[Preparation of dealcholized onetaxotere®, docetaxel injection formulation and its pharmacokinetics in rats]

Gan To Kagaku Ryoho. 2013 Jul;40(7):891-6.
[Article in Japanese]

Abstract

Onetaxotere®(OTAX)injection, which is a docetaxel(DOC)injection formulation, cannot be administered to those patients with alcohol intolerance or hypersensitivity, because it contains ethanol as a dissolving agent. To broaden treatment options for those patients, we tried to eliminate ethanol from OTAX injection. Under sterile conditions, dealcoholization was carried out using nitrogen gas in a hot water bath at 50°C. By this method, the ethanol included in OTAX injection was almost completely removed and DOC in the formulation was stable for 28 days. When the dealcoholized or untreated OTAX injection was intravenously injected in rats, no significant differences in the pharmacokinetic parameters of DOC were observed between those with dealcoholized and untreated OTAX injections. It is expected that dealcoholized OTAX may be useful in patients with alcohol-related difficulties.

MeSH terms

  • Animals
  • Docetaxel
  • Dosage Forms*
  • Drug Stability
  • Ethanol
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Taxoids / administration & dosage
  • Taxoids / blood*
  • Taxoids / chemistry

Substances

  • Dosage Forms
  • Taxoids
  • Docetaxel
  • Ethanol