9623 AP List de Produits GB REVUE:frt:210x297mm … de Produits_GB_REVUE:.....frt:210x297mm ......
Transcript of 9623 AP List de Produits GB REVUE:frt:210x297mm … de Produits_GB_REVUE:.....frt:210x297mm ......
9623_AP_List de Produits_GB_REVUE:.....frt:210x297mm
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ROQUETTE, through its production units (in Europe, in Asia and in the United States) and its international distribution network, will assure a constant quality of products and services throughout the whole world.
® Registered trademark of Roquette Frères - © Roquette Frères S.A. - 07/2010
Supplier performance and reliability as good as it should be?
FILM FORMING AND COATING POLYMERS
• Modifi ed starch-based polymers - LYCOAT® • Tablet coating - LYCOAT® RS
FAST DISSOLVE AND CHEWABLE TABLETS (ODT)• Mannitol powders - PEARLITOL® C • Mannitol compound - PEARLITOL® Flash • Sorbitol powders - NEOSORB® P
DILUENTS AND FILLERS FOR TABLETS/CAPSULES
• Mannitol powders - PEARLITOL® C • Starches (native, modifi ed and pregelatinized) • Maltodextrin - GLUCIDEX®
DIRECT COMPRESSION
• Mannitol powders - PEARLITOL® DC and SD • Sorbitol powders - NEOSORB® P and NEOSORB® P DC • Xylitol powders - XYLISORB® DC • Partially pregelatinized starch - LYCATAB® C
BINDERS FOR WET GRANULATION
• Pregelatinized starch - LYCATAB® PGS
MOLECULAR ENCAPSULATION, TASTE-MASKING AND DISSOLUTION ENHANCER
• Betacyclodextrin - KLEPTOSE® • Methyl Cyclodextrin - CRYSMEB
SYRUPS, SEMI-SOLIDS AND SOFTGELS
• Liquid Sorbitol - NEOSORB® 70% • D-Sorbitol and sorbitan solution - POLYSORB® 85/70/00 as plasticizer
PYROGEN-FREE CARBOHYDRATES FOR INJECTABLE AND DIALYSIS SOLUTIONS
• Dextrose - LYCADEX® PF • Sorbitol - NEOSORB® PF • Hydroxy-Propyl betacyclodextrin - KLEPTOSE® HP and HPB Parenteral grades
DISINTEGRANTS AND SUPERDISINTEGRANTS
• Wheat starch, corn starch, potato starch
DIETARY FIBER, PROTEINS AND MINERAL SUPPLEMENTS
• Soluble dextrin - NUTRIOSE® FB and NUTRIOSE® FM • Non-GMO pea protein - NUTRALYS®
• Ready to use system – ReadiLYCOAT™• Thin fi lm delivery systems - LYCOAT® NG
• Mannitol powders - PEARLITOL® DC and SD• Xylitol powders - XYLISORB®
• Maltitol powders - SweetPearl™ • Partially pregelatinized starch - LYCATAB® C • Dextrose
• Mannitol compound - PEARLITOL® Flash• Maltitol powders - SweetPearl™ DC • Co-processed starch and lactose – STARLAC ®• Betacyclodextrin for direct compression - KLEPTOSE® DC
• Maltodextrin - LYCATAB® DSH
• Hydroxy-Propyl Betacyclodextrin - KLEPTOSE® HP and HPB
• Maltitol syrup - LYCASIN®
• Mannitol - PEARLITOL® PF• Sodium Gluconate Pharma
• Sodium starch glycolate - GLYCOLYS®
• Co-processed starch and CaCO3 - LYCATAB® Mineral• Chlorella microalga - ALGOMED®
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KLEPTL i n e ®
KLEPTL i n e ®®
KLEPTL i n e ®
KLEPTL i n e ®
KLEPTL i n e ®®
KLEPT pL 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 ® LL 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 ® LL 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 ® LL 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 ® LL i n e c a p s KLEPTOSE ® L i n e c a p s ®
New taste
masking Solutions
KLEPTOSE ® Linecaps
w w w . r o q u e t t e p h a r m a . c o mThe 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
© Copyright August 2011
E n h a n c e d s o l u b i l i t y o f A P I
Pure Water KLEPTOSE ® Linecaps 17 (100 mg/ml)
G o o d c o m p l e x a t i o n
KLEPTOSE ® Linecaps 17
Hydrocortisone (x 2 fold),
Dexamethasone (x 6 fold),
Ketoprofen (x 2 fold)
Carrier
0.32 ± 0.05
0.09 ± 0.01
0.22 ± 0.04
Hydrocortisone
Dexamethasone
Ketoprofen 7
0.70 ± 0.06
0.60 ± 0.04
0.39 ± 0.02
Ligand
Menthol
Methyl paraben
Propyl paraben
Complex level
100%
100%
100%
®
®
®
®®
®
11274DepMaltodextrine.indd 2-311274DepMaltodextrine.indd 2-3 10/08/11 13:0810/08/11 13:08
KLEPTOSE ® Linecaps
is a good taste masking technology applicable for:
• A wide range of dosage forms: liquids, chewable tablets, ODT,suspensions…
• Cost effective solution for OTC and nutraceutical products (ex: herbal products)
KLEPTOSE ® Linecaps
is a pea maltodextrin which forms a fl exible
adaptable amylose helix freely soluble in water
Amylose derived from pea starch is organized in helices with a hydrophilic external
surface due to the presence of hydroxyl groups and with a hydrophobic internal
surface due to the presence of hydrogen atoms. This helical structure confers the
amylose the necessary characteristics for the encapsulation of active principles
or fl avourings. Amylose is capable of masking bitter taste of drugs by decreasing
the overall amount of drug particles exposed to taste buds.
Key Technical benefi ts –Tested and Approved based on data available
The taste profi le of Paracetamol solutions has been determined in presence of
KLEPTOSE® Linecaps 17 using a taste sensing system SA 402B, Insent Inc.,
Japan, equipped with 7 lipid membrane sensors.
Encapsulating agent in 1:1 and 2:1 molar ratio
The use of KLEPTOSE® Linecaps 17 reduces the bitterness ofparacetamol.
MwSolubility in
waterRetrogradation
risk
12000KLEPTOSE ® Linecaps 17
Very soluble Low
M a s k i n g b i t t e r t a s t e o f p a r a c e t a m o l
30
20
10
0
-10
-20
-30
-40
-50
-60
-70
-80
Sen
sora
n tw
ort
(mV
)
Paracetamol
2 mg/ml
Paracetamol
150 mg + 2 mg/ml
75 mg + 2 mg
KLEPTOSE ® Linecaps 17
150 mg
75 mg
KLEPTOSE ® Linecaps 17
+
▲
New taste
masking Solutions KLEPTOSE ® Linecaps®
11274DepMaltodextrine.indd 4-511274DepMaltodextrine.indd 4-5 10/08/11 13:0810/08/11 13:08
KLEPTOSE ® Linecaps
is a good taste masking technology applicable for:
• A wide range of dosage forms: liquids, chewable tablets, ODT,suspensions…
• Cost effective solution for OTC and nutraceutical products (ex: herbal products)
KLEPTOSE ® Linecaps
is a pea maltodextrin which forms a fl exible
adaptable amylose helix freely soluble in water
Amylose derived from pea starch is organized in helices with a hydrophilic external
surface due to the presence of hydroxyl groups and with a hydrophobic internal
surface due to the presence of hydrogen atoms. This helical structure confers the
amylose the necessary characteristics for the encapsulation of active principles
or fl avourings. Amylose is capable of masking bitter taste of drugs by decreasing
the overall amount of drug particles exposed to taste buds.
Key Technical benefi ts –Tested and Approved based on data available
The taste profi le of Paracetamol solutions has been determined in presence of
KLEPTOSE® Linecaps 17 using a taste sensing system SA 402B, Insent Inc.,
Japan, equipped with 7 lipid membrane sensors.
Encapsulating agent in 1:1 and 2:1 molar ratio
The use of KLEPTOSE® Linecaps 17 reduces the bitterness ofparacetamol.
MwSolubility in
waterRetrogradation
risk
12000KLEPTOSE ® Linecaps 17
Very soluble Low
M a s k i n g b i t t e r t a s t e o f p a r a c e t a m o l
30
20
10
0
-10
-20
-30
-40
-50
-60
-70
-80
Sen
sora
n tw
ort
(mV
)
Paracetamol
2 mg/ml
Paracetamol
150 mg + 2 mg/ml
75 mg + 2 mg
KLEPTOSE ® Linecaps 17
150 mg
75 mg
KLEPTOSE ® Linecaps 17
+
▲
New taste
masking Solutions KLEPTOSE ® Linecaps®
11274DepMaltodextrine.indd 4-511274DepMaltodextrine.indd 4-5 10/08/11 13:0810/08/11 13:08
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KLEPTL i n e ®
KLEPTL i n e ®®
KLEPTL i n e ®
KLEPTL i n e ®
KLEPTL i n e ®®
KLEPT pL 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 ® LL 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 ® LL 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 ® LL 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 ® LL i n e c a p s KLEPTOSE ® L i n e c a p s ®
New taste
masking Solutions
KLEPTOSE ® Linecaps
w w w . r o q u e t t e p h a r m a . c o mThe 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
© Copyright August 2011
E n h a n c e d s o l u b i l i t y o f A P I
Pure Water KLEPTOSE ® Linecaps 17 (100 mg/ml)
G o o d c o m p l e x a t i o n
KLEPTOSE ® Linecaps 17
Hydrocortisone (x 2 fold),
Dexamethasone (x 6 fold),
Ketoprofen (x 2 fold)
Carrier
0.32 ± 0.05
0.09 ± 0.01
0.22 ± 0.04
Hydrocortisone
Dexamethasone
Ketoprofen 7
0.70 ± 0.06
0.60 ± 0.04
0.39 ± 0.02
Ligand
Menthol
Methyl paraben
Propyl paraben
Complex level
100%
100%
100%
®
®
®
®®
®
11274DepMaltodextrine.indd 2-311274DepMaltodextrine.indd 2-3 10/08/11 13:0810/08/11 13:08
PEARLITOL® FlashMELT-IN-THE-MOUTH MAGIC WITH MANNITOL?
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 1
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 2
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 1
• A uniquely pleasing taste experience . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 3
• An intrinsic composition . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 4• No superdisintegrant required . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 4• A low lubricant level required . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 5
• Robust tablets . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 7
• Excellent compactibility . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 8• Good dilution potential . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 9• Impact of tabletting speed . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 10
• Quick disintegration . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 11
• In vivo disintegration test . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 12• Pharmacopoeial testing . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 13• In vitro test correlated with in vivo test . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 14
• Easy formulation. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 15
• PEARLITOL® Flash. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 17
• Definition and regulation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 18• Powder characteristics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 18• Particle size . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 19• Low hygroscopicity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . page 19
C O N T E N T S
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PEARLITOL®
FlashPEARLITOL ® Flash
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 1
P A G E 2
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 2
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 3
A uniquely pleasing taste experience
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 3
P A G E 4
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
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A u n i q u e l y p l e a s i n g t a s t e e x p e r i e n c e
An intrinsiccompositionPEARLITOL® mannitol is already well-known for itspleasant and mild sweet taste.
With PEARLITOL® Flash, a mannitol starchcompound, orodispersible tablets melt in the mouthwith a very creamy, smooth texture and a uniquelypleasing taste experience.
No superdisintegrantrequiredTo achieve rapid disintegration of orodispersibletablets, superdisintegrants are usually added in largequantity and can impair the mouthfeel.
PEARLITOL® Flash is a self-disintegrating mannitolcompound so no superdisintegrant is required in theformulation of orodispersible tablets.
PEARLITOL® Flash gives
orodispersible tablets (ODT) of
exceptional taste thanks to its:
• intrinsic composition
• self-disintegrating properties
• low level of lubricant required
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 4
Better compliance thanks to a uniquely pleasing taste experience, largely appreciatedfrom paediatrics to geriatrics.
Clean labelling with two long-established ingredients of natural origin that opens upopportunities in nutraceutical formulations.
A u n i q u e l y p l e a s i n g t a s t e e x p e r i e n c e
A low lubricant level requiredUsing PEARLITOL® Flash, 0.4% lubricant issufficient to ensure a direct compression process.
This also contributes to a better taste of the tablet, ashigh levels of lubricant produce a taste that manyconsumers find objectionable.
At 0.3% ejection force drastically increased. Above0.4% no significant differences were observed in thecompression process and in tablet characteristics.Hence the optimum lubricant level in the testedconditions is 0.4%.
Trials were carried out on a single-punch press KorschXP1 fitted with 13mm diameter flat punches withbevelled edges. Magnesium stearate (Barlöcher vegetal)was used as lubricant at levels varying from 0.3% to1.2%.
Compression force (kN)
Mg stearate 1.2% Mg stearate 0.8% Mg stearate 0.4% Mg stearate 0.3%
Ejec
tion
forc
e (N
)
10 15 20 250
100
200
300
400
500
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Ejection force as a function of lubricant ratio
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 5
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 5
P A G E 6
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 6
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 7
Robust tablets
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 7
P A G E 8
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
ExcellentcompactibilityPEARLITOL® Flash enables the production of highquality orodispersible tablets, with classical DirectCompression.
A 15 kN compression force is sufficient to obtaintablets with suitable hardness, friability anddisintegration time characteristics as illustrated below.
Trials carried out on a Korsch XP1 press fitted with13mm diameter flat bevelled-edge punches. 500 mgorodispersible tablets, evaluated using PharmacopoeialTests.
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R o b u s t t a b l e t s
Compression force (kN)
Disintegration time (s)Hardness (N)Friability (%)
Dis
inte
grat
ion
time
(s)
Har
dnes
s (N
)
Fria
bilit
y (%
)
100
20
40
60
80
100
120
15 20 250.0
0.5
1.0
1.5
2.0
2.5
3.0
3.5
PEARLITOL® Flash has been
specifically designed for
ordispersible tablets using a
Direct Compression process.
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Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 9
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R o b u s t t a b l e t s
Good dilutionpotentialPEARLITOL® Flash makes it possible to produce veryrobust tablets, even at high dilution. Dilution potentialis illustrated with acetaminophen.
Trials carried out on a Korsch XP1 press fitted with13mm diameter flat bevelled-edge punches. 500 mgorodispersible tablets, evaluated using PharmacopoeialTests. Results shown for a 25 kN compression force.
% Acetaminophen
% PEARLITOL® Flash
Disintegration time (s)Hardness (N)Friability (%)
Dis
inte
grat
ion
time
(s)
Har
dnes
s (N
)
Fria
bilit
y (%
)
0
10
20
30
40
50
10 20 30 40 50
90 80 70 60 50
60
70
80
0
0.1
0.2
0.3
0.4
0.5
0.6
0.7Disintegration time (s)Hardness (N)Friability (%)
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 9
P A G E 10
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
Impact of tablettingspeedTrials were carried out on a single-punch press with atabletting speed varying from 10 to 60 tablets /minute. Tabletting speed has limited impact ondisintegration time.
Trials carried out on a Korsch XP1 press fitted with13mm diameter flat bevelled-edge punches. 500 mgorodispersible tablets, evaluated using PharmacopoeialTests. Results shown for a 15 kN compression force.
Tabletting speed (tablets/mn)
Disintegration time
Dis
inte
grat
ion
time
(s)
8.5 20 30 40 50 600
20
40
60
80
100
120
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R o b u s t t a b l e t s
Disintegration time as a function of tabletting speed
Classical Direct Compression equipment can be used, thanks to excellent compactibility.
Robustness of tablets allows traditional blister packaging to be used.
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Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 11
Quick disintegration
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P A G E 12
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
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Q u i c k d i s i n t e g r a t i o n
Trials were carried out on a Korsch XP1 press, fittedwith 13mm diameter flat bevelled-edge punches forhydrochlorothiazide tablets and fitted with 7mmdiameter flat bevelled-edge punches for sodiumfluoride tablets.
Other NUTRIOSE® grades have been developed for specific applications.
PEARLITOL® Flash
Active
Magnesium stearate
In vivodisintegration testTests have been carried out on tablets containingdifferent actives to evaluate the in vivo disintegrationtime. Tablets formulas and characteristics are givenin the table below.
Total
Weight (mg)
Thickness (mm)
Hardness (N)
Friability (%)
Hydrochlorothiazidetablets
94.6%
5.0%
0.4%
Sodium fluoridetablets
97.4%
2.2%
0.4%
77.4 ± 1.3
0.26
82.8 ± 2.3
0.16
505.4 ± 0.7
2.96 ± 0.01
104.4 ± 0.2
1.93 ± 0.01
100% 100%
Quick disintegration is the key
parameter for orodispersible
tablets. Consumers expect a
complete disintegration in
about 30-40s. In vivo and in
vitro tests have been developed
to measure this time on tablets.
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Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 13
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Q u i c k d i s i n t e g r a t i o n
PharmacopoeialtestingODT must disintegrate within 3 minutes, accordingto European Pharmacopoeia disintegration testconditions. In vitro disintegration tests according tomajor pharmacopoeias are performed in a largequantity of water, and therefore do not match exactlywhat happens in the mouth, where a limited quantityof saliva is available for disintegration. No correlation exists between Pharmacopoeiadisintegration test and in vivo disintegration test.
ODT tablets with PEARLITOL® Flash lead typicallyto disintegration times of less than 3 minutes usingthe Pharmacopoeial test, depending on the ODTformulation and the tablet size. The above describedtablets were evaluated using Pharmacopoeialdisintegration test. Results are given below.
In vitro disintegration time (s)
Hydrochlorothiazidetablets
81 ± 13
Sodium fluoridetablets
70 ± 7
In vitro disintegration time was measured below 3 minutes.
In vivo disintegration time was measured by a panelof 8 people. Results are given below.
In vivo disintegration time (s)
Hydrochlorothiazidetablets
20 ± 5
Sodium fluoridetablets
22 ± 2
In vivo disintegration time was measured below 1 minute.
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 13
P A G E 14
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
In vitro testcorrelated with invivo testAn in vitro test has been developed to mimic the invivo disintegration, with excellent correlation.
A charge of 3N is applied on top of an ODT. Twomillilitres of water are added (equivalent to the salivavolume). The change in charge is recorded. As thetablet disintegrates, charge decreases. The typicalcurve obtained is given for illustration.0 10
0.0
0.5
1.0
1.5
2.0
2.5
3.0
Time (s)
Char
ge (N
)
20 30 40 50 60 70 80
Tablet desagregates in lessthan 40s, as visualized by the sudden collapse of applied charge
Quick disintegration of PEARLITOL® Flash ODTs makes possible “On-the-go” use andquick onset of action.
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Q u i c k d i s i n t e g r a t i o n
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 14
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 15
Easy formulation
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 15
P A G E 16
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
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E a s y f o r m u l a t i o n
With PEARLITOL® Flash, formulation is simplifiedbecause fewer excipients are required:• no superdisintegrant• minimum level of lubricant• minimum quantity of intense sweeteners or flavours
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 16
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 17
PEARLITOL® Flash
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 17
Definition andregulationPEARLITOL® Flash is a compound of mannitol andextra white maize starch. Both ingredients comply withpharmaceutical and food regulations and can be usedfor pharmaceutical and nutraceutical orodispersibletablets.
PowdercharacteristicsPEARLITOL® Flash is designed for Direct Compressionorodispersible tablets. It has excellent flow properties.
Indicative values; Hosokawa and Pharmacopoeia funnel test.
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P E A R L I T O L ® F l a s h
Bulk density (g/ml) 0.52
Tapped density (g/ml) 0.62
Haussner ratio 1.19
Angle of repose (°) 43
Ability to settle (ml) 16
Flowability (funnel, s) 5.5
Loss on drying (%) 1.1
P A G E 18
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 18
Particle size
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P E A R L I T O L ® F l a s h
D10 (µm) 80
Mean diameter (µm) 200
D90 (µm) 300
Target R.H. (%)
Chan
ge In
Mas
s (%
) - D
ry
0.0
5.0
10.0
15.0
20.0
25.0
30.0
0 10 20 30 40 50 60 70 80 90 100
Low hygroscopicityPEARLITOL® Flash is stable to humidity as illustratedin the figure below.
Particle Diameter (µm)
Cum
ulat
ive
> V
olum
e (%
)
Diff
eren
tial
Volu
me
(%)
00.4 1 2 4 6 10 20 40 60 100 200 400 1000 2000
0
1
2
3
4
5
6
7
8
20
40
60
80
100
Roquette PEARLITOL® Flash: Melt- in-the-mouth magic with mannitol?
P A G E 19
Indicative values; Beckman Coulter Laser Particle sizeanalyser.
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 19
To contact us:
ROQUETTEPharmaceutical and Cosmetics Business Unit
62080 Lestrem Cedex France
Telephone: 33 (0)3 21 63 36 00Fax: 33 (0)3 21 63 94 64
Pharma.business.unit@roquette.comwww.roquettepharma.comwww.roquettenutra.com
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 20
The information contained in this document is to the best of our knowledge true and accurate but all instructions, recommendations or suggestions are made without
any guarantee. Since the conditions of use are beyond our control, we disclaim any liability for loss and/or damage suffered from use of these data or suggestions.
Furthermore, no liability is accepted if use of any product in accordance with these data or suggestions infringes any patent.
No part of this document may be reproduced by any process without our prior written permission.
® Registered trademarks of Roquette Frères
© Roquette Frères S.A. - 09/2009
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 21
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mROQUETTE WORLDWIDE
FRANCERoquette FrèresCorporate Headquarters62080 Lestrem cedex – FranceTelephone: + 33 3 21 63 36 00Fax: + 33 3 21 63 38 50
FINLANDRoquette Nordica OyPL 11 P.O.BFIN-02171 Espoo – FinlandTelephone: + 358-9502 4410Fax: + 358-9-502 44111
GERMANYRoquette GmbHSchaumainkai 4560596 Frankfurt - DeutschlandTelephone: + 49 69 60 91 050Fax: + 49 69 60 91 05 59
ITALYRoquette Italia S.p.AVia Serravalle 2615063 Cassano SpinolaAlessandria - ItaliaTelephone: + 39 0 143 7741Fax: + 39 0 143 477 295
ROMANIARoquette Romania S.A.Platforma IndustrialàSud-Vest Nr 5Calafat – Dolj - RomaniaTelephone: + 40 251 333 065Fax: + 40 251 329 215
SPAINRoquette Laisa España, S.AAvenida Jaime I, S/N.46450 Benifaió - Valencia - EspañaTelephone: + 34 96 178 98 00Fax: + 34 96 178 98 10
UNITED KINGDOMRoquette UK LtdSallow RoadWeldon Industrial EstateCorby Northants NN17 5JXUnited KingdomTelephone: + 44 15 36 273000Fax: + 44 15 36 263873
CHINARoquette ShanghaiRoom 501, 505, 506, K. Wah CentreNo. 1010, Huai Hai Zhong RoadShanghai 200031 - ChinaTelephone: + 86 21 54039922Fax: + 86 21 54036606
INDIARoquette India Private LimitedOffice n° 702, 7th Floor Powai PlazaHiranandani GardensPowaiMumbai 400 076 - IndiaTelephone: + 91 22 2570 6775Fax: + 91 22 2570 6770
JAPANRoquette Japan K.K.Tokyo Head Office2F, Kasuga Business Center Building1-15-15 NishikataBunkyo-KuTokyo 113-0024 - JapanTelephone: + 81 3 3830 1510Fax: + 81 3 3830 1525
KOREARoquette Korea Ltd.17th floorKangnam Building. 1321 - 1Seocho-dong, Seocho-KuSeoul 137 – 070 - KoreaTelephone: + 82 2 2141 3400Fax: + 82 2 2141 3482
EUROPE
AMERICA
ASIA
USARoquette America, Inc.1417 Exchange StreetPO Box 6647Keokuk. IA 52632 – 6647 - USATelephone: + 1 319 524 - 5757Fax: + 1 319 526 – 2345
RUSSIAOOO Roquette Rus1A, Semenovskaya squareBusiness center “Sokolinaya Gora”13-th floor107023 Moscow - RussiaTelephone : + 7 495 627 76 61Fax : + 7 495 627 76 62
9539_BRO_Pearlitol_FLASH4 23/09/09 10:47 Page 22
XXYLISORB DCx y l i t o l
XXYLISORB® DCx y l i t o l
XXYLISORB® DCx y l i t o l
XXYLISORB®DCx y l i
XXYLISOx y l
XXYLISOx y
XXYLISx y
XXYLISORB® DCx y l i t o l
XXYLISORB® DCx y l i t o l
XYLISORB DCx y l i t o l
XYLISORB® DCx y l i t o l
XYLISORB® DCx y l i t o l
XYLISORB® DCx y l i t o l
XYLISORB® DCx y l i t o l
XYLISORB® DCx y l i t o l
XYLISORB® DCx y l i t o l
XYLISORB® DCx y l i t o l
XYLISORB® DCx y l i t o l
®
®
®®
®
®®®®®®®®®®®®®®®®®®®®
XYLISORB® DC is a new granulated
xylitol specifically designed for Direct
Compression of smooth chewable
tablets.
Create pleasant smooth chewable tablets with new
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
© Copyright September 2010
XYLISORB® DC XYLISORB® DC gives smooth chewable tablets with
◗ an attractive mouthfeel resulting from the singular combination of its refreshing taste and smooth texture
◗ fl exibility in formulation, with this robust DC ingredient
◗ reliability of a pharma supplier
XYLISORB® DC:k e y b e n e f i t s
www.roquettenutra.com
XYLISORB® DC is part of the Roquette Direct Compression polyols range, which includes sorbitol, maltitol,
mannitol and other xylitol powders.
Powder characteristics
Burst of freshness For smooth texture tablets
Nutrition benefits
Formulation benefits
Formulation example
Slightly hygroscopic powder
Dynamic Vapor Sorpt ion at 20°C
Excellent compactibility
Particle size adapted to smooth chewable tablets
Beckman Coulter Laser Part ic le s ize analyser
0.4 0.6 200010006004002001006040201086421
Particle Diameter (µm)
Diffe
rent
ial V
olum
e (%
)
9
8
7
6
5
4
3
2
1
0
A directly compressible granulated xylitol For appealing smooth chewable tablets
20
15
10
5
00
Relative humidity (%) 5010 20 30 40 60 70 80 90
Wat
er U
ptak
e at
Equ
ilibriu
m (%
)
◆
◆
◆◆◆◆◆◆◆◆◆◆◆◆◆◆◆
◆ ◆ ◆ ◆ ◆◆
300
250
200
150
100
50
00
Compression Force (kN)1510 20 25
Hard
ness
Erw
eka
TBH3
0 (N
)
◆
◆
◆
◆
400
350
300
250
200
150
100
50
01.25
Tablet Density1.35 1.40 1.451.30 1.551.50
Hard
ness
Erw
eka
TBH3
0 (N
)
◆
◆
◆
0.71
0.79
10
6
43
Aerated bulk density (g/ml)
Tapped bulk density (g/ml)
Compressibility (%)
Flowability funnel (time, s)
Angle of repose (°)
140
300
460
D10 (µm)
Mean (µm)
D90 (µm)
Fette P1000 rotative press, biconvex tablets, 10 mm diameter, 5 mm thickness, 1% Mg stearate
Frogerais Single Punch Press, biconvex tablets, 13 mm diameter, 6 mm thickness, 1% Mg Sterate
XYLISORB® DC Xylitol freshness is a combination of its high solubility at mouth temperature and negative heat of dissolution. This intense refreshing effect combines well with cool fl avors such as mint. Xylitol sweetness is equivalent to sucrose’s one, which gives the tablet an astonishing sweet cool taste.
XYLISORB® DC Xylitol gives a very smooth texture to the chewable tablets, that almost melt in the mouth.Whether used alone or in combination with other polyols of Roquette portfolio, XYLISORB® DC offers the formulator a full palette of textures.
XYLISORB® DC Xylitol provides also benefi ts thanks to
◗ Well established dental benefi ts
◗ Low calorie ingredient
◗ Low glycaemic index
These nutrition benefi ts are valuable in nutraceutical applications.
XYLISORB® DC Xylitol provides benefi ts for the formulator thanks to
◗ easy-to-use ingredient
◗ natural origin ingredient
◗ stability and compatibility
◗ reliability
◗ formulation fl exibility enabling creativity
I N D I C A T I V E V A L U E S