IPS1 - A1 - Physical Pharmacy Principles

Physical Pharmacy

___-

• is the application of physical, chemical, and biological principles in the formulation of a drug product

• To understand and develop dosage forms and drug delivery systems

Drug

___- is an agent or substance intended for use in the diagnosis, cure, mitigation, treatment and prevention of disease

Drug

____- is the pure form of the drug

Dosage form

____ - is a form suited for the administration of the patient

Dosage form

____ - is the form suited for administration of drugs

Drug product

____ - is a finished dosage form that contains an active drug ingredient (palatable, convenient, safe, and effective)

Drug product

drug + dosage form = ____ ?

Physical Pharmacy

____- is the study of physical and chemical properties of drugs

Physical Pharmacy

____ - deals with the physicochemical principles underlying the development of a successful dosage form

• Theoretical approach

• Quantitative approach

Physical Pharmacy have two approaches such as ___[2]

Pharmaceutics

____- is a branch of pharmaceutical sciences that is all about the FORMULATION

Pharmaceutics

____-is a branch of pharmaceutical sciences that deals with Investigations of physical and chemical properties of drug molecules

Pharmaceutics

____-is a branch of pharmaceutical sciences that deals with Design, fabrication and evaluation of drug delivery systems

Pharmaceutics

___-is a branch of pharmaceutical sciences that deals with Monitoring how drug products are absorbed, distributed, metabolized and excreted in the body

Pharmacokinetic

ADME principle is under ___ [Pharmacodynamic/Pharmacokinetic]

Pharmacodynamic

Mechanism of drug action is under ______ [Pharmacodynamic/Pharmacokinetic]

Pharmacology

PK + PD = _____ ?

Pharmaceutics

____- is a branch of pharmaceutical sciences that deals with Mechanism of drug action

1. Intramolecular Forces

2. Intermolecular Forces

Types of General Forces [2]

Intramolecular Forces

[Types of General Forces]

• ____ - within molecules

• Ionic Bonds (transfer of e-)

• Covalent Bonds (sharing of e-)

• Metallic bonds

• Hydrogen bonds

Type of Bonds in Intramolecular Forces [4]

• Pure Covalent

• Polar Covalent

• Ionic

[Bond Type] — Electronegativity (EN) Difference

• EN Difference : < 0.4 = _____ ?

• EN Difference : 0.4 – 1.7 (2.0) = ____ ?

• EN Difference: > 1.7 (2.0) = ____ ?

Intermolecular Forces

[Types of General Forces]

• ____- between molecules

• Van der Waals Forces

• Ion–Dipole

• Ion–Induced Dipole Interaction

• Hydrogen Bonds

Types of Intermolecular Forces [4]

• Higher EN difference = higher polarity

• Dipole moment

Requirements for Polarity [2]

High Polarity

Higher EN difference = ___[high/low] Polarity

Polar

If a compounds have a Dipole moment it is considered as ____[polar/nonpolar]

high polarity

High EN difference =___ [high/low] polarity

UNDERSTAND 🙃

Order of increasing polarity:
H–H < S–H < Cl–H < O–H < F–H

Non-polar

[Polar/Non-polar]

• ____- Perfect symmetry

zero dipole moment

____- means that a molecule has no overall separation of positive and negative charges.

Polar

[Polar/Non-polar]

• Asymmetric

• have nonzero dipole moments

Non-polar

[Polar/Non-polar]

• CO₂

• Carbon tetrachloride (CCl₄)

Polar

[Polar/Non-polar]

• HCl (Hydrogen chloride)

• H₂O (Water)

• NH₃ (Ammonia)

Polar

[Polar/Non-polar]

• NH₃ (Ammonia)

Polar

[Polar/Non-polar]

• HCl (Hydrogen chloride)

Polar

[Polar/Non-polar]

• H₂O (Water)

• Attractive Forces

• Repulsive Forces

Manifestations of Intermolecular Forces can be __[2]

• Attractive Forces (“together”)

• Repulsive Forces (“apart”)

• Attractive Forces = ___ [together/apart]

• Repulsive Forces = ___ [together/apart]

• Cohesive forces

• Adhesive forces

Types of Attractive Forces [2]

Cohesive forces

[Types of Attractive Forces]

_____-

• like molecules

• between same molecule

Adhesive forces

[Types of Attractive Forces]

____-

• unlike molecules

• between different molecule

3−4×10⁻⁸cm

At ______ cm distance, the attractive and repulsive forces are equal.

• Van der Waals Forces

• Ion-Dipole Forces

• Ion-Induced Dipole

• Hydrogen Bonds

Type of Intermolecular Forces [4]

1. Keesom Forces

2. Debye Forces

3. London Forces

Types of Van der Waals Forces [from strongest to weakest] [3]

• polar

• non polar

►Dipole = ____[polar/non polar]

►Induced dipole = ___ [polar/non polar]

Keesom Forces

[Types of Van der Waals Forces]

____-

• have Orientation / Alignment effect

• Dipole–Dipole Forces

Keesom Forces

[Types of Van der Waals Forces]

• Polar molecule + Polar molecule

• Example: water, alcohols, acetone

Keesom Forces

Water ,alcohol , acetone is an example of what Van der Waals Forces __ ?

Keesom Forces

[Types of Van der Waals Forces]

___-

• Strength: 1–7 kcal/mole

Debye Forces

[Types of Van der Waals Forces]

• have Induction effect

• Dipole–Induced Dipole Forces

Debye Forces

[Types of Van der Waals Forces]

• Polar molecule + Nonpolar molecule

• Example: ether, ethyl acetate

Debye Forces

Ether, ethyl acetate is an example of what Van der Waals Forces __ ?

Debye Forces

[Types of Van der Waals Forces]

___-

• Strength: 1–3 kcal/mole

London Forces

[Types of Van der Waals Forces]

____-

• Dispersion effect

• Induced Dipole–Induced Dipole

London Forces

[Types of Van der Waals Forces]

____-

• Originate from molecular vibrations

London Forces

[Types of Van der Waals Forces]

• Nonpolar + Nonpolar

• Example: hexane, Carbon tetrachloride (CCl₄)

London Forces

hexane, Carbon tetrachloride (CCl₄) is an example of what Van der Waals Forces __ ?

London Forces

[Types of Van der Waals Forces]

_____-

• Strength: 0.5–1 kcal/mole

Ion–Dipole Forces

• (+/–) charged ion + polar molecule

• Example: quaternary ammonium + tertiary amine, solubility of salts in water

Ion-Dipole Forces

• quaternary ammonium + tertiary amine

• solubility of salts in water

The following are example of what Type of Intermolecular Forces ?

Ion–Induced Dipole

[Type of Intermolecular Forces]

• (+/–) charged ion + nonpolar molecule

• Example: iodine + KI (formation of tri-iodide complex)

Ion-Induced Dipole

Iodine + KI (formation of tri-iodide complex) is an example of what Type of Intermolecular Forces ?

Hydrogen Bonds

[Type of Intermolecular Forces]

____-

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

Hydrogen Bonds

[Type of Intermolecular Forces]

_____-

• Special type of dipole–dipole interaction

• Strength: 2–8 kcal/mole

a.)Hydrogen Bonds

Examples:

• Water

• Alcohol

• Carboxylic acids

• Esters

• Aldehyde

• NOT ethers and ketones

a.)Hydrogen Bonds

b.) Ion–Induced Dipole

c.) Ion–Dipole Forces

• ether

• ketones

All functional groups have H-bond except ___[2]

• High dielectric constant (universal solvent)\

• High boiling point

• Abnormally low vapor pressure

Responsible for unusual properties of water:[3]

High dielectric constant

Our universal solvent have ___[high/low] dielectric constant

• In proteins: α-helices, β-sheets

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

Hydrogen Bonds can also exist intramolecularly in our ___[2]

Guanine (G) -Cytosine (C)

In our DNA what nitrogenous bases have 2 hydrogen bond ?

Adenine(A) - Thymine(T)

In our DNA what nitrogenous what nitrogenous bases have 3 hydrogen bond ?

strength of attractive forces

The _____ of the attractive forces governs the physical and chemical properties of substances.

True

[T/F] The strength of the attractive forces governs the physical and chemical properties of substances

strong interaction

Stronger IMFA = ____ [strong/weak] interaction

high BP, MP, viscosity, surface tension.

Stronger IMFA = ____ [high/low] BP, MP, viscosity, surface tension.

Trend: [strongest to weakest]

• Hydrogen bonding

• Dipole-dipole

• London Dispersion

Increasing Boiling Point: [low to high]

• Methane (CH₄) → weakest IMFA

• Chloromethane (CH₃Cl) → Moderate IMFA

• Methanol (CH₃OH) → Strongest IMFA

EXAMPLE

Stronger IMFA = stronger interaction = higher BP, MP, viscosity, surface tension.

• Additive

• Constitutive

• Colligative

Physical Properties of Drug Molecule [3]

Additive

[Physical Properties of Drug Molecule]

___-

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

• depends on the amount

EXAMPLE: mass, molecular weight, volume

a.) Additive

mass, molecular weight, volume is an example of what Physical Properties of Drug Molecule ?

a.) Additive

b.) Constitutive

Constitutive

[Physical Properties of Drug Molecule]

____-

• Dependent on the structural arrangement of the atoms within the molecule

EXAMPLE: optical activity, surface tension, viscosity and refraction of water

b.) Constitutive

optical activity, surface tension, viscosity and refraction of water is an example of what Physical Properties of Drug Molecule ?

a.) Additive

b.) Constitutive

c.) Colligative

vapor pressure lowering, BP elevation, FP depression, osmotic pressure is an example of what Physical Properties of Drug Molecule ?

a.) Additive

b.) Constitutive

c.) Colligative

Colligative

[Physical Properties of Drug Molecule]

_____ -

• Dependent upon the total number of nonvolatile solute particles present in the solution

• depends on the structural arrangement

EXAMPLE: vapor pressure lowering, BP elevation, FP depression, osmotic pressure

Molar refraction

____ -

• is an example of a combined additive–constitutive property

• measure in moles / substance