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Philippe Lefvre
Agenda
Direct compression requirements API & excipients powder properties Formulation ROQUETTE range of DC excipients Mannitol PEARLITOL SD: the ideal DC excipient NEOSORB P300DC & P150DC, SWEETPEARL P300DC & XYLISORB DC Indicative formulation guidelines StarLac
Weighing
Blending
Lubricating
Tabletting
4 steps !
Easy!
Philippe Lefvre 2012
The DC is born!
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API stability by avoiding heat and humidity Good disintegration, especially for dispersible tablets/ODT Better mouth-feeling (chewable tablets, suckable tablets) Less process steps for manufacture and quality control High production rate Cost saving (equipments, energy, process control, staff)
Pharmaceutical Technology,2005
Philippe Lefvre 2012 ROQUETTE range of excipients for direct compression
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Configuration (Aspect ratio<1.5 For an homogeneous blend, same particle size and density than API For water sensible API or tablet, use a not hygroscopic excipient as mannitol PEARLITOL
Philippe Lefvre 2012 ROQUETTE range of excipients for direct compression
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For unstable and water sensible drug, the ideal excipients: Mannitol PEARLITOL SD, DC or Flash
Philippe Lefvre 2012 ROQUETTE range of excipients for direct compression
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PEARLITOL FLASH:
Compound composed mainly of mannitol with a small proportion of starch added Ideal excipient for Orally Dispersible Tablets Formulation
Philippe Lefvre 2012 ROQUETTE range of excipients for direct compression
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A range of particle sizes adapted to the diversity of drug particle sizes Highest particle sizes required by specific technologies (as coated micro granules) Corresponding to the majority of drugs requirements (as particle size), PEARLITOL 200SD is by far the most used
Philippe Lefvre 2012 ROQUETTE range of excipients for direct compression
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Mannitol is the only excipient being not hygroscopic and soluble (opposite properties)
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PEARLITOL 25C + 10% LYCATAB DSH PEARLITOL 50C + 10% LYCATAB DSH PEARLITOL 160C + 10% LYCATAB DSH
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Benefits of PEARLITOL 200SD: Wrap-up PEARLITOL 200SD an ideal excipient for pharmaceutical and nutraceutical tablets:
Unstable or water sensitive API Unstable or water sensitive tablets As effervescent tablets Fast disintegrating tablets Orally dispersible tablets all the type of tablets
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Maltitol
Xylitol
PEARLITOL SD, DC
XYLISORB DC XYLISORB DC
PEARLITOL SD, DC NEOSORB P20/60DC NEOSORB P60W NEOSORB P20/60DC NEOSORB P60W NEOSORB P300DC, P150DC NEOSORB P20/60DC NEOSORB P60W NEOSORB P20/60DC NEOSORB P60W NEOSORB P300DC, P150DC
PEARLITOL SD, DC
SWEETPEARL P300DC
XYLISORB DC
PEARLITOL SD, DC
PEARLITOL SD, DC
SWEETPEARL P300DC
PEARLITOL Flash
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Suckable
Fast dissolving
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Philippe Lefvre
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Philippe Lefvre
Drawbacks
Animal original (BSE) Lactose intolerance Reducing sugar (Maillard reaction )
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Drawbacks
High water content (7.0) Easy to catch water Bad taste (Sand feeling ) Sensitive to magnesium stearate
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Drawbacks
Insoluble Alkaline surface
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Advantages
Fast disintegration Self lubricating
Drawbacks
Hygroscopicity Sensitive to magnesium stearate Water content (about 8%)
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Drawbacks
Animal original (BSE) Lactose intolerance Reducing sugar(maillard reaction )
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Advantages
Very good compactibility Sweet, cooling effect Very soluble Cost saving
Drawbacks
Slightly hygroscopic
NEOSORB P300DC is a new grade with a high specific surface (high oil adsorption)
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PEARLITOL SD/DC
Advantages
Non hygroscopic Stability versus drug Quick disintergration (SD) High compactibility Free flowing soluble Sweet, slight cooling effect
Drawbacks
Generally high Magnesium stearate
?
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PEARLITOL Flash
Advantages
Fast disintegration Easy to lubricate good compactibility Good mouthfeel Avoid patent issue
Drawbacks
USA DMF, no pharma regulation in China
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