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CA2258679A1 - Solid solution of an antifungal agent with enhanced bioavailability - Google Patents

Solid solution of an antifungal agent with enhanced bioavailability

Info

Publication number
CA2258679A1
CA2258679A1 CA002258679A CA2258679A CA2258679A1 CA 2258679 A1 CA2258679 A1 CA 2258679A1 CA 002258679 A CA002258679 A CA 002258679A CA 2258679 A CA2258679 A CA 2258679A CA 2258679 A1 CA2258679 A1 CA 2258679A1
Authority
CA
Canada
Prior art keywords
solid solution
antifungal agent
enhanced bioavailability
formula
compound
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.)
Granted
Application number
CA002258679A
Other languages
French (fr)
Other versions
CA2258679C (en
Inventor
Surendra A. Sangekar
Ping I. Lee
Winston A. Vadino
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.)
Merck Sharp and Dohme LLC
Original Assignee
Individual
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 Individual filed Critical Individual
Priority claimed from PCT/US1997/010120 external-priority patent/WO1998000113A1/en
Publication of CA2258679A1 publication Critical patent/CA2258679A1/en
Application granted granted Critical
Publication of CA2258679C publication Critical patent/CA2258679C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

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
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds

Landscapes

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

Abstract

A pharmaceutical composition in the form of a substantially amorphous solid solution comprising an antifungal compound of formula (I), wherein X is F; and R1 is formula (1) or an ester or ether of said compound of formula (I); and a soluble or insoluble polymer such as:
povidone or crospovidone, wherein the ratio of said compound to said polymer is about 1:3 to about 1:6 is disclosed.
CA002258679A 1996-06-28 1997-06-25 Solid solution of an antifungal agent with enhanced bioavailability Expired - Fee Related CA2258679C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US67270696A 1996-06-28 1996-06-28
US08/672,706 1996-06-28
PCT/US1997/010120 WO1998000113A1 (en) 1996-06-28 1997-06-25 Solid solution of an antifungal agent with enhanced bioavailability

Publications (2)

Publication Number Publication Date
CA2258679A1 true CA2258679A1 (en) 1998-01-08
CA2258679C CA2258679C (en) 2007-05-29

Family

ID=38151061

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002258679A Expired - Fee Related CA2258679C (en) 1996-06-28 1997-06-25 Solid solution of an antifungal agent with enhanced bioavailability

Country Status (1)

Country Link
CA (1) CA2258679C (en)

Also Published As

Publication number Publication date
CA2258679C (en) 2007-05-29

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Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed