Pharmaceutics Exam 3 + Cumulative Stuff

Pharmaceutics

The science of designing, developing, and formulating drugs into dosage forms that are safe, effective, and convenient for patient use.

Importance of Pharmaceutics

Ensures proper drug formulation for desired therapeutic effects, improves drug bioavailability, stability, and patient compliance.

Pharmaceutical Formulation Process

Involves designing a drug product with active pharmaceutical ingredients (APIs) and excipients to ensure stability, efficacy, and patient acceptability.

Difference Between Formulation and Compounding

Formulation is large-scale and standardized for commercial use, while compounding is small-scale and tailored to specific patient needs.

Stages of Drug Development

Include preclinical studies, IND application, clinical trials, NDA, and post-marketing surveillance.

FDA Approval Process

Involves application submissions at various stages to ensure drug safety and efficacy.

Importance of Pharmaceutics in Drug Development

Ensures drugs are formulated for optimal absorption, distribution, metabolism, and excretion (ADME).

United States Pharmacopeia (USP)

Sets standards for the quality, purity, strength, and consistency of medicines.

National Formulary (NF)

Focuses on excipients and inactive ingredients in pharmaceutical formulations.

Typical Drug Monograph Components

Includes official drug name, physical properties, identification tests, assay, permissible impurities, storage conditions, and dosage forms.

USP

Regulates sterile compounding and prevents contamination.

USP

Regulates non-sterile compounding and addresses stability and hygiene.

Reasons for Drug Dosage Forms

To improve stability, enhance bioavailability, ensure controlled release, and improve patient compliance.

Principles of Dosage Form Design

Safety, efficacy, stability, acceptability, and convenience of dosage forms.

Importance of Pre-Formulation Studies

Assess the physical, chemical, and biopharmaceutical properties of drugs for better formulation.

Routes of Administration Consideration

Determines drug formulation and impacts formulation requirements based on intended effect.

Principal Objective of Dosage Form Design

Ensure safe, effective, and consistent delivery of the active ingredient.

Five Qualities of an Ideal Dosage Form

Efficacy, safety, stability, convenience, and cost-effectiveness.

Excipients

Inactive substances used in formulations to support drug delivery.

Importance of Excipients

Improve stability, taste, solubility, and facilitate manufacturing.

Reference Book for Excipients

Handbook of Pharmaceutical Excipients, detailing compatibility and safety.

Properties of Excipients

Include physical, chemical, and functional properties.

Functions of Excipients

Include binders, disintegrants, and preservatives.

Safety Issues with Excipients

Can cause allergic reactions or toxicity at high doses.

Flavoring and Sweetening Agents

Improve patient compliance, especially in pediatric populations.

Dyes vs. Lakes

Dyes are water-soluble, while lakes are insoluble pigments used in solid dosage forms.

Levels of Flavors in Pharmaceuticals

Typically used at 0.1% to 1% of the formulation.

Levels of Colorants in Pharmaceuticals

Typically used at 0.001% to 0.01%, depending on dosage form.

Four Key Processes of Pharmacokinetics

Absorption, distribution, metabolism, and excretion (ADME).

Covalent Bonds

Strong, stable bonds formed by sharing electrons.

Ionic Bonds

Attraction between oppositely charged ions.

Hydrogen Bonds

Weak interactions involving hydrogen and electronegative atoms.

Intermolecular Forces

Forces between molecules affecting solubility and boiling points.

Intramolecular Forces

Forces within a molecule that determine structure.

Dipole

Separation of charges within a molecule due to electronegativity.

Types of Attractive Forces

Include van der Waals forces, dipole-dipole interactions, hydrogen bonds, and ionic bonds.

Repulsive Forces and Molecular Distance

Increase as molecules come closer due to electron cloud overlap.

States of Matter

Solid: fixed shape and volume; Liquid: fixed volume, variable shape; Gas: neither fixed shape nor volume.

Advantages of Solid Dosage Forms

Stable, convenient, controlled release, cost-effective.

Amorphous Solids vs. Crystalline Solids

Amorphous: disordered, higher solubility; Crystalline: ordered, more stable.

Melting Point

Temperature at which a solid becomes a liquid, indicating purity.

Polymorphism

Existence of a substance in multiple crystalline forms affecting properties.

Solvates

Crystals incorporating solvent molecules, impacting stability.

Cocrystals

Formed by combining API with co-former to enhance properties.

Particle Sizes for Various Dosage Forms

Tablets: 50–500 µm; Inhalation powders: 1–5 µm.

Advantages of Particle Size Reduction

Improves dissolution, uniform mixing, and stability.

Definitions of Solution and Solubility

Solution: homogeneous mixture; Solubility: max amount dissolved.

Importance of Water Solubility

Affects absorption, bioavailability, and therapeutic efficacy.

USP Solubility Expressions

Soluble: 1–10 parts; Sparingly Soluble: 30–100 parts.

Noyes-Whitney Dissolution Model

Describes the dissolution rate as influenced by various factors.

Factors Affecting Dissolution Rate

Particle size, temperature, and solvent viscosity.

Tablet Dissolution Process

Includes disintegration, dissolution, and absorption.

Lowry-Bronsted Definition of Acids/Bases

Acid donates a proton; Base accepts a proton.

Ionization of Strong vs. Weak Acids

Strong: fully ionized; Weak: partially ionized.

Degree of Ionization

Depends on pH relative to pKa for acids and bases.

Understanding Acidic and Basic Salts

Acidic: sodium acetate; Basic: ammonium chloride.

Advantages of Salt Formation

Improves solubility, stability, and absorption.

Buffers

Solutions resisting pH changes, composed of weak acid and conjugate base.

Henderson-Hasselbalch Equation

Used for calculating pH based on acid/base concentrations.

Drug Stability Types

Include physical, chemical, microbial, therapeutic, and toxicological.

Major Types of Chemical Instability

Hydrolysis, oxidation, photolysis, and racemization.

Hydrolysis Mechanism

Involves breaking chemical bonds using water.

Stratergies to Minimize Hydrolysis

Includes using desiccants and non-aqueous solvents.

Drug Oxidation Mechanism

Loss of electrons, initiated by various factors.

Photolysis

Degradation from light exposure.

Examples of Microbial Preservatives

Include parabens, benzalkonium chloride.

Shelf Life

Time during which a drug maintains potency; Expiry Date: end of this time.

Zero-Order Reaction

Constant rate of reaction independent of concentration.

First-Order Reaction

Rate depends on concentration of one reactant.

Calculations for Zero and First Order Kinetics

Different mathematical representations for each order of reactions.

Zero-Order Kinetics Applicability

Observed in suspensions due to continuous solid dissolution.

Identify Dosage Forms by Administration Route

Oral: Tablets; Parenteral: IV solutions; Topical: Creams.

Blood Plasma Concentration-Time Curve

Visual representation of drug absorption, distribution, metabolism, and excretion.

Biopharmaceutics

Studies the effects of formulations and physiology on ADME.

Absorption and First-Pass Effect

Drugs in GI tract pass through the liver, affecting bioavailability.

Concentration Gradients in Drug Diffusion

Higher concentrations lead to faster diffusion rates.

One-Compartment Pharmacokinetic Model

Assumes the body acts as a single compartment.

Clearance in Pharmacokinetics

Volume of plasma cleared of drug per unit time.

Predicting Half-Life Changes

Increased clearance reduces half-life; increased Vd prolongs half-life.

Q10 Method for Shelf Life Determination

Predicts degradation rate changes with temperature.

Stability Testing Protocols

Assess physical and chemical stability over time.

Types of Containers by Material

Include glass, plastic, and metal with respective applications.

Single Dose Containers vs. Multiple-Dose Containers

Single-use without preservatives; multiple-use with preservatives.

Well-Closed vs. Tight-Closed Containers

Protects against contamination and air/moisture entry.

Sorption and Leaching in Containers

Involves drug absorbing into and container components migrating into drug.

Biotechnology Impact on Pharmaceuticals

Enables production of biologics and personalized therapies.

Small Molecule vs. Biotech Drugs

Small molecules are chemically synthesized; biotech drugs are complex proteins.

Applications of Polymers

Controlled-release delivery systems, stabilizers, bioadhesive systems.

Pharmaceutical Nanotechnology

Focuses on nanoparticle design for targeted drug delivery.

Advantages of Nano-Based Delivery Systems

Enhanced solubility and reduced side effects.

Phospholipids

Amphiphilic molecules forming liposome structures for drug delivery.

Types of Liposomes

Include conventional, stealth, and immunoliposomes for varied applications.

Immunoliposomes

Targeted drug delivery vehicles functionalized with antibodies.

Polymeric Micelles vs. Lipid Micelles

Polymeric are more stable; lipid are formed from phospholipids.

Construction of Dendrimers

Highly branched macromolecules for targeted drug delivery applications.

Applications of Dendrimers

Targeted delivery, gene therapy, drug solubilization.

Types of Solid Nanoparticles

Includes nanospheres and nanocapsules for drug delivery.

Nanospheres vs. Nanocapsules

Nanospheres: matrix-type; Nanocapsules: core-shell structure.