PREFORMULATION STUDIES
SUBMITTED BY-ADARSH,POONAM SUBMITTED TO-MS. CAHRU SAXENA
ROLL NO-16BPH053,16BPH054
PREFORMULATION
It is prior to formulation as a name suggest before
initiating formulation development preformulation is the
step to understand physiochemical properties of drug
substance. In other words preformulation study describe
as the process of optimising the delivery of drug through
determination of physiochemical property of the new
compound that could affect drug performance and
development of stable and safe dosage form.
OBJECTIVES
To stablish the physio-chemical parameters of a new
drug entity.
To determine its kinetics and stability.
To stablish its compatibility with common excipients.
It provides insights into how long drug products should
be processed and stored to ensure their quality.
PHYSICAL PROPERTIES
ORGANOLEPTIC CHARACTERS:
Organoleptic tests are sometimes conducted to
determine if food or pharmaceutical products can
transfer tastes or odors to the materials and components
they are packaged in.Shelf life studies often use taste,
sight, and smell (in addition to food chemistry and
toxicology tests) to determine whether a food product is
safe to consume.
BULK CHARACTERISATION
PARTICLE SIZE DETERMINATION:
Particle size analysis, particle size measurement, or
simply particle sizing is the collective name of the technical
procedures, or laboratory techniques which determines
the size range, and/or the average, or mean size of the particles in
a powder or liquid sample.
It concludes various methods like-
* Sieving, centrifugation method, coulter counter
method, sedimentation method, microscopic method etc.
POWDER FLOW PROPERTY:
Powder flow properties can be affected by change in
particle size, shape, and density. The flow property
depends upon force of friction and cohesion between
one particle to another. Fine particle possess poor flow
by filling void spaces between large particles causing
packing and densification of particles.
CRYSTALLISATION:
Crystallization is also a chemical solid–liquid separation
technique, in which mass transfer of a solute from the
liquid solution to a pure solid crystalline phase occurs. In
chemical engineering, crystallization occurs in a
crystallizer.
HYGROSCOPICITY:
It is the capacity of a product (e.g. cargo, packaging
material) to react to the moisture content of the air by
absorbing or releasing water vapor. Of decisive significance
for the absorption or release of water vapor is the water
content of a product.
POLYMORPHISM:
Polymorphism is the ability of solid materials to exist in two or
more crystalline forms with different arrangements or
conformations of the constituents in the crystal lattice. These
polymorphic forms of a drug differ in the physicochemical
properties like dissolution and solubility, chemical and physical
stability, flowability and hygroscopicity. These forms also differ
in various important drug outcomes like drug efficacy,
bioavailability, and even toxicity.
PHYSIOCHEMIAL PROPERTIES
PARTITION COEFFICIENT:
The ratio of the concentrations of a solute in two immiscible or
slightly miscible liquids, or in two solids, when it is in equilibrium
across the interface between them.
pH SOLUBILITY PROFILE:
It is the property of solid, liquid or gaseous substance called
solute to dissolve in solid, liquid or gaseous substance. pH It
is defined as negative logarithm of hydrogen ion
concentration in a substance.(Acidic- 0 to 7) (Alkaline/ Basic-
7 to 14).
COMMON ION EFFECT:
Some of the salt will be precipitated until the ion product is
equal to the solubility product. In short, the common ion
effect is the suppression of the degree of dissociation of a
weak electrolyte containing a common ion.
SOLUBILITY ANALYSIS:
Solubility is an essential and extensively studied preformulation
parameter. It focuses on drug-solvent system that could
occur during drug delivery. Such information is important to
the formulator, for it enables him to select the best solvent
medium for a drug, identify and overcome certain challenges
that arise in the formulation of pharmaceutical solutions, and,
furthermore, estimate the level of all known and significant
impurities and contaminants in the drug molecule under
evaluation.
ASSAY DEVELOPMENT
Assay Development is a procedure in molecular biology for
testing or measuring the activity of a drug or biochemical in
an organism or organic sample. A quantitative assay may
also measure the amount of a substance in a sample.
Bioassays and immunoassays are among the many varieties
of specialized biochemical assays. Other assays measure
processes such as enzyme activity, antigen capture, stem cell
activity, and competitive protein binding.
Typical steps involved in the development of a mass
spectrometry-based targeted assay include: (1)
selection of surrogate or signature peptides
corresponding to the targeted protein or modification of
interest; (2) iterative optimization of instrument and
method parameters for optimal detection of the
selected peptide; (3) method development for protein
extraction from biological matrices such as tissue, whole
cell lysates, or blood plasma/serum and proteolytic
digestion of proteins (usually with trypsin); (4) evaluation
of the assay in the intended biological matrix to
determine if endogenous analyte is detected; if target
analytes are of low abundance, an enrichment step
may be necessary; and (5) assay validation applying fit-
for-purpose principles on biological samples to
characterize assay performance.
STABILITY STUDIES
Stability studies are an essential component of pharmaceutical
development, allowing evaluation of active pharmaceutical ingredient
(API) stability or drug product stability under the influence of a variety of
environmental factors such as temperature, humidity and light.
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