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Controlled Release Delivery System

Mayne Pharma specializes in the formulation and production of technologies that permit controlled-release of active pharmaceutical ingredients (APIs) in pellets. We focus on all drugs in pellet form achieving a highly desired physicochemical and pharmacokinetic profile, which ensures finely controlled dosing and optimal drug efficacy.

Pellets as a dose form have many advantages including maintained blood plasma levels over entire intestinal transit time and reduced gastrointestinal (GI) side effects. Spreading the therapeutic dose over many hundreds of individual particles reduces the variability sometimes seen with larger singular dose forms (which are more susceptible to variable GI transit times). The particles generated by pellet technology are generally spheroidal in shape and can have a diameter ranging from 300 to 1,700µm. The rate and site of active drug release is dictated by specifically formulated polymer coatings applied to active drug cores that can have drug loadings of up to 90%. The controlled-release pellets can be filled into hard gelatin capsules and/or sachets, or incorporated into a compressed tablet.

Scanning electron micrographs of pellets

Whole Pellets 

1. Whole Pellets
(30x magnification)

Pellet Cross Section

2. Pellet Cross Section
(1500x Magnification)

Tablet Cross Section

3. Tablet Cross Section
30x Magnification

Mayne Pharma has developed a number of proprietary and/or patented controlled-release pellet technologies that provide improved therapeutic outcomes for patients. Products including Eryc™ (delayed-release erythromycin), Doryx™ (delayed-release doxycycline) Kapanol™/ Kadian™ (extended-release morphine) and Astrix™ (delayed-release, low dose aspirin) have established market success internationally.

Customized release profiles are achieved by coating the drug ‘core’ with different quantities and types of polymers, usually in combination with other agents to ‘fine tune’ release and improve stability. These profiles include:

Pulsed-release

Pulses of drug over 12 or 24 hours following a single dose.

Outcomes

  • Increased systemic bioavailability of pulse-release formulations may be achieved when pre-systemic metabolism is saturated by high drug load “pulsed” a number of times a day into the GI tract.
  • Chronotherapy improving the safety and efficacy of drugs by proportioning their peak plasma concentrations during 24 hours in synchrony with biological rhythm.

Pulsed Release

Sustained release

Steady level of drug over 12 or 24 hours following a single dose.

Outcomes

  • Increased efficacy through improved patient compliance resulting from reduced dosage frequency compared to immediate-release drugs.
  • Reduced local and systemic side effects due to the gradual-release of drug into the GI tract, which reduces peak plasma concentrations.
  • Increased duration of efficacy by ensuring that the drug plasma levels remain above the minimum effective concentration.
  • When used in the treatment of strong pain, a sustained-release product reduces sleep disturbance due to break-through pain, or alternatively being woken by nursing/medical staff providing 4-hourly dosing.

Sustained Release

Delayed Release

Release of a drug at a time later than that immediately following its administration.

Outcomes

  • Improved oral bioavailability of drugs that degrade in acid by protecting them from the acidic environment of the stomach. Related to this, improved bioavailability of drugs that have a reduced activity when administered with food.
  • Reduced gastric side-effects achieved by minimizing the release of drug in the stomach.
  • Improved efficacy for drugs that require targeted release at specific sites in the GI tract.

Delayed Release