1.  Objectives / Deliverables  Strategy  Ideas  First Results  Recent and Next Steps G&H Meeting 22-26 th April, 2002 Leipzig, Germany WP 7 Pharmaceutics (Lichtwer Pharma)

2. Objectives / Deliverables Objectives / Deliverables  Development of an improved pharmaceutical formulation Garlic of the future!

3. Objectives / Deliverables Objectives / Deliverables  Improved pharmaceutical formulation  Quality  Stability  Quantity of release  Release profile  Costs  Consumer attraction (look, “story”)  Consumer compliance (odour, size)

4. Objectives / Deliverables Objectives / Deliverables  Low costs  Poor and unpredictable quality  Unstable  Uncontrolled release profile  Steadily decreasing consumer attraction  Moderate consumer compliance  Market products

5. Objectives / Deliverables Objectives / Deliverables  Where to improved?  Quality  Stability  Quantity of release  Release profile  Costs  Consumer attraction  Consumer compliance

6. Strategy Strategy  “Economic” Approach  Quality  Stability  Controlling of costs  “High End” Approach  Quality  Stability  Quantity of release  Release profile  Consumer attraction  Consumer compliance  Two Approaches for Improvements

7. Strategy Strategy  Garlic Powder  Content active substances  Higher microbial purity  Results from Garlic&Health project?  Finished Product  Optimised packaging  “Nothing else to do?!”  Economic Approach – Quality

8. Strategy Strategy  Garlic Powder  Dryer Powder < 1 % residual water)  Pre-Formulation of Garlic Powder Granulation, Micro-capsulation  Finished Product  Processing under dryer conditions process under air condition  Enhanced Protection from Humidity  Enhanced Protection from Oxygen enhanced packaging material  Economic Approach – Stability

9. Ideas Ideas  Economic Approach – Comparison  Dragee (Market Standard)  100 mg Garlic powder  15 – 20 Excipients  Production time:  24 h  Film coated tablet  100 mg Garlic powder  7-8 Excipients  Production time:  8 h

10. First results First results  Film coated tablet containing pre-dried ingredients I

11. First results First results  Film coated tablet containing pre-dried ingredients II

12. Strategy Strategy  Garlic Powder  Higher alliin content  Combination of powder and alliin rich extract (= substrate for alliinase)  Finished Product  Protection of alliinase from inactivation in acid gastric media  up-concentrating of alliin in the “neighbourhood“ of alliinase  “High End” Approach – Quantity of Release

13. Strategy Strategy  Garlic Powder  Pre-formulation of garlic powder for prolonged release of alliinase products  Finished Product  Matrix-, compartment tablets creating a prolonged release profile ...combined with alliin rich extract (substrate for alliinase)  “High End” Approach – Release Profile

14. Strategy Strategy  Garlic Powder  “Higher dosis” declarated  “The story behind” European garlic with a research background  Finished Product  More efficacy – less side effects (odour)  (Self) explaining product “one can see what one get and how it works”, “yes it’s different from the usual”  “High End” Approach –Consumer Attraction Consumer Compliance

15. = Alliinase containing garlic powder Ideas Ideas  High End Approach – functionalised tablet = Alliin rich garlic extract = Inner coating = Outer coating 20 - 30 mm 2 - 3 mm

16. Recent and Next Steps Recent and Next Steps  On-going stability tests on pre-dried formulation  Lab experiments to gain an alliin up- concentrated extract  Technical production of an alliin enriched extract  Orientating and lab scale galenic experiments for a new dosage form  “What’s going on at Lichtwers...?”