Lipids for Fluid Bed Microencapsulation

PRSENTATIONSTITEL

Lipids for API microencapsulationEffect of processing conditions on product performance

Diogo G. LopesIndexMicroparticles Market demandTechnologiesAdvantages of Lipids as coating excipientPhysical behavior of lipidsAging effectLipid compositionPolymorphismMicrostructureBlooming effectApproaches to have stable productsOur approach

21.08.2014RCPE Prsentationstitel 21. i. Market demand for microparticlesImproving product performanceMaximize drug absortionMinimizing mucosa irritationReducing inter- and intrapatient variability

Increasing patient adherenceImproving swallowingSize reductionTaste and smell maskingPersonalize dosesNasogastric feeding

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1. ii. Microencapsulation technologies

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S. Gouin / Trends in Food Science & Technology 15 (2004) 330 - 347MicrocapsuleMicrosphere / Micromatrix1. ii. Fluidized bed coatingFluidized bedVery efficientFlexibleEither microcapsules or microspheresBasically any kind of coating material21.08.2014RCPE Prsentationstitel 5

Schematic process of fluid bed microencapsulationHot-melt fluid bed coater

2. Lipids as coating excipientsFunctional propertiesImprove stability by preventing the physical or chemical dregradationTaste maskingSustain drug releaseLubrificationCompressebility

Using GRAS excipientsPediatricsPredominant digestible

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Lipid coatingDrug

2. Advantages of Lipids as coating excipientIndustrial point of viewToxicity and risk of explosionCostly solvents and residue recovery stepEnergy inputMicrobial contamination risk

Advantages over polymersGenerally less amount Relatively inexpensiveDrug release should not be influenced by the presence of alcohol

21.08.2014RCPE Prsentationstitel 7Organic solventsAqueous solvents

3. i. Aging effect10% Cafene dispersion in Gelucire 50/13Storage at 37 C21.08.2014RCPE Prsentationstitel 8

N. Khan; D. Craig / Journal of Pharmaceutical Sciences 93 (2004) 2962-71

Drug release profileDSC analysisSEM images3. Physical behavior of Lipid excipients21.08.2014RCPE Prsentationstitel 9Processing Conditions3. ii. Lipid composition21.08.2014RCPE Prsentationstitel 10

Hydrogenated vegetable oils

PEGs 200 - 2000

Saturated Polyoxylglycerides(Gelucires)WaxesFatty acids and partial glycerides(Compritol; Precirol)3. iii. Polymorphism of triglycerides21.08.2014RCPE Prsentationstitel 11

K. Sato / Chemical Engineering Science 56 (2001) 2255-22653. iv. Microstructure21.08.2014RCPE Prsentationstitel 12

A. Marangoni / Soft Matter 8 (2012) 1275-13003. v. Blooming effect21.08.2014RCPE Prsentationstitel 13

H. Mayama / Soft Matter 5 (2009) 856-859

4. Approaches to have stable productsAging Step S. Salle / EP 1 479 383 A1 2004Fluid bed at 10-15 C below the solidification pointCuring at 40C for 1 day

Tempering Step K. Chansanroj / J.Drug Del. Sci. Tech 17 2007Fluid bed at solidification pointCuring at solidification point temperature for 3 hours

seeds approach Y. Kakiguchi / US 2003/0091648 A1Fluid bed at no higher than solidification pointAdding -form seeds to the fluid bedCuring for ten to several tens hours

21.08.2014RCPE Prsentationstitel 144. Approaches to have stable productsTempering Step Hydrogenated soybean oil (HSO)Fluid bed at solidification pointCuring at solidification point temperature for 3 hours

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N. Chansanroj / J. Drug Del. Sci. Tech 17 (2007) 347-352

5. i. Our ApproachAimProduce stable lipid coatings:To have controlled drug releaseAvoiding the aging stepAvoiding the bloomed surfaceProduce microcapsules with:Taste maskingProtection of the core drug from the environment

21.08.2014RCPE Prsentationstitel 165. i. TheoryTheory

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