PPHARM - Introduction

https://www.livingston.org/cms/lib4/NJ01000562/Centricity/Domain/826/intermolecular_forces%20_worksheet_and_key%20college.pdf

Physical Pharmacy

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

Takeru Higuchi

Father of Physical Pharmacy

Higuchi Model

used to describe drug release from a matrix; the release rate of a drug from a solid matrix is proportional to the square root of time

Dosage Form

to deliver; form suited for administration

Drug

to act; Agent for use in diagnosis, cure, mitigation, treatment, or prevention of disease;

Drug Product

Finished dosage form containing an active drug ingredient that is palatable, convenient, safe, and effective

Functional Modifiers, Replenishers, Diagnostics, Chemotherapeutics

4 types of Drug Action

Functional Modifiers

[Drug Action] Changes properties of the body

Replenishers

[Drug Action] Restores supply of a specific deficiency in the body

Diagnostics

[Drug Action] Used to identify the presence of a disease/sickness

Chemotherapeutics

[Drug Action] used to treat or cure cancers/microbiotics

Anti-Neoplastic Agents and Anti-Microbials

2 Types of Chemotherapeutics

Pharmaceutical Sciences

scientific disciplines critical to drug discovery and development

Drug Discovery and Design

Design and synthesis of new drug molecules; includes medicinal chemistry, combinatorial chemistry, structural biology, and assay development

Drug Delivery / Dosage Form Design

Design of dosage forms (tablets, injections, patches) to deliver drugs effectively at the site of action

Drug Action

Study of how drugs work in living systems at molecular, cellular, organ, and animal levels; includes pharmacology, pharmacodynamics, toxicology

Pharmaceutics

Science of developing drug products; includes study of physical and chemical properties of drugs and design of drug delivery systems

Physical Pharmacy

Branch dealing with physico-chemical and biological principles of dosage form development, ensuring stability, efficacy, and safety

Biopharmaceutics

Study of drug properties related to onset, duration, and intensity of drug action; relates to bioavailability, pharmacokinetics, and toxicology

Pharmacokinetics

Study of time course of drug absorption, distribution, metabolism, and excretion (ADME)

Pharmacodynamics

Study of how drugs act on living organisms, including response magnitude and duration related to drug concentration

Liberation, Absorption, Distribution, Metabolism, Excretion

LADME — stages of drug processing in the body

Disintegration and Dissolution

2 types of Liberation

GI Tract

Part of the body where Liberation occurs

Circulatory System

Part of the body where Administration occurs

Tissues

Part of the body where Distribution occurs

Liver

Part of the body where Metabolism occurs

Urine, Feces, and exhaled air

Part of the body where Excretion occurs

Extensive Property

Physical property dependent on amount of matter (e.g., mass, volume)

Extrinsic Property

other name for Extensive Property

Intensive Property

Physical property independent of amount of matter (e.g., temperature, pressure, density)

Intrinsic Property

Other name for Intensive Property

Additive Property

Property based on the sum of individual components (e.g., molecular weight)

12

Atomic weight of Carbon

16

Atomic weight of Oxygen

Molecular Weight

Example of Additive Property

Constitutive Property

Property based on type and arrangement of components (e.g., melting point)

Melting Point, Electrical Properties, Optical Rotation, and Solubility

MEPORS; Example of Constutive Property

Colligative Property

Property depending on the number of components in a solution (e.g., boiling point elevation)

Boiling Point Elevation, Freezing Point Depression, Vapor Pressure Lowering, and Osmotic Pressure

Example of Colligative Property

Intramolecular Forces

Strong forces within molecules due to sharing/transferring of electrons (e.g., ionic and covalent bonds)

Intermolecular Forces

Weaker forces between molecules (e.g., Van der Waals forces, hydrogen bonds)

Attractive Forces

Forces molecules together

Cohesive Force and Adhesive Force

2 types of Attractive Forces

Cohesive Force

Attraction between like molecules

Adhesive Force

Attraction between unlike molecules

Repulsive Forces

Forces molecules Apart

3-4×10^-8 cm

distance which attractive and repulsive forces are equal

Pauli’s Exclusion Principle

Principle where no 2 electrons can occupy the same quantum space and prevents interpenetration

Covalent Bond

Sharing of electrons between atoms (nonmetal + nonmetal); polar or nonpolar depending on electronegativity difference

Fluorine

most electronegative element

Polar Covalent

unequal sharing of electron

Electronegativity

tendency of atoms to attract electrons

Non-polar Covalent

Equal sharing of electrons

Water

Example of Polar Covalent

Diatomic Molecules (Have no Fear of Ice Cold Beer) and Noble Gases

Examples of Nonpolar Covalent

Hydrogen, Nitrogen, Fluorine, Oxygen, Iodine, Chlorine, and Bromine

Have No Fear Of Ice Cold Beer

Ionic Bond

Transfer of electrons from metal to nonmetal; large electronegativity difference

Electro-covalent Bond

Other name for Ionic Bonds

<0.4 Electronegativity

Electronegativity difference of Non-Polar Covalent

0.4 - 1.8 Electronegativity

Electronegativity difference of Polar Covalent

>1.8 Electronegativity

Electronegativity difference of Ionic Covalent

Van der Waals Forces

Weak intermolecular forces; includes Keesom (dipole-dipole), Debye (dipole-induced dipole), and London (induced dipole-induced dipole) forces

KeeSom Force

Dipole - Dipole; Force that stabilizes structures and is the strongest type of intermolecular force

Debye(I) Force

Dipole - Induced Dipole; Force that induces a temporary electric charges

LonDon Force

Induce Dipole - Induced Dipole; Force that disperses molecules and liquifies gas

Polar + Polar

Bonds present in Dipole - Dipole

Polar - Nonpolar

Bonds present in Dipole - Induced Dipole

Nonpolar - Nonpolar

Bonds present in Induced Dipole - Induced Dipole

Ion-Dipole Forces

Attraction between ions and polar molecules

Ion-Induced Dipole Forces

Attraction between ions and nonpolar molecules due to induced dipoles

Hydrogen Bond

Strong dipole-dipole interaction between hydrogen and electronegative atoms (F, O, N, S); responsible for water’s unusual properties

Hydrogen Bridge

also known as Hydrogen Bond

Fluorine, Oxygen, Nitrogen, and Sulfur

FONS; Electronegative elements that bonds with Hydrogen

High Dielectric Constant, High Boiling Point, and Abnormally Low Vapor Pressure

unusual properties of water caused by Hydrogen Bonding