title: Formulation and evaluation of a single vial lyophilized preparation of technetium-99m labeled ethylene dicysteine as a renal scintigraphic agent.
abstract: (99m)Tc labeled N-N-ethylene-L, L-dicysteine (EC) was introduced in form of multiple-step kit as an alternate renal imaging radiopharmaceutical for commonly used (99m)Tc-MAG3. We developed a single component lyophilized kit of EC ready to be labeled with (99m)Tc. We present the optimization of the components of our formulation, its evaluation in animal models, normal human volunteers and patients of various renal diseases, in comparison with (99m)Tc-MAG3. Efficient labeling of EC was achieved with our preparation at pH 7 to 12. The formulation at pH 8 was used further for bio distribution studies in organs of sacrificed Sprague Dawley rats and a live rhesus monkey using scintigraphy. After satisfactory bio-distribution results, the kit was then evaluated in normal human volunteers through renography. But the renogram parameters of (99m)Tc-EC (pH 8) were statistically inferior to (99m)Tc-MAG3. Surrogate kit at pH 10 was therefore developed and re-evaluated in rats for organ bio distribution. After favorable results the kit was then assessed further in normal volunteers and a group of patients with various renal disorders via scintigraphy. The EC kit developed at pH 10 gave images better than and scintigraphic parameters comparable to (99m)Tc-MAG3. It was concluded that single vial kit we formulated easy to prepare than three-vial kit and can be used as an alternate to (99m)Tc-MAG3.
authors.affiliation: Department of Medical Sciences, Pakistan Institute of Engineering and Applied Sciences, Islamabad, Pakistan.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Sohaib
authors.affiliation: PAEC General Hospital, Islamabad, Pakistan.
authors.forename: Anjum
authors.initials: A
authors.lastname: Afshan
authors.affiliation: Department of Medical Sciences, Pakistan Institute of Engineering and Applied Sciences, Islamabad, Pakistan.
authors.forename: Shabana
authors.initials: S
authors.lastname: Saeed
authors.affiliation: Nuclear Medical Centre, Armed Forces Institute of Pathology, Rawalpindi, Pakistan.
authors.forename: Mujahid Ali
authors.initials: MA
authors.lastname: Khalid
authors.affiliation: Department of Medical Sciences, Pakistan Institute of Engineering and Applied Sciences, Islamabad, Pakistan.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Yousuf
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D003545:Cysteine / Q000031:analogs & derivatives*; D005612:Freeze Drying; D006863:Hydrogen-Ion Concentration; D007668:Kidney / Q000000981:diagnostic imaging*; D008253:Macaca mulatta; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals; D051381:Rats; D017207:Rats, Sprague-Dawley; D013667:Technetium; D017263:Technetium Tc 99m Mertiatide
chemical_list: D019275:Radiopharmaceuticals; C109063:ethylene dicysteine; D017263:Technetium Tc 99m Mertiatide; D013667:Technetium; D003545:Cysteine