1
Minisamy M, Gokulakrishnan S, Vignesh K
COLLEGE OF PHARMACY
MADURAI MEDICAL COLLEGE
MADURAI-20
, 2
Minisamy M, Gokulakrishnan S, Vignesh K
INDEX
CHAPTER NAME OF THE CHAPTER PAGE NO
I PHARMACEUTICS 3
II PHARMACOLOGY & MEDICINAL CHEMISTRY 57
III ORGANIC CHEMISTRY(STEREOCHEMISTRY) 177
IV PHARMACEUTICAL IN ORGANIC CHEMISTRY 181
V PHARMACOGNOSY 185
VI PHARMACEUTICAL ANALYSIS 236
VII PHARMACEUTICAL MICROBIOLOGY 266
VIII BIOCHEMISTRY 277
IX PHARMACEUTICAL JURISPRUDENSE 293
, 3
Minisamy M, Gokulakrishnan S, Vignesh K
PHAMACEUTICS
PREFORMULATION
Preformulation commences when a newly synthesized drug shows sufficient pharmacologic
promise in animal models.
I. Bulk Characterization
Crystallinity and Polymorphism
Hygroscopicity
Fine Particle Characterization
Bulk Density
Powder Flow Properties
II. Solubility Analysis
Ionisation Constant – pKa pH
Solubility Profile
Common Ion Effect – Ksp
Thermal Effects
Solubilization
Partition Coefficient
Dissolution
III. Stability Analysis
Stability in Toxicology Formulations
Solution Stability
pH Rate Profile
Solid State Stability
Bulk Stability
Compatibility
Crystallinity
• Outer appearance (External structure) – “Habit”
• Inner appearance (Internal structure) – “Crystal”
Polymorphism
The state of a substance existing in more than one crystalline form is called Polymorphism”
Classification:
(i) Enantiotropic - one polymorph can be reversibly changed into another by varying
temperature or pressure, e.g. sulphur.
(ii) Monotropic - in which one polymorphic form is unstable at all temperatures and
pressures. It is irreversible, e.g. glyceryl stearates.
, 4
Minisamy M, Gokulakrishnan S, Vignesh K
Transition temperature: The temperature at which two polymorphs have identical free
energies (same solubility and vapour pressure), is the transition temperature.
• Transition temperature is obtained by extrapolation of Van’t Hoff plots.
Van’t Hoff plot is a graph of Log Molar Solubility vs. Temperature
Bridging solvent – Helps in the conversion of one polymorph to another.
Microscopy
• Single refractive index – Isotropic
• More than one refractive index – Anisotropic
Anisotropic:
(i) Uniaxial (two refractive indices)
(ii) Biaxial (three refractive indices)
Moisture Content:
• TGA (Thermogravimetric analysis)
• Karl Fischer
• Gas Chromatography
• Gravimetry
Fine Particle Characterization:
1. Particle Size:
• Coulter counter (stream counting device)
• HIAC (stream counting device)
• Optical microscopy
2. Surface Area:
• Brunauer-Emmett-Teller BET adsorption
Temperature: -196oC
Each nitrogen molecule (N2) occupies an area of 16A2
• Gas adsorption
No. of moles = Wt. in gram / molecular weight
Note: Effective S.A exposed to dissolution media.
Morphology:
• Scanning Electron Microscope (SEM)
• Gold coating (to make surface superconductive)
Minisamy M, Gokulakrishnan S, Vignesh K
COLLEGE OF PHARMACY
MADURAI MEDICAL COLLEGE
MADURAI-20
, 2
Minisamy M, Gokulakrishnan S, Vignesh K
INDEX
CHAPTER NAME OF THE CHAPTER PAGE NO
I PHARMACEUTICS 3
II PHARMACOLOGY & MEDICINAL CHEMISTRY 57
III ORGANIC CHEMISTRY(STEREOCHEMISTRY) 177
IV PHARMACEUTICAL IN ORGANIC CHEMISTRY 181
V PHARMACOGNOSY 185
VI PHARMACEUTICAL ANALYSIS 236
VII PHARMACEUTICAL MICROBIOLOGY 266
VIII BIOCHEMISTRY 277
IX PHARMACEUTICAL JURISPRUDENSE 293
, 3
Minisamy M, Gokulakrishnan S, Vignesh K
PHAMACEUTICS
PREFORMULATION
Preformulation commences when a newly synthesized drug shows sufficient pharmacologic
promise in animal models.
I. Bulk Characterization
Crystallinity and Polymorphism
Hygroscopicity
Fine Particle Characterization
Bulk Density
Powder Flow Properties
II. Solubility Analysis
Ionisation Constant – pKa pH
Solubility Profile
Common Ion Effect – Ksp
Thermal Effects
Solubilization
Partition Coefficient
Dissolution
III. Stability Analysis
Stability in Toxicology Formulations
Solution Stability
pH Rate Profile
Solid State Stability
Bulk Stability
Compatibility
Crystallinity
• Outer appearance (External structure) – “Habit”
• Inner appearance (Internal structure) – “Crystal”
Polymorphism
The state of a substance existing in more than one crystalline form is called Polymorphism”
Classification:
(i) Enantiotropic - one polymorph can be reversibly changed into another by varying
temperature or pressure, e.g. sulphur.
(ii) Monotropic - in which one polymorphic form is unstable at all temperatures and
pressures. It is irreversible, e.g. glyceryl stearates.
, 4
Minisamy M, Gokulakrishnan S, Vignesh K
Transition temperature: The temperature at which two polymorphs have identical free
energies (same solubility and vapour pressure), is the transition temperature.
• Transition temperature is obtained by extrapolation of Van’t Hoff plots.
Van’t Hoff plot is a graph of Log Molar Solubility vs. Temperature
Bridging solvent – Helps in the conversion of one polymorph to another.
Microscopy
• Single refractive index – Isotropic
• More than one refractive index – Anisotropic
Anisotropic:
(i) Uniaxial (two refractive indices)
(ii) Biaxial (three refractive indices)
Moisture Content:
• TGA (Thermogravimetric analysis)
• Karl Fischer
• Gas Chromatography
• Gravimetry
Fine Particle Characterization:
1. Particle Size:
• Coulter counter (stream counting device)
• HIAC (stream counting device)
• Optical microscopy
2. Surface Area:
• Brunauer-Emmett-Teller BET adsorption
Temperature: -196oC
Each nitrogen molecule (N2) occupies an area of 16A2
• Gas adsorption
No. of moles = Wt. in gram / molecular weight
Note: Effective S.A exposed to dissolution media.
Morphology:
• Scanning Electron Microscope (SEM)
• Gold coating (to make surface superconductive)
