PREFORMULATION STUDIES

PHYSICAL
CHARACTERISTICS
 INTRODUCTION
• Preformulation is branch of Pharmaceutical science that
utilizes biopharmaceutical principles in the
determination of physicochemical properties of the drug
substance.
• Prior to the development of any dosage form new drug ,
it is essential that certain fundamental physical &
chemical properties of drug powder are determined .
• Investigation of physico-chemical properties of the new
drug compound that could affect drug performance and
development of an effective dosage form”.
PHYSICAL CHARACTERISTIC AND
BULK CHARACTERISTIC

• Crytallinity
• Polymorphism
• Hygroscopicity
• Powder flow
 CRYSTALLINITY
• Crystal habit & internal structure of drug can affect
bulk & physicochemical property of molecule.
• Crystal habit is description of outer appearance of
crystal.
• Internal structure is molecular arrangement within
the solid.
• Change with internal structure usually alters crystal
habit.
 AMORPHOUS CRYSTALINE

High thermodynamic Lesser than amorphous

energy
High solubility and Less solubility and
dissolution rates dissolution rates
Upon storage becomes Crystal takes water and
solid form produces hydrates
 POLYMORPHISM
• This is the ability of a solid material to crystallize
forming at least two different crystalline species
with distinct internal lattice.
• These different molecular arrangements disappear in
liquid and vapour states.
• Polymorphs differ from one another with respect to
their physical properties.
• Polymorphs are of 2 types
1. Enatiotropic
2. Monotropic
 HYGROSCOPICITY
• Many drug substances usually absorb or lose
moisture from the atmosphere to achieve
equilibrium with the water in the atmosphere.
• Many substances, particularly water soluble salt
form have a tendency to absorb atmospheric
moisture.
• The amount of moisture absorbed or lost by a given
quantity of a drug substance can vary significantly
and continually depending on the relative humidity
and air temperature.
• These cyclic changes lead to constant variations in
the moisture content of unprotected drug substances
and excipients.
 POWDER FLOW
Powder flow properties can be affected by change in
particle size, shape & density.
The flow properties depends upon following
1.Force of friction
2.Force of cohesion
Fine particle posses poor flow by filling void spaces
between larger particles causing packing & densification
of particles.
By using glidant we can alter the flow properties.
DETERMINATION OF POWDER FLOW
PROPERTIES
By determining Angle Of
Repose.
A greater angle of repose
indicate poor flow.
It should be less than 30°.
& can be determined by
following equation.
tan θ = h/r.
where, θ = angle of
repose.
h=height of pile.
r= radius
REFERENCES

1. Saha A. CHAPTER – 1 Preformulation Studies [Internet]. Academia.edu.

[cited 2019Oct12]. Available from:
https://www.academia.edu/7720904/CHAPTER_1_Preformulation_Studi
es
2. Cascade Impactor [Internet]. Cascade Impactor - an overview |
ScienceDirect Topics. [cited 2019Oct12]. Available from:
https://www.sciencedirect.com/topics/materials-science/cascade-
impactor
3. Lachman, L, Leiberman, HA and Kanig, JL, 1999. The Theory and Practice
of Industrial Pharmacy, Lea and Febiger, Philadelphia.
4. Kumar, P., Vaishnavi, G., Divya, K. and Lakshmi, U. (2015). An Overview
on Preformulation Studies. Indo American Journal of Pharmaceutical
Science, 2(10): 1399-1407.