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PenicillinPenicillin
Group member:Yiu Tsz Fai
Ng Yun Chung
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Introduction Lead compound discovery Molecular modification Formulation development Safety Test and Human Trials Approval for marketing
Contents
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Introduction antibiotics
derived from penicillin fungi.
Definition of antibiotics: killing or stopping the growth of a disease-causing bacteria.
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How penicillin works
preventing some bacteria from forming new cell walls.
Bacteria cannot complete the process of division
Cannot produce two new ‘daughter’ bacteria from a single ‘parent’ bacterium.
resist bacterial inflections.
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Lead Compound Discovery
Alexander Fleming contributed to the discovery of penicillin
Discovery process:① arranging a pile of Petri dishes where he
had been growing bacteria ② not uncommon: some mold was
growing on one of the dishes ③ very unusual: the bacteria around the
mold had been killed.
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Lead Compound Discovery
Conclusion: The mold was releasing a substance that
could inhibit the growth of bacteria.
Notwithstanding, he was never able to purify his samples of penicillin.
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Molecular modification
Two different categories of penicillin. Biosynthetic penicillin 1. natural penicillin 2. harvested from the mold itself by fermentation.
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Molecular modification
The other form of penicillin is called semi-synthetic.
Semi-synthetic compounds: basic structure of penicillin modified chemically by adding acyl
groups that produce new properties.
Ampicillin Carbenicillin
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Advantages:resist the acid in the stomach so as to take the drugs orally.
The modification also increases the degree of resistance to penicillinase.
It has an extended range of activity against some Gram-negative bacteria.
Molecular modification
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Formulation development
developed into different types of derivatives
Cause: the narrow range of treatable diseases
Derivatives: treating a wider range of infections.
Benzylpenicillin, procaine benzylpenicillin, benzathine benzylpenicillin and phenoxymethylpenicillin are the four main types of drugs used nowadays.
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Formulation development
Benzylpenicillin: injection into a vein or muscle, or via a
drip into a vein.
treat infections of the lungs and airways, mouth and throat, skin or soft tissue, or ears, as well as other more rare infections.
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Formulation development
Procaine benzylpenicillin: Injection a sustained release drug that is slowly
hydrolysed to benzylpenicillin after deep intramuscular injection.
Its microbiological properties are the same as those of benzylpenicillin.
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Formulation development
Benzathine benzylpenicillin Injection slowly absorbed into the circulation, after in
tramuscular injection, and hydrolysed to benzylpenicillin.
drug-of-choice when prolonged low concentrations of benzylpenicillin are required and appropriate
allowing prolonged antibiotic action over 2–4 weeks after a single IM dose.
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Formulation development
Phenoxymethylpenicillin: has a similar spectrum of action to
benzylpenicillin
less active
not used for serious infections
taken by mouth and is more resistant to the action of gastric acids
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Safety Test and Human Trials
Safety Test on animals:
inject penicillin in rabbits and mice
cured rabbits and mice can resist bacterial infections.
The test on animals is successful
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Safety Test and Human Trials
Human research trials:
began around 1940-1941
Penicillin was tried on a policeman
This was one of the first tests of penicillin. It had taken four days for him to improve.
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Approval for marketing
A new drug application must include:
the drug's test results
manufacturing information to demonstrate the company can properly manufacture the drug
the company's proposed label for the drug
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Manufacturing process It was difficult to produce enough
penicillin.
There were three methods to mass-produce penicillin:
① Creating the right environment ② corn steep liquor ③ A moldy cantaloupe
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The End