Innovations in Design: NIA-West. Missy Lowery, MSc Head of Integrated Marketing Capsugel, now a Lonza company 11/13/2017

Transcription

1 Innovations in Design: NIA-West Missy Lowery, MSc Head of Integrated Marketing Capsugel, now a Lonza company 11/13/2017 1

2 Innovations in Design: How Do You Stand Out? If all other competitors are the same be different.

3 Innovations in design 3

4 Dosage form selection can help to answer consumer demand Bioavailability Enhancement Targeted Release Capsule Technologies / Encapsulation Specialized Applications Salt Screening / Selection Micronization Enteric / Delayed Release Capsule Technologies Gelatin Capsules (Coni-Snap) Specialty Polymer Capsules Taste-Masking Approaches Pediatric Applications Spray-Dried Dispersions Multi-particulate Technologies Vcaps Plus (HPMC) MP formulations Hot-Melt Extrusion Fluid-bed layering PlantCaps and OceanCaps Sprinkle Capsules Extrusion/Spheronization Lipid-Based Formulations Enteric Capsules Biotherapeutics Liquid / Solvent-Based Formulations Nanotechnologies Lipid Multiparticulates (LMP) DRcaps Bio-processing Mini-tabs Vcaps Enteric Bio-formulations Fixed Dose Combinations entrinsic DDT Nano-milling Inhalation Bi/Tri Layer Matrix DPI Capsules (inhalation) SD-based formulations Nano-crystals Capsule-in-Capsule Sprinkle Capsules DPI capsules Multiparticulates Extended / Controlled Release Osmotic / zero order release Matrix and MP / 1st order release Colonic Delivery / Liquid Fill Tech Encapsulation Technologies Specialized Clinical Trial Capsules Abuse Deterrent Forms Key Services API Characterization / Pre-formulation Studies API-in-Capsule / Micro-dosing Evaluations Technology Selection Models / Methodologies Clinical Trial Material (CTM) Manufacture CTM Primary / Secondary Packaging & Distribution Commercial Manufacturing Specialized Handling (highly potent API, controlled substances, cold chain, hormones, probiotics, other) Product Range Drug Product Intermediate Hard Capsules Powder / Multi-particulate Filled Capsules Osmotic, Matrix, Orally Dissolving Tablets Liquid-filled Hard Capsules Soft Gelatin Capsules Sachet 4

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6 Licaps unique liquid-filled capsule delivery Innovative Liquid Supplement Delivery ü Gelatin, vegetarian and organic capsule options which includes Non GMO Verified and Clean Label benefit ü Filled with liquids, lipids, pastes, and semi-solids ü Timed release options leveraging polymer choice and combinations DUOCAP ü Proprietary filling and sealing (fusion) technology Licaps Beadlets DUOCAP with ü Nitrogen bubble helps enhance stability Beadlets Health conscious customers ü Combine incompatible ingredients into single dose ü Great protection combination depending on ingredient needs Target markets ü Consumer preferring liquid form for faster absorption ü Unique solution to differentiate performance and consumer identification 6

7 Liquid Dosage Forms Gelatin Capsules Functionality: 1. Low oxygen permeability 2. Instant sealing (Low viscosity requirement) 3. Nitrogen bubble helps maintain stability Benefits: Enhanced protection for oxygen sensitive products Example: Ubiquinol very unstable when exposed to air Efficient odor and aftertaste protection Example: Krill Oil Eliminates odor Increase capabilities versus softgels High solid load, lower viscosity, tolerant to heat 7

8 Liquid Solution in a Capsule Encapsulation of a pre-solubilized ingredient which is soluble in water or oil Designed for improved rate of dissolution for fast release and better bioavailability Example uses for this form: ül-arginine- creation of a free-flowing solution allows for a higher concentration of active ingredient ü L-Carnitine- liquid form can contain pure L- Carnitine rather than the less soluble salts L-Arginine in suspension L-Arginine solubilized

9 Micronized Liquid Suspension in a Capsule Encapsulation of an insoluble ingredient that has been micronized to a particle size less than 10 microns üsuspended in a lipid or solvent fill üparticles flow freely and are barely detectable Also designed for improved rate of dissolution and better bioavailability

10 Beadlets in a liquid-filled capsule 10

11 Beadlets in a Liquid-filled Capsule Multi component, multi-sized beadlets are suspended in a liquid-fill ü Liquid can also contain active ingredients Designed to offer flexibility in multiple release rates (immediate, delayed) Good for combining incompatible actives or allowing an active to by-pass gastric acids Beads allow for targeting and varying levels of controlled release Can combine fast acting liquid with slow release ingredients

12 Powder-filled Inner Capsule in a Liquid-filled Outer Capsule Size 3 or 4 HPMC capsule filled with a moisture sensitive compound and suspended in a liquid filled HPMC capsule Benefits of the MDS/Capsule-in-a-Capsule: ü Designed for a delayed release: inner capsule will rupture 1-2 hours after ingestion ü Protects moisture sensitive compounds Water activity in the liquid fill is lower than that of the inner capsule contents, drawing moisture away from the active HPMC capsule creates a protective barrier from the outside environment Ideal for moisture sensitive compounds such as probiotics and enzymes

13 for Probiotics DUOCAP capsule Stability Study Results Study confirmed stability of probiotics in DUOCAP capsule Capsugel recommendation to use Glycerol as liquid fill in outside capsule Source: Capsugel Lab Research *recent registration change 13

14 DUOCAP Dissolution Case Study Capsule design eliminates the need for any coatings Slower dissolution of the inner capsule 100 PERCENTAGE DISSOLVED Outer Inner Gelatin TIME (HOURS) Dissolution testing was performed using an acetaminophen marker in the outer capsule and a caffeine marker in the inner capsule; medium was USP simulated gastric fluid for the first two hours and then changed to USP simulated intestinal fluid 14

15 Beadlet-filled Capsule in a Liquid-filled Capsule Combines benefits of a capsule in a capsule with the controlled release properties of beadlets for added extended release Designed to offer multiple release ratesbeadlets in an inner HPMC capsule can release over 6 to 8 hours Good uses for this delivery system would be melatonin or caffeine. Immediate release for rest or energy that will keep working over a period of time

16 Timed release of ingredients is important to consumer experience during preworkout, during workout and recovery % dissolved (LC) Sampling Time (min) % dissolved (LC) Sampling Time (min) Caffeine Theacrine CAFFEINE CONTROLLED-RELEASE CASE STUDY 16

17 Providing protection for acid-sensitive ingredients Unlike other consumer health products, enzymes and probiotics are damaged when exposed to harsh stomach conditions and must be maintained as such in order to be efficient. A number of sports nutrition ingredients benefit from the delay in release as well Humidity Temperature Acid stomach condition 17

18 DRcaps capsules - Proven Targeted Release DRcaps Capsule Human Clinical Study Key Study Findings DRcaps capsules displayed delayed release properties Disintegration started approximately 45 minutes later than a typical immediate release capsule of about 5 minutes For the majority of subjects, complete release took place in the intestine Complete release occurred 20 minutes after the onset of release DRcaps capsules significantly reduced opportunity for nutritional ingredient degradation compared with standard immediate release capsules 18

19 Lipid Multi-particulate (LMP) dosage form versatility Can improve the performance of nutritional actives in two distinct categories: LMPs LMP Applications Curcumin ü ü ü Avoid clumping of loose ingredients and low electrostatic attraction Consistent release for up to 6 hours (no spikes) Use for combination ingredients RTD Powder Beverage Capsules Sprinkle Capsules Sachets Energy Drinks Orally Disintegrating Tablets (ODTs) 19

20 Case Study: Improving the delayed release of a mood enhancing product Dissolution Study conducted on LMP filled into DRcaps capsules Controls: LMP filled into gelatin capsule; 2 commercial enteric coated tablets Dissolution was tested in two stage media: 0.1N HCl for two hours followed by ph 6.8 phosphate buffer USP Apparatus 1, 100 rpm, 37 C % Released Time (Hrs) LMP in DR Cap LMP in Hard Gelatin Cap Commercial Product A Commercial Product B LMP in DRcaps capsules release about 10% active at 2 hr 20

21 BCAA sustained-release LMP BCAAs (L-Leucine, L-Isoleucine & L-Valine) comprise 35% of the amino acids that build muscle. L-Leucine is a regulator that activates protein synthesis through the mtor (mammalian target of rapamycin) Some BCAA products are cheap, synthetic versions that are not water soluble BCAAs also have been shown to degrade after being subjected to stomach acids BCAAs are bitter in taste and have an unpleasant smell Sustained Release Taste Masking Bioavailability Enhancement Min. 4h sustained release For protein shakes with (fast and) slow release BCAA Neutral taste and smell Less sugar and flavor needed Improved stability in stomach acids Less dosage needed 21

22 We ve helped many companies deliver their next market success! 22

23 We re making a big splash!