1. Preformulation studies involve characterizing the physical and chemical properties of a new drug substance to help design an optimal dosage form. This includes determining solubility, stability, and compatibility with excipients. 2. The physical properties studied include polymorphism, solubility, and organoleptic characteristics. Chemical properties like hydrolysis, oxidation, reduction, racemization, and polymerization are analyzed to understand the drug's degradation pathways. 3. Understanding the preformulation properties helps ensure development of a safe, stable, and effective dosage form to deliver the drug to patients.

1. NARASARAOPETA INSTITUTE OF PHARMACEUTICAL SCIENCES
Practice School Review-1 Presentation on
PREFORMULATION STUDIES
GUIDED BY :
DR. K.VENKATA GOPAIAH M. Pharm, Ph.D.
Associate Professor
Department of Pharmaceutics
NIPS.
PRESENTED BY:
Name: Shaik Vahedunnisa
Reg no:20CD1R0091
IV-B. Pharmacy
Department of Pharmaceutics
NARASARAOPETA INSTITUTE OF PHARMACEUTICAL SCIENCES
Kotappakonda road, Narasaraopet(M), Palnadu (D) Pin : 522601
2023-24

2. INTRODUCTION
● Preformulating involves the application of biopharmaceutical
principles to the physicochemical parameters of a drug with the goal of
designing an optimum drug delivery system. [1]
● Each drug substance has intrinsic chemical and physical
characteristics that must be considered before development of a
pharmaceutical formulation.
● So, the characterization of drug molecule is very important step at the
preformulating phase of product development.

3. DEFINITION
● The word pre - formulation refers to the step to be undertaken
before formulation. It includes determination of physical and
chemical properties of drug substances. Preformulating main goal
is to develop a new drug with safe, stable and effective[1]

4. ADVANTAGES
● Help in lead identification during drug discovery phase.
● Preformulating provide information regarding degradation
process adverse
condition relevant to the drug.
● Quick and statistically meaningful.

5. DISADVANTAGES
● Resistance arises from a spherical particle, thus
nanospheres are sized inaccurately.
● Tendency of needle shaped crystal to block the aperture
hole.
● Dissolution of compound in the aqueous conducting
medium.

6. IMPORTANCE OF
PREFORMULATION
● To form desired quality dosage form.[2]
● To develop an optimum dosage form.
● For targeted drug delivery system.
● To minimize cost of finished product.
● To minimize errors in formulations of dosage form.

7. GOALS AND OBJECTIVES
● To establish the physio-chemical parameters of a new drug
entity.[2]
● To determine its kinetics and stability.
● To establish its compatibility with common excipients
● To develop optimal drug delivery system

8. PHYSICAL PROPERTIES
1.Organoleptic characteristics:[3]
● Color, odor, taste of the new drug must be recorded.
2.Physical forms:
● Depending on internal structure compounds is classified as
A.Crystalline (Solid)
B. Amorphous (powder form

9. Crystalline (Solid):
In crystalline form atoms or molecules are arranged in highly ordered form
and is associated with a three - dimensional array.
Amorphous (powder form):
● In amorphous form atom or molecule are randomly placed
● Solubility & dissolution rate are greater for amorphous form than
crystalline, as amorphous form has higher thermodynamic energy.
Eg. Amorphous form of Novobiocin is well absorbed
Where crystalline form results poor absorption.

10. POLYMORPHISM
● It is the ability of the compound to crystallize as more than one distinct crystalline species
with different internal lattice. [4]
● Different crystalline forms are called polymorphs
● Polymorphs are of 2 types
A. Enantiotropic
B. Monotropic
● The polymorph which can be changed from one form into another by varying temperature
or pressure is called as Enantiotropic polymorph. Eg. Sulphur.
● One polymorph which is unstable at all temperature & pressure is called as Monotropic
polymorph.
Eg. Glyceryl stearate

11. DESCRIPTIVE TERM PARTS OF SOLVENT REQUIRED
FOR 1PART OF SOLUTE
Very soluble Less than 1
Freely soluble From 1-10
Soluble From 1-30
Sparingly soluble From 30-100
Slightly soluble From 100-1,000
Very slightly soluble From 1,000-10,000
Practically soluble 10,000 and over

12. STABILITY ANALYSIS
There are three types of stability analysis
1.Solid state stability
2. Solution state stability
3. Drug - excipient compatibility studies.

13. CHEMICAL PROPERTIES
1. Hydrolysis
2. Oxidation
3. Reduction
4. Racemization
5. Polymerization.

14. 1.HYDROLYSIS
● If breaking of molecule is due to reaction with water, then it is
called Hydrolysis.[5]
● It is a step in degradation of substance. Drugs such as esters,
amides and lactams undergo hydrolysis.
● Follows second order kinetics.

15. 2.OXIDATION
● Semiconductors can be oxidized by various methods,
including thermal oxidation and plasma enhanced
chemical vapor deposition.
● Among these thermal oxidation is most commonly
used.
● It is a key process in modern silicon technology
● Loss of electron

16. 3.REDUCTION
● Reduction is a relatively more common pathway of drug
metabolic process.
● Hepatic microsomes catalyze diverse reductive chemical
reaction
and require NADPH for this purpose Azo and Nitro reduction is
catalyzed by cytochrome P-450
● Chloral hydrate is reduced to it's active metabolite trichloro
ethanol by alcohol dehydrogenase.
● Gain of electrons.

17. 4.RACEMIZATION
● A Process of conversion of optically active compound into an
optically inactive compound.
● Half of the compound become its mirror images
● Rate of racemization depends in the presence of catalytic
hydrogen, hydroxyl ion, heat, light, temperature and solvent.
● These conversion can make the drug inert

18. 5. POLYMERIZATION
● Polymerization is a form of chemical degradation where
two/more identical molecule combined to form large
complex molecule known as polymers
● It can also be defined as a process in which simple
monomer molecules combined to form large complex.

19. CONCLUSION
● Preformulation studies on a new drug molecule provide
useful information for subsequent formulations of a
physicochemical stable & bio pharmaceutically suitable
dosage form.
● Preformulation work is the foundation of developing
efficacious and economical formulations.

20. REFERENCE
1. CH, Popovich GN and Allen VL. Ansel‟s Pharmaceutical Dosage Forms
and Drug Delivery Systems. Lippincott Williams and Wilkins, New York,
2005. P. 042-111.
2. Preformulation in: Aulton ME (Ed). Pharmaceutics -The Science of
Dosage form Design Churchill Livingston; 1996. P. 113-138.
3. The Theory and Practice of Industrial Pharmacy. Lachman L, Lieberman H
A, Joseph L K. 3 rd Ed, Varghese publishing house, Mumbai, 2008 p. 171-
196.Vilegave et. Al., Am. J. Pharmacy & Health Res 2013;1(3) ISSN:
2321-3647 www.ajphr.com 20
4. Absorption of drugs in: Brahmankar DM, Jaiswal SB. Biopharmaceutics
and Pharmacokinetics A treatise.1 st ed. Vallabh Prakashan; 1995. P. 5-
75.

21. REFERENCE
4. Leon Lachman, Liberman. The theory and practice of Industrial
pharmacy, Edn 4. CBS publishing house, New Delhi.2013 p:217-307.
Banker GS, Rhodes CT. Modern pharmaceutics, Edn 4. Marcel Dekker,
New York. 2002 p:167-184.
5. Loyd V. Allen, Nicholas Popovich, Howard C. Ansel. Ansel’s
pharmaceuticalDosage forms & Drug delivery systems, Edn 8.
B.I.Publication pvt. Ltd, p:187- 193,42 & 43,126-133.
6. Brahmankar D.M, Jaiswal BS. Biopharmaceutics and
pharmacokinetics aTreatise, Edn 2. Vallabh Prakashan, Nagpur. 2009; p:
37-45