Analytical, Characterization, and Stability Studies of Organic Chemical, Drugs, and Drug Formulation

Abstract

Although the overall purpose of this contract was to perform chemical/physical analyses on bulk pharmaceutical substances and formulated drug products of interest to the USAMRMC Drug Development Program for applications such as treatment of parasitic and infectious diseases and chemical/biological defense, the majority of time and effort during the first year was expended to select, award, and monitor three subcontractors to produce a second and larger batch of current good manufacturing practices (cGMP) artesunic acid (AS) IV drug product. As a part of the cGMP manufacture, a program of stability studies was maintained over the entire contract period to ensure the continued integrity of the drug in its clinical use. Because our manufacturing process involves batch API sterilization with ethylene oxide, a procedure that does not lend itself to large-scale manufacturing, we studied the feasibility of lyophilization of AS in t-butanol, a process that involves easy sterile filtration, precise unit vial filling, lyophilization, and facile automation. We demonstrated the method in principle, but were unable to remove the residual t-butanol to <0.5%. With additional research using more sophisticated equipment, an acceptable AS lyo product should be possible. A modest synthesis program was carried out at the request of our COR. We prepared and fully characterized four very-highpurity 1,2,4-triazolidine derivatives and one high-purity quinazoline derivative. All were submitted to the COR. In addition to the above activities, the core project team continued to serve all areas of the Army by performing chemical analyses when required. Reports on these analyses were submitted to the COR. Drug substances studied include paromomycin and gentamicin, pentostam, and 17 -ethynlestradiol-3-sulfate, sodium.

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Document Details

Document Type
Technical Report
Publication Date
May 21, 2014
Accession Number
ADA601351

Entities

People

  • Peter Lim

Organizations

  • SRI International

Tags

DTIC Thesaurus Topics

  • 2-Ring Heterocyclic Compounds
  • Alkenes
  • Automation
  • Biomedical Research
  • Chemical Analysis
  • Contractors
  • Contracts
  • Diseases And Disorders
  • Ethylene Oxide
  • Ethylenes
  • Freeze Drying
  • Infectious Diseases
  • Magnetic Resonance
  • Nuclear Magnetic Resonance
  • Oxides
  • Residuals
  • Sterilization

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  • Parasitology and Pharmacology of Malaria.
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