Mayne Pharma specialises in the formulation and production 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.
The particles generated by pellet technology are generally spheroidal in shape and can have a diameter ranging from 300 to 1,700µm. The pellets are manufactured by polymer coating drug cores that can have drug loadings of up to 90%.
Pellets can be filled into hard gelatin capsules and/or sachets, or incorporated into a compressed tablet.
Scanning electron micrographs of ‘pellets in a tablet’
Mayne Pharma has developed a number of proprietary and/or patented sophisticated pellet technologies that have allowed for the formulation of pharmaceuticals with modified release profiles. Products including Eryc™ (delayed release erythromycin), Doryx™ (delayed release doxycycline) Kadian™ (extended release morphine), Astrix™ (delayed release, low dose aspirin) and pulsed release Diltiazem have established market success and generate current combined market sales in excess of US $500 million per annum.
Customised release profiles are achieved by coating the drug ‘core’ with different magnitudes and types of polymers. These profiles include;
1. Pulsed release
Pulses of drug over 12 or 24 hours following a single dose.
- 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.
- Improved bioavailability by delivery of drugs to specific sites in the GI tract.
- Treatment of GI conditions through the delivery of drugs directly to the site of action.
- Chronotherapy improving the safety and efficacy of drugs by proportioning their peak plasma concentrations during 24 hours in synchrony with biological rhythm.
2. Sustained release
Steady level of drug over 12 or 24 hours following a single dose.
- 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.
3. Delayed Release
Release of a drug at a time later than that immediately following its administration.
- 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 minimising the release of drug in the stomach.
- Improved efficacy for drugs that require targeted release at specific sites in the GI tract.