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A radiopharmaceutical may be a
radioactive element such as 133Xe, or a
labeled compound such as 131I-iodinated
proteinsand 99mTc-labeled compounds.
In designing a radiopharmaceutical, a
pharmaceutical is first chosen on the
basis of its preferential localization in a
given organ or its participation in the
physiologic function of the organ.
1. Easy Availability
A radionuclide decays with a definite halflife, which is called the physical half-life,
denoted Tp (or t1=2).
e = p + b
Since = 0.693/t1/2, it follows that
1/Te = 1/Tp + 1/Tb
OR
Te
=(
Tp X Tb) / ( Tp + Tb )
Problem 6.1
The physical half-life of 111In is 67 hr and the biologic half-life of
111In-DTPA
used for measurement of the glomerular filtration rate is 1.5 hr.
What is the
eective half-life of 111In-DTPA?
Answer
Using Eq. (6.3),
Te
1:5 67
67 1:5
100:5
68:5
1:47 hr
Radiopharmaceuticals
3. Particle Emission
:.
3.
Once a radiopharmaceutical is
conceptually designed, a definite protocol
should be developed based on the
physicochemical properties of the basic
ingredientsto prepare the
radiopharmaceutical.
In the medical field, compounds labeled with emitting radionuclides are mainly restricted to in
vitro experiments and therapeutic treatment,
whereas those labeled with emitting
radionuclides have much wider applications.
Denaturation or Alteration
Isotope Effect
Carrier-Free or No-Carrier-Added
(NCA) State
Radiopharmaceuticals tend to be
adsorbed on the inner walls of the
containers if they are in a carrierfree or NCA state.
Techniques have to be
developed in which the labeling yield
is not afected by the low
concentration of the tracer in a
carrier-free or NCA state.
Storage Conditions
Specific Activity
Radiolysis
Radiolysis
( cont,)
(cont,..)
Shelf Life
In
Nucleophilic substitution:
Electrophilic substitution:
The labeling yield is not very high, but the method allows
iodination without alteration of protein molecules whose
tyrosine moieties are susceptible to alteration, although
in vivo dehalogenation is encountered in some instances.
Furthermore, 99mTc is readily available in a sterile, pyrogenfree, and carrier-free state from 99Mo99mTc generators.