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Suppositories,

Inserts, and Sticks


Razon
Recabo
Rendon
Sagun
Songcuya

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Formulation Variables

A. nature and form of the active principle


(esters, salts, complexes, etc)
B. physical state, particle dimensions and
specific surface of the product
C. solubility of drug in various bases
D. Presence or absence of adjuvants added to
the active principle
E. nature and type of dosage form the active
drug is incorporated
F. Pharmaceutical procedures in the
preparation of the dosage form

Physical State
Solid Active Drug
Drugs particle size is important,
especially if not very soluble
Increase in surface area, decreased
particle size enhances activity

Physical State
Liquid Active Drug
Necessary to take into a suppository base
such as forming an emulsion, adding a drying
powder, or adding a suitable thickening agent
Semisolid Active Drug
Paste-type drugs
Either be mixed with a solid to thicken drug or
Mixed with a base with a thickener being
added

Particle Size
If drug is readily soluble, influence of particle
size may be minimal
Highly water-soluble drugs
tendency to
dissolve and migrate in the rectal barrier
Poorly water-soluble drugs
dissolution rate
is slower
-reduction in particle size may increase the
rate of dissolution
by exposing a greater
surface area
This can also be affected by the nature of the
suppository base

Solubility
Increased solubility of the active drug in the base
can improve product homogeneity
However, it may also delay the release of active
drug of the affinity is too great for the suppository
vehicle
If the product is insoluble, an emulsion or suspension
is formed, it may possess different problems
Necessary to obtain homogeneity of the total
mixture
-constant agitation of mixture during processing
and filling
Select a temperature just above the melting point of
the suppository mixture

Viscosity

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