Week 1 Bridging Pharmaceutics to Biopharmaceutics

Page 1: Course Introduction

• Course Title: PHRM 604 - Pharmaceutics II

• Instructor: Joe Su, PhD

Page 2: Contact Information

• Coordinator & Instructor: Ayda Awaness, PhD

  • Email: AAwaness@westcoastuniversity.edu

  • Zoom link: Join Meeting

• Instructor: Joe Su, PhD

  • Email: jSu@westcoastuniversity.edu

  • Zoom link: Join Meeting

Page 3: Statement of Values

• Adapted from Tricia Bertram Gallant, PhD, Director, Academic Integrity Office, UC San Diego.

• Core Values:

  • Honesty: Demonstrate knowledge and abilities honestly according to school standards.

  • Responsibility: Show up on time, prepared to contribute to the learning environment.

  • Respect: Speak openly while honoring diverse viewpoints.

  • Courage: Act when witnessing actions undermining these values.

• Students and teachers are tasked with promoting a respectful exchange of ideas.

Page 4: Course Goals

1. Perform calculations and conversions in formulation design and pharmaceutical compounding.

2. Describe use and processes for sterile compounded parenteral solutions, including USP <797> requirements.

3. Analyze advantages and disadvantages of various dosage forms and relevant design factors.

4. Discuss bioavailability and bioequivalence significance.

5. Explain factors affecting drug absorption including formulation, administration route, properties, food interactions, and genetics.

6. Detail drug product composition and patient factors influencing drug delivery.

Page 5: Bridging Pharmaceutics to Biopharmaceutics

• Presents the fundamental relationships between formulation, pharmacokinetics, and drug absorption represented by the rate equation.

Page 6: Learning Objectives

1. Define biopharmaceutics.

2. List necessary steps for drug effect.

3. Identify routes of administration (ROA).

4. Explain the selection of a ROA.

5. Mathematically describe drug absorption extent.

6. Understand the relevance of rates in pharmacy.

Page 7: Definition of Biopharmaceutics

• Biopharmaceutics examines the relationships between a drug’s physical/chemical properties, its dosage form, and its administration route on the rate and extent of drug absorption.

• Reference: Shargel, Applied Biopharmaceutics & Pharmacokinetics.

Page 8: Drug to Effect Cascade

• Describes the successive stages from drug release and dissolution to systemic circulation and elimination, leading to pharmacologic effects.

Page 9: Routes of Administration (ROA)

• Types of Administration:

  • Oral

  • Buccal

  • Sublingual

  • Parenteral (IM, IV, SC)

  • Nasal

  • Pulmonary

  • Otic

  • Ophthalmic

  • Topical

  • Transdermal

  • Rectal

  • Vaginal

  • Urethral

Page 10: Choosing a Route of Administration

• Considerations include:

  • Disease being treated

  • Patient’s condition

  • Local vs. systemic effect

  • Rate of release

  • Drug characteristics and pharmacokinetics (Absorption, Distribution, Metabolism, Elimination).

Page 11: Understanding Extent

• Extent refers to the peak concentration achieved and the area under the serum concentration-time curve.

• Key Components:

  • Peak Height: Maximum drug concentration

  • Time of Peak Concentration: Interval after administration.

Page 12: Concept of Rate

• Definition: The change of one variable concerning another, usually time.

• Examples of Rates:

  • Speed of movement (mile/hr)

  • Rate of a chemical reaction (moles/sec)

  • Rate of drug infusion (mg/min)

Page 13: Types of Rates

• Average Rate: Overall change over a period.

• Instantaneous Rate: Change at a specific point in time.

Page 14: Example of Average Speed Calculation

• Scenario: Driving from Los Angeles to San Francisco

  • Departure: 11:00 AM

  • Arrival: 5:00 PM

  • Distance: 420 miles

  • Average Speed = Distance / Time = 420 miles / 6 hours = 70 miles/hr

Page 15: Average Speed Graph

• Graph illustrating distance over time affirming the average speed calculation.

  • Slope = Average Speed = 70 miles/hr

Page 16: Realistic Trip Speeds

• Varied speeds throughout a trip illustrated by intervals, demonstrating the variability of instantaneous rates.

Page 17: The Tangent Line Concept

• Definition: Shows instantaneous rate of change of distance over time in a driving scenario.

Page 18: Instantaneous Rates Explained

• Mathematically represented as the instantaneous change in Y concerning time.

Page 19: Rate Equations

• Differential equations that illustrate the rate of change for a parameter, crucial for pharmacokinetics where Y reflects drug amount or concentration.

Page 20: Formulating a Rate Equation

• General Form:

  • Represents the concentration of drug as a function of time and order of reaction.

Page 21: Writing a Rate Equation as Equality

• Establishing an equation where Z is a constant and reflects the change in Y (drug concentration).

Page 22: Rate Law Definition

• Expresses the relationship between the reaction rate, rate constant, and reactant concentrations raised to specific powers.

Page 23: Order of Reaction Overview

• Overview of how to classify reactions based on their orders (Zero, First, Second).

Page 24: Law of Logarithms

• Important logarithmic properties relevant to pharmacokinetic equations and calculations.

Page 25: Derivatives and Integrals in Pharmacy

• Introduction to calculus concepts applied in pharmacokinetics for analyzing functions of concentration over time.

Page 26: First-order Reaction Dynamics

• Characteristics: Concentration decreases exponentially with time. Representation through equations and graphing.

Page 27: First-order Reaction Graphing

• Graphing ln[A] vs. time illustrates the negative slope that represents the first-order rate constant.

Page 28: First-order Reaction Analysis

• Application of half-lives in first-order reactions represented in tabular form for easier calculations.

Page 29: Half-life Calculations

• Example calculation illustrating the relationship between half-life and concentration over time for a medication.

Page 30: Relating Half-life to Rate Constant

• Formula showing the half-life relationship in a first-order reaction, reinforcing the independence from initial concentration.

Page 31: Importance of Rates in Pharmacy

• Benefits of understanding rates in pharmacy:

  • Predicting drug absorption, elimination, and degradation.

  • Optimization of drug handling, stability, and effectiveness.

Page 32: Summary of Learning Objectives

• Reiteration of learning objectives for PHRM 604, emphasizing the importance of understanding biopharmaceutics and pharmacokinetics in pharmacy practice.