Solubility and
Complex Equilibria (PHS 991)
Instructor: Michalakis
Savva, Ph.D. Fall 2005
Contact
Information: Office: HS
610
Telephone: 488-1471
e-mail: msavva@liu.edu
Website: myweb.brooklyn.liu.edu/msavva/
Course description
This is a core course in the Ph.D. program. It
investigates solution’s theory and emphasizes solubility and solubilization of
drug molecules. The approach to this study is based on theoretical and physical
foundations, and leads to the application of the theory to systems of
pharmaceutical importance. The prerequisites for this course are Physical
Chemistry I (PHS 701) and Calculus I and II (MAT 40 and MAT 100, respectively).
Physical Chemistry II (PHS 702) and Differential Equations I (MAT 610) are not
required but they are highly recommended.
Grades will be based on three quizzes (5% each), one
Midterm exam (35 %) and a cumulative final exam (50 %). The grading scale will be determined at the
end of the course. No grades will be dropped. If an exam is missed for any reason, the
lowest numerical grade from the other exams (Quizzes, Midterm and Final) will
be entered for the missed exam grade at the end of the semester. If both
midterm and final exam are missed, zero will be entered for both exams. It the
final exam is missed, a grade of incomplete will be submitted to the registrar
and a make up will be given at a time and day determined by the instructor.
The material for the exams will be extracted from the assigned text books, from
lectures and other handouts/scientific articles.
Required Texts
Samuel
H. Yalkowsky, Solubility and Solubilization in Aqueous Media,
Book
can be purchased from PolySurfaces Bookstore at www.polysurfacesbookstore.com
tel. 603 5430038
A.
Martin, et al, Physical Pharmacy, 4th
Edition, Lea & Febiger, 1993.
Physical
Chemistry
Objective
Upon completing this course, students should be able
to:
● Describe and calculate the properties
of solutions.
● Understand factors that govern
solubility, in general, and aqueous solubility in particular.
● Describe and determine the properties
of solute, critical in evaluating the solubility and solubilization of it in
aqueous media.
● Apply the various techniques available
for altering the solubility and dissolution rate of organic compounds in
aqueous media.
Chapter 0: Fluids
0.1. Fluid Classification
0.2. Properties of Fluids
0.2.1. Density
0.2.2. Pressure
0.3.
Fluids at rest
0.3.1.
Applications of Pascal’s Principle
0.4.
Archimedes’ Principle
0.4.1.
Apparent Weight in a Fluid
0.5
Ideal Fluids in Motion
0.5.1
Streamlines and Velocity of Fluids
0.6.
The Equation of Continuity
0.7.
Bernoulli’s Equation
Chapter
1: Mixing and Properties of Mixing
1.1. Thermodynamics of Mixing
1.2. Description of Mixtures
1.3. Colligative Properties
1.4. Other Properties of Mixtures
CHAPTER 2: Characterization of
Solutions
2.1. Ideal Solutions
2.2. Athermal Nonideal Solutions
2.3. Regular Solutions
2.4. Solvated Solutions
2.5. Self-Associated Solutions
2.6. Solvated, Self-associated solutions
2.7. Aqueous Solutions
CHAPTER 3: Solubility and Partial
Miscibility
3.1. Partial Miscibility of Liquids
3.2. Critical Solution Temperatures
3.3. Solubility and Activity Coefficient of Liquid
Solutes
3.4. Solubility of Crystalline Solutes
3.5. Dependence of Solubility on Gas Properties
3.6. Alteration of Aqueous Solubility
3.7 Temperature and Solution Composition
CHAPTER 4: Physical Modification
of the Solute
4.1. Apparent Solubility and Dissolution Rate
4.2. Particle Size and Crystal Quality
4.3. Amorphic Solid Modification
4.4. Crystal Form Modification
4.5. Crystal Hydrate Formation
4.6. Complex Systems
4.7. Factors Affecting Reversion
CHAPTER 5: Solubilization by pH
Control
5.1. Buffers
5.2. Dependence of Solubility on pH
5.3. Dependence of pKa on Solute Structure
5.4. Temperature and Solution Composition
5.5. Pharmaceutical Aspects of pH Solubilization
CHAPTER 6: Solubilization by
Cosolvents
6.1. Properties of Pure Cosolvents
6.2. Solubilization by Cosolvents
6.3. Dependence of Solubilization on Cosolvents
6.4. Dependence of Solubilization on Solute Structure
6.5. Temperature and Solution Composition
6.6. Pharmaceutical Aspects of Solubilization by
Cosolvents
CHAPTER 7: Solubilization by
Surfactants (Briefly)
7.1. Solubilization by Micellar Surfactants
7.2. Pharmaceutical Aspects of Solubilization by
Surfactants
CHAPTER 8: Solubilization by
Complexation
8.1.
Complex Stoichiometry
8.2.
Chemical Classification of Complexes
8.3.
Solubilization by Inclusion Complexation
8.4.
Solubilization by Stacking Complexation
8.5.
Temperature and Solution Composition
8.6.
Pharmaceutical Aspects of Solubilization by Complexing Agents
CHAPTER 9: Effect of Cosolutes on
Solubility
9.1. Liquid Solutes
9.2. Solid Solutes and Liquid Cosolutes
9.3. Solid Solutes and Solid Cosolutes
Lecture, Quiz,
Midterm and Final Exam Schedule
|
September |
October |
November |
December |
|
7 |
5 |
2 |
7 |
|
14 |
12 (Quiz 2) |
16 |
14 (Final Exam) |
|
21 (Quiz 1) |
19 |
23 (Quiz 3) |
|
|
28 |
26 (Midterm Exam) |
30 |
|