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9 protocols using aerosil 200 pharma

1

Excipient Evaluation for DAP-CA Cocrystal

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DAP-CA cocrystal (99.9% purity) was obtained from Sun Pharm. Industries, Ltd. (Mumbai, India). Anhydrous lactose (Supertab 21AN) was obtained from DFE Pharma (Goch, Germany). Lactose monohydrate (Tablettose) was obtained from Meggle Pharma (Wasserburg, Germany). Microcrystalline cellulose (Avicel PH-101) was purchased from FMC biopolymer (Philadelphia, PA, USA). Microcrystalline cellulose (Vivapur 12) was obtained from JRS Pharma (Rosenberg, Germany). Mannitol (Pearlitol 100 SD) was obtained from ROQUETTE Pharma (Lestrem, France), crospovidone (Polyplasdone XL) was provided by Ashland (DA, USA), colloidal silicon dioxide (Aerosil 200 pharma) was purchased from Evonik (Essen, Germany), and magnesium stearate was purchased from FACI (Genova, Italy). Opadry was purchased from Colorcon (Stoughton, WI, USA). DAP amorphous (99.9% purity) and DAP-PH (99.9% purity) were provided by Dr. Reddy (Hyderabad, India), and Forxiga® 10 mg, a control agent, was provided by AstraZeneca Korea (Seoul, Korea).
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2

Pharmaceutical Excipient Formulations

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d-sorbitol (CE) was purchased from Carlo Erba. Polyethylene oxide, PEO(PolyoxN10, Dow Chemical, Midland, TX, USA), was donated. Glycerol (Glycerol, VWR, Radnor, PA, USA) was purchased. Colloidal anhydrous silica (Aerosil 200 Pharma, Evonik, Rheinfelden, DE, USA) was purchased. Amiodarone hydrochloride was donated from Sanofi, FR.
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3

Sorafenib Tosylate Formulation Development

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Sorafenib tosylate was purchased from BIOSYNTH Carbosynth (Compton, Newbury, United Kingdom). Cremophor EL, tetraglycol, triethylamine, and polyvinylpyrrolidone (PVP K 30) (average molecular weight 40 kDa) were purchased from Sigma-Aldrich (St. Louis, MO, USA). Triacetin, isopropyl myristate (IPM), soybean oil, corn oil, tween 80, span 80, span 20, mineral oil, and glycerin were acquired from Daejung Chemicals Co. (Siheung, South Korea). Peceol, labrafil M 1994 CS, labrafil M 2125, labrasol, transcutol P, lauroglycol 90, capryol 90, and labrafac lipophile WL 1349 were obtained from Gattefossé (Saint-Priest Cedex, France). Capmul MCM and captex 355 were gifted from Abitec Corporation (Columbus, OH, USA). Propylene glycol, tween 20, olive oil, and phosphoric acid were purchased from Duksan Pure Chemical (Ansan, South Korea). Polyethylene glycol (PEG) 400 was purchased from Samchun Pure Chemical (Gyeonggi-Do, South Korea). Colloidal silica (Aerosil® 200 Pharma) was purchased from Evonik industries AG (Essen, Germany). Ethanol (EtOH) and high-performance liquid chromatography (HPLC)-grade acetonitrile (ACN) were purchased from Honeywell Burdick & Jackson® (Muskegon, MI, USA). All other chemicals used were of the analytical grade.
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4

Ibuprofen Powder and Tablet Formulation

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The materials used in this study included IBU as an API and excipients. API (≥98% GC grade) was purchased from Sigma-Aldrich (Millipore Sigma, St. Louis, MO, USA). Four excipients were used and blended with IBU to obtain powders and tablets in the concentration range tested. Lactose monohydrate (LM; granular; Meggle Pharma, MEGGLE Group, Wasserburg, Germany), microcrystalline cellulose (MCC; Vivapur® 102, JRS Pharma LP, Patterson, New York, NY, USA), colloidal silicon dioxide (C-SiO2) (Aerosil® 200 Pharma, Evonik Industries AG, Essen, Germany), and magnesium stearate (MgSt) (Mallinckrodt Inc., Raleigh, NC, USA) were used.
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5

Sorbitol and Polyethylene Oxide Formulation

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D-Sorbitol Parteck SI150 (SI150) and Parteck SI200 (SI200) were donated from Merck, Darmstadt, Germany. D-Sorbitol (CE) was purchased from Carlo Erba, Italy and D-Sorbitol (GLT) was purchased from Glentham, Corsham, UK. Polyethylene oxide, Polyox N10 (PEO) was donated from Dow Chemical, Midland, TX, USA. Glycerol was purchased from VWR, Radnor, PA, USA. Colloidal anhydrous silica (Aerosil 200 Pharma) was purchased from Evonik, Rheinfelden, Germany, USA. Amiodarone hydrochloride was donated from Sanofi, France.
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6

Formulation Development of Tablet Binders

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Table 1 gives an overview of used binders. Different types of hyprolose were used. Table 2 lists their molecular weight and particle size. Additional applied substances were lactose monohydrate (Granulac® 200, Meggle, Wasserburg am Inn, Germany) as filler, silicium dioxide (Aerosil® 200 Pharma, Evonik, Hanau-Wolfgang, Germany) to improve flow properties, and magnesium stearate (LIGAMED® MF-2-V, Peter Greven Nederland C.V., Venlo, The Netherlands) as a lubricant for tableting.
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7

Formulation Development of Metoprolol Tartrate

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Metoprolol tartarate (MPT) was purchased from Esteve Quimica (Barcelona, Spain). Glyceryl behenate (GB, Compritol® 888 ATO) and glyceryl palmitostearate (GPS, Precirol® ATO 5) were obtained from Gattefosse (St. Priest, France). Magnesium stearate (Mg St) was purchased from ABC Chemicals (Wauthier-Braine, Belgium), colloidal silica dioxide (Aerosil® 200 Pharma) from Evonik (Hanau-Wolfgang, Germany), pancreatin from Sigma Aldrich (USA), sodium taurocholate from Prodotti Chimici e Alimentari (Basaluzzo, Italy) and egg phosphatidylcholine (LIPOID E PC S) from Lipoid (Steinhausen, Switzerland). All other reagents were of analytical grade. The quantitative composition of the formulations processed via the four different techniques is given in Table 1.
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8

Formulation and Characterization of Controlled-Release Tablets

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D-mannitol, D-sorbitol, magnesium stearate, bismuth(III) oxide and barium sulphate were purchased from Sigma–Aldrich (Poole, UK). Polyplasdone XL-10 (crospovidone) was obtained from ISP (Switzerland). Avicel PH102 (MCC) was obtained from FMC Biopolymer (Philadelphia, USA). Aerosil 200 Pharma (colloidal silicon dioxide) was obtained from Evonik Industries (Essen, Germany). A coating polymer Kollicoat IR (BASF, Germany) and a fluorescent dye riboflavin 5′-monophosphate sodium salt (Sigma-Aldrich, Pool, UK) were obtained for film coating work.
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9

Formulation and Evaluation of KCl-FHA Varnish

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KCl (AnalaR ® BDH, VWR International, Poole, England) and FHA 10% (w/w) were mixed with fully hydrogenated rosin (Foral ™ AX-E, Eastman Chemical BV, Capelle aan den IJssel, The Netherlands), hydrophilic fumed silica (Aerosil ® 200 Pharma, Evonik Industries AG, Rheinfelden, Germany) and absolute ethanol (Merck, Merck KGaA, Darmstadt, Germeny) (Table 1). The KCl-FHA varnish was placed into a capped syringe and stored at room temperature.
Three additional varnishes were prepared (Table 1) to investigate the effects of the ingredients of the KCl-FHA varnish: plain varnish (a mixture of fully hydrogenated rosin, hydrophilic fumed silica, and absolute ethanol), which served as control, KCl varnish (plain varnish containing 10% (w/w) KCl), and FHA varnish (plain varnish containing 10% (w/w) FHA). These varnishes were placed into capped syringes and stored at room temperature.
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