transmucosal drug delivery using the mucofilm … · transmucosal drug delivery drug delivery and...
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TRANSMUCOSAL DRUG DELIVERYUsing the Mucofilm® technology to bypass the first pass effect
Drug Delivery and Formulation Summit 2019, March 11 – 13, Berlin
WHO IS tesa Labtec GmbH?
COMPANY AFFILIATION
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tesa is a part of the Beiersdorf Group of Companies
tesa SE is a member of the Beiersdorf Group,
manufacturer of successful international cosmetic brands
including NIVEA, Eucerin, and la prairie
OUR TECHNOLOGIES
• Rapidfilm® Fast dissolving oral dispersible films - No swallowing- No water required- Perfect for children and the elderly
• Transfilm® Transdermal and topical patches
- No first pass effect- Less side effects- Less metabolites
• Mucofilm® Buccal and sublingual films - Fast onset of action- Ease of use- No first pass effect
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Innovative dosage forms
Drug Delivery and Formulation Summit Berlin 2019 March 13th, 2019
ORAL FILMS (RAPIDFILM® AND MUCOFILM®)
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RapidFilm®
Orodispersible film (Ph.Eur., EMA) Soluble film (FDA):
Oral film, thin strip, flash-release wafer, quick-dissolve film, orally dissolving film, rapidly dissolving film
Typical components of our Rapidfilm®
Drug Delivery and Formulation Summit Berlin 2019 March 13th, 2019
TRANSMUCOSAL DRUG DELIVERY
March 13th, 2019Drug Delivery and Formulation Summit Berlin 2019
The Mucofilm® technology
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TRANSMUCOSAL DRUG DELIVERY
March 13th, 2019Drug Delivery and Formulation Summit Berlin 2019
The Mucofilm® technology
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WHAT WE CAN DO WITH OUR TECHNOLOGIES…
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LOCAL TREATMENT
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USE CASE: LOCAL TREATMENT
March 13th, 2019Drug Delivery and Formulation Summit Berlin 2019
Research
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M. Preis et al. / European Journal of Pharmaceutics and Biopharmaceutics 86 (2014) 552–561
Fact sheet
API Lidocaine HCl
Indication Local pain relief
Dosage form Solvent casting, bilayer
system consiting of an
HPC+API inner layer
and an outer backing
layer using different
polymers and polymer
cominations
USE CASE: LOCAL TREATMENT
March 13th, 2019Drug Delivery and Formulation Summit Berlin 2019
Research
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H.E. Colley et al. / Biomaterials 178 (2018) 134-146
Fact sheet
API Clobetasol-17-propionate
Indication Oral lichen planus (OLP) and recurrent aphthous
stomatitis (RAS, also termed aphthous ulcers)
Dosage form Electrospun dual-layer mucoadhesive system
comprising of an outer hydrophobic
polycaprolactone (PLC) backing layer and an
inner, mucoadhesive component formed by
electrospinning polyvinylpyrrolidone (PVP) and
Eudragit® RS100, as fibre-forming polymers.
SYSTEMIC RELEASE
.
USE CASE: PARKINSON‘S DISEASE „OFF EPISODES“
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Overview
Managing PD Mid-Stride – A Treatment Guide to Parkinson‘s Disease, Parkinson‘s Foundation
USE CASE: PARKINSON‘S DISEASE „OFF EPISODES“
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Treatment of off episodes with apomorphine
Managing PD Mid-Stride – A Treatment Guide to Parkinson‘s Disease, Parkinson‘s Foundation
Apomorphine, Drugbank.ca
S. Gancher, Pharmacokinetics of apomorphine in Parkinson’s disease,
J. Neural Transm. Suppl. 45 (1995) 137–141.
M.J. Tsai, Y.B. Huang, P.C. Wu, Y.S. Fu, Y.R. Kao, J.Y. Fang, et al., Oral apomorphine delivery
from solid lipid nanoparticles with different monostearate emulsifiers: pharmacokinetic and
behavioral evaluations, J. Pharm. Sci. 100 (2) (2011) 547–557
Characteristics
Half life 33 min
MW 267 Da
Oral BA <2%
logP 3.1
pKa 8.9
USE CASE: PARKINSON‘S DISEASE „OFF EPISODES“
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Apomorphine – Subcutaneous delivery
USE CASE: PARKINSON‘S DISEASE „OFF EPISODES“
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Apomorphine – Subcutaneous delivery
Gebauer Company website, 2019
myIV.com, website, 2019
Healthunlocked.com, website, 2019
USE CASE: PARKINSON‘S DISEASE „OFF EPISODES“
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Apomorphine – buccal transmucosal delivery
Sunovion.com, website, 2019
SPECIAL PATIENT GROUPS
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USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS
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Clinical trial using placebo films developed and manufactured by tesa Labtec
Prospective, single-centre, open,
randomised, single dose, age-stratified two-
way cross-over design with three age sub-
groups
150 patients aged 2 days – 12 months
To investigate the acceptability,
swallowability and palatability of placebo
ODF (2 x 3 cm) in comparison to glucose
syrup 15 % in children aged 2 days to 12
months Klingmann et al. 2018, EuPFI
USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS
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Clinical trial using placebo films developed and manufactured by tesa Labtec
Klingmann et al. 2018, EuPFI
USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS
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Clinical trial using placebo films developed and manufactured by tesa Labtec
ODF
• Everything swallowed
• Chewed / partially swallowed
• Spat out
• Inhaled / coughed
• Refused to take / termination
of examination by parents
Syrup
• Everything swallowed
• Partially swallowed
• Spat out
• Inhaled / coughed
• Refused to take / termination
of examination by parents
➢ Criterion 1 = Swallowability
➢ Criterion 1 + 2 = Acceptability
USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS
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Clinical trial using placebo films developed and manufactured by tesa Labtec
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ODF > syrup over all age groups
Difference 14.7 % (95 % CI 7.91-21.43), p < 0.0001
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ODF Syrup
Acceptability over all age groups
USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS
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Clinical trial using placebo films developed and manufactured by tesa Labtec
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ODF > syrup ODF > syrup ODF = syrup
p = 0.002 p < 0.001 p = 0.5
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ODF Syrup
Acceptability AG 1 (2 – 28 d)
0
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ODF Syrup
AcceptabilityAG 2 (29 d – 5 m)
0
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ODF Syrup
AcceptabilityAG 3 (6 – 12 m)
USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS
March 13th, 2019Drug Delivery and Formulation Summit Berlin 2019 - 24 -
Clinical trial using placebo films developed and manufactured by tesa Labtec
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ODF > syrup
Difference 21.3 %
(95 % CI 11.11-31.55),
p < 0.0001
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ODF Syrup
Swallowabilityover all AGs
Palatability
Assessments are in favour of
the ODF because the rates of
“unpleasant” judgments were
clearly smaller for ODF than
for syrup.
USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS
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Clinical trial using placebo films developed and manufactured by tesa Labtec
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Safety
• Galenic formulations well tolerated
• None of the children choked on ODF
• 2 children choked on syrup (age group 2 and 3), both events
without clinical relevance
• But: the number of patients and duration of application do not
provide sufficient data for reliable judgement on safety!
USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS
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Clinical trial using placebo films developed and manufactured by tesa Labtec
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Conclusion:
• Acceptability of ODF significantly superior to syrup over all age
groups, particularly prominent in age group 2
• ODFs are therefore suitable alternatives to liquid paediatric
formulations for young children as of preterm neonates
THANK YOUtesa Labtec GmbH
Dr. Sebastian Braun
Head of Science and Technology
Raiffeisenstr. 4
40764 Langenfeld
Germany
Phone: +49 2173 9735 0
E-Mail: [email protected]
Internet: www.tesa-labtec.com
tesa® products prove their impressive quality day in, day out in demanding conditions and are regularly subjected to strict controls. All technical information and data above mentioned are provided to the best of our knowledge on the basis of our practical
experience. They shall be considered as average values and are not appropriate for a specification. Therefore tesa SE can make no warranties, express or implied, including, but not limited to any implied warranty of merchantability or fitness for a particular
purpose. The user is responsible for determining whether the tesa® product is fit for a particular purpose and suitable for the user’s method of application. If you are in any doubt, our technical support staff will be glad to support you.