Presentation include chapter solubility of drugs from second yr B-Pharm
Solubility, solubility expression, solute solvent interactions, solubility parameters, solvation and dissolution, factors affecting solubility, solubility of gases in liquids, liquids in liquids, fractional distillation, azeotropes, dissolution and drug release and diffusion.
The suspension dosage form has long been used for poorly soluble active ingredients for various therapeutic indications. Development of stable suspensions over the shelf life of the drug product continues to be a challenge on many fronts.
The presentation provides a concise information regarding various methods or techniques for enhancing solubility of different drugs and will prove useful to students & researchers.
Presentation include chapter solubility of drugs from second yr B-Pharm
Solubility, solubility expression, solute solvent interactions, solubility parameters, solvation and dissolution, factors affecting solubility, solubility of gases in liquids, liquids in liquids, fractional distillation, azeotropes, dissolution and drug release and diffusion.
The suspension dosage form has long been used for poorly soluble active ingredients for various therapeutic indications. Development of stable suspensions over the shelf life of the drug product continues to be a challenge on many fronts.
The presentation provides a concise information regarding various methods or techniques for enhancing solubility of different drugs and will prove useful to students & researchers.
Methods of Solubility Enhancement bt Mr.Vishal Shelke
https://youtube.com/vishalshelke99
https://instagram.com/vishal_stagram
Sub :- Biopharmaceutics & Pharmacokinetics
M.Pharmacy Sem 1
Savitribai Phule Pune University
Introduction :-
Solubility :-
“Solubility is the property of a solid, liquid, or gaseous chemical substance called solute to dissolve in a solid, liquid, or gaseous solvent to form a homogeneous solution of the solute in the solvent.”
Solubalization :-
“ A Preparation of thermodynamically stable isotropic solution of a substance normally insoluble or slightly soluble in a given solvent by introduction of an additional component
Importance of Solubility :-
Therapeutic efeectivness of a drug depends upon the bioavailability & ultimately upon the solubility of drug molecules
Solubility is one of the important parameter to achieve desired concentration of a drug in systemic circulation for pharmacological ressponse to be shown.
Currently only 8% of new drugs have both high solubility & Permeability.
Nearly 40% of the new chemical entities currently being discovered are poorely water soluble
Methods :-
Spray freezing into liquid (SFL)
Ultra-Rapid Freezing
Kneading Technique
Co-precipitation
Solubalizing Agents
Methods of Solubility Enhancement bt Mr.Vishal Shelke
https://youtube.com/vishalshelke99
https://instagram.com/vishal_stagram
Sub :- Biopharmaceutics & Pharmacokinetics
M.Pharmacy Sem 1
Savitribai Phule Pune University
Introduction :-
Solubility :-
“Solubility is the property of a solid, liquid, or gaseous chemical substance called solute to dissolve in a solid, liquid, or gaseous solvent to form a homogeneous solution of the solute in the solvent.”
Solubalization :-
“ A Preparation of thermodynamically stable isotropic solution of a substance normally insoluble or slightly soluble in a given solvent by introduction of an additional component
Importance of Solubility :-
Therapeutic efeectivness of a drug depends upon the bioavailability & ultimately upon the solubility of drug molecules
Solubility is one of the important parameter to achieve desired concentration of a drug in systemic circulation for pharmacological ressponse to be shown.
Currently only 8% of new drugs have both high solubility & Permeability.
Nearly 40% of the new chemical entities currently being discovered are poorely water soluble
Methods :-
Spray freezing into liquid (SFL)
Ultra-Rapid Freezing
Kneading Technique
Co-precipitation
Solubalizing Agents
A co solvent system is one in which a water miscible or partially miscible organic solvent is mixed with water to form a modified aqueous solution. And the phenomenon called Cosolvency
cosolvents have some degree of hydrogen bond donating and or hydrogen bond accepting ability as well as small hydrocarbon regions.
The resulting solution will have physical properties that are intermediate to that of the pure organic solvent and water through the reduction of water–water interaction.
Methods of enhancing Dissolution and bioavailability of poorly soluble drugsRam Kanth
Greetings!
Good Day to all...
Topic: Methods of Enhancing Bioavailability
Several approaches discussed are
1. Micrnoization
2. Use of Surrfactants
3. Use of Salt forms
4. Alteration of pH of microenvironment
5. Use of metastable polymorphs
6. Solute-Solvent Complexation
7. Solvent Deposition
8. Selective Adsorption on Insoluble Carriers
9. Solid Solutions
10. Eutectic Mixtures
11. Solid Dispersions
12. Molecular Encapsulation with Cyclodextrins
Please do clarify for doubts if any....
Thank you all for watching this presentation.
solubility enhancement and cosolvency by madhavishaikhazaroddin
“cosolvency and soluility enhancement” Pharmatech 2003, 160-166. They had developed simultaneous determination of sitagliptin phospate monohydrate and metformin by ultra performance liquid chromatographic (uplc)method.
A note on Microsperes , general introduction and method of preparationsNEELAMSOMANI4
This presentation is related to Microspheres. Microspheres as a part of novel drug delivery system relevant to Pharmaceutics. The general introductions and methodology is described that will be helpful to all pharmacy students .
Acorn Recovery: Restore IT infra within minutesIP ServerOne
Introducing Acorn Recovery as a Service, a simple, fast, and secure managed disaster recovery (DRaaS) by IP ServerOne. A DR solution that helps restore your IT infra within minutes.
This presentation, created by Syed Faiz ul Hassan, explores the profound influence of media on public perception and behavior. It delves into the evolution of media from oral traditions to modern digital and social media platforms. Key topics include the role of media in information propagation, socialization, crisis awareness, globalization, and education. The presentation also examines media influence through agenda setting, propaganda, and manipulative techniques used by advertisers and marketers. Furthermore, it highlights the impact of surveillance enabled by media technologies on personal behavior and preferences. Through this comprehensive overview, the presentation aims to shed light on how media shapes collective consciousness and public opinion.
0x01 - Newton's Third Law: Static vs. Dynamic AbusersOWASP Beja
f you offer a service on the web, odds are that someone will abuse it. Be it an API, a SaaS, a PaaS, or even a static website, someone somewhere will try to figure out a way to use it to their own needs. In this talk we'll compare measures that are effective against static attackers and how to battle a dynamic attacker who adapts to your counter-measures.
About the Speaker
===============
Diogo Sousa, Engineering Manager @ Canonical
An opinionated individual with an interest in cryptography and its intersection with secure software development.
Have you ever wondered how search works while visiting an e-commerce site, internal website, or searching through other types of online resources? Look no further than this informative session on the ways that taxonomies help end-users navigate the internet! Hear from taxonomists and other information professionals who have first-hand experience creating and working with taxonomies that aid in navigation, search, and discovery across a range of disciplines.
This presentation by Morris Kleiner (University of Minnesota), was made during the discussion “Competition and Regulation in Professions and Occupations” held at the Working Party No. 2 on Competition and Regulation on 10 June 2024. More papers and presentations on the topic can be found out at oe.cd/crps.
This presentation was uploaded with the author’s consent.
Sharpen existing tools or get a new toolbox? Contemporary cluster initiatives...Orkestra
UIIN Conference, Madrid, 27-29 May 2024
James Wilson, Orkestra and Deusto Business School
Emily Wise, Lund University
Madeline Smith, The Glasgow School of Art
4. Solubilisation of poor water soluble drug and further
to improve its bioavailability
Most of drugs are weakly acidic and weakly basic with
poor aqueous solubility
Solubility is one of the important parameter to
achieve desired concentration of drug in systemic
circulation for pharmacological response
Definition
Parts of solvent required for one part of
solute
Very soluble < 1
Freely soluble 1 - 10
Soluble 10 - 30
Sparingly soluble 30 - 100
Slightly soluble 100 - 1000
Very slightly soluble 1000 - 10,000
Insoluble > 10,000 4
5. Process of Solubilization
Step 1: Holes opens in the solvent
Step2: Molecules of the solid breaks away from the bulk
Step 3:The freed solid molecule is intergrated into the hole in the solvent
5
7. Factors affecting solubility:-
Particle Size:
The effect of particle size on solubility is given by Kelvin
equation
Where,
S =is the solubility of infinitely large
particles
S=is the solubility of fine particles
V= is molar volume
γ= is the surface tension of the solid
r =is the radius of the fine particle 7
10. I .PHYSICAL MODIFICATIONS
A. Particle size reduction
a. Micronization
b. Nanosuspension
B. Modification of the crystal habit
a. Polymorphs
b. Pseudopolymorphs
C. Drug dispersion in carriers
a. Eutectic mixtures
b. Solid dispersions
c. Solid solutions
D. Complexation
a. Use of complexing agents
E. Solubilization by surfactants
a. Microemulsions
b. Self microemulsifying drug delivery systems
10
12. A. Particle size reduction:
Particle size reduction can be achieved by
a.Micronization
b.nanosuspension
a. Micronization:
Colloidal mill
12
Micronization increases the dissolution rate of drugs
through increased surface area.
Micronization of drugs is done by milling techniques using
jet mill, rotor stator colloid mills etc.
Micronization is not suitable for drugs having a high dose
number because it does not change the saturation solubility
of the drug.
colloid mill
13. B.Nano suspensions
Homogenasation
The suspension is forced under pressure through a valve
that has nano aperture. This causes bubbles of water to
form which collapses as they come out of valves. This
mechanism cracks the particles.
Wet milling:
Active drug in the presence of surfactant is
defragmented by milling.
Other technquies
a)Sonocrystilisation
b)supercritical fluidprocess
13
14. Polymorphism
Drug dispersion carriers
The term “solid dispersions” refers to the dispersion of
one or more active ingredients in an inert carrier in a
solid state, frequently prepared by the
1.Hot melt method
2.Solvent evaporation method
3.Hotmelt extrusion method.
14
Amorphous >Metastable polymorph >Stable polymorph
17. Complexation:
Complexation is the reversible association between two or more
molecules to form a nonbonded entity with a well defined stiochiometry.
Complexation relies on relatively weak forces such as vanderwaal
forces, hydrogen bonding and hydrophobic interactions.
There are many types of complexing agents and a partial list can be
found in table.
17
18. Inclusion complex
Inclusion are formed by the insertion of the nonpolar
molecular the nonpolar region of one molecule (known as
guest) into the cavity of another molecule or group of
molecules (known as host).
Cyclodextrins are non-reducing,crystalline, water soluble,
cyclic, oligosaccharides. Cyclodextrins consist of glucose
monomers arranged in a donut shape ring
18
19. Staching complex :
Staching complexes are formed by the overlap of the planar
regions of aromatic molecules.
This causes some molecules to minimize the contact with water
by aggregation of their hydrocarbon moieties.
This aggregation is favored by large planar nonpolar regions in
the molecule.
Stached complexes can be homogeneous or mixed. The former
is known as self association and latter as complexation.
19
20. Surfactants
20
Surfactants are molecules with distinct polar
and nonpolar regions. Most surfactants consist
of a hydrocarbon segment connected to a
polar group. The polar group can be anionic,
cationic, zwitterionic or nonionic.
The presence of surfactants may lower the
surface tension and increase the solubility of
the drug within an organic solvent
21. Advantages of microemulsion over coarse emulsion ,It’s ease of
preparation due to spontaneous formation, thermodynamic
stability, transparent and elegant appearance, increased drug
enhanced penetration through the biological membranes,
increased bioavailability and less inter- and intra-individual
variability in drug pharmacokinetics.
21
Microemulsion
Internal
Co-
surfactant
External
surfactant
22. ii. CHEMICAL MODIFICATIONS
1) By change of pH:
For organic solutes that are ionizable,changing the pH of the
system is the simplest and most effective means of increasing
aqueous solubility.
2) Use of buffer:
Buffer maintains the pH of the solution overtime
and it reduces or eliminate the potential for precipitation upon
dilution. On dilution pH alteration occurs that decrease solubility .
22
Change of pH by 1 fold increase solubility by 10 fold
If it changes by one pH unit ,that decrease ionization of the drug and
solubility decreases by 10 fold.
24. Co-crystallization:
A co-crystal may be defined as a crystalline material that
consists of two or more molecular (and electrically neutral)
species held together by non-covalent forces.
Co-crystals are more stable, particularly as the co-
crystallizing agents are solids at room temperature.
Only three of the co-crystallizing agents are classified as
generally recognised as safe (GRAS) it includes saccharin,
nicotinamide and acetic acid limiting the pharmaceutical
applications.
Co-crystals can be prepared by evaporation of a
heteromeric solution or by grinding the components
together. Another technique for the preparation of co-
crystals includes sublimation, growth from the melt, and
slurry preparation. 24
25. 25
• Contd…
Hydrotrophy : It designate the increase in solubility in
water due to the presence of large amount of additives.
ex: sodium acetate, sodium alginate
Solubilizing agents: The solubility of poorly soluble
drug can also be improved by various solubilizing
materials
Ex:peg400,nimodipine
26. A drug administered in solution form immediately available for
absorption .
Solubility is a most important parameter for the oral
bioavailability of poorly soluble drugs.
Dissolution of drug is the rate determining step for oral
absorption of the poorly water soluble drugs, which can
subsequently affect the in vivo absorption of drug.
Currently only 8% of new drug candidates have both high
solubility and permeability.
Because of solubility problem of many drugs the bioavailability of
them gets affected and hence solubility enhancement becomes
necessary.
It is now possible that to increase the solubility of poorly soluble
drugs with the help of various techniques.
CONCLUSION
27. REFERENCES
1. Improving solubility & permeability in drug candidates.
Conference: 23rd & 24th June 2005,Pre-conference workshop:
22nd June 2005, Thistle Marble Arch, London, UK
2. http://www.sciencebyjones.com/Teaching%20Menu.htm
3. Solubility, From Wikipedia, the free encyclopedia. Retrieved
from http://en.wikipedia.org/wiki/Solubility
4.Lachman herbert A.libereman the thoery ofpractise industrial
pharmacy 2009;171-196
5.www.google.com
6.Review article:varunraj vemula
International journal pharmaceutics volume5 issue1 on
November –December 10th
7.Encylopedia of solubilisation & solubility