Enhancing Pharmaceutical Formulations with Garlic of the Future

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

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

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

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

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

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

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

8. Strategy • Economic Approach – Stability • 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 Oxygenenhanced packaging material

9. 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 • Film coated tablet containing pre-dried ingredients I

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

12. Strategy • “High End” Approach – Quantity of Release • 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

13. Strategy • “High End” Approach – Release Profile • 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)

14. Strategy • “High End” Approach – Consumer Attraction Consumer Compliance • 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”

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

16. Recent and Next Steps • “What’s going on at Lichtwers...?” • 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