PHY PHARM (edited)

Deals with the physicochemical principles underlying the development of a successful dosage form

Physical Pharmacy

Application of physical, chemical, and biological principles in the formulaton of a drug product

Physical Pharmacy

Helps explain how factors such as solubility, stability, particle size, pH, diffusion, and interfacial phenomena affect drug products

Physical Pharmacy

Bioavail

Pharmaceutics

All about formulations

Pharmaceutics

Is a branch of pharmaceutical sciences that deals with:

a. Investigations of physical and chemical properties of drug molecules

b. Design, fabrication, and evaluation of drug delivery systems

c. Monitoring how drug formulation affects drug liberation, absorption, distribution, metabolism, and excretion.

d. Basic relationship between formulation and therapeutic effect

Pharmaceutics

Investigations of physical and chemical properties of drug molecules

Pharmaceutics

Design, fabrication, and evaluation of drug delivery systems

Pharmaceutics

Monitoring how drug formulation affects drug liberation, absorption, distribution, metabolism, and excretion.

Pharmaceutics

Basic relationship between formulation and therapeutic effect

Pharmaceutics

Ideal route and formulations

Drug delivery systems

Pharmacokinetics

LADME

LADME

Liberation, Absorption, Distribution, Metabolism, and Excretion

XR, MR

Therapeutic Effect

Eto may pinakatherapeutic effect

Agent or substance intended for use in the diagnosis, cure, mitigation, treatment, and prevention of disease

Drug

Form suited for administration to the patient

Dosage form

A finished dosage form that contains an active drug ingredient (palatable, convenient, safe, and effective)

Drug product

Forces that hold atoms, ions, or molecules together

Binding Forces Between Molecules

“Within” molecules or compounds

Intramolecular Forces

Hold atoms together and are generally stronger

Intramolecular Forces

Ionic
Covalent Bonds
Metallic bonds
Hydrogen bonds

Intramolecular Forces

Transfer of e-

Ionic Bonds

Between metal and nonmetal

Ionic Bonds

Sharing of e-

Covalent Bonds

Between nonmetals

Covalent Bonds

EN Difference: <0.4

Pure Covalent

EN Difference: 0.4 - 1.7 (2.0)

Polar Covalent

EN Difference: >1.7 (2.0)

Ionic

“Between” molecules

Intermolecular Forces

weaker than intramolecular forces

Intermolecular Forces

Van der Waals Forces
Ion-Dipole
Ion-Induce dipole Interaction
Hydrogen bonds

Intermolecular Forces

Keesom Forces

Debye Forces
London Forces

Van der Waals Forces

Orientation/Alignment effect

Keesom Forces

Dipole-Dipole Forces

Keesom Forces

Polar molecule + Polar molecule

Keesom Forces

force of water, alcohols, acetone

Keesom Forces

1-7 kcal/mole

Keesom Forces

Dipole = ?

Polar

Induction effect

Debye Forces

Dipole-induced dipole

Debye Forces

Polar molecule + Nonpolar molecule

Debye Forces

forces of Ether, ethylacetate

Debye Forces

1-3 kcal/mole

Debye Forces

Dispersion effect

London Forces

Induced dipole - induced dipole

London forces

Orginate from molecular vibrations

London Forces

Non polar + Non polar

London Forces

Forces of Hexane, CCl4

London Forces

0.5-1 kcal/mole

London Forces

(+/-) charged ion + polar

Ion-Dipole Forces

Forces of Quarternary ammonium + Tertiary amine, solubility of salts in water

Ion-Dipole Forces

(+/-) charged ion + non polar

Ion-Induced Forces

forces of: Iodine + KI (formation of tri-iodide complex)

Ion-Induced Forces

Interaction between molecules containing H and highly EN atom (F, S, O, N)

Hydrogen Bonds

Special type of dipole dipole interaction

Hydrogen Bonds

2-8 kcal/mole

Hydrogen Bonds

forces of Water, Alcohol, Carboxylic acids, Esters, Aldehyde, NOT Ether, and Ketones

Hydrogen Bonds

HYDROGEN BONDS examples

• water

• Alcohol

• Carboxylic acids

• Esters

• Aldehyde

• NOT __ and __

Responsible for unusual properties of water
- HIGH dielectric constant (universal solvent)
- Abnormally LOW vapor pressure
- HIGH boiling point

Hydrogen Bonds

HYDROGEN BONDS are Responsible for unusual properties of water
- __ dielectric constant (universal solvent)
- Abnormally __ vapor pressure
- __ boiling point

- HIGH dielectric constant (universal solvent)
- Abnormally LOW vapor pressure
- HIGH boiling point

Can also exist intramolecularly
- In proteins: a helices, b sheets

-In nucleic acids: DNA (A-T and G-C bonds)

Hydrogen Bonds

How many bonds in A-T (DNA)

2 hydrogen bonds

How many bonds in G-C (DNA)

3 Hydrogen Bonds

Attractive Forces and Repulsive Forces

Manifestation of Intramolecular Forces

“together”

Attractive Forces

Cohesive and Adhesive forces

Attractive Forces

Like molecular

Cohesive Forces

Unlike molecules

Adhesive Forces

“apart”

Repulsive Forces

At __ distance, the attractive and repulsive forces are equal

Repulsive Forces

Unequal distribution of electrons in a bond or molecule

Polarity

Requirements for polarity

Electronegativity difference and Symmetry of the molecule

Higher EN difference = higher polarity

Electronegativity difference

Dipole moment

Electronegativity difference

Asymmetric and have nonzero dipole moments → HCl, H2O, NH3

Polar molecules

Zero dipole moments → CO2, CCl4

Nonpolar molecules with perfect symmetry

The strength of the attractive forces governs the physical and chemical properties of substances

The stronger the IMFA = stronger interaction = higher BP, MP, viscosity, surface tension

Application of Bonds

The stronger IMFA = Stronger interaction = ?

Higher BP, MP, viscosity, surface tension

yes i

CH4 < CH3Cl < CH3OH

Increasing Boiling Point

Derived from the sum of individual properties of atoms or functional groups present in molecules

Additive

Mass, Molecular Weight, Volume

Additive

Dependent on the structural arrangement of the atoms within the molecule

Constitutive

Optical activity, surface tension, viscosity

Constitutive

Dependent upon the total number of non-volatile solute particles present in the solution

Colligative

Vapor pressure lowering, BP elevation, FP depression, Osmotic pressure

Colligative

Combined Additive-Constitutibe Property: _____

Molar Refraction

Molecules packed closely in an orderly arrangement

Solid

Definite shape

Solid

Definite volume

Solid

Neglible compressibility

Solid

Negligible expansibility

Solid

Rigid/does not flow

Solid

Molecules close together but randomly arranged

Liquid

Takes shape of container

Liquid

Definite volume

Liquid

Slight compressibility

Liquid

Slight expansibility

Liquid

Flows

Liquid