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Process for the preparation of cefuroxime axetil in an amorphous form

Patent 6060599 Issued on May 9, 2000. Estimated Expiration Date: Icon_subject June 17, 2018. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

Cephalosporin antibiotics
Patent #: 4267320
Issued on: 05/12/1981
Inventor: Gregson ,   et al.

Amorphous form of cefuroxime ester
Patent #: 4562181
Issued on: 12/31/1985
Inventor: Crisp ,   et al.

Preparation of a highly pure, substantially amorphous form of cefuroxime axetil
Patent #: 4820833
Issued on: 04/11/1989
Inventor: Crisp ,   et al.

Process for preparation of cefuroxime ester
Patent #: 4994567
Issued on: 02/19/1991
Inventor: Crisp, et al.

Process for preparing cefuroxime axetil
Patent #: 5013833
Issued on: 05/07/1991
Inventor: Crisp, et al.

Process for converting crystalline erythromycin ethylsuccinate into stable amorphous erythromycin ethylsuccinate
Patent #: 5118799
Issued on: 06/02/1992
Inventor: Rossignol

Methods for the manufacture of amorphous cefuroxime axetil Patent #: 5847118
Issued on: 12/08/1998
Inventor: Karimian, et al.

Inventors

Application

No. 098513 filed on 06/17/1998

US Classes:

540/222Additional hetero ring containing

Examiners

Primary: Berch, Mark L.

Attorney, Agent or Firm

Foreign Patent References

  • 98/43980 WO. 10/13/1998

International Class

C07D 501/02

Foreign Application Priority Data

1997-09-29 IN

Abstract

A process for preparing cefuroxime axetil in substantially amorphous form comprises forming a mixture of crystalline cefuroxime axetil and at least one pharmaceutically acceptable excipient, and subjecting the mixture to milling for a period of time sufficient to convert the crystalline cefuroxime axetil to substantially amorphous form, i.e., the crystallinity is less than 5%. The amorphous cefuroxime axetil has a chemical purity of at least 95%. Desirably, the particles of the milled material are reduced to a size of less than 2 μm. The amorphous cefuroxime axetil prepared by this method may consist of R isomer, S isomer, or a racemic mixture of the R and S isomers.

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