When it comes to encapsulating stomach-irritating or sensitive ingredients such as probiotics and omega-3 fatty acids, one issue has often blighted the use of softgel capsules: delivering the intact active to the appropriate site! To address this problem, GELITA has developed a new technology: DELASOL®. This novel approach allows the production of enteric capsules that dissolve in the small intestine instead of in the stomach.
Enteric tablets and capsules play a vital role in drug or active delivery applications: they protect the stomach from a potentially irritating ingredient; they prevent gastric acid-induced degradation of the drugs themselves; and play a key role in targeting the colon for site-specific delivery. Furthermore, when marine oils are released in the stomach, they float to the top and can cause gastric reflux, which is one of the reasons why many producers have tried to make their capsules resistant to the harsh environment of the stomach to ensure that the contents are not released until the capsule has passed into the intestine.
As such, one of the most critical aspects to consider when formulating for capsule-based fill release is to identify where in the body the active ingredient or supplement should be delivered. Probiotics, for example, which are often taken during or after antibiotic treatment, are notoriously susceptible to inactivation and denaturation in the stomach.
Likewise, and unlike many other medications that are designed to release their active ingredient in the stomach, when it comes to an omega-3 oil capsule, most manufacturers want to achieve the exact opposite to avoid the undesired and much maligned fishy burps.
The same is true for delicate plant oils, such as eucalyptus — which is used in softgel capsules to treat the common cold and reduce the formation of mucus in the throat and bronchi. For these applications, enteric DELASOL® would be the right choice for the capsule; it’s resistant to gastric juice, ensuring that capsule fill contents are only released — safe and undamaged — in the intestine.
According to US the Pharmacopeias of US and EU dissolution parameters, tests have shown that DELASOL® capsules remain intact for up to 2 hours in 37 °C simulated gastric fluid (representing the stomach), but are fully dissolved within 45 minutes in simulated intestinal fluid. Inhouse investigations involving enteric fish oil capsules produced with DELASOL® showed impressive results – none of the capsules released the fill in simulated gastric acid nor did they leak.
What’s more, most enteric delivery systems are produced by applying an acid-insoluble coating to soft gelatin capsules. However, this not only increases the time and costs involved in producing the capsules, the coating can also create an unattractive opaque shell that is visually unappealing to consumers. GELITA’s new pharmaceutical gelatin product enable manufacturers to produce brilliantly clear enteric dosage forms using existing equipment in a one-step process.
Got a tricky or sensitive ingredient to deliver and need some advice? Contact us today for the solutions you need.
