PREFORMULATION STUDIES OF TABLETS IT ALSO INCLUDES SEDEM STUDIES WHICH IS BASED ON THE QBD DESCRIBED ICH Q 8 . IN THIS STUDIES CANNABIDIOL IS CONSIDERED AND IT IS BCS CLASS 2 HENCE DISSOLUTION WAS CHALLENGING IN THEM SO IN THE ABOVE STUDIES THEY CAME UP WITH THE IDEA OF AN ORODISPERSIBLE TABLET OF CANNABIDIOL. THE ABOVE CASE STDUY IS TAKEN FROM SAUDI JOURNAL OF PHARMACEUTICS AND HAS A IMPACT FACTOR OF 4.66. THE CREDITS OF CASE STUDIES GO TO THE RESPECTIVE RESEARCH SCIENTIST.

1. BHARATI VIDYAPEETH (DEEMED UNIVERSITY)
POONA COLLEGE OF PHARMACY, PUNE
PREFORMULATION STUDIES OF TABLETS
DEPARTMENT OF PHARMACEUTICS
Presented By
Nagabhushan Shet
M. Pharm 1st Year ( I semester)
POONA COLLEGE OF PHARMACY, PUNE 1

2. CONTENTS
1.Introduction
2.Objectives
3.Major area of pre-formulation research
- Organoleptic characters
- Bulk characterization
- Solubility characters
- Stability characters
4.Case study
5. Results and discussion
6. conclusions
7. References
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3. PREFORMULATION
 Pre-formulation is a group of studies that focus on the physicochemical properties of a new drug candidate
that could affect drug performance and the development of a dosage form.
 This could provide important information for formulation design or support the need for molecular modification.
 Every drug has intrinsic chemical and physical properties which have been considered before development of
pharmaceutical formulation.
 This property provides the framework for drugs in combination with pharmaceutical ingredients in the
fabrication of dosage forms.
 The overall objective of pre formulation testing is to generate information useful to the formulator in developing
stable and bioavailable dosage forms which can be mass-produced.
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4. POONA COLLEGE OF PHARMACY, PUNE 4

5. OBJECTIVES
 To establish the Physicochemical parameters of a new drug entity.
 To determine its kinetics and stability.
 To establish its compatibility with common excipients.
 It provides insights into how products should be processed and stored to ensure their quality.
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6. PRINCIPLE AREAS OF RESEARCH IN PREFORMULATION STUDIES
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7. Organoleptic properties of the drug:
 Organoleptic properties are the aspects that can be experienced through ones senses like taste, smell, sight, and
touch.
 Thus, it includes a recording of the colour,odour, and taste of the drug.
Bulk characters of the drug:
 Crystallinity-Crystallinity refers to the outer appearance and internal structure of the drug molecule and can
affect its physicochemical properties.
 Polymorphism is the ability of a compound to crystallize in different shapes with different internal structure.
 Hygroscopicity-It is the measure of the tendency to adsorb atmospheric moisture by the drug substance. It
characterizes the drug stability with respect to the environmental humidity.
 Fine particle characterization- The size of the drug particle can influence its dissolution rate, suspend ability
and other properties. Thus, it becomes important to classify the drug substances as coarse, moderately coarse,
very coarse, fine, and very fine.
 Powder flow properties- Since the majority of active pharmaceutical ingredients are delivered as powders,
either as a pill or for dissolution, understanding and controlling the powder behavior of drugs are extremely
important. Powder flow properties help you understand the ease with which the drug powder will flow under a
set of specific conditions like humidity, pressure.
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8. Solubility analysis
 Ionization constant- pKa is the measurement of the acidity of the compound. Its determination helps in understanding the
solubility, protein binding, and permeability of the drug substance to characterize its properties like absorption, distribution,
metabolism and excretion from the body.
 pH solubility profile helps to understand the influence of pH on drug solubility, stability, and absorption.
 Common ion effect (Ksp) determines the solubility of the drug substance when a soluble compound having a common ion
with the drug is added to the test solution.
 Thermal effects help to evaluate the drug solubility with respect to the changes in the temperature of the solvent.
 Solubilization is the method of increasing the solubility of sparingly soluble drug substance by various techniques like
adding a co-solvent, changing the pH and temperature, adding a surfactant, reducing the particle size etc.
 Partition co-efficient is the measurement of the drug lipophilicity or ability to cross a cell membrane.
 Dissolution is the process of resolving the drug substance into its individual components and characterizing their properties.
Stability analysis
The stability of the drug is studied with respect to various factors like-
 Solution stability
 pH-rate profile
 Solid state stability
 Bulk stability
 Compatibility
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9. POONA COLLEGE OF PHARMACY, PUNE 9

10. AIM
To select suitable excipients for developing orodispersible tablet (ODT) containing cannabidiol (CBD) by direct
compression method.
OBJECTIVE
Obtaining Oro dispersible tablets (ODT) containing substances from the second Biopharmaceutical Class has
raised concerns as the dissolution test is challenging.
CASE STUDY
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11. Year of Publication:
2021
Impact factor:
4.33

12.  In this studies the drug compatibility
with excipients was verified by DSC
and FTIR spectroscopy
 Excipients were characterized by
using SeDeM-ODT tool and one with
best results was taken into
consideration.
Materials and methods
Role Materials Abbreviations
API Cannabidiol CBD
Fillers Lactose LCT
Fillers Microcrystalline
cellulose
CelMC
Disintegrants Sodium starch
glycolate
SSG
Disintegrants Sodium
croscarmellose
CCS
Sweetners Sorbitol SRB
Sweetners Mannitol MNT
Co-processed
excipients
Prosolv-ODTG2 PODTG2
Co-processed
excipients
Prosolv easy tab
sp
PETSp
POONA COLLEGE OF PHARMACY, PUNE 12

13. Drug cannabidiol
IUPAC name 2-[(1R,6R)-3-methyl-6-prop-
1-en-2-ylcyclohex-2-en-1-
yl]-5-pentylbenzene-1,3-
diol
Molecular formula C21H30O2
Molecular weight 314.5g/mol
BCS classification Type II
Solubility 0.7 µg/mL
Melting point 66 °C (151 °F)
Drug class hallucinogen
DRUG PROFILE
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14.  SeDeM diagram is based on the quality by design (QBD) described in ICH Q8 .since it evaluates
critical quality attributes that have impact on the final product quality.
 The SeDeM diagram expert system provides the profile of excipients and API in powder form
with the respect to their suitability for direct compression.
 Three numerical forms are
• IGCB –Index for good compressibility and bucCo dispersibility.
• IP – Index Parameter
• IPP – Index Profile Parameter
 Index parameter (IP) = NP≥5/ NPt
where , NP≥5 = number of parameters with a value equal or higher than 5.
NPt = Total number of parameters studied.
 The acceptability limit would correspond to IP ≥5
SEDEM STUDIES
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15.  Index Profile Parameter (IPP) = mean r of all parameters studied.
 The acceptance limit is IPP = Mean r ≥ 5.
 Index of Good Compressibility and Bucco dispersibility (IGCB) is calculated as follows i.e.,
IGCB =IPP *f
where , f- reliability factor and is calculated by
f= polygon area / circle area
 The acceptance limit is IGCB ≥ 5
 NOTE that IGC and IGCB are not same

16.  Under SeDeM – ODT tool 6 factors were described they are
1. Dimensions
2. Compressibility
3. Flowability
4. lubricity/ dosage
5. Lubricity/stability
6. Disintegration abilItiy
Results and discussions
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17. SEDEM – ODT RESULTS

18.  SeDeM – ODT expert sytem for fillers :

19.  SeDeM – ODT expert system for sweeteners :

20.  SeDeM – ODT expert system for CBD and co processed excipients :

21.  SeDeM – ODT expert system for disintegrants:

22.  Taking into consideration the results obtained using the SeDeM-ODT diagrams, the API and possible excipients
that could be used for developing orodispersible tablets were evaluated.
 IGCB showed us that the best excipients that could be used to obtain orodispersible tablets were PODTG2 and
PETsp, also LCT and CELMC presented good IGCB values.
 From the two co-processed excipients PODTG2 needs just one improvement represented by the taste, while if
PETsp is used to obtain ODT, a sweetener and a flavour should be added to the composition.
 Fast disintegration represents another critical parameter. The possibility of using a mixture of super disintegrants
could improve this property.
 In the end, we can conclude that from an analytical point of view each excipient could be used to obtain ODTs but
from a pharmacotechnical point of view, some of the excipients need improvement.
conclusions
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23. THEORY
 Lachman and Liebermann's “ The Theory and Practice of Industrial Pharmacy” Fourth Edition, page no- 91-92
 Remington, “The Science and Practice of Pharmacy” Volume-I, Chapter 2, page no.83
CASE STUDY
 J.Sauri,D.Millan,J.M.Sune-Negre,P.Perez-Lozano,C.Carrillo,M.Minarro,J.R.Tico “The use of the SeDeM diagram
expert system for the formulation of Captopril SR matrix tablets by direct compression” International Journal of
Pharmaceutics, 2014 July 29: 38-45
 Robert-Alexandru Vlad, Paula Antonoaea, Nicoleta Todoran, Daniela-Lucia Muntean, Emoke Margit Rédai , Oana
Alexandra Silași, Anamaria Ta˘taru , Magdalena Bîrsan, Silvia Imre , Adriana Ciurba “Pharmacotechnical and
analytical preformulation studies for cannabidiol orodispersible tablets” Saudi Pharmaceutical Journal, 2021 July 4:
43-56
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REFERENCES