Case Study I

Colpermin^®

Our Colpermin^® Case Study showcases the expertise available within Tillotts with respect to the design, development and commercial manufacture of a liquid-fill formulation for lower GI tract drug delivery.

How it Works

Colpermin^® capsules are enteric-coated with a proprietary coating that was discovered and developed at Tillotts. This particular enteric coat begins to disintegrate at higher pH and provides a predictable and sustained release of the active ingredient (Peppermint oil) along the distal small intestine and throughout the colon.

Targeted Drug Delivery & Mechanism of Action

Tillotts novel enteric coating technology enables the Colpermin^® capsule to survive the acid environment of the stomach and disintegrate only in the less acidic environment of the illeum at a pH of 6.8 or higher (Figure 1). The Colpermin^® oleo-gel formulation provides an optimal delivery profile of the active ingredient. Pharmacokinetic studies shown that the Peppermint oil is available from 12 to 14 hours after the administration of Colpermin^®.

Colpermin^® relieves painful bowel cramps and bloating associated with IBS. (-)-Menthol is a major constituent of Peppermint oil which exhibits powerful anti-spasmodic effects. These result from the inhibition of calcium channels in the intestinal smooth muscle cells.

Commercial Manufacturing Process

Colpermin^® is commercially manufactured on a global scale in a two-piece hard gelatine capsule by Tillotts Services using our liquid-fill encapsulation technology. During the filling process, the formulation is heated and agitated which produces the liquid form and once injected into the capsules it sets as a semi-solid gel. The Capsule is then sealed with the characteristic blue band which also acts as an anti-tamper mechanism.

Key Facts

• Originally launched in 1981 as an Rx product; licensed to J&J for the UK and Ireland, GSK for Germany (as Medacalm^®) and by Tillotts Pharma AG in selected other European territories.
• Herbal remedy based on Peppermint oil for the treatment of regular symptoms of IBS (pain, spasm, bloating)