A better therapeutic effect with spheroids?

In many cases the main reason for the use of pellets in the manufacture of products with controlled release properties. However there are reasons to believe that pellets or spheroids in any case can offer a superior therapeutic effect even when modified release is not the prime objective. Pellets are not only....

• Able to provide the ability to mix pellets with different release rates

but also are.....

• Easy to coat
• A convenient way to manage the separation of incompatible drugs
• products with a reduced risk of dose dumping
• products with a reduced risk of local irritation in gastro-intestinal tract
• products with less variable bioavailability
  • because particles < 1 mm behave more like liquids in terms of gastric emptying
  • and they distribute evenly over the GI tract

This has led to EMEA regulation CPMP/QWP/604/96 that states ....(in part)

• “The development of single unit non-disintegrating dosage forms is discouraged since their residence time in the stomach is unpredictable and in general longer than disintegrating dosage forms with multiple units of pellets. Therefore, such single unit non-disintegrating dosage forms are liable to a higher risk of dose dumping.”

• EMEA = European Agency for the Evaluation of Medicinal Products