2. contents
The contents are:
1. Drug Degradation
2. Types of drug degradation
Physical degradation
Chemical degradation
Microbial degradation
3. Factors Affecting the Rate of drug
degradation
ph
Complexation
Surfactants
Presence of heavy metals
Light
Humidity/ Moisture
3. DEGRADATION
Drug degradation is defined as:
THE CONDITION OR PROCESS OF
DEGRADING OR BEING
DEGRADED
OR
It is also defined as:
DECLINE TO A LOWER QUALITY
CONDITION OR LEVEL
4. PHARMACEUTIC
AL DEGRADATION
Pharmaceutical degradation is defined as:
THE INCAPACITY OR INCAPABILITY
OF A PARTICULAR FORMULATION
IN A SPECIFIC CONTAINER TO
REMAIN WITHIN A PARTICULAR
CHEMICAL ,MICROBIOLOGICAL ,
THERAPUTICAL, PHYSICAL ,
TOXICOLOGICAL SPECIFICATION
5. TYPES OF DEGRADATION
TYPES OF
DEGRADATION
DEFINITIONS FACTORS AFFECTING
THEIR RATE OF
DEGRADATION
PHYSICAL • This degradation results in
change in nature of
physical nature of drug.
• Change in physical
appearance of drug
• Loss of volatile components
• Loss of water
• Crystal growth
• Polymeric changes
• Changes in color
CHEMICAL • Separation of chemical into
elements or simpler
compounds.
• Change in chemical nature of
drug.
• Hydrolysis
• Oxidation
• Decarboxylation
• Isomerization
• polymerization
MICRO-
BIAL
• It is the use of bioremediation
and biotransformation to
harness the naturally
occurring ability of drug.
• No addition of antimicrobial
substance as presentative
• No proper storage
containers
6. FACTORS AFFECTING THE RATE OF
DEGRADATION
•pH:
The acidity or alkalinity of a solution has a profound
influence on the decomposition of drug.
pH influence the rate of oxidation. The system is less
readily oxidized when pH is low.
As little as 1 pH unit can change ten folds the rate
constant .
STABLE DRUGS pH : 4-8
7. Graph of pH
pH effect on
aspirin
pH is 2.4
pH effect on
fluorouracil pH is
8.6-9.4
8. • COMPLEXATION
Complexation is the association between
two or more molecules to form non
bounded entity with well defined
stereochemistry
Complex formation reduces the rate of
hydrolysis and oxidation
EXAMPLE:
Caffeine with local anesthetics cause a
reduction in their hydrolytic degradation.
10. • SURFACTANTS
Non-ionic ,cationic and
anionic surfactants when
added to solutions containing
drugs from micelle and drug
particles become trapped in
micelles .
The hydrolytic group such as
OH cannot penetrate this
micelle cover and reach drug
particles , hence Hydrolysis is
decreased
micelle
12. • PRESENCE OF
HEAVY METALS
Free radicals such as:
• Copper (Cu')
• Iron (Fe')
• Cobalt (Co')
• Nickel (Ni')
increase the rate of formation of free radicals and
enhance oxidative decomposition.
13. • LIGHT
Extreme light effects the rate of drug degradation by
photolysis.
(Decomposition or separation of molecules by the
action of light)
UV light enhances the photolysis of drug.
14. • MOISTURE /
HUMIDITY
The level of humidity greatly effect the degradation of
drugs. Degradation of tablets or capsules start when they
are exposed to moisture.
Humidity enhances the hydrolytic decomposition of drug.
The humidity conditions that lead to unexpected change
in physical state of tablet :
• Hydration/dehydration
• Melting point
• Boiling point
15. CONCLUSION
A pharmaceutical product must appear elegant ,
fresh and professional for as long as it remains on
the shelf.
Dose of active ingredient over time must be ensured.
Drugs must be protected from photolysis.
Drugs must be stored at cool and dry place.
The pH of drugs must be maintained at a narrow
range.