Download - Evonik Industries

More documents

Recommendations

Info

20 HealtH & nutrition New technology platforms improve the bioavailability of active ingredients in tablets A tablet instead of an injection “In the right place at the right time“ is the motto of Evonik’s innovative drug-delivery systems and active ingredient formulations. Now, it also applies to poorly soluble active ingredients: Evonik‘s newly developed melt extrusion technology platform significantly improves the bioavailability of these active ingredients, thereby increasing the efficiency and effectiveness of oral forms of administration—tablets and capsules. While melt extrusion cannot serve the new class of biopharmaceuticals (drugs of a biological nature), another new development from Evonik can: the modular drug delivery system (MDD) of the Pharma Polymers Business Line enables a change in the administration route for biopharmaceuticals from the unpopular but often necessary injection to a tablet. With these new developments, Evonik offers cutting-edge technologies for the therapy of many diseases. [ text Dr. Rosario Lizio, Dr. Kathrin Nollenberger, Dr. Norbert Windhab, Dr. Firouz Asgarzadeh, Dr. Thomas Riermeier ] elements34 Issue 1|2011
For over 50 years, functional polymers from Evonik‘s EUDRA GIT® family of products have controlled the release of active ingredients from tablets and ensured that they are delivered to the desired place in the gastrointestinal tract based on either time or pH value. But these functional polymers can do much more than determine the time and place of drug delivery: as a tablet coating, they mask the odor and taste of a drug—a key advantage especially when it comes to the treatment of children— and make sure the active ingredient reaches the target location undamaged. Used in this way, the polymers shield the active ingredient against moisture, for example, or stomach acid, and transport it safely to the absorption point in the small or large intestine. The enteric coating of the tablet can protect not only the active ingredient but the stomach itself. A good example is the acetylsalicylic acid, that is taken longterm at low doses by those with high blood pressure to prevent heart attack. Here, the ultrathin polymer coating protects the stomach against the damaging effect of the acetylsalicylic acid. Through the use of special polymers, active ingredients can also be released uniformly over a longer period of time. These retard formulations, as they are called, are always used when the drug, such as a beta blocker, needs to work throughout the entire day. Scientists in the research centers of Evonik‘s Pharma Polymers Business Line in Germany, India, China, Japan and the United States are researching new polymers and developing for their customers specific formulations with EUDRAGIT® polymers. They are also working on completely new concepts that further functionalize the polymers to meet the pharmaceutical market’s growing demand for new functionalities. Bioavailability determines the efficiency of the active ingredient The bioavailability of an active ingredient indicates how much of it will be absorbed into the bloodstream following application of a drug. It is a key performance indicator and therapeutic control variable, and tells us, among other things, how efficient a medicine is. Generally, the bioavailability of an active ingredient is better the more soluble it is, and the better it is absorbed by the cells of the target location (gastrointestinal tract, mucous membranes, skin, etc.). In these cases the absorption of the active ingredient in the bloodstream is increased. The Biophar HealtH & nutrition 21 maceutical Classification System (BCS) divides ac tive ingredients into four classes based on their solubility and permeability (Fig. 1): if they are highly watersoluble and permeable—like the beta blocker metoprolol, for example—they belong to Class I. If an active ingredient shows poor sol ubility but is highly permeable, it is grouped in BCS Class II. High solubility and poor 333 Figure 1 The Biopharmaceutical Classification System (BCS). According to estimates, about 95 percent of all future chemical entities will show poor bioavailability Permeability Solubility II I IV III Distribution of the development candidates in BCS classes Class IV: 20% Class III: 5% Source: L. Benet, C.-Y. Wu et al 2006, Bulletin technique Gattefosse 99; p. 9–16 Class I: 5% Class II: 70% elements34 Issue 1|2011
Page 1 and 2: elements34 Quarterly Science Newsle
Page 3 and 4: Expansion and transition A pill or
Page 5 and 6: there are no significant amounts of
Page 7 and 8: evonik innovation aWard 2010 07 Evo
Page 9 and 10: evonik innovation aWard 2010 09 ele
Page 11 and 12: The simulation, on the other hand,
Page 13 and 14: in Antwerp, only part of the MTBE r
Page 15 and 16: evonik innovation aWard 2010 15 The
Page 17 and 18: establishing a suitable synthesis p
Page 19: Evonik and AU Optronics conclude st
Page 23 and 24: Figure 2 Solid solutions can signif
Page 25 and 26: additional polymer platForm Evonik
Page 27 and 28: Figure 8 Image from a scanning elec
Page 29 and 30: In this process, the sodium cyanide
Page 31 and 32: Spinal column implant: The greater
Page 33 and 34: Evonik has proven the biocompatibil
Page 35 and 36: Lead-free—not just gasoline Histo

Download - Evonik Industries

Create successful ePaper yourself

Delete template?

Save as template?