Search International and National Patent Collections
Some content of this application is unavailable at the moment.
If this situation persists, please contact us atFeedback&Contact
1. (EP0561883) POLYMORPHS OF CRYSTALLINE MUPIROCIN
Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters
Claims

1. A crystalline mupirocin polymorph (FORM III) having a melting point in the range 82.5-86°C and characterised by an X-ray powder diffractogram substantially as shown in accompanying Fig.3.
  2. A crystalline mupirocin polymorph according to claim 1 further characterised by an IR spectrum substantially as shown in accompanying Fig.6.
  3. A process for preparing a crystalline mupirocin polymorph (FORM III) as defined in claim 1 which comprises recrystallizing mupirocin from a solution of mupirocin in an organic solvent (or solvent mixture) while maintaining the temperature at 40°C or above.
  4. A process according to claim 3 in which the organic solvent has a water content of less than 0.1% w/v.
  5. A process according to claim 3 or 4 in which the initially formed crystalline precipitate is stirred while maintaining the temperature at 40°C or above until the crystalline precipitate is substantially all FORM III.
  6. A mixture of mupirocin polymorphs that contains at least 90% by weight of the polymorph of claim 1.
  7. A pharmaceutical or veterinary composition comprising the mupirocin polymorph of claim 1 or a polymorph mixture of claim 6 together with a pharmaceutically or veterinarially acceptable carrier.
  8. A composition according to claim 7 comprising from 1 to 3% of mupirocin polymorph, from 65 to 96% of white soft paraffin, from 0 to 15% of liquid paraffin and from 3 to 7% of lanolin or a derivative or synthetic equivalent thereof.
  9. A composition according to claim 7 comprising from 1 to 3% of mupirocin polymorph, from 25 to 60% of liquid paraffin, from 20 to 50% of water and from 3 to 30% of emulsifier.
  10. A mupirocin polymorph or polymorph mixture as defined in claim 1 or 7 for use in therapy.
  11. The use of a mupirocin polymorph or polymorph mixture as defined in of claim 1 or 7, for the manufacture of a medicament for the treatment of infections.
  12. A veterinarily acceptable premix formulation comprising a mupirocin polymorph or polymorph mixture as defined in claim 1 or 7 in association with a veterinarily acceptable carrier.
 

Claims

1. A process for preparing a crystalline mupirocin polymorph (FORM III) which comprises recrystallizing mupirocin from a solution of mupirocin in an organic solvent (or solvent mixture) while maintaining the temperature at 40°C or above.
  2. A process according to claim 1 in which the organic solvent has a water content of less than 0.1% w/v.
  3. A process according to claim 1 or 2 in which the initially formed crystalline precipitate is stirred while maintaining the temperature at 40°C or above until the crystalline precepitate is substantially all FORM III.
  4. A process according to any one of claims 1,2 or 3 in which the product is a crystalline mupirocin polymorph (FORM III) having a melting point in the range 82.5-86°C and characterised by an X-ray powder diffractogram substantially as shown in accompanying Fig.3.
  5. A process according to claim 4 in which the product is further charactersied by an IR spectrum substantially as shown in accompanying Fig.6.
  6. The use of a mupirocin polymorph which is crystalline mupirocin polymorph (FORM III) having a melting point in the range 82.5-86°C and characterised by an X-ray powder diffractogram substantially as shown in accompanying Figure 3 for the manufacture of a medicament for the treatment of infections, in particular bacterial and fungal infections.
  7. A process for preparing a pharmaceutical or veterinary composition which process comprises admixing a crystalline mupirocin polymorph as defined in any one of the preceeding claims with a pharmaceutically or veterinarily acceptable carrier or excipient.
  8. A process according to claim 7 in which the composition has from 1 to 3% of mupirocin polymorph, from 65 to 96% of white soft paraffin, from 0 to 15% of liquid paraffin and from 3 to 7% of lanolin or a derivative or synthetic equivalent thereof.
  9. A process according to claim 7 in which the composition has from 1 to 3% of mupirocin polymorph, from 25 to 60% of liquid paraffin, from 20 to 50% of water and from 3 to 30% of emulsifier.
  10. A process for preparing a veterinarily acceptable premix formulation which process comprises admixing a mupirocin polymorph or polymorph as defined in any one of claims 1 to 5 with a veterinarily acceptable carrier.