Pharmaceutics, Intermolecular Forces, and Dosage Forms Review

Comprehensive vocabulary flashcards generated from Pharmaceutics I lecture transcripts covering intermolecular forces, physical states of matter, biopharmaceutics, LADME, and dosage form principles.

Pharmaceutics

A major division of the pharmaceutical sciences that studies the conversion of a drug into medicine and the design of effective drug-delivery systems.

Active Pharmaceutical Ingredient (API)

Any substance or mixture of substances intended to be used in the manufacture of a pharmaceutical dosage form that produces the therapeutic action.

Pharmaceutical Excipient

Any substance other than the active ingredient added to a dosage form that has no therapeutic action, but aids in manufacture, protection, stability, or bioavailability.

Drug

An agent intended for use in the diagnosis, mitigation, treatment, cure, or prevention of disease in humans or other animals.

Dosage Form

The gross pharmaceutical physical form containing active ingredients and excipients ready for administration to a patient.

Biopharmaceutics

The branch of pharmaceutical sciences studying the physicochemical properties of drugs, dosage forms, bioavailability, and the fate of the drug in the body.

Pharmacokinetics

The study of what the body does to the drug, encompassing liberation, absorption, distribution, metabolism, and excretion.

Pharmacodynamics

The study of what the drug does to the body, focusing on the relationship between drug concentration at the site of action and the resulting physiological effect.

LADME

An acronym representing the five stages of drug disposition: Liberation, Absorption, Distribution, Metabolism, and Excretion.

Ionic Bond

A chemical bond formed between two oppositely charged ions when one or more valence electrons are completely transferred from one atom to another.

Covalent Bond

A strong chemical bond formed when two atoms share a pair of valence electrons.

Keesom Forces

Dipole-dipole intermolecular attractions occurring between permanent dipole molecules; they are the strongest of the Van der Waals forces.

Debye Forces

Dipole-induced dipole intermolecular attractions that occur when a permanent dipole molecule induces a temporary dipole in a nearby nonpolar molecule.

London Forces

Induced dipole-induced dipole intermolecular interactions caused by transient electron cloud distortions in nonpolar molecules; they are the weakest Van der Waals forces.

Hydrogen Bond

An attractive interaction between a hydrogen atom covalently bonded to a strongly electronegative atom ($\text{N}$, $\text{O}$, $\text{Cl}$, $\text{F}$, $\text{S}$) and a nearby electronegative atom.

Maraviroc

An FDA-approved therapeutic HIV entry inhibitor that acts as an antagonist and negative allosteric modulator at chemokine receptor 5 ($\text{CCR5}$).

Vapor Pressure

A temperature-dependent physical property of liquids occurring when the rate of evaporation equals the rate of condensation in a closed system.

Boiling Point

The temperature at which the vapor pressure of a liquid equals the external or atmospheric pressure.

Surface Tension

The force pulling liquid molecules inward at the liquid-gas interface, contracting the liquid surface.

Crystals

Solid forms composed of structural units arranged in fixed, repeating geometric patterns with definite, exact melting points.

Polymorphism

The ability of a solid substance to exist in two or more distinct crystalline forms with different crystal lattice arrangements or molecular conformations.

Theobroma oil

Cocoa butter suppository base possessing 4 polymorphic forms ($\alpha$, $\beta'$, $\beta$, $\gamma$), where the stable $\beta$ form has a melting point of $34.5\,^∘\text{C}$.

Amorphous Forms

Non-crystalline solid materials lacking long-range molecular order, behaving as super-cooled liquids without sharp melting points.

Solvate

A crystalline complex formed when solvent molecules are entrapped in a fixed stoichiometric ratio within a crystal lattice during crystallization.

Hydrate

A solvate in which the entrapped solvent molecule within the crystalline structure is water.

$$\log P$$

The octanol-water partition coefficient; a measure of a molecule's lipophilicity where negative values denote hydrophilicity, $0$ denotes equal partitioning, and positive values denote lipophilicity.

First-Pass Metabolism

Enzymatic degradation of an orally administered drug in the gut wall or liver before reaching systemic circulation, reducing overall absorption.

Passive Diffusion

Movement of non-ionized drug molecules across a membrane down a concentration gradient from higher to lower concentration without energy consumption.

Active Transport

Carrier-mediated transport of molecules across a cell membrane against a concentration gradient requiring cellular energy ($\text{ATP}$).

Biopharmaceutics Classification System (BCS)

A classification framework that categorizes drug substances into four classes based on their aqueous solubility and intestinal permeability.

Class I (BCS)

Category of drug substances exhibiting high solubility and high permeability.

Class II (BCS)

Category of drug substances exhibiting low solubility and high permeability.

Class III (BCS)

Category of drug substances exhibiting high solubility and low permeability.

Class IV (BCS)

Category of drug substances exhibiting low solubility and low permeability.

Total Body Water Volumes

In a standard $70\,\text{kg}$ individual, total body water is $\sim 42\,\text{L}$, split into $28\,\text{L}$ intracellular volume and $14\,\text{L}$ extracellular volume ($10\,\text{L}$ interstitial, $4\,\text{L}$ plasma).

Phase I Metabolism

Enzymatic processes (oxidation, reduction, hydrolysis) occurring in the endoplasmic reticulum that introduce polar functional groups into drug molecules.

Phase II Metabolism

Conjugation reactions attaching endogenous molecules (such as glucuronic acid) to Phase I metabolites to form highly water-soluble compounds suitable for excretion.

Clearance ($\text{Cl}_{\text{S}}$)

The quantitative measure of systemic drug removal from plasma per unit time, calculated as renal clearance plus hepatic clearance ($\text{Cl}_{\text{S}} = \text{Cl}_{\text{R}} + \text{Cl}_{\text{H}}$).

Elimination Half-Life ($t_{1/2}$)

The time required to reduce the plasma concentration of a drug by $50\%$ of its initial value.

Onset of Action

The time required after drug administration for plasma drug concentration to reach the minimum effective concentration necessary to produce a response.

Duration of Action

The period of time during which the plasma drug concentration remains at or above the minimum effective concentration.