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Pre Formulation Studies 1 2 3

Pre-formulation studies are essential for understanding the physical and chemical properties of drugs and excipients, as well as their interactions, to optimize dosage forms and ensure stability. These studies can help determine the suitability of a drug for marketing and guide necessary modifications for effective formulation. The overall goal is to establish critical parameters that influence the development and success of new therapeutic agents.

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18 views27 pages

Pre Formulation Studies 1 2 3

Pre-formulation studies are essential for understanding the physical and chemical properties of drugs and excipients, as well as their interactions, to optimize dosage forms and ensure stability. These studies can help determine the suitability of a drug for marketing and guide necessary modifications for effective formulation. The overall goal is to establish critical parameters that influence the development and success of new therapeutic agents.

Uploaded by

f20210378
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Pre-Formulation Studies

Its Importance in the Formulation of


Dosage Forms

1
• What is pre-formulation studies?
• Why do we perform pre-formulation
studies?
• What type of information is gathered from
such studies?
• Physical chemical properties of drugs and excipients
• Intrinsic and derived properties
• Potential interactions between a drug and the
excipients
2
• Possibility of dosage form development
• Optimization of therapeutic agents
• Preliminary data on the stability of
drugs
• Suitable closures and containers
• Powder properties such true density,
apparent density, porosity, specific
surface, and surface area
3
Rational for
Pre-formulation Studies

4
• Approximately one out 5,000 to 10,000 chemical entities,
synthesized and investigated for its potential to treat a
disease, makes to the market.
• Therefore, new dug development is rather a cost
ineffective or a very expensive process.

5
• A drug is synthesized and tested or screened for
pharmacological action;

•A drug is found sufficiently interesting to


warrant further study.

6
Prior to a chemical entity becomes a therapeutic agent and, pharmacists
and physicians begin to use that therapeutic agent, through a dosage form,
to treat a specific physiological or pathological abnormality or a disease, it
(the therapeutic agent) undergoes various kinds of investigations which
may take approximately 10 to 12 years and may cost approximately $ 1 to
3 billion.
"According to a
2014 study by the Tufts Center for the Study of Drug Development (TCSDD
)
, the cost of developing a new drug, from research and development (R&D)
to marketing approval, is approximately $2.9 billion. This includes actual
out-of-pocket costs averaging $1.4 billion, opportunity costs of nearly $1.2
billion, and the cost of post-approval studies amounting to $312 million" 7
Pre-formulation studies provide the scientists the
insight into the potential problems confronted in
the formulation of the dosage form of a drug.

8
Additionally, pre-formulation studies may even
provide useful information to scientists, which
may determine the fate of that therapeutic agent
as to its suitability for the purpose of marketing.

9
Sufficient quantity of a compound is synthesized
to perform:

• Initial toxicity studies


• Analytical work, and
• Initial pre-formulation work

10
Goals of Pre-formulation Studies

11
The goals of the program, therefore, are:
• To establish necessary physiochemical parameters of a
new drug substance.
• To determine the suitability of a drug for the desired
dosage form.
• To recommend changes or modification in the
compound, if necessary, to develop the desired dosage
form (Molecular optimization)
• To determine its kinetic rate profile (stability).
12
• To establish its compatibility with common and routinely
used excipients.
• The study of drug-excipient interactions.

13
Pre-formulation Research

14
Bulk Characterization
• Crystallinity and polymorphism
• Hygroscopicity
• Particle or powder characterization (size and
size distribution, shape, surface characteristics,
true density etc.)
• Derived powder properties: Bulk density,
porosity, flow properties, bound and unbound
moisture content, etc. 15
Solubility Analysis
• Ionization constant – pKa

• pH-solubility profile (pH range of 1.2 to about 7.5)


• Partition coefficient
• Solubility of a drug in commonly used solvents
• Dissolution rate and intrinsic dissolution rate constant
of a drug
• Thermal effects
• Common ion effect 16
Stability Analysis

• Solution stability studies


• Solid state stability studies
• Stability in the presence of commonly used excipients
or compatibility studies

17
Analytical Research & Development

18
Analytical Research

• Assay development: HPLC assay, G.C. assay, stability


indicating assay, UV/Visible spectroscopy;
• Identification of probable degradation product, etc.

19
Analytical Development

• Bulk drug analysis


• Formulation drug assay (analysis)
• IND formulation stability

20
Molecular Optimization

21
• Identification of pharmacologically active
compound
• Developing an optimum drug molecule from the
point of view of the development (formulation)
of a dosage form, administration of the dosage
form, drug solubility, drug stability, and
bioavailability.
22
• Salts, pro-drugs, solvates, polymorphs, or even
new analogs may emerge as a result of this
molecular modification efforts.

23
• Erythromycin and doxycycline are good examples.
• Erythromycin estolate is an example of a pro-drug with
improved pharmaceutical properties.

24
• Erythromycin, a weak base, is water soluble, has a
very bitter taste, and its is very rapidly hydrolyzed
in gastric acid (t10%= 9 seconds) to yield the
degradation product.

25
• To overcome this problem, a water insoluble
(estolate) salt was formed for suspension and
capsule dosage forms.

Erythromycin estolate
26
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