1.  Objectives Improved Tablet  focus on stability  focus on low costs High-End Tablet  maximum dose  controlled release G&H Meeting 1-2 October, 2002 Montpellier, France WP 7 Pharmaceutics (Lichtwer Pharma)

2. Improved Tablet Improved Tablet A A Comparison  Dragee (Market Standard)  300 mg Garlic powder  15 – 20 Excipients  Production time:  24 h  Film coated tablet  300 mg Garlic powder  7-8 Excipients (pre dried)  Production time:  8 h

3. Improved Tablet Improved Tablet Film coated tablets (FCT) vs Dragees 25°C / 60% r.h.

4. Improved Tablet Improved Tablet  Film coated tablets (FCT) vs Dragees 30°C / 70% r.h.

5. Improved Tablet Improved Tablet  Dragees produced by a water based sugar-coating process are a non suitable galenic formulation when pharmaceutical stability demands must be met  100% water vapour resistant packaging is necessary (HDPE/Glas bottles)  No kind of transparent polymer blister quality provide sufficient protection  Significant improvement in stability for film coated tablets – meeting international pharmaceutical standards!  Conclusions

6. High-End Tablet High-End Tablet  Laboratory experiments to gain a alliin enriched extract were successful  4-5 fold enrichment of alliin (up to 7%) without transformation to allicin by a economic single-step extraction procedure  Extract seems to be suitable for direct use for production (“crystalline like” – not sticky)  Technical production – open  Garlic powder combined with a alliin rich extract

7. High-End Tablet High-End Tablet  Development of a slow release matrix tablet – open  Additional development time of 9-15 months necessary (only with orientation stability data) – End of the project in Jan 2004!  Garlic powder combined with a alliin rich extract

8. Discussion/Suggestions Discussion/Suggestions  Use of film coated tablets for clinical trials  Should the film provide a gastric acid protection? Guarantee of allicin release in the duodenum  High-End tablets as a possible target of Lichtwer’s project activities?! – not for the human intervention study (HIS) of the project  Appointment in Leiden – discussing details of HIS?