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22 March 2017 Tablets & Capsules The future of functional capsules In vivo tests show that soluble compounds are well absorbed from both gelatin and HPMC capsules. In most cases, capsules of either material perform similarly, but in some applications they don't. HPMC capsules, for example, can interact with poorly soluble APIs in a way that leads to a lower crystallization rate in the GI tract. This can be important when there are supersaturated APIs in the intestine, as can occur when dosing either a high-energy salt form or a weakly basic API. In those cases, HPMC capsules can help maintain supersaturation by inhibit- ing crystallization. The degree to which crystalliza- tion inhibition affects in vivo performance depends on the particular applica- tion, but HPMC has the potential to play a role as a functional excipient that improves bioavailability [8]. Among the molecules Capsugel has formulated at its Bend, OR, site, approximately 40 percent are weakly basic, with a basic pKa between 2 and 7, and almost all the compounds are poorly water soluble. This indicates that there are many compounds that could benefit from HPMC capsules. Today's HPMC capsules are more than an alternative to gelatin capsules. They offer an array of opportunities to improve drug delivery. From research to human dosing, HPMC capsules provide predictable delivery of simple immediate-release formulations and address the complex needs of targeted release, moisture protection, and enteric delivery. The variety of HPMC capsules now available, combined with a host of innovative strategies and tech- nologies for drug delivery, offer a new means of address- ing the challenges of today's APIs and provide a platform to develop patient-centric formulations that incorporate the next generation of molecules in development. T&C References 1. Stegemann S., Vishwanath S., Kumar R., Cade D., Lowery M., Hutchison K., Morgen M., Goodwin A., and Lee C. Comparative human in-vivo study of an immedi- ate release tablet over-encapsulated by gelatin and hydroxypropyl methyl cellulose capsules: Impact of dis- solution rate on bioequivalence. Am. Pharm. Rev. 18(7) (2015) 38-45. 2. Cade D, Groshens E, He XW. Alcohol dose dump- ing for controlled release formulations: Is DRcaps acid resistant capsule an option? Poster W4209, annual meet- ing of the American Association of Pharmaceutical Scientists, October 2014, San Diego, CA. 3. He XW, Groshens E, et al. Prolonged gastric acid resistance using a new double hypromellose capsule approach. Poster W4158, annual meeting of the American Association of Pharmaceutical Scientists, October 2015, Orlando, FL. 4. Amo R. DRcaps capsules achieve delayed release properties for nutritional ingredients in human clinical study. Capsugel-commissioned study conducted by Bio- Images Research, Glasgow, Scotland (2014). 5. Hodges LA, Stevens HNE, Connelly SM, Cade D, Lee C. Novel HPMC capsules dis- play acid resistant behaviour: A scintigraphic imaging study. Poster W5173, annual meeting of the American Association of Pharmaceutical Scientists, October 2014, San Diego, CA. 6. Youngster I et al. Oral, capsulized, frozen fecal micro- biota transplantation for relapsing clostridium difficile infection. JAMA 312(17) (2014) 1772-1778. 7. Benameur H. Enteric capsule drug delivery technol- ogy: Achieving protection without coating. Drug Development & Delivery, 18(5) (2015) 34-37. 8. Richardson M and Morgen M. Next generation HPMC capsules bioequivalence and functional perfor- mance. Sponsored content, Pharm Tech, March 2016. Matt Richardson, PhD, is manager of pharmaceutical business development and Keith Hutchison, PhD, is senior vice president of research and development at Capsugel, 535 North Emerald Road, Greenwood, SC 29646. Tel. 864 223 2270. Website: www.capsugel.com. Vcaps Enteric capsules after 2 hours in gastric conditions (pH 1.2). They were not sealed or banded. Capsules made from an HPMC-HPMC-AS polymer blend are inherently enteric, simplifying the move from early-stage development to commercial manufacturing. www.tabletscapsules.com