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Preformulation Intro Goal Objective PPD

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Deepak Bhosale
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35 views

Preformulation Intro Goal Objective PPD

Uploaded by

Deepak Bhosale
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPTX, PDF, TXT or read online on Scribd
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D.S.T.S. Mandal’S College of Pharmacy, Solapur.

Preformulation

BY MR. D S BHOSALE
ASSISTANT PROFESSOR
INTRODUCTION
Activities done prior to formulation development are called as
preformulation studies. It provides the scientific basis for
formulation development.
Preformulation studies can be broadly classified into two
classes
(i) fundamental properties and (ii) derived properties.
Fundamental Preformulation properties are specific to the
drug molecule and are dependent on the chemical structure
of the drug molecule.
In contrast, derived pre-formulation properties are carried out
to learn about the issues related to development of a particular
dosage form like solid oral, liquid oral or parenteral.
Fundamental preformulation properties include
-Solubility, dissociation constant (pKa), salt formation, partition
or distribution coefficient, pH solubility profile and dissolution
kinetics, permeability, solid state properties like polymorphism,
stability profile etc. Derived preformulation properties are
specific to the intended dosage form to be developed.
The last activity performed in pre-formulation studies is the
compatibility studies, wherein the physical and chemical
stability of the drug molecule is studied in presence of
excipients. Obviously, the choice of excipients is dictated by the
type of dosage form to be developed.
Preformulation studies strengthen the scientific foundation of the
guidance, provide regulatory relief and conserve resources in the
drug development and evaluation process, improve public safety
standards, enhance product quality in the fabrication of dosage
form.
Preformulation studies were evolved in 1950 & early 1960.
Preformulation testing is the first step in the rational development
of dosage forms of a drug substance. It can be defined as an
investigation of physical and chemical properties of a drug
substance alone and when combined with excipients.
The overall objective of preformulation testing is
to generate information useful to the formulator in developing
stable and bioavailable dosage forms that can be mass produced.
Preformulation investigations are designed to deliver all
necessary data especially physicochemical, physico-mechanical
and biopharmaceutical properties of drug substances, excipients
and packaging material Which may influence ……….
•Formulation design
•Method of manufacture of API and drug product
•Pharmacokinetic/biopharmaceutical properties of the resulting
product.
•Packaging of the product (stability).
Preformulation during Drug Discovery
Apart from helping formulation development,
preformulation studies also help in lead identification
during drug discovery phase. A new chemical entity
should possess optimal biopharmaceutical properties
to become a drug molecule. Mere possession of
potency and selectivity does not ensure ‘drug ability’.
Preformulation studies help in assessing the ‘drug ability’ of a
molecule.
Preformulation can thus be considered as critical decision-
making tool during both
1,drug discovery and 2. development phase.
A comprehensive understanding of physicochemical
properties and its effect on biological performance, allows
selection of potential lead molecules and in identification of
drug delivery challenges.
Objectives
To develop the elegant, stable, effective and safe dosage form by
establishing kinetic rate profile, compatibility with the other
ingredients and establish Physico-chemical parameter of new drug
substances.

It is important to have an understanding of the physical description


of a drug substance before dosage form development.

It is 1st step in rational development of a dosage form of a drug subt


before dosage form development
GOALS OF PREFORMULATION
To establish the necessary physicochemical parameters of a new
drug substance.
 To determine its kinetic rate profile.
 To establish its physical characteristics and,
To establish its computability with common excipients.
To choose the correct form of a drug substance.
Generate a thorough understanding of the material stability
under the conditions that will lead to development of an optimal
drug delivery system.
Discovery of a new drug entity is a huge milestone in
science and it becomes even more important if it passes
toxicity screening as the potential benefits overweigh
the side effects.
The ultimate effect of the new chemical entity depends on
its availability at the site of action once it is administered
through appropriate route in appropriate form. So for this
reason, a new challenge is offered after successful
pharmaceutical and toxicological screening that is to
transform potential active new drug entity into a
pharmaceutical formulation.
It can be broadly elaborated as “a phase which works on study of
physical, chemical, analytical, pharmacokinetic, and
pharmacodynamic properties of new chemical entity and utilize
the obtained results to design and develop an effective, stable,
and a safer dosage form. Preformulation study is there for the
multidisciplinary approach and utilizes involvement of several
aspects of pharmacology, toxicology, clinical pharmacy,
biochemistry, medicinal chemistry, and analytical chemistry
(Fig 1).
The preliminary objective of preformulation phase or study is
to lay down foundation for transforming a new drug entity into
a pharmaceutical formulation in such a way that it can be
administered in a right way, in right amount, and on perhaps
the most important at right target.
The secondary objective preformulation study is to provide
longer stability to the formulation by proper designing and
protecting drugcomponent from environmental condition and
to evaluate performance of developedformulation.
PREFORMULATION PARAMETERS
A. PHYSICAL CHARACTERISTICS
1) Organoleptic properties
2) Bulk characteristics
a) Solid state characteristics
b) Flow properties
c) Densities
d) Compressibility
e) Crystalline
f) Polymorphism
g) Hygroscopicity
3) Solubility analysis
a) Ionization constant (Pka)
b) Partition co-efficient
c) Solubilization
d) Thermal effect
e) Common ion effect (Ksp)
f) Dissolution
4) Stability analysis
a) Solution-state stability
b) Solid-state stability
c) Drug-excipients compatibility
B. CHEMICAL CHARACTERISTICS
1) Hydrolysis
2) Oxidation
3) Photolysis
1) ORGANOLEPTIC PROPERTIES
A typical preformulation program should begin with the
description of the drug substance. The color, odour and taste
of the new drug must be recorded using descriptive
terminology. The color, odor and taste of the new drug must be
recorded using descriptive terminology. It is important to
establish a standard terminology to describe these properties
in order to avoid confusion among scientists using different
terms to describe the same property.
A list of some descriptive terms to describe the most commonly
encountered colors, tastes and odours of pharmaceutical
powders is provided in table. The color of all the early batches of
the new drug must be recorded using the descriptive
terminology. A record of color of the early batches is very useful
in establishing appropriate specifications for later production.
When the color attributes are undesirable or variable,
incorporation of a dye in the body or coating of the final product
could be recommended.
Terminology to describe organoleptic properties of
pharmaceutical powders
Colour odour Taste
Off-white Acidic Bland
Pungent Bitter intense sweet
Cream yellow Fruity tasteless
Sulfurous Aromatic -
Tan Odouerless -
2. BULK CHARACTERISTICS
a) Solid state characteristics:
Powders are masses of solid particles or granules surrounded by air
(or other fluid)and it is the solid plus fluid combination that
significantly affects the bulk properties of the powder. It is
perhaps the most complicating characteristic because the
amount of fluid can be highly variable. Powders are probably
the least predictable of all materials in relation to flow ability
because of the large number of factors that can change their
rheological properties.
Physical characteristics of the particles, such as size, shape,
angularity, size variability and hardness will all affect flow
properties. External factors such as humidity, conveying
environment, vibration and perhaps most importantly aeration
will compound the problem.

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