STUDI PRAFORMULASI

SEDIAAN FITOFARMASI

Indah Yulia Ningsih, S.Farm., M.Farm., Apt.

Phytopharmaceutical development

Traditional medicine
Early sreening

Selected medicinal plants

Crude drug
Extraction Isolation
Extract Isolate

Pre clinical test &

standardization

Standardized extract Single compound

Structure modification
Clinical test Pre clinical test

Phytomedicines Active compound

Clinical test
Phytotherapy Pharmacotherapy
Reasons for not isolating
• Extracts known to contain a range of
similar active compounds, with well
documented clinical activity for whole
or semi-purified extract
• Unsure of active constituents even if
some chemistry known
• Actives known or suspected to be
unstable
• Synergy or antagonism
 Inside of extract
Extracts :
• Small amount of active principle(s)
• Large quantities of secondary
material (organic & inorganic salts,
organic bases & acids, sugars,
polysaccharides, tannins,
polyphenols, saponins)
These can cause formulation problem!!
Formulating an extract
Which one is better?
• Adapted the extract to the desired
dosage form; or
• Adapted the dosage form to the
characteristic of extract?
Formulating the dosage form

• It is preferable to formulate simple

preparations containing not more
than 2 or 3 extracts
• Avoid to include several extracts
having same type of activity
(ex.laxative)
– Extract cascara & frangula
– Extract cascara & aloes
– Extract frangula & aloes, etc.
Advantages of simple preparation

• The problem of control of the various

active principles is simplified
• The interference between difference
extracts is greatly reduced with
obvious gains in stability
• Therapeutic activity is more well
defined
Formulating with > 1 extracts

• In formulation containing > 1 extracts

interactions may occur between the
components of the different extracts
• It can alter the characteristic of
extracts
e.g. : solubility characteristic
Formulating with > 1 extracts

• Extracts containing alkaloids +

extracts containing tannins 
sparingly soluble products  slow
bioavailability
• Extracts containing alkaloids +
extracts containing organic acids 
stable salts of alkaloids  soluble
salts  rapid bioavailability
Formulating with > 1 extracts

• Solid dosage form  preparing the

separate granules of each extract,
suitably coated with resins, which can
then be mixed
• Liquid dosage form 
– Add cosolvent or surfactant, or
– Purification of individual extract
Interaction of extracts with gelatin

• Soft gelatin capsules made with

tannin-containing extracts tend to
harden with time, thereby considerably
increasing their disintegration time

• This phenomenon is
probably due to
interaction between
gelatin and tannins
Formulating extract into semisolid

• Saponins make the HLB value of

cream more hydrophilic  breakdown
w/o emulsions (HLB<10) with phase
separation
• When extract is formulated into o/w
emulsion there will be no problems
with physical stability
TERIMA
KASIH