The document summarizes key aspects of preformulation studies. It discusses the objectives of preformulation which are to establish physicochemical parameters, stability, and compatibility with excipients. It then examines various physicochemical properties of drugs including organoleptic characteristics, bulk properties, solubility, crystallinity and polymorphism. Methods for analyzing properties like hygroscopicity, powder flow, and partition coefficient are also outlined. The importance of preformulation in developing stable dosage forms is emphasized.
The chapter deals with the preformulation studies that have to be considered while designing a dosage form and developing a formulation that is suitable for a patient. Here, physical and chemical properties of a drug substance are studied along with biopharmaceutical classification of drugs. Also a detailed study on the application of preformulation studies in different dosage forms are also studied.
Preformulation and physicochemical property of the drugSHIVANEE VYAS
“It is the study of the physical and chemical properties of the
drug prior to compounding process”.
Preformulation commences when a newly synthesized drug shows sufficient pharmacologic promise in animal models towarrant evaluation in man.
These studies should focus on physicochemical properties of new compound that affect drug performance & development of efficaciouss dosage form.
This properties may provide;
A rationale for formulation design
Support the need for molecular modification.
The chapter deals with the preformulation studies that have to be considered while designing a dosage form and developing a formulation that is suitable for a patient. Here, physical and chemical properties of a drug substance are studied along with biopharmaceutical classification of drugs. Also a detailed study on the application of preformulation studies in different dosage forms are also studied.
Preformulation and physicochemical property of the drugSHIVANEE VYAS
“It is the study of the physical and chemical properties of the
drug prior to compounding process”.
Preformulation commences when a newly synthesized drug shows sufficient pharmacologic promise in animal models towarrant evaluation in man.
These studies should focus on physicochemical properties of new compound that affect drug performance & development of efficaciouss dosage form.
This properties may provide;
A rationale for formulation design
Support the need for molecular modification.
Acetabularia Information For Class 9 .docxvaibhavrinwa19
Acetabularia acetabulum is a single-celled green alga that in its vegetative state is morphologically differentiated into a basal rhizoid and an axially elongated stalk, which bears whorls of branching hairs. The single diploid nucleus resides in the rhizoid.
Acetabularia Information For Class 9 .docxvaibhavrinwa19
Acetabularia acetabulum is a single-celled green alga that in its vegetative state is morphologically differentiated into a basal rhizoid and an axially elongated stalk, which bears whorls of branching hairs. The single diploid nucleus resides in the rhizoid.
2024.06.01 Introducing a competency framework for languag learning materials ...Sandy Millin
http://sandymillin.wordpress.com/iateflwebinar2024
Published classroom materials form the basis of syllabuses, drive teacher professional development, and have a potentially huge influence on learners, teachers and education systems. All teachers also create their own materials, whether a few sentences on a blackboard, a highly-structured fully-realised online course, or anything in between. Despite this, the knowledge and skills needed to create effective language learning materials are rarely part of teacher training, and are mostly learnt by trial and error.
Knowledge and skills frameworks, generally called competency frameworks, for ELT teachers, trainers and managers have existed for a few years now. However, until I created one for my MA dissertation, there wasn’t one drawing together what we need to know and do to be able to effectively produce language learning materials.
This webinar will introduce you to my framework, highlighting the key competencies I identified from my research. It will also show how anybody involved in language teaching (any language, not just English!), teacher training, managing schools or developing language learning materials can benefit from using the framework.
A workshop hosted by the South African Journal of Science aimed at postgraduate students and early career researchers with little or no experience in writing and publishing journal articles.
June 3, 2024 Anti-Semitism Letter Sent to MIT President Kornbluth and MIT Cor...Levi Shapiro
Letter from the Congress of the United States regarding Anti-Semitism sent June 3rd to MIT President Sally Kornbluth, MIT Corp Chair, Mark Gorenberg
Dear Dr. Kornbluth and Mr. Gorenberg,
The US House of Representatives is deeply concerned by ongoing and pervasive acts of antisemitic
harassment and intimidation at the Massachusetts Institute of Technology (MIT). Failing to act decisively to ensure a safe learning environment for all students would be a grave dereliction of your responsibilities as President of MIT and Chair of the MIT Corporation.
This Congress will not stand idly by and allow an environment hostile to Jewish students to persist. The House believes that your institution is in violation of Title VI of the Civil Rights Act, and the inability or
unwillingness to rectify this violation through action requires accountability.
Postsecondary education is a unique opportunity for students to learn and have their ideas and beliefs challenged. However, universities receiving hundreds of millions of federal funds annually have denied
students that opportunity and have been hijacked to become venues for the promotion of terrorism, antisemitic harassment and intimidation, unlawful encampments, and in some cases, assaults and riots.
The House of Representatives will not countenance the use of federal funds to indoctrinate students into hateful, antisemitic, anti-American supporters of terrorism. Investigations into campus antisemitism by the Committee on Education and the Workforce and the Committee on Ways and Means have been expanded into a Congress-wide probe across all relevant jurisdictions to address this national crisis. The undersigned Committees will conduct oversight into the use of federal funds at MIT and its learning environment under authorities granted to each Committee.
• The Committee on Education and the Workforce has been investigating your institution since December 7, 2023. The Committee has broad jurisdiction over postsecondary education, including its compliance with Title VI of the Civil Rights Act, campus safety concerns over disruptions to the learning environment, and the awarding of federal student aid under the Higher Education Act.
• The Committee on Oversight and Accountability is investigating the sources of funding and other support flowing to groups espousing pro-Hamas propaganda and engaged in antisemitic harassment and intimidation of students. The Committee on Oversight and Accountability is the principal oversight committee of the US House of Representatives and has broad authority to investigate “any matter” at “any time” under House Rule X.
• The Committee on Ways and Means has been investigating several universities since November 15, 2023, when the Committee held a hearing entitled From Ivory Towers to Dark Corners: Investigating the Nexus Between Antisemitism, Tax-Exempt Universities, and Terror Financing. The Committee followed the hearing with letters to those institutions on January 10, 202
Exploiting Artificial Intelligence for Empowering Researchers and Faculty, In...Dr. Vinod Kumar Kanvaria
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at Integral University, Lucknow, 06.06.2024
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Francesca Gottschalk - How can education support child empowerment.pptxEduSkills OECD
Francesca Gottschalk from the OECD’s Centre for Educational Research and Innovation presents at the Ask an Expert Webinar: How can education support child empowerment?
A Strategic Approach: GenAI in EducationPeter Windle
Artificial Intelligence (AI) technologies such as Generative AI, Image Generators and Large Language Models have had a dramatic impact on teaching, learning and assessment over the past 18 months. The most immediate threat AI posed was to Academic Integrity with Higher Education Institutes (HEIs) focusing their efforts on combating the use of GenAI in assessment. Guidelines were developed for staff and students, policies put in place too. Innovative educators have forged paths in the use of Generative AI for teaching, learning and assessments leading to pockets of transformation springing up across HEIs, often with little or no top-down guidance, support or direction.
This Gasta posits a strategic approach to integrating AI into HEIs to prepare staff, students and the curriculum for an evolving world and workplace. We will highlight the advantages of working with these technologies beyond the realm of teaching, learning and assessment by considering prompt engineering skills, industry impact, curriculum changes, and the need for staff upskilling. In contrast, not engaging strategically with Generative AI poses risks, including falling behind peers, missed opportunities and failing to ensure our graduates remain employable. The rapid evolution of AI technologies necessitates a proactive and strategic approach if we are to remain relevant.
Macroeconomics- Movie Location
This will be used as part of your Personal Professional Portfolio once graded.
Objective:
Prepare a presentation or a paper using research, basic comparative analysis, data organization and application of economic information. You will make an informed assessment of an economic climate outside of the United States to accomplish an entertainment industry objective.
A review of the growth of the Israel Genealogy Research Association Database Collection for the last 12 months. Our collection is now passed the 3 million mark and still growing. See which archives have contributed the most. See the different types of records we have, and which years have had records added. You can also see what we have for the future.
1. Sinhgad Technical Education Society’s
Sinhgad institute of pharmacy narhe, Pune 3/17/2023
1
Presented by –
Mr. Pavan B. Zalte
1st year M. Pharm
(Pharmaceutics)
Guided by-
Prof. Supriya Nikam
Department of pharmaceutics
3. PREFORMULATION
Introduction
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Investigation of physical, chemical and mechanical properties of drug
molecule in order to develop safe, effective, and stable dosage form.
This information may dictate many of subsequent event & approaches
in formulation development. This first learning phase is called as
preformulation
4. To establish the physicochemical parameters of drug entity
To determine its kinetics and stability
To establish its compatibility with common excipients
It provides insights into how drug products should be processed and
stored to endure their quality
Objectives
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6. • Colour, odour, taste of the drug must be recorded
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COLOUR ODOUR TASTE
white Pungent Acidic
Cream yellow Sulphurous Bitter
tan Fruity Bland
shiny Aromatic Intense
Odourless Sweet
Tasteless
Organoleptic characters
7. 3/17/2023 7
Physicochemical properties of drug
Bulk
character
Hygroscopicity
Powder flow
properties
Fine particle
characterization
Crystallinity &
polymorphism
8. Crystallinity
• A crystalline particle is characterized by definite external and internal
structures.
• Crystal habit - external shape of a crystal
• Polymorphic state - refers to the definite arrangement of molecules
inside the crystal lattice.
• During crystallization, molecule may arrange themselves in various
geometric configurations, resulting in distinct packing arrangement or
orientation in crystal structure.
3/17/2023 8
10. • Amorphous:
Amorphous drug has atoms or molecules randomly placed (without definite
structure) within them. The amorphous form is of higher thermodynamic
energy, greater solubility as well a higher dissolution rate than the
corresponding crystalline form.
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Low mobility
(crystalline)
Moderate mobility
(Amorphous)
11. It is the ability of the compound to crystallize as more than one distinct
crystalline species with different internal lattice.
Polymorphs are of 2 type
• Enantiotropic
• Monotropic
The polymorph which can be reversibly changed from one form into another
by varying temp or pressure is called as enantiotropic polymorph.
Eg. Sulphur.
3/17/2023 11
Polymorphism
12. Polymorph which is unstable at all temperature & pressure is called as
Monotropic polymorph. Eg. Glyceryl stearate.
Polymorphs differ from each other with respect to their physical
property such as
• Solubility
• Melting point
• Density
• Hardness
• Compression characteristic
Eg. Chloromphenicol exist in A,B & C forms, of these B form is more
Stable & most preferable. 3/17/2023 12
13. Methods for analysing polymorphs
• Microscopy
• Optical crystallography
• DSC (Differential Scanning Calorimetry)
• TGA (Thermogravimetric Analysis)
• XRD (X Ray Diffraction)
• IR (Infra Red)
• SEM (Scanning Electron Microscopy) 3/17/2023 13
14. Hygroscopicity
• Many drug substances have tendency to adsorb atmospheric moisture.
• Hygroscopicity classified into four classes:
1. Slightly hygroscopic: increase in weight is >0.2%w/w & <2%w/w
2. Hygroscopic: increase in weight is >2%w/w & <15%w/w
3. Very hygroscopic : increase in weight is >15%w/w.
4. Deliquescent : Sufficient water is adsorbed to form solution
Change in moisture level can influence
• Chemical stability
• Flowability
• Compactibility 3/17/2023 14
15. •Powder flow properties
3/17/2023 15
Test to evaluate the flowability of
powder
Carr’s compressibility index
Hausner ratio
The angle of repose (θ)
16. • A volume of powder is filled into a glass cylinder and repeatedly
tapped for a known duration.
• The volume of powder after tapping is measure.
Bulk density = weight/ bulk volume
Tapped density = weight/ true volume
• Carr’s compressibility index
3/17/2023 16
20. 3/17/2023 20
Hausner ratio and flow
propertes
Flow character Hausner ratio
Excellent 1.00-1.11
Good 1.12-1.18
Fair 1.19-1.25
Passable 1.26-1.34
Poor 1.35-1.45
Very poor 1.46-1.59
Very Hauser poor >1.60
21. The angle of repose
• The maximum angle which is formed between the surface of pile of powder and
horizontal surface is called the angle of repose.
tan θ = h / r
where,
h = height of pile
r = radius of base of pile
3/17/2023 21
25. 3/17/2023 25
Solubility studies
Descriptive term Parts of solvent required for 1
part of solute
Very soluble <1
Freely soluble 1 to 10
soluble 10 to 30
Sparingly soluble 30 to 100
slightly solube 100 to 1000
Very slightly soluble 1000 to 10000
Practically insoluble or insoluble 10000 and over
26. • Solubility and absorbtion can altered by changing pH
• The Henderson -Hasselbach equation provides an estimate of the ionized
and unionized durg concentration at a particular pH.
For acidic compounds,
pH = pKa + log (un-ionized drug) / [ionized drug]
for basic compounds,
pH = pKa + log (ionized drug) / [un-ionized drug]
3/17/2023 26
Ionization constant- pKa
27. • For very weakly acidic drug (pKa >8) such as phenytoin and ethosuximide,
or for very weakly basic drugs, (pKa<5), such as diazepam the unionized
form is present throughout the GIT and there absorption is rapid.
• For weakly acidic drug (pKa= 3-7), such as aspirin and ibuprofen, the
unionized form is present within the acidic contents of the stomach, but the
drug is ionized in intestinal media. Such drugs are better absorbed from
stomach.
• For weakly basic drug (pKa=5-8), such as morphine and choroquine the
unionized form is present within the basic content of the intestine, but drug
is ionized in acidic media of stomach. Such drug are better absorbed from
intestine.
• For strongly acidic drugs, such as cromolyn sodium or strongly basic drugs
such as erythromycin ,the ionized form is in both the stomach and intestine.
3/17/2023
27
28. An incompatibility in the dosage form can result in any of the
following changes :
3/17/2023 28
Drug-excipient compatibility
Changes in
organoleptic
properties
Changes in dissolution
performance
Physical
form
conversion
Decrease in
potency
An increase in
degradation
products
29. • Dissolution of drug particle is controlled by following factors:
3/17/2023 29
Dissolution
Dissolution
Crystal habit
Particle
size
Temperature
Surface
area
30. Partition coefficient
• The ratio of unionized drugs dispersed between the organic (n-octanol) and
aqueous (water) phases at equilibrium is known as the partition coefficient
(P).
• This is helpful to predict drugs’ ability to cross cell membrane.
3/17/2023 30
Partition coefficient
Partition coefficient =0 drug equally soluble in water and organic solvent
Partition coefficient >1 = drug is lipophilic
Partition coefficient <1 = drug is hydrophilic
32. Stability analysis
3/17/2023 32
The primary objective of this study is investigation and identification of stable
storage condition for drug in the solid state and identification of compatible
excipients for a formulation.
Types of stability Conditions
maintained during
the shelf life of
product
Chemical Retains its chemical
integrity and
potency
Physical Retains appearance,
palatability
Threapeutic effect Drug action remains
unchanged
33. • Preformulation study helps to develop safe, effective and stable dosage form.
• Preformulation has an impact on the selection of the drug candidate,
formulation components, physicochemical properties of drug.
• Preformulation studies focus on the physicochemical properties of new
compound that could affect the drug performance.
• Preformulation study also focus on the stability and solubility of drug
3/17/2023 33
Conclusion
34. Refrences
1. Vilegave K, Vidyasagar G, Chandankar P. Preformulation studies of
pharmaceutical new drug molecule and products: an overview. The american
journal of pharmacy. 2013;1(3):1-20.
2. Chaurasia G. A review on pharmaceutical preformulation studies in formulation
and development of new drug molecules. International J. Of pharmaceutical
science and research. 2016 june 1;7(6):2313-0
3. Hasan MM, Al Habib S, islam MM, Islam MM, Karim MS, Banik K, Rashid
HA. Pharmaceutical preformulation for product development & analytical
techniques use in new dosage form. International journal of pharmacy &
therapeutics. 2017;8(1):16-32.
4. Leon lachman / Lieberman’s , The theory and practice of Industrial Pharmacy .
Indian 4rth edition CBS publisher, reprint 2020, page no.217-251
3/17/2023 34
35. 5. Michael E Aulton, Pharmaceutics- The design and manufacture of medicines, 3rd
International edition, page no. 23-24
6. Remington, Pharmaceutics- The science and practice of pharmacy, Volume 1, 20th edition,
Page no. 705.
7. D. M. Brahmankar and Sunil B. Jaiswal, Biopharmaceutics and Pharmacokinetics- a
treatise, Vallabh Prakashan, Page no. 27-29.
3/17/2023 35