Novel Multifunctional Excipients by Co-processing with Mg-Silicate Dr. Faisal Al-Akayleh Faculty of Pharmacy, Petra University

Solid dosage forms  Active + Inactive  Tablets Capsule blends  Excipients: Inactive substances used as carriers for the active ingredients

Pharmaceutical excipients Type of excipient Examples Binders Starch, cellulose or modified cellulose such as microcrystalline cellulose, hydroxypropyl cellulose, lactose, or sugar alcohols like xylitol, sorbitol or maltitol Fillers Lactose, dibasic calcium phosphate, cellulose, sucrose, glucose, mannitol, sorbitol, calcium carbonate Disintegrants Polyvinyl pyrrolidone, sodium starch glycolate, crosslinked sodium carboxymethyl cellulose (crosscarmellose) Lubricants Talc and fats, e.g. magnesium stearate or stearic acid

Pharmaceutical excipients

Conventional excipients Limitations  Large gelling behavior of most disintegrants  Low compressibility of most fillers  Low disintegration of most binders AvicelAc-Di-SolL-HPC Primojel under 100% RH

Excipients development Excipients which function as binders, fillers, disintegrate /sustained release) Multifunctional excipients Suitable for direct compression (time, energy, cost, high speed tableting machines)

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

Processing Chemical modifications Cross-linking PVP-xl, Na, Starch glycolate Acid hydrolysisDextrins and MCC Physical modifications and/or co-processing GelatinizationStarch 1500 Spray drying Lactose DC, maltodectrins Roll compaction Excipients processing

Roll compaction in the pharmaceutical industry Roll Compaction Drug Formulations Densification Drug content uniformity Powder flowability Excipients Development and processing

Resources of Mg Silicate from Jordan

Mg Silicate Processing

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 Soap and detergent Agriculture Adsorbent Refining Purifying agent Anticaking agent Decoloring of sugar Fermentation industry Pharmaceutical Multifunctional Excipient Fillers Binders Disintegrant Lubricant

Processing with magnesium silicate by Roll Compaction  Improved flow  Increase in plasticity

Chitin-metal silicates..crystallography Metal silicates Chitin-metal silicates Metal silicates

 Mg silicate has high surface area ( m 2 /g)-minimized upon compaction with starch to 8 m 2 /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

Dissolution of Paracetamol

Compacted Lactose with Mg silicate excipient

Microcrystalline cellulose-Mg silicate excipient

Thank you