PHR2021: Workshop 8

Learning Objectives

  • Explore different mechanisms of modified release
  • Compare the effect of modified release on pharmacokinetics
  • Understand why we use modified release formulation
PHR2021: Workshop 8

Today's Agenda

Product Selection

  • Cordilox SR
  • Sandoz Pantoprazole
  • Concerta
  • Covera
  • Rocaltrol

Prepare presentation

  1. What is the product for?
  2. Technology
  3. Excipient(s) responsible for MR
  4. Predict in vitro release profile
  5. Predict in vivo pharmacokinetics
  6. Formulate patient advice/information
PHR2021: Workshop 8

Helpful things to consider

Formulation

  • What kind of MR is it?
  • How does it work (release mechanism)?
  • Which excipient is reponsible for the mechanism?
  • What is its release profile?
  • Any physicochemical characteristics?

Predicting release profile and PK

  • In vitro: Mass release over time
  • In vivo: Plasma concentration over time
PHR2021: Workshop 8

Helpful things to consider

For the patient

  • How does this MR formulation affect dosing frequency?
  • What specific patient populations might benefit most from this formulation?
  • Are there particular administration considerations (e.g., "Do not crush") that impact patient use?
  • How might the MR mechanism affect cost and accessibility?
PHR2021: Workshop 8

Name of the game

PHR2021: Workshop 8

Cordilox SR

  • Antihypertensive
  • Macrogols 4000, 6000 to form a hydrogel matrix
  • Once daily dosing, improved patient compliance
PHR2021: Workshop 8

Sandoz (Enteric coated)

  • For GERD, enteric granules from Eudragit L30D-55 etc.
  • Insoluble in acidic pH, soluble in neutral pH
  • Improved target release in the intestine
PHR2021: Workshop 8

Concerta (Osmotic Pump)

  • For ADHD, controlled release of methylphenidate
  • PEO/Cellulose etc. for osmotic control
  • Minimises fluctuations in plasma concentration
PHR2021: Workshop 8

Covera (Delayed, not osmotic)

  • For hypertension, controlled release of verapamil via osmotic pump
  • PEO/Cellulose etc. for osmotic control
  • Timing of release can be adjusted to suit patient needs
PHR2021: Workshop 8

Rocaltrol (Efficacy-related)

  • For osteoporosis, improved bioavailability of calcitriol
  • Triglycerides for solubility/enhanced absorption
  • Improved bioavailability and reduced variability
PHR2021: Workshop 8

Summary

Explore different mechanisms of modified release

Diverse MR technologies:

  • Matrix systems (Cordilox SR)
  • Enteric coating (Sandoz Pantoprazole)
  • Osmotic pumps (Concerta, Covera HS)
  • Lipid-based formulations (Rocaltrol)
PHR2021: Workshop 8

Summary

Compare the effect of MR on pharmacokinetics

MR formulations modify plasma concentration profiles to:

  • Reduce peak-to-trough fluctuations
  • Extend duration of therapeutic effect
  • Target specific absorption sites
  • Enhance bioavailability of poorly soluble drugs
PHR2021: Workshop 8

Summary

Understand why we use MR formulations

Patient-centred benefits include:

  • Improved adherence through reduced dosing frequency
  • Decreased side effects by avoiding high peak concentrations
  • Enhanced efficacy through targeted delivery
  • Better therapeutic outcomes through optimised drug exposure