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Alubra® Our Lubricant Brings More to the Tablet Nutrition & Biosciences

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Alubra® Our Lubricant Brings More to the Tablet Nutrition & Biosciences Nutrition & Biosciences Pharma Solutions Alubra® Our lubricant brings more to the tablet Nutrition & Biosciences Alubra® sodium stearyl fumarate delivers Lubricants are a vital part of the tablet and capsule Product Benefits manufacturing process. Formulators have typically Compared with the widely used lubricant selected magnesium stearate to meet their needs as a magnesium stearate, Alubra® offers familiar, well-established lubricant for oral solid dosage forms. Enhanced disintegration and dissolution Magnesium stearate’s hydrophobic structure provides excellent lubrication but it may also affect other product Improved compactability properties. Previous studies demonstrate that magnesium stearate can negatively impact disintegration and Less sensitivity to blending time dissolution1. Blend times must be limited to avoid over- lubrication. Similar lubrication performance Formulators should consider these factors before selecting the appropriate lubricant for their formulation. Poorly Compatibility with a range of APIs soluble drugs, orally disintegrating tablets (ODTs)2, and effervescent dosage forms will typically require a more hydrophilic lubricant. Alubra® sodium stearyl fumarate offers many advantages compared to magnesium stearate. Our lubricant brings more to the tablet. The chemistry of Alubra® provides important advantages Typical Alubra® Properties Alubra® sodium stearyl fumarate is less hydrophobic than Molecular Formula: C22H NaO4 magnesium stearate due to the presence of a fumarate 39 group on the end of the structure. In addition to offering Formula Weight: 390.53 improved water dispersibility, the fumarate moiety of Alubra® increases the melting temperature, which allows Melting Point: 220-240° C greater functionality at high press speeds. The stearate Recommended Use 0.5-2.0% of Formulation chain of Alubra® maintains the lubricity of the compound, level: supporting low ejection forces and preventing sticking. 2-Butenedioic acidiconoctadecyl Chemical name: Chemical Structure of Alubra® Sodium Stearyl Fumarate ester, sodium salt Acidity: pH 8.3 (5% water solution at 90° C) acetone practically insoluble ethanol practically insoluble Solubility: methanol slightly soluble Water 1:5 90° C Water 1:20,000 25° C BET surface area 2.0 – 4.0 m2/g Density (bulk) 0.2 to 0.3 g/cm3 Density (tapped) 0.3 to 0.4 g/cm3 EINECS # 223-781-1 CID # 23665634 CAS No. 4070-80-8 1. Chowhan, Z.T. and Chi, L.H. (1986); Drug Excipient Interactions Resulting from Powder Mixing IV: Role of Lubricants and their Effect on In Vitro Dissolution; Journal of Pharmaceutical Sciences, 75: 542-545. doi: 10.1002/jps.2600750604 2. Gebert, K. Meyer-Bohm, A. Maschke and K. Kolter; Compression Characterization and Lubricant Sensitivity of Orally Disintegrating Tablets Based on Lubiflash; Pharmaceutical Technology Europe, January 1, 2009, Volume 21, Issue 1 2 The surface area of Alubra® is tightly controlled SEM of Alubra® Sodium Stearyl Fumarate. Product morphology (specifically surface area) has a significant impact on lubricant performance. Since the lubricating properties of SSF are dependent on its ability to coat other particles in a formulation during mixing, variations in surface area will impact the effectiveness of the coating and the amount of lubrication provided. Specific surface area can be measured several different ways including laser scattering particle size distribution analysis. However, this method does not account for surface texture and assumptions are made regarding particle morphology. A more accurate and widely used technique is the BET method. With BET, specific surface area is measured through the adsorption of gas molecules (i.e. nitrogen) onto a solid surface. DuPont BioPolymer uses the BET method to measure the specific surface area of Alubra® since it is a widely accepted and reproducible method. Alubra® PG-100 has an internal surface area specification range of 2.0 – 4.0 m2/g using the BET method. Alubra® meets the highest quality standards Alubra® is manufactured under IPEC and cGMP conditions, Alubra® Commercial Information which comply with recognized global quality standards. DuPont’s own quality initiatives assure that the finished Alubra® complies with all major pharmacopoeias: product is chemically, physically, and functionally consistent, • NF • Ph. Eur. as well as compliant with the stringent requirements of all • CP major pharmacopoeias. DuPont carries out systematic product • JPE • BP evaluation to ensure that Alubra® continues to meet or surpass these high standards. Commercial packaging: • 1 KG drum • 5 KG drum • 25 KG fiber drum Available supporting documentation for Alubra®: • Specification Sheet • MSDS • COAs • BSE/TSE Statement • GMO Statement (Generally Modified Organism) • Residual Solvent Statement (as per USP Chapter 467) • Not of Human/Animal Origin Statement • Allergen-Free Statement 3 300 250 ) N ( 200 e ® c Avicel PH-1 02 neat r o F 1 50 Avicel® ® PH-1 02 + 1 % Alubra n o i Nutrition & Biosciences t ® c Avicel PH-1 02 + 1 % MgSt e j 1 00 E 50 Alubra® offers the lubrication performance Comparative Ejection Forces you need 0 5 1 0 1 5 20 25 30 35 300 During the tableting process, an extensive amount of C ompression Force (kN) friction is generated between the tablet and the surfaces of the die and punch as the tablet is ejected. This can 250 ) impart considerable amounts of strain and shear on a N ( 200 e ® tablet, resulting in defects such as sticking, capping, and c Avicel PH-1 02 neat r o lamination. Lubricants decrease ejection force, prevent F 1 50 Avicel® ® PH-1 02 + 1 % Alubra n o sticking, and reduce overall manufacturing costs by i t ® c Avicel PH-1 02 + 1 % MgSt preventing wear and tear on the tablet press. e j 1 00 E The chemistry of Alubra® is unique in promoting improved 50 wettability of the tablet, while still providing excellent lubricity even at higher tableting speeds. Alubra® has a higher melting point than magnesium stearate which 0 5 1 0 1 5 20 25 30 35 allows for prolonged compression times at elevated C ompression Force (kN) compression forces. Alubra® delivers lubrication comparable to magnesium stearate and allows for higher compression forces and faster press speeds. Alubra® improves the properties of Comparative Disintegration Times of effervescent tablets Vitamin C Effervescent Tablets Lubrication of effervescent tablets presents formulators 60 with a challenge. Insoluble lubricants like magnesium ) c e 50 stearate can negatively affect disintegration and solution s ( clarity while water-soluble lubricants may not be as e 40 m i T effective and may require high usage levels. n 30 o i t a 20 r Alubra® provides excellent lubrication along with g e t n 1 0 improved tablet hardness and disintegration time. After i s i disintegration, magnesium stearate will also form a more D 0 visible surface film layer compared to Alubra®. MgSt MgSt MgSt Alubra® Alubra® Alubra® (0.5%) (1.0%) (1.5%) (0.5%) (1.0%) (1.5%) FORMULA PROCEDURE60 ) c e 50 s Ingredient % Formula ( e 40 m i Vitamin C 19.2% T • Blend all ingredients except for lubricant for 2 minutes n 30 o i Mannitol 30.3 - 31.3% • Addt lubricant and blend for an additional minute a 20 r Anhydrous citric acid 18.7% g e • ZP8t tablet press fitted with 20mm flat punch n 1 0 Sodium bicarbonate 30% i s i Aspartame 0.3% • TabletD 0hardness: ~50 N ® ® ® Alubra® or Magnesium Stearate 0.5 - 1.5% • Tablet weight:MgSt 2600 mgMgSt MgSt Alubra Alubra Alubra (0.5%) (1.0%) (1.5%) (0.5%) (1.0%) (1.5%) 4 3500 3000 Acetaminophen DC Acetaminophen DC + 2% Alubra® ) c e 2500 Acetaminophen DC + 2% Magnesium Stearate s ( e m i 2000 T n o i t 1500 a r g e t n i 1000 s i ComparativeD Disintegration Times of 500mg Alubra® offers improved disintegration 500 Acetaminophen Tablets In the case of oral solid dosage forms dissolution is dependent, in part, on the disintegration of the tablet 0 or capsule. Disintegration increases the surface area of the drug formulation which increases dissolution rate. 3500 Disintegration time will increase if a hydrophobic lubricant like magnesium stearate forms a film around drug/ 3000 Acetaminophen DC Acetaminophen DC + 2% Alubra® ) excipient particles. c e 2500 Acetaminophen DC + 2% Magnesium Stearate s ( To illustrate this point, consider a directly compressible e m i 2000 T acetaminophen grade that contains starch and stearic acid. n o By using a high level of lubricant (2%) and blending for 5 i t 1500 a r minutes, a sufficient amount of coating or film is formed g e t around the API. n i 1000 s i D If the lubricant is a hydrophobic material like magnesium 500 stearate then disintegration will be considerably slower compared to an unlubricated control. Since Alubra® is 0 less hydrophobic, it will have significantly less impact on disintegration time. Alubra® enhances API dissolution Comparative Disintegration Times of 500mg For an API to have acceptable bioavailability, it must Acetaminophen Tablets dissolve in a reasonable period of time. This is a significant issue for drugs with poor or medium solubility. 1 20 Hydrophobic lubricants like magnesium stearate exacerbate the problem since dissolution is further 1 00 delayed3. 80 d e Alubra® sodium stearyl fumarate is more hydrophilic s a e than magnesium stearate so it interferes less with l 60 e r disintegration and dissolution. I P A 40 ® % 98% acetaminophen + 2% Alubra In the same APAP model described above, the formulation (Hardness 1 56N; relative density 84.58% ) with Alubra® results in significantly faster dissolution 20 98% acetaminophen + 2% Mg St compared
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