modified release technologies

case study Zydis ODT Provides Better Treatments

Improved Therapeutic Profile
Zydis fast-dissolve formulation for Zelapar (Selegiline anti-Parkinsons compound) had a positive impact on therapeutic profile vs. Selegiline in traditional tablets: fig. 1 selegiline vs. zelapar fast-dissolve tablets
Tablet/Capsule Selegiline (traditional formulation) Lower Dose and Less Frequent Dosing Tmax=1 hour. Digested in the gut, adsorbed through the small intestine, processed by the liver. Zelapar formulated with Zydis fast-dissolve (innovative formulation) 1.25-mg or 2.5-mg doses, taken once a day (QD). Tablet that dissolves in mouth within seconds, without water. Tmax=15 minutes. Innovative transmucosal drug delivery adsorbed rapidly through the lining of the mouth directly into the blood. Significantly by-passes the liver, producing lower undesired metabolites.

Increased Bioavailability/Faster Onset of Action

Tmax=1 hour. Digested in the gut, adsorbed through the small intestine, processed by the liver.

Lower Side Effect Potential

Processed through the liver, producing undesired metabolites.

Patient Preference & Adherence To Prescriptions

Zydis formulation demonstrates higher patient preference and adherence to prescriptions for Selegiline, and other therapeutic areas vs. traditional tablets: fig. 2 zydis patient preference & adherence data
Disease Parkinsons Diesease 1 Parkinsons Diesease 1 Allergy Rhinitis 2 Schizophrenia 3 Molecule Selegiline Selegiline Ebastine Olanzapine Study Type 12 month longitudinal patient records 12 week investigator study patient preference survey 16-week investigator study Patient Number 1520 197 420 149 % Patients Preferring Zydis ODT vs. Standard Tablets NA 86% preferred Zydis ODT 83% preferred Zydis ODT NA Compliance: Zydis ODT vs. Standard Tablets 98.5% vs. 81.0% Medicare patients NA NA 92.9% vs. 78.5% (P=0.015)

Allergy (Antihistamine) 4

Zydis ODT placebo

patient preference study; patients told they were given active dose, but it was a Zydis ODT placebo

>7500

94.3% Zydis ODT convenient to use 95.3% Zydis ODT easy to take 87.7% would change current antihistamine for Zydis ODT formulation

NA

1 2 3 4

12-month longitudinal patient records analysis by SDI Health, a division of IMS Health, conducted in January, 2011. Study included 1,520 US patients prescribed Zelapar, Eldepryl, or generic Selegiline. Ciprandi G. Clinical utility and patient adherence with ebastine for allergic rhinitis, patient preference and adherence. Volume 4. PubMed Central, October 14, 2010. Karagianis J, Grossman L, Landry J, et al. A randomized controlled trial of the effect of sublingual orally disintegrating olanzapine versus oral olanzapine on the body mass index: The PLATYPUS study. Schizophr Res. 2009;113:41-48. Reig AR, Fernandez JP, Cervera JG, Navarro JH, Ferragud MA, Hortal EG. Acceptance survey of a fast dissolving tablet pharmaceutical formulation in allergic patients. satisfaction and expectancies. Allergol Immunopathol. 2006;34:107-112.

DEVELOPMENT

DELIVERY

SUPPLY

fig. 3 us sales selegiline class: anti-parkinson market

$25M

Market Performance
Zelapar (Zydis fast-dissolve formulation) launched into an already generic market, gained and retained market share at higher revenue growth rates compared to other Selegiline branded and generic compounds with the same labeled indications. Catalents unmatched range of innovative technologies, combined with our formulation, production scale-up, regulatory, and commercial expertise can optimize your therapeutic profile.

Zelapar (Zydis)
$20M

Eldepryl Selegiline Generics

sales

$15M $10M $5M $0 2005

year

2010

Add Catalent Modified Release Technologies into your Product Profile for Better Treatments
controlled release OSDrC OptiDose Enables the design of dividable, multi-layer, single or multi-core tablets with a practically endless variety of core numbers, shapes, sizes, and placement within the tablet. The flexible-core capability provides new alternatives in controlled release designs for drug formulators, developers, and marketers. Extended (long-acting) Release Decreased dosing frequency compared to IR formulations. Specific amount of drug released at specific time intervals. Delayed Release Drug released at specific targeted points in the body, based on pH or other characteristics. Pulsed Release Short term and long term combined release (IR plus ER) in one dose form. orally disintegrating tablets Zydis Fast Dissolve Lyophilized orally disintegrating tablets that disperse instantly (usually <3 seconds) without the need for water. Taste masking can be integrated into tablet formulation if desired. Lyopan Fast Dissolve Zydis ODT applications for increased taste masking and/ or higher API loading requirements, requiring less water during manufacturing.

Zelapar 5 Eldepryl year $ CAGR (non-ODT 95.9% branded) 6 year $ CAGR -12.7%

Selegiline Generics 6 year $ CAGR 15.8%

Stick Pack Loose free flowing granules that dissolve instantly without the need for water, also available in liquid formulation single dose packets. OptiMelt Hot Melt Extrusion Technology Improve bioavailability of poorly water soluble (BCS II/III/IV) compounds in a tablet form, in addition to our gold standard softgel bioavailability solutions.

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Catalent Pharma Solutions 14 Schoolhouse Road Somerset, NJ 08873 USA solutions@catalent.com T + 1 888 SOLUTION F + 1 732 537 6480

2011 Catalent Pharma Solutions. All Rights Reserved. OSDrC is a registered trademark of Sanwa Kagaku Kenkyusho Co., Ltd. Lyopan is a registered trademark of Pantec AG. Zydis is a registered trademark of Catalent Pharma Solutions. mrt/zydis/ss (10/11)