Characterization of the role of physicochemical factors on the hydrolysis of dipyrone

Ergun H., Frattarelli D., Aranda J.

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, cilt.35, sa.3, ss.479-487, 2004 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 35 Sayı: 3
  • Basım Tarihi: 2004
  • Doi Numarası: 10.1016/j.jpba.2004.02.004
  • Dergi Adı: JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.479-487
  • Anahtar Kelimeler: dipyrone, hydrolysis, HPLC, 4-methylaminoantipyrine, COLIC PAIN, METAMIZOL, METABOLITES, INVOLVEMENT, DRUGS
  • Ankara Üniversitesi Adresli: Evet

Özet

Dipyrone is a prodrug which is used mainly for its analgesic and antipyretic effects. After oral intake, dipyrone is rapidly hydrolyzed to its main metabolite, 4-methylaminoantipyrine (4-MAA), from which many other metabolites are produced by enzymatic reactions. Even though it is well known that dipyrone is a prodrug and hydrolyzed non-enzymatically, in most of the studies of dipyrone the prodrug form is tested using in vitro methodologies, which do not represent or predict the actual in vivo activity of dipyrone. In this study, we characterize the hydrolysis kinetics of dipyrone as functions of concentration, temperature, and pH using a HPLC assay.