Radio-Pharmaceuticals – Pharmaceutical Inorganic Chemistry B. Pharma 1st Semester

Radio-Pharmaceuticals

Contents

• Radioactivity

• Alpha radiation

• Beta rays

• Gamma rays

• Geiger-Muller counter method

• Scintillation counter method

• Biological Effects of Radiation

• Storage of Radio Active Material

• Handling Radio Active Materials

• Application of Radiopharmaceuticals

Learning
Objectives

At the end of this
lecture, student will be able to

• Explain the basic concept of radio activity

• Differentiate alpha,beta and gamma rays

• Describe the instruments used to measure radio activity

• Explain the principle involved in the working of
instruments used to measure radio activity

• Choose a method for handling and storing radioactive
material

• Indicate the clinical application of radiopharmaceuticals

Radioactivity

• The spontaneous emission of radiations by atomic nuclei
resulting in their integration is called natural radioactivity

Types

• Alpha rays

• Beta rays

• Gamma rays

Properties
of Radiations

Alpha Rays

Beta Rays

Gamma Rays

Helium atoms with a mass of four a.m.u. and with two positive charge

Highly energetic electrons

Neutral

Penetrating power is less

100 times more than alpha rays

Penetrating power is immensely high

Highest ionizing power

100 time less than alpha rays

No ionizing power

Key Words

• Z = The Atomic Number.

• It’s the Number of Protons in the nucleus of an Atom.

• Nucleus: It’s where the Protons and Neutrons are located
in an Atom.

• Protons: Positively Charged Particles in the Nucleus of
the atom. Mass = (approx) 1 AMU

• Neutrons: Neutrally charged particles in the nucleus of an
atom Mass = (approx) 1 AMU

• Mass Number of an atom: Number of Protons + Number of Neutrons
in the nucleus of an atom

Sources of
Radioactivity

• Naturally Occurring
Sources:

– Radon from the decay of Uranium and Thorium

– Potassium -40 – found in minerals and in plants

– Carbon 14 – Found in Plants and Animal tissue

• Manmade Sources:

– Medical use of Radioactive Isotopes

– Certain Consumer products –(eg Smoke detectors)

– Fallout from nuclear testing

– Emissions from Nuclear Power plants

Stable
Isotopes

• The nucleus of each atom contains protons and neutrons.

• While the number of protons defines the element (e.g.,
hydrogen, carbon, etc.)

• The sum of the protons and neutrons gives the atomic mass,
the number of neutrons defines the isotope of that element.

• For example, most carbon (≈ 99 %) has 6 protons and 6
neutrons and is written as 12C to reflect its atomic mass.

• However, about 1 % of the carbon in the Earth’s biosphere
has 6 protons and 7 neutrons (13C) forming the heavy stable isotope
of this important element.

• Stable isotopes do not decay into other elements. In
contrast, radioactive isotopes (e.g., 14C) are unstable and will
decay into other elements

Radioactive
Decay

• Process by which an unstable atomic nucleus loses energy
by emitting radiation

 Alpha particle

 Beta particle

 Gamma particle

Half Life

• The time it takes for half the R.A. nuclei to decay is
called the half life

• The time taken for the radioactivity to half is the same.

• Different R.A. substances have different half-lives.

Example:

Units of
Radioactivity

• Physical Units

• Roentgen (R)

• Curie (Ci)

• Biological units

• Gray (Gy)

• Rad (rad)

• Relative Biological Effectiveness (RBE)

Detection
and Measurement of Radio Activity

• Geiger-Muller counter method

• Scintillation counter method

• Ionization chamber method

• Cloud chamber method

Geiger-Muller
Counter Method

Argon gas is filled in the tube at reduced pressure of 0.1
atmospheres.

A potential difference of about 1000 volts is applied across
the two electrodes.

 

• Argon gas is ionised wherever any alpha or beta particles
enters in the tube through the mica window

• The positively charged argon ions are attracted to the
cathode

• The negatively charged electrons to the anode

• Thus an electrical impulse flows between the electrodes
whenever one alpha or beta particle enters the tube

• The electrical pulses are counted in an automatic counter

• The intensity of the radioactivity of any radioactive
material can be found out by finding the number of pulses per minute

Scintillation
Counter Method

• Scintillation means a flash of light

• Phosphor, photomultiplier tube

• In conjunction with a high voltage supply, an amplifier, a
pulse height discriminator and a scalar

• Charged particles or gamma radiations from radioactive
source cause phosphor to emit scintillations (flashes of light)

• Which are made to fall on light sensitive photomultiplier
tube which detects and amplifies and converts it into electrical impulses

• This impulse recorded directly by means of scalar

Scintillators

• Inorganic scintillators

• Alkali halide (NaI, CsIetc)

• Organic scintillators

• Anthracene

Biological
Effects of Radiation

Delayed
Effects of Radiation

• The hair greys quickly

• Premature ageing

• Cancer of skin, lung cancer, leukaemia

• Sterility

• Chromosomal damage

• Mutations

Storage of
Radio Active Material

• Stored in an area not frequently visited by people

• Thick glass provides sufficient shielding

• Protect from gamma radiations, lead shielding has to be
used

• The storage area must be regularly checked for the
radioactivity

• Radioactive materials have to be stored in suitable
labelled containers, shielded by lead bricks and preferably in a remote corner

Handling
Radio Active Materials

• Carried in trays having absorbent tissue paper

• Rubber gloves have to be used

• Pipettes operated by mouth should never be employed

• One should not touch radioactive emitter with hand

• It should be handled by means of forceps or suitable
instruments

• Smoking, eating and drinking activities should not be done

• Sufficient protective clothing or shielding

• Areas should be monitored (tested for radioactivity
regularly)

Pharmaceutical
application of radioisotopes

• Radioisotopes in therapeutics

• Radio isotopes in Diagnosis

• Research

• Sterilization

Radiopharmaceuticals

• These are pharmaceutical preparations having a radioactive
isotope

• Used internally

• These are prepared by Scientists at the Bhabha atomic
research Centre (BARC)

• Supplied to approved hospitals and approved laboratories

• E.g.. Sodium radio iodide injection

• sodium iodide-I131capsules

• I P does not include any radioactive pharmaceutical
preparation

Application
of Radiopharmaceuticals

Treatment of disease

• They are radio labeled molecules designed to deliver therapeutic
dose so ionizing radiation to specific diseased sites

As an aid in the
diagnosis of disease

• The radio pharmaceutical accumulated in an organ of inter estimate
gamma radiation which are used for imaging of the organs with the help of a next
Ernal imaging device called gamma camera

Clinical
Application

• Calcium (Ca-44 and Ca-45)-used to study bone structure and
in the treatment of carcinoma of bone

• Cyanocobalamine (Co-57)-in the diagnosis of pernicious
anaemia

• Gold (Au-198) solution –neoplasticsuppressant, used for
the estimation of reticuloendothelial activity

• Hydrogen (H-2 an H-3) –determine total body water

• Iron (Fe-59) –investigation of iron metabolism and to
measure red cell life span

• Sodium (Na-22 and Na-24) –used in the estimation of extra
cellular fluid

• Iodine (I-131) –used in the study of functioning of
thyroid gland

Opaque
Contrast Media

• Radio opaque substances are chemical compounds

• Contains elements of high atomic number

• Will stop the passage of X-rays hence appear opaque on
X-ray examination

• Such compounds and their preparations are known as X-ray contrast
media

• Diagnostic aids in radiology

Barium
sulphate suspension

• Barium meal or shadow meal

• Dry mixture of barium sulphate having suitable colouring flavouring,
preservatives and suspending or dispersing agents

• Composition:

Barium sulphate1000g

Saccharin sodium0.25g

Vanillin0.10g

• Preparation: It is prepared by mixing saccharin and
vanillin with barium sulphate and is given to the patient immediately

• Use: Diagnostic aid

Summary

• The spontaneous emission of radiations by atomic nuclei
resulting in their integration is called natural radioactivity

• Alpha rays, beta rays and gamma radiations are the
radiations

• Alpha radiations are nuclei of helium atoms with a mass of
four a.m.u. and with two positive charges

• Their penetrating power is less and has got highest
ionising power

• In G M counter Argon gas is ionised wherever any alpha or
beta particles enters in the tube through the mica window

• Cationsand anions are attracted to the respective
electrodes

• Electrical pulses are counted in an automatic counter

• Scintillation counter consists of phosphor,
photomultiplier tube, high voltage supply, an amplifier, a pulse height
discriminator and a scalar

• Charged particles or gamma radiations from radioactive
source cause phosphor to emit scintillations

• Radioactive materials are stored in an area not frequently
visited by people

• Lead shielding has to be used to protect from gamma
radiations

• One should not touch radioactive emitter with hand

• Sufficient protective clothing or shielding are required

• Radio pharmaceuticals are pharmaceutical preparations
having a radioactive isotope

• E.g.. Sodium radio iodide injection, sodium
iodide-I131capsules etc

• Radio pharmaceuticals are used in the treatment of diseases,
as an aid in the in the diagnosis of disease

 

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