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Erythromycin

M.Sc. Biotechnology Part II (Sem III)


Paper III - Unit III
Mumbai University
BY: Mayur D. Chauhan

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Introduction
• Erythromycin belongs to the group of Macrolide
antibiotics.
• Macrolide antibiotics slow the growth of, or
sometimes kill sensitive bacteria by reducing the
production of important proteins needed by the
bacteria to survive.
• It has an antimicrobial spectrum similar to or
slightly wider than that of penicillin and is often
used for people who have allergy to penicillin.
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• It is used to treat many different types of
infections caused by various bacteria.
• It is used to prevent bacterial endocarditis and
attacks of rheumatic fever.
• Also used to prevent outbreaks of sexually
transmitted diseases like chlamydia, syphilis
and gonorrhea. Prevents respiratory tract
infections.
• Erythromycin is produced from the strain of
actinomycete Saccharopolyspora erythraea
formerly known as Streptomyces erythraeus.

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Structure
• It is a macrocyclic compound containing 14-
membered lactone ring with 10 asymmetric
centers and two sugars – L-Cladinose and D-
Desoamine.
• Trade name is E-mycin or Erythrocin

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Mechanism of Action
• Erythromycin displays a bacteriocidal activity
particularly at higher concentrations.
• It prevents the growth of bacteria by inhibiting
their protein synthesis.
• Erythromycin binds to the 23s rRNA molecule
in the 50S ribosomal subunit.
• This binding blocks thee exit of the growing
peptide thus inhibiting the translocation of
the peptides.
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Erythromycin interferes with the aminoacyl translocation preventing the transfer of the
tRNA bound at the A site to the P site of the rRNA complex.
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Pharmacokinetics
• Erythromycin is easily inactivated by gastric acids,
therefore all orally administered formulations are
given as either enteric coated or more stable salts
or esters, such as erythromycin ethylsuccinate.
• It is rapidly absorbed and diffused into most
tissues and phagocytes.
• Due to high concentration in phagocytes,
erythromycin is actively transported to the site of
infection, where during active phagocytosis, large
concentration of erythromycin is released.
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Metabolism
• It is mostly metabolised by demethylation in
the liver.
• It’s main elimination route is Bile and a small
portion in Urine
• It’s half-life is 1.5 hours

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Production Process

2 steps

Biomass Production
accumulation phase

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Biomass Accumulation
• The sporulating culture of Streptomyces
erythraeus is done on Trypton agar slant.
• Cells are harvested from agar plates and the
suspension is taken in Sterile water.
• The suspension is then stored at 4o C.

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Production Phase
• Media which used in a stirred tank fermenter
consists of,
• Sucrose – 5%
• Corn steep liquor – 0.5%
• Soyabean oil meal – 1.5%
• Yeast – 1.0%
• NaCl – 0.5%
• CaCo3 precipitate – 0.3%
• pH – 7.0 -7.2
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• Production of Erythromycin production occurs
when froth reaches stationary phase.
• Addition of n-propanol as precursor increases
the production of erythromycin..

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Isolation and Extraction

Mycelium is separated from the broth by


centrifugation or drum filtration

Acidic condition is maintained by addition of


Butyl acetate which favors the separation of
the mycelium. Also it dissolves the antibiotic

Wash with water

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pH is adjusted at 9.5
using Acetone

Precipitate formed in the


form of Crystals

Erythromycin is obtained
as a dihydrate salt
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Available Forms of Erythromycin
• Erythromycin is available in enteric coated
tablets, slow release capsules, oral
suspensions, opthalmic solutions, ointments,
gels and injections.
• Erythromycin base (Capsules, tablets)
• Erythromycin ethylsuccinate (Oral suspension,
tablets)
• Erythromycin stearate (Oral suspension,
tablets).
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Injections
• Erythromycin Gluceptate
• Erythromycin lactobionate

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