X-ray powder diffractometry of intact film coated tablets - An approach to monitor the physical form of the active pharmaceutical ingredient during processing and storage

Hiroyuki Yamada, Raj Suryanarayanan

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

The antiviral compound, 2-amino-6-(4-methoxyphenylthio)-9-[2- (phosphonomethoxy)ethyl]purine bis(2,2,2-trifluoroethyl)ester (MCC-478), can exist in several anhydrous polymorphic forms and also as a hemihydrate. The XRD patterns of the tablets, containing each form of the active pharmaceutical ingredient (API), revealed at least one peak unique to each form. A semiquantitative microdiffractometric method was developed to nondestructively characterize the physical form of the API in intact film-coated tablets. This was accomplished even though the weight fraction of the API was <0.2 and that of mannitol, a highly crystalline excipient, was ∼0.6. The method was used to determine the effect of aqueous film-coating process on the physical form of the API. The final dosage form was also monitored following storage at 40°C/75% RH for 6 months. There was no phase transformation of the API either due to the film-coating process or following accelerated storage. This technique has potential utility not only for process control during manufacture, but also for the quality control of the final product.

Original languageEnglish (US)
Pages (from-to)2029-2036
Number of pages8
JournalJournal of Pharmaceutical Sciences
Volume96
Issue number8
DOIs
StatePublished - Aug 2007

Bibliographical note

Funding Information:
The financial support of Mitsubishi Pharma Corporation is gratefully acknowledged. We thank Mr. Katsuyoshi Yoshizawa and Mr. Takeshi Wakasugi for their assistance.

Keywords

  • Film-coated tablet
  • Microdiffractometry
  • Penetration depth
  • Physical form
  • Process control
  • Stability

Fingerprint

Dive into the research topics of 'X-ray powder diffractometry of intact film coated tablets - An approach to monitor the physical form of the active pharmaceutical ingredient during processing and storage'. Together they form a unique fingerprint.

Cite this