This document discusses preformulation studies, which characterize a drug molecule's physical and chemical properties to develop a safe, effective, and stable dosage form. Preformulation helps assess a molecule's suitability for development and reduces risks. It provides data to screen lead compounds and guide appropriate dosage design. The objective is to select the right drug substance, excipients, and packaging to minimize issues in later development stages. Key preformulation study parameters include solubility, permeability, compatibility, and properties like pH and polymorphism. Preformulation assists both drug discovery and development.

1. Pharmacy Practice School
2021
Session- 02
FORMULATION & DEVELOPMENT
SPEAKER:
Mr. Namdeo G. Shinde
Assistant Professor,
Department of Pharmaceutics,
Satara College of Pharmacy,
Degaon, Satara MS India

3. Preformulation is defined as the phase of research
and development in which preformulation studies
characterize physical and chemical properties of
drug molecule in order to develop safe , effective and
stable dosage form.

4. Preformulation studies help in assessing the
‘drugability’ of a molecule. Preformulation can thus
be considered as critical decision-making tool during
both drug discovery and development phase.

5. In any pharmaceutical company, the R&D team is at
the forefront in generating newer concepts for
furthering the brand development of the company

6. This department is responsible for identifying a new
potential moiety amongst several screened
compounds based on the physicochemical as well
as biological activities for treatment of target
maladies.

7. Preformulation becomes an effective tool assisting
researchers in generation of physicochemical and
biopharmaceutical data for screening of lead
compounds.
Hence, this necessitates a scientific collaboration
between drug discovery and formulation scientists
for avoiding the risk of failure in the later stage of
product development.

8. preformulation provides comprehensive knowledge
about the characteristics of new chemical entity that
is crucial at the early development stage.
This will also enhance the fundamental knowledge
required for screening and the design of appropriate
dosage form. Thus, reducing the overall drug
development expenditure and facilitate the
commercialization of the product.

9. The objective of preformulation studies is to select
the right drug substance, excipients, and packaging
material used in product development.

10. Hence to minimize all these formulation and delivery
issues during the later stages of product
development and registration, there is always a need
for preformulation studies before the development
stage

11. Drug Product Life Cycle

12. Solubility
The Permeability of the Drug
Bulk Characterization: Physical,
Analytical, and
Physicochemical
Inherent Properties: pH, pKa, Log P, Log D, and
Intrinsic
Dissolution
Preformulation study parameters

13. Drug-Excipient Compatibility
Particle Size and Distribution
Thermal Properties
Hygroscopicity
Bulk Properties
Mechanical Properties and
Compatibility
Crystallinity
Polymorphism

14. Role of Preformulation Study in Drug Discovery
 Material Properties in Lead
 Selection, High Throughput Preformulation
Studies
 “Drugability” of New Chemical Entities
 Tools to Assist in Lead Selection

15. Role of Preformulation in Drug
Development
 Identification of Challenges
 During Formulation Development: Pre-
Assumptions
 The Dosage Form Specific Studies

16. o Preformulation Studies of Proteins and Peptides
o Preformulation in Vaccine Development: Critical
Views
oPreformulation Studies of Packaging Components

17. Computerization and Aid of Software in the
Preformulation Studies
Artificial Neural Network Tool Used in the Factorial
Design: An Optimization Approach