Novel Multifunctional Excipients

by Co-processing with Mg-Silicate

Dr. Faisal Al-AkaylehFaculty of Pharmacy, Petra University

Solid dosage forms

Active + Inactive Tablets Capsule

blends

Excipients: Inactive substances used as carriers for the active ingredients

Pharmaceutical excipientsType of excipientType of excipient ExamplesExamples

BindersBinders Starch, cellulose or modified cellulose Starch, cellulose or modified cellulose such as microcrystalline cellulose, such as microcrystalline cellulose, hydroxypropyl cellulose, lactose, or hydroxypropyl cellulose, lactose, or sugar alcohols like xylitol, sorbitol or sugar alcohols like xylitol, sorbitol or maltitolmaltitol

Fillers Fillers Lactose, dibasic calcium phosphate, Lactose, dibasic calcium phosphate, cellulose, sucrose, glucose, mannitol, cellulose, sucrose, glucose, mannitol, sorbitol, calcium carbonatesorbitol, calcium carbonate

Disintegrants Disintegrants Polyvinyl pyrrolidone, sodium starch Polyvinyl pyrrolidone, sodium starch glycolate, crosslinked sodium glycolate, crosslinked sodium carboxymethyl cellulose carboxymethyl cellulose (crosscarmellose)(crosscarmellose)

LubricantsLubricants Talc and fats, e.g. magnesium stearate Talc and fats, e.g. magnesium stearate or stearic acidor stearic acid

Pharmaceutical excipients

Function Application

Disintegration Filling Binding Wet

granulation

Direct

compression

Primojel • • •

Croscarmellose • • •

SuperTab • • •

Pharmatose • •

Avicel • • • • •

Conventional excipientsLimitations

Large gelling behavior of most disintegrants

Low compressibility of most fillers

Low disintegration of most binders

Avicel Ac-Di-Sol L-HPC

Primojel

under 100%

RH

Excipients development

Our Strategies of Excipient Development

Development of Excipient with multifunctional purposes(Binder, filler, disintegrant)

Processing of the natural bioplymers(Example: Chitin, starch, cellulose, Lactose, Microcrystalline Cellulose) with Mg silicate

Co precipitation and dry granulation (Roll compaction) with Mg silicate

Excipients processing

Roll compaction in the pharmaceutical industry

Resources of Mg Silicate from Jordan

Sand Dead Sea

Na silicate production Mg chloride-rich brine production

Mg Silicate Processing

Slurry Starch, or Chitin, or Cellulose or Lactose

For use in pharmaceutical industries

Mixing Mg silicate suspension

Decantors

Drying & sieving Mg silicate Mixing

30% MgCl2 45% Na silicate

For use in chemical industries

• The pH of the media of the co-precipitation of Ca, Mg, and Al silicates on chitin particles was measured as 10, 9, and 4, respectively

• The resulted co-precipitate was found to be an amorphous powder

Industrial Applications

Mg silicate

Chemical Pharmaceutical

Multifunctional Excipient

Fillers

Binders

Disintegrant

Soap and detergent

Lubricant

Agriculture

Adsorbent

Refining

Purifying agent

Anticaking agent

Decoloring of sugar

Fermentation industry

Processing with magnesium silicate by Roll Compaction

Improved flow Increase in

plasticity

Chitin-metal silicates..crystallography

Metal silicates

Chitin-metal silicatesMetal silicates

Mg silicate has high surface area (600-900 m2/g)-minimized upon compaction with starch to 8 m2/g… no drug adsorption observed

High water penetration and infiltration rates

Neutral pH surface acidity

Processing starch with Mg silicate

Permeability of processed starch

Swelling Abilities

Tensile strength of compacts

Disintegration time of compacts

Sensitivity to Mg stearate lubrication

Chitin – Metal Silicates

Chitin – Metal Silicates

Dissolution of Paracetamol

Compacted Lactose with Mg silicate

excipient

Microcrystalline cellulose-Mg silicate excipient

Thank you