009-11-18 Pharmaceutical composition for topical application
US16/005,149 Continuation US20180289688A1 (en) 2008-11-21 2018-06-11 Pharmaceutical composition for topical application

Publications (1)

Publication Number Publication Date
WO2010058349A1 true WO2010058349A1 (fr) 2010-05-27

Family

ID=40230623

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2009/055140 WO2010058349A1 (fr) 2008-11-21 2009-11-18 Composition pharmaceutique pour application topique

Country Status (3)

Country Link
US (2) US9993468B2 (fr)
GB (1) GB2465746B (fr)
WO (1) WO2010058349A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003101434A2 (fr) 2001-12-21 2003-12-11 Sampad Bhattacharya Compositions pharmaceutiques intranasales comprenant un antihistaminique et un inhibiteur de leucotrienes
WO2004082589A2 (fr) 2003-03-20 2004-09-30 Ranbaxy Laboratories Limited Composition pharmaceutique biodisponible de loratadine a administration nasale
US20070048384A1 (en) * 2005-08-26 2007-03-01 Joerg Rosenberg Pharmaceutical compositions
US20070207201A1 (en) * 2006-03-06 2007-09-06 Wyeth Liquid and Semi-Solid Pharmaceutical Formulations and Processes

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4776229B2 (ja) * 2002-07-16 2011-09-21 エラン ファーマ インターナショナル，リミティド 安定なナノ粒子活性物質の液体投与組成物
US7758877B2 (en) * 2004-02-05 2010-07-20 Taro Pharmaceuticals U.S.A., Inc. Stable loratadine spill resistant formulation
WO2006069213A1 (fr) * 2004-12-22 2006-06-29 Schering Corporation Preparations pharmaceutiques
WO2007143382A2 (fr) 2006-06-07 2007-12-13 Morton Grove Pharmaceuticals, Inc. Formulations de loratadine liquide pour voie orale et procédés
GB0625322D0 (en) * 2006-12-19 2007-01-24 Pharmakodex Ltd Pharmaceutical compositions
BRPI0809164B8 (pt) * 2007-03-22 2023-02-28 Berg Llc Composição para administração tópica e composição farmacêutica compreendendo a referida composição
JP2012505236A (ja) * 2008-10-10 2012-03-01 シェーリング コーポレイション コルチコステロイド組成物およびそれの治療方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003101434A2 (fr) 2001-12-21 2003-12-11 Sampad Bhattacharya Compositions pharmaceutiques intranasales comprenant un antihistaminique et un inhibiteur de leucotrienes
WO2004082589A2 (fr) 2003-03-20 2004-09-30 Ranbaxy Laboratories Limited Composition pharmaceutique biodisponible de loratadine a administration nasale
US20070048384A1 (en) * 2005-08-26 2007-03-01 Joerg Rosenberg Pharmaceutical compositions
US20070207201A1 (en) * 2006-03-06 2007-09-06 Wyeth Liquid and Semi-Solid Pharmaceutical Formulations and Processes

Also Published As

Publication number Publication date
GB2465746B (en) 2011-02-16
GB0821298D0 (en) 2008-12-31
US9993468B2 (en) 2018-06-12
US20140088134A1 (en) 2014-03-27
US20180289688A1 (en) 2018-10-11
GB2465746A (en) 2010-06-02

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