Tablets & Capsules

TC0115A

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M 18 January 2015 Tablets & Capsules capsule coating Applying an enteric coating to empty capsule shells to accelerate clinical trials Yogesh Chachare, Theresa Estep, and Mark Geis Patheon Pharmaceuticals Michael Gosselin Aptalis, formerly of Patheon John Dela Cruz formerly of Patheon This article describes a study in which an enteric coating was applied to empty capsule shells to protect an insulin compound from the acidic environment of the stomach. The method enabled the compound to enter clinical trials quickly, saving time and money. as proteins and peptides. In addition to protecting APIs from gastric acid to maximize bioavailability and efficacy, enteric coatings can be used to prevent the immediate release of the entire quantity of an API and thereby reduce side effects. Enteric coatings also improve the tolerability of drugs by releasing them only in the small intestine. Developing the coating process Purpose The goal was to conduct trials that would lead to the development of an optimized fluid-bed coat- ing process for applying an enteric coating onto empty hypromellose capsule caps and bodies to achieve acid resistance after filling. In this case, enteric-coated cap- sules were a better option than developing pellets or tablets because only a limited supply of the insulin com- pound was available during the early stages of develop- ment. Furthermore, for liquid APIs that are unstable in acid, enteric-coated capsules are often the only way to administer them. The aim of the trials was to evaluate the reproducibility of the manufacturing process and to assess the dissolution performance of an insulin product prior to clinical trials. Methodology. All the preliminary coating trials were performed using clear, size 00 hypromellose capsule shells (Vcaps from Capsugel, Greenwood, SC, and Quali-V from Qualicaps, Whitsett, NC). The shells were separated into caps and bodies using a Qualicaps F40 filler equipped with two custom-fabricated Plexiglas vac- uum shoes, one installed at the filling position and the other after the ejection position. As the capsules passed beneath the vacuum shoes, the bodies and caps were sucked out of the body or cap disk and pneumatically conveyed (Line-Vac from Exair, Cincinnati, OH) into 5- gallon high-density polyethylene pails lined with poly- ethylene bags and covered with perforated lids to vent any active pharmaceutical ingredients (APIs) require enteric protection to prevent the acidic environment of the stomach from degrading them or to achieve a desired therapeutic effect by targeting absorption in the lower gastrointestinal tract. Enteric coatings provide a polymer barrier to high acidity but break down rapidly at a less acidic (higher) pH, such as that of the small intestine. Solid ingredients, such as pellets and tablets, readily accept enteric coatings, and they can later be filled into capsules for oral delivery. But other ingredients—such as the liquid fills within hard capsules—cannot accept them. In those cases, there are two options: 1) Fill the capsules and then apply the enteric coating, or 2) coat the empty capsule shells first and then fill them. One drawback to applying the coating to capsules after filling is the possi- bility that the enteric properties will not be retained at the capsule junction. Coating the capsules before they're filled eliminates that possibility. In the study described here, capsules received an enteric coating before they were filled and were then subjected to dissolution testing. The goal was develop an efficient process for coating capsules to protect an insulin compound from the acidic stomach environment. It was important to protect the insulin compound because insulin is a large-molecule compound that is not absorbed in gastric acid. The same strategy could be used in the delivery of other large-molecule compounds, such

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