KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
Other applications
L i n e c a p s KLEPTOSE
L i n e c a p s KLEPTOSE
solubility
KLEPTOSE L i nEnhanced
e c a p sdrug
KLEPTOSE
Linecaps
encapsulation
potential of amylose is also
able
to e
improve
the
cold
water
solubility
L i n e cThe
a
p
s
KLEPTOSE
L
i
n
c
a
p
s
KLEPTOSE
of certain drug molecules. In order to meet the solubilisation capacity of cyclodextrins,
are
needed,
higher quantities
ini weight
(about
10pfold
more)
of Kleptose Linecaps
KLEPTOSE
L
n
e
c
a
s
KLEPTOSE
L
i
necaps
this is due to its higher molecular weight. On a molar scale, Kleptose Linecaps and
comparable effects.
L i n e c a p s KLEPTOSE
L i n e ccyclodextrins
a p s have
KLEPTOSE
KLEPTOSE L i n e c a p s(100KLEPTOSE
Linecaps
mg/ml)
(100 mg/ml)
Pure Water
KLEPTOSE
HP–
betaL
i
n
e
c
a
p
s
KLEPTOSE
L i n e c a p s KLEPTOSE
Linecaps 17
cyclodextrin
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
Improved oxidation stability of herbal extracts and flavors
KLEPTOSE
L i n e c a p s KLEPTOSE L i n e c a p s
Used as a carrier, Kleptose Linecaps can contribute to the stabilisation of substances
L i n e csensitive
a p tos oxidation.
KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
Literature
L i n e c a p s KLEPTOSE
L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
®
®
®
®
®
®
®
®
®
®
®
®
®
®
®
®
®
®
Table:®cold water solubility of API’s in the presence of 100mg/ml of encapsulating
agents
®
®
®
Hydrocortisone
Dexamethasone
Ketoprofen
Lidocaine7
®
0.32 ± 0.05
0.09 ± 0.01
0.22 ± 0.04
4.45 ± 0.23
0.70 ± 0.06
0.60 ± 0.04
®
0.39 ± 0.02
4.51 ± 0.51
®
®
®
®
17.85
7.21
10.36
8.50
®
®
®
®
®
®
®
®
®
®
®
®
[1] Woertz K.,®2010. Performance qualification of an electronic tongue based on ICH guideline
Q2. Journal
®
of Pharmaceutical and Biomedical Analysis 51: 497-506.
[2] Preis M. et al, Pharmaceutics 2012, 4, 551-562; doi:10.3390/pharmaceutics4040551
®
[3] Preis M. et al, Poster; Electronic taste sensing system to evaluate taste masking properties of maltodextrins;
APGI - Poorly Soluble Drugs Workshop – Lille 2011
®
[4] Messner M.
® et al, Poster; Solution Enhancement of Drug Substances using Soluble®Amylose ; 8th World
Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, Istanbul 2012
®
®
®
®
®
®
®
The information contained in this technical bulletin is to our best knowledge true and accurate but all instructions,
recommendations or suggestions are made without guarantee.
Furthermore, no liability is accepted if use of any product in accordance with these data or suggestions infringes any patent.
® Registered trademark from ROQUETTE Frères / D3C
© Copyright May 2013
®
12854DepliantKleptoseLinecaps.indd 1-2
®
®
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
®
®
L i n e c a p s KLEPTOSE
Linecaps
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
q u e t t e p h a r®mLa .icno m
L i n e cw aw wp .sr oKLEPTOSE
ecaps
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
New taste
masking Solutions
KLEPTOSE L ine caps
®
®
®
®
®
®
®
®
®
®
®
®
15/05/13 07:44
KLEPTOSE L inec ap s
®
Key technical benefits
Taste Masking
A taste masking technology suitable for:
•A
wide range of dosage forms: solids, liquids, sachets, dry syrups and
orodispersible films
•O
TC and food supplements (ex: herbal products) as a cost effective
solution for taste masking
•P
aediatric and nutraceutical formulations
KLEPTOSE L inec ap s
®
A pea maltodextrin:
Example : Loperamide
Due to its origin from pea starch, Kleptose® Linecaps is rich in linear and
soluble amylose. This amylose fraction enables the formation of inclusion
compounds as required for taste masking and other applications.
Amylose exists as helical structures, and like a cyclodextrin these bear a hydrophilic
external surface and a hydrophobic internal cavity, created by the presence of
glycosidic ether bonds.
This cavity enables amylose to mask the bitter or unpleasant taste of drugs by
decreasing the amount of drug exposed to taste buds.
Kleptose® Linecaps is easily soluble in cold water without major risk of
physical instability such as recrystallization. This enables simple analysis and the
industrial production of robust and reproducible formulations.
Mw
KLEPTOSE ®
Linecaps 17
12000
The taste masking capacity of KLEPTOSE® Linecaps 17 has been screened
against various API’s using taste sensing systems, such as the SA 402B, Insent
Inc., Japan, equipped with 7 lipid membrane sensors. A shift in the signal generated
by a material from one or several sensors indicates a successful taste masking.
Kleptose® Linecaps demonstrated a taste masking with nearly all tested
APIs. By comparison a standard maltodextrin shows no improvement on taste
under same conditions. The efficiency of taste masking by the amylose molecules
is comparable with that of cyclodextrins, the optimal choice depends on the
structure of the API.
Solubility in
water
Very soluble
Retrogradation
risk
Loperamide HCl (0.5 mmol/l at 20°C) was successfully taste masked, particularly
when increasing amounts of Kleptose® Linecaps were added (from 0.5 to
1.5 mmol/l). Mixtures using hydroxypropyl-ß-cyclodextrin showed little variance
from the pure drug substance, demonstrating that taste masking by Kleptose®
Linecaps 17 was more successful than by modified cyclodextrin.
API+KlepLin
API+HPBCD
excipient
pure API
3
2
1
HPBCD
Ioperamide+HPBCD
pure Ioperamide
0.5
0
1.0
Low
1.5
Ioperamide+Kleptose Linecaps
-1
-2
Kleptose Linecaps
KLEPTOSE L inec ap s
®
Compliance:
- EU General Food Law 178/2002
- Current edition of the European Pharmacopoeia
New taste
masking Solutions
12854DepliantKleptoseLinecaps.indd 3-4
-3
-6
-4
-2
0
2
4
6
Figure: Principal component analysis (PCA map) of pure loperamide hydrochloride (red),
mixtures with hydroxypropyl-ß-cyclodextrin (grey), mixtures with Kleptose® Linecaps 17
(purple) and pure excipients (blue). Testing system SA 402B, Insent Inc., Japan. All seven
sensors displayed (R² values: PC-1: 0.79; PC-2: 0.17)
KLEPTOSE L i n e c a p s
®
15/05/13 07:44
KLEPTOSE L inec ap s
®
Key technical benefits
Taste Masking
A taste masking technology suitable for:
•A
wide range of dosage forms: solids, liquids, sachets, dry syrups and
orodispersible films
•O
TC and food supplements (ex: herbal products) as a cost effective
solution for taste masking
•P
aediatric and nutraceutical formulations
KLEPTOSE L inec ap s
®
A pea maltodextrin:
Example : Loperamide
Due to its origin from pea starch, Kleptose® Linecaps is rich in linear and
soluble amylose. This amylose fraction enables the formation of inclusion
compounds as required for taste masking and other applications.
Amylose exists as helical structures, and like a cyclodextrin these bear a hydrophilic
external surface and a hydrophobic internal cavity, created by the presence of
glycosidic ether bonds.
This cavity enables amylose to mask the bitter or unpleasant taste of drugs by
decreasing the amount of drug exposed to taste buds.
Kleptose® Linecaps is easily soluble in cold water without major risk of
physical instability such as recrystallization. This enables simple analysis and the
industrial production of robust and reproducible formulations.
Mw
KLEPTOSE ®
Linecaps 17
12000
The taste masking capacity of KLEPTOSE® Linecaps 17 has been screened
against various API’s using taste sensing systems, such as the SA 402B, Insent
Inc., Japan, equipped with 7 lipid membrane sensors. A shift in the signal generated
by a material from one or several sensors indicates a successful taste masking.
Kleptose® Linecaps demonstrated a taste masking with nearly all tested
APIs. By comparison a standard maltodextrin shows no improvement on taste
under same conditions. The efficiency of taste masking by the amylose molecules
is comparable with that of cyclodextrins, the optimal choice depends on the
structure of the API.
Solubility in
water
Very soluble
Retrogradation
risk
Loperamide HCl (0.5 mmol/l at 20°C) was successfully taste masked, particularly
when increasing amounts of Kleptose® Linecaps were added (from 0.5 to
1.5 mmol/l). Mixtures using hydroxypropyl-ß-cyclodextrin showed little variance
from the pure drug substance, demonstrating that taste masking by Kleptose®
Linecaps 17 was more successful than by modified cyclodextrin.
API+KlepLin
API+HPBCD
excipient
pure API
3
2
1
HPBCD
Ioperamide+HPBCD
pure Ioperamide
0.5
0
1.0
Low
1.5
Ioperamide+Kleptose Linecaps
-1
-2
Kleptose Linecaps
KLEPTOSE L inec ap s
®
Compliance:
- EU General Food Law 178/2002
- Current edition of the European Pharmacopoeia
New taste
masking Solutions
12854DepliantKleptoseLinecaps.indd 3-4
-3
-6
-4
-2
0
2
4
6
Figure: Principal component analysis (PCA map) of pure loperamide hydrochloride (red),
mixtures with hydroxypropyl-ß-cyclodextrin (grey), mixtures with Kleptose® Linecaps 17
(purple) and pure excipients (blue). Testing system SA 402B, Insent Inc., Japan. All seven
sensors displayed (R² values: PC-1: 0.79; PC-2: 0.17)
KLEPTOSE L i n e c a p s
®
15/05/13 07:44
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
Other applications
L i n e c a p s KLEPTOSE
L i n e c a p s KLEPTOSE
solubility
KLEPTOSE L i nEnhanced
e c a p sdrug
KLEPTOSE
Linecaps
encapsulation
potential of amylose is also
able
to e
improve
the
cold
water
solubility
L i n e cThe
a
p
s
KLEPTOSE
L
i
n
c
a
p
s
KLEPTOSE
of certain drug molecules. In order to meet the solubilisation capacity of cyclodextrins,
are
needed,
higher quantities
ini weight
(about
10pfold
more)
of Kleptose Linecaps
KLEPTOSE
L
n
e
c
a
s
KLEPTOSE
L
i
necaps
this is due to its higher molecular weight. On a molar scale, Kleptose Linecaps and
comparable effects.
L i n e c a p s KLEPTOSE
L i n e ccyclodextrins
a p s have
KLEPTOSE
KLEPTOSE L i n e c a p s(100KLEPTOSE
Linecaps
mg/ml)
(100 mg/ml)
Pure Water
KLEPTOSE
HP–
betaL
i
n
e
c
a
p
s
KLEPTOSE
L i n e c a p s KLEPTOSE
Linecaps 17
cyclodextrin
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
Improved oxidation stability of herbal extracts and flavors
KLEPTOSE
L i n e c a p s KLEPTOSE L i n e c a p s
Used as a carrier, Kleptose Linecaps can contribute to the stabilisation of substances
L i n e csensitive
a p tos oxidation.
KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
Literature
L i n e c a p s KLEPTOSE
L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
KLEPTOSE L i n e c a p s KLEPTOSE L i n e c a p s
L i n e c a p s KLEPTOSE L i n e c a p s KLEPTOSE
®
®
®
®
®
®
®
®
®
®
®
®
®
®
®
®
®
®
Table:®cold water solubility of API’s in the presence of 100mg/ml of encapsulating
agents
®
®
®
Hydrocortisone
Dexamethasone
Ketoprofen
Lidocaine7
®
0.32 ± 0.05
0.09 ± 0.01
0.22 ± 0.04
4.45 ± 0.23
0.70 ± 0.06
0.60 ± 0.04
®
0.39 ± 0.02
4.51 ± 0.51
®
®
®
®
17.85
7.21
10.36
8.50
®
®
®
®
®
®
®
®
®
®
®
®
[1] Woertz K.,®2010. Performance qualification of an electronic tongue based on ICH guideline
Q2. Journal
®
of Pharmaceutical and Biomedical Analysis 51: 497-506.
[2] Preis M. et al, Pharmaceutics 2012, 4, 551-562; doi:10.3390/pharmaceutics4040551
®
[3] Preis M. et al, Poster; Electronic taste sensing system to evaluate taste masking properties of maltodextrins;
APGI - Poorly Soluble Drugs Workshop – Lille 2011
®
[4] Messner M.
® et al, Poster; Solution Enhancement of Drug Substances using Soluble®Amylose ; 8th World
Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, Istanbul 2012
®
®
®
®
®
®
®
The information contained in this technical bulletin is to our best knowledge true and accurate but all instructions,
recommendations or suggestions are made without guarantee.
Furthermore, no liability is accepted if use of any product in accordance with these data or suggestions infringes any patent.
® Registered trademark from ROQUETTE Frères / D3C
© Copyright May 2013
®
12854DepliantKleptoseLinecaps.indd 1-2
®
®
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
KLEPTOSE
Linecaps
®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
®
®
L i n e c a p s KLEPTOSE
Linecaps
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
L i n e c a p s KLEPTOSE ® L i n e c a p s
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
q u e t t e p h a r®mLa .icno m
L i n e cw aw wp .sr oKLEPTOSE
ecaps
KLEPTOSE ® L i n e c a p s KLEPTOSE ®
New taste
masking Solutions
KLEPTOSE L ine caps
®
®
®
®
®
®
®
®
®
®
®
®
15/05/13 07:44