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Presented by : -
Shiva kant Thakur .
B pharma7th sem.
 A detailed knowledge of ADME
characteristics of drug is essential in the
design of controlled release product.
 An optimum range of given
pharmacokinetic parameter of a drug is
necessary beyond which controlled delivery
is difficult.
 Criteria to be met by drug proposed to be
formulated in controlled release dosage
forms are as follows.
 The half life of a drug is an index of its
residence time in the body.
 If the drug has a short half life less than 2
hours , the dosage form may contain a
prohibitively large quantity of the drug.
 Drug with elimination half life of 8hrs or
more are sufficiently sustained in the body.
 Ideally ,the drug should have half-life of
three to four hours.
 Drug with low therapeutic index are
unsuitable for incorporation in controlled
release formulations.
 If the system fails in the body, dose dumping
may occur , leading to fatalities .
E.g. Digitoxin.
 If the dose of a drug in the conventional
dosage is high, its suitability as a candidate
for controlled release is seriously
undetermined.
 This is chiefly because the size of a unit dose
controlled release formulation would become
too big to administer without difficulty.
 Absorption of poorly water soluble drug is
often dissolution rate limited.
 Incorporating such compounds into
controlled release formulations is therefore
unrealistic and may reduce overall absorption
efficiency.
 Certain drugs when administered orally are
absorbed only from a specific part of GIT
tract.
 This part is referred to as the ’absorption
window ’. Drugs exhibiting an absorption
window like fluorouracil , thiazide diuretics ,if
formulated as controlled release dosage from
are unsuitable.
 Delivery of the drug to the body in desired
concentration is seriously hampered in case
of drugs undergoing extensive hepatic first
pass metabolism when administered in
controlled release forms.

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Selection of drug candidates cdds.pptx

  • 1. Presented by : - Shiva kant Thakur . B pharma7th sem.
  • 2.  A detailed knowledge of ADME characteristics of drug is essential in the design of controlled release product.  An optimum range of given pharmacokinetic parameter of a drug is necessary beyond which controlled delivery is difficult.  Criteria to be met by drug proposed to be formulated in controlled release dosage forms are as follows.
  • 3.  The half life of a drug is an index of its residence time in the body.  If the drug has a short half life less than 2 hours , the dosage form may contain a prohibitively large quantity of the drug.  Drug with elimination half life of 8hrs or more are sufficiently sustained in the body.  Ideally ,the drug should have half-life of three to four hours.
  • 4.  Drug with low therapeutic index are unsuitable for incorporation in controlled release formulations.  If the system fails in the body, dose dumping may occur , leading to fatalities . E.g. Digitoxin.
  • 5.  If the dose of a drug in the conventional dosage is high, its suitability as a candidate for controlled release is seriously undetermined.  This is chiefly because the size of a unit dose controlled release formulation would become too big to administer without difficulty.
  • 6.  Absorption of poorly water soluble drug is often dissolution rate limited.  Incorporating such compounds into controlled release formulations is therefore unrealistic and may reduce overall absorption efficiency.
  • 7.  Certain drugs when administered orally are absorbed only from a specific part of GIT tract.  This part is referred to as the ’absorption window ’. Drugs exhibiting an absorption window like fluorouracil , thiazide diuretics ,if formulated as controlled release dosage from are unsuitable.
  • 8.  Delivery of the drug to the body in desired concentration is seriously hampered in case of drugs undergoing extensive hepatic first pass metabolism when administered in controlled release forms.