BIOAVAILABILITY It is defined as the rate and extent of absorption of unchanged drug from it’s dosage form.

1. ROUTE OF ADMINISTRATION AND
IMPLICATION ON BIOAVAILABILITY
Department of Pharmacy (Pharmaceutics) | Sagar savale
Mr. Sagar Kishor savale
[Department of Pharmaceutics]
avengersagar16@gmail.com
2015-016

2.  INTRODUCTION
 OBJECTIVE
 BIOAVALIBILITY
 FACTORS AFFECTING SELECTION OF ROUTES OF
ADMINISTRATION
 CLASSIFICATION OF ROUTES OF ADMINISTRATION
 IMPLICATION ON BIOAVALIBILITY
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3. INTRODUCTION1,2
Dosage form designing deals with the process of
turning of new chemical entity into a medication to
be used safely and effectively by a patient.
BIOAVAILABILITY
It is defined as the rate and extent of absorption
of unchanged drug from it’s dosage form.
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4. OBJECTIVE2
To achieve a predictable therapeutic
response
To ensure product quality
Chemical and physical stability
Uniformity of dose
Improve patient compliance
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5. Route of Administration
Systemic
Oral
(Sublingual,
Buccal)
Parenteral
(S.C., I.M.,
I.V.)
Local
Topical
(Skin,
Mucosa)
Classification1,2,3
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6. FACTORS AFFECTING DESIGN OF DOSAGE FORM1
Physical & chemical properties of drug-
Site of desired action-
Rate & extent of absorption from various
routes
Effect of digestive juices & first pass effect
Rapidity of the desired response-
Accuracy of dosage
Condition of the patient
Nature and formulation of drug
Route of administration.
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7. Administration of drug by ingestion. Intended for
systemic effects resulting from drug absorption
through the various epithelia and mucosa of the GIT.
eg. Capsules, Tablets, Syrup, Emulsion ,Suspension
Safe
Convenient
Economical
 No need for
sterilization
Advantages
Oral Route2
Drug action has slower onset son
not suitable in case of
emergency.
Drug instability in GI fluid
First-pass effect
Irritation to gastric mucosa
Disadvantages
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8. FIRST-PASS EFFECT1
 The first-pass effect is the term used for
the hepatic metabolism of a
pharmacological agent when it is absorbed
from the gut and delivered to the liver via
the portal circulation. The greater the
first-pass effect, the less the agent will
reach the systemic circulation when the
agent is administered orally.
Where ?
Liver
Gut wall
Gut Lumen
Result ?
Low bioavailability.
Short duration of action (t ½).
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9. SUBLINGUAL ROUTE
Sublingual administration is where the
dosage form is placed under the tongue
rapidly absorbed by sublingual mucosa
Advantages
Rapid absorption
Drug stability
Avoid first-pass effect
Disadvantages
 Inconvenient
 Small doses
 Unpleasant taste of drugs
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10. BUCCAL ROUTE
Buccal administration is where the dosage
form is placed between gums and inner lining
of the cheek (buccal pouch) absorbed by
buccal mucosa
ADVANTAGES
Avoid first pass effect
Rapid absorption
Drug stability
DISADVANTAGES
Inconvenience
advantages lost if
swallowed
Small dose limit
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11. RECTAL ROUTE
Advantages
 Bypasses the portal circulation
 This route of administration has the additional
advantage of preventing the destruction of the drug
by intestinal enzymes or by low pH in the stomach.
 The rectal route is also useful if the drug induces
vomiting when given orally, if the patient is already
vomiting, or if the patient is unconscious.
Disadvantages
 On the other hand, rectal absorption is often erratic
and incomplete, and many drugs irritate the rectal
mucosa.
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12. Parenteral administration is
injection or infusion by means of a
needle inserted into the body.
Para, meaning outside
enteron, meaning the intestine
PARENTERAL2,3
ADVANTAGE
100% bioavailability
large quantities
vomiting & diarrhea
emergency situations
 avoided FPM
gastric manipulation
avoided
DISADVANTAGES
 Irritation ,belonephobia
 Thrombophelebitis
 Less safe
 Technical assistance
required
 Danger of infection
 Expensive
 less convenient and painful
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13. INTRAVENOUS
Drug solution is injected directly
in one of superficial vein either as
bolus or infusion.
I.M.ROUTE OF ADMINISTRATION2
Drug is injected deep between the layers
of one of large skeletal muscle because
these are richly supplied with blood and
less with nerves.
Drug suspended in oily vehicle a
preparation provide slower absorption
characteristics .
Provide depot preparation.
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14. The drug preparation is deposited
in the loose subcutaneous tissue
(under skin).It is richly supplied
with nerve but less blood supply
absorption of drugs is slower than
im and iv.
It is suitable for depot preparations.
SUBCUTANEOUS
INTRAARTICULAR INJ.
Inject the drug in Joints for the
treatment of arthritis More skill is
required Painful application Damage
the cartilage
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15. INTRADERMAL
Drug is given within skin layers
(dermis)
Painful
Mainly used for testing sensitivity to
drugs.
Drugs which cannot cross BBB are
administered through this route
INTRA THECAL INJECTION
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16. INHALATION
1.Gaseous and volatile agents and aerosols
2.Rapid onset of action due to rapid access to
circulation Particles size 0.5-1um absorb
from alveolar sacs.
a. Large surface area
b.Thin membranes separates alveoli
from circulation
c. High blood flow
ADVANTAGES
The nasal cavity is well
vascularised.
Avoid FPM.
Suitable ROA for drug which
is degraded in the gut.
DISADVANTAGES
Irritation to respiratory
track
Most addictive route of
administration.
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17. TRANSDERMAL1,2
Transdermal drug delivery system
are topically administered
medicaments in the form of patches
that deliver drugs for systemic
effects at a predetermined and
controlled rate.
Highly lipid soluble drug can be
applied over skin for slow and
prolonged absorption
Eg. nitroglycerine ointment .
•Administering medications to
the skin
–Lotions, creams,
ointments.
–Transdermal patches
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18. TOPICAL ROUTE1
Topical administration is the application of
a drug directly to the surface of the skin
Includes administration of drugs to any
mucous membrane
Topical application is used when a local
effect of the drug is desired. Dermal - rubbing
in of oil or ointment (local
action)
eye – vagina
nose – urethra
ears – colon
lungs 18
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19. EYE PREPARATION
 Application of drug into cornea of
eye .
REQUIRMENTS
pH of preparation.
Isotonicity
Sterility
Foreign material
Viscosity
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20. ROUTE OF ADMINISTRATION:
TIME UNTIL EFFECT2
 intravenous 30-60 sec
 inhalation 2-3 minutes
 sublingual 3-5 minutes
 intramuscular 10-20 minutes
 subcutaneous 15-30 minutes
 rectal 5-30 minutes
 ingestion 30-90 minutes
 Transdermal (topical) variable (minutes to
hours)
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21. Parenteral>
Inhalation>
Oral(Sublingual>Buccal)>
Rectal>
Topical
BIOAVAILABILITY COMPARISION1
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Pathway Of Drug2
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23. 1)Brahmankar D.M. ,Sunil B.Jaiswal,
Bioavailability and Bioequivalence,
Biopharmaceutics and pharmacokinetics
A treatise, 2nd edition, Vallabh
prakashan,2009,315-318, 499.
2)Aulton M. E. , “Pharmaceutics the
science of dosage form design ’’2nd edition,
Churchill livingstone prakashan, 2002,1-6.
3)Leon lachman ,H. A. Lieberman, J. L.
Kanig, Theory & Practice of Industrial
Pharmacy,3rd edn Varghese publishing
House,1976, Pg no. 223-226
REFERENCES:
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24. Queries??? 24
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