Radiolabeling, quality control and kit formulation of a new Tc-99m-labeled antibiotic: Tc-99m-doxycycline hyclate


ILEM-OZDEMIR D. , AŞIKOĞLU M. , ÖZKILIÇ H.

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, cilt.298, ss.1635-1642, 2013 (SCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 298 Konu: 3
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1007/s10967-013-2547-2
  • Dergi Adı: JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • Sayfa Sayıları: ss.1635-1642

Özet

Since radiolabeled antibiotics specifically bind to the bacterial components they are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline hyclate (DOX) was chosen to investigate as a new radiolabeled antibacterial agent since its bacteriostatic activity against a wide variety of microorganisms. The aim of the present study is to develop simple and easy formulation of DOX with Tc-99m ready to use kit. Tc-99m-DOX was developed and standardized under varying conditions of reducing and antioxidant agent concentration, pH, radioactivity dose and reducing agent type. Labeling studies were performed by changing the selected parameters one by one and optimum labeling conditions were determined. After observing the conditions for maximum labeling efficiency and stability, lyophilized freeze dry kits were prepared accordingly. Radiochemical purity was determined with RTLC and RHPLC which was found more than > 95 %. Two different freeze dry kits were formulated with optimum labeling conditions. The improved kits were found stable up to 6 months.