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7 protocols using kollidon 12 pf

1

Aripiprazole Formulation Development and Characterization

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Aripiprazole (melting point at 137–142°C) was obtained from Nexconn Pharmatechs Ltd. (Tseung Kwan O, Hong Kong). Phenacetin (internal standard, IS, Figure S1B) was purchased from Tokyo Chemical Industry Co., Ltd (Tokyo, Japan). Acidifiers (adipic acid, citric acid, fumaric acid, malic acid, maleic acid, stearic acid, succinic acid, and tartaric acid) were purchased from Spectrum Quality Products, Inc. (Gardena, CA, USA). Kollidon® 12 PF and Soluplus® were generously supplied by BASF Corporation (Florham Park, NJ, USA). AquaSolve™, HPMCAS-LG, Klucel™ EXF, Benecel™ E15, Benecel™ K15M, and Natrosol™ 250L were gifted by Ashland, Inc. (Lexington, KY, USA). All other chemicals used were reagent grade and were used without further purification.
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2

Formulation and Characterization of Mefenamic Acid

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Mefenamic acid (MA) was purchased from Sigma Aldrich (Bellefonte PA.
USA); Kollidon 12PF and Kollidon 17PF were obtained as gift samples from BASF
(PEGPVCLPVA, BASF, Germany). Magnesium oxide and polyethylene glycol 3350 were
purchased from Fisher Scientific. All other chemicals used in this study were of
analytical grade.
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3

Amorphous and Crystalline IBR Formulation

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Amorphous and crystalline IBR were acquired from a GMP-approved drug supplier. Poly(vinyl pyrrolidone-vinyl acetate) copolymer (PVPVA or copovidone, brand name Kollidon® VA64), Poly(vinylpyrrolidone) (PVP or povidone of grade K12, brand name Kollidon® 12PF), and Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (brand name Soluplus®) were obtained from BASF (Ludwigshafen, Germany). Hypromellose Acetate Succinate (HPMCAS grade MF, brand name AQOAT®) was kindly donated by Shin-Etsu (Totowa, NJ), and polyvinyl alcohol (PVOH, brand name Parteck® MXP) was obtained from Merck Millipore (Darmstadt, Germany). Polyethylene glycol (PEG6000) grade 6000 was acquired from Clariant (Hoechst) (Muttenz, Switzerland), and Poloxamer 407micro (P407), brand name Kolliphor® P407, was also obtained from BASF (Ludwigshafen, Germany).
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4

Synthesis and Characterization of Celecoxib Nanosuspensions

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Celecoxib (CCX, Mw = 381.4 g/mol), indomethacin (IND, Mw = 357.8 g/mol), naproxen (NAP, Mw = 230.3 g/mol) and magnesium stearate (Mw = 591.3 g/mol) were purchased from Fagron Nordic A/S (Copenhagen, Denmark). Kollidon® 12 PF (polyvinylpyrrolidone (PVP), PVP12, Mw ~2500 g/mol), Kollidon® 17 PF (PVP17, Mw ~9000 g/mol) and Kollidon® 25 (PVP25, Mw ~24,000 g/mol) were a kind gift from BASF (Ludwigshafen, Germany).
Silver acetate (99.8% anhydrous) was purchased from Alfa Aesar (Kandel, Germany). Hexamethyldisiloxane (≥98%), acetonitrile (99.8% anhydrous) and 2-ethylhexanoic acid (99%) were purchased from Sigma-Aldrich (Stockholm, Sweden). The oxygen gas (flow: 5.0 L/min) for the flame-spray-pyrolysis synthesis was from Strandmøllen (Ljungby, Sweden).
Ethanol (>99.7%, HPLC grade) was purchased from VWR International (Leuven, Belgium). acetonitrile (HPLC grade) and trifluoroacetic acid were purchased from Sigma-Aldrich (Søborg, Denmark). Purified water used for the mobile phase in the HPLC experiments was prepared using a MilliQ water system from LabWater (Los Angeles, CA, USA). All chemicals were used as received.
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5

Solubility Enhancement of Indomethacin

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Soluplus® (SOL) (M w ¼ 118.000 g/mol) and Kollidon® 12 PF (PVP) (M w ¼ 2000e3000 g/mol) were received as a gift from BASF (Ludwigshafen, Germany). Indomethacin (IND) (M w ¼ 357.79 g/ mol) and magnesium stearate (MgSt) (M w ¼ 591.27 g/mol) were obtained from Fagron Nordic A/S (Copenhagen, Denmark). Glycerol (GLY) (M w ¼ 92.10 g/mol) was a kind gift of Merck KGaA (Darmstadt, Germany). All chemicals were used as received.
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6

Enteric-coated Naproxen and Esomeprazole Formulation Development

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Naproxen (pKa 4.15) (Fagron, Waregem, Belgium) and esomeprazole magnesium trihydrate (Nifty labs, Hyderabad, India) were chosen as model drugs. Vimovo ® (AstraZeneca, Brussels, Belgium), containing 500 mg enteric-coated Naproxen and 20 mg non-enteric coated esomeprazole Mg, was used as a commercially available reference. The following enteric polymers were used: methacrylic acid -ethyl acrylate copolymer (1:1) Type A (Eudragit ® L100-55, Evonik, Darmstadt, Germany), hydroxypropyl methylcellulose acetate succinate (HPMC-AS-LF, Aqoat ® AS-LF, Shin-Etsu, Tokyo, Japan) and hydroxypropyl methylcellulose phthalate (HPMCP-HP-50, Shin-Etsu, Tokyo, Japan). Triethyl citrate (TEC, Sigma-aldrich, Bornem, Belgium) and talc (Luzenac ® Pharma, Imerys Talc, Gent, Belgium) were used as excipients in the core formulation. The polymers used in the coat formulation were polyethylene oxide 100K (PEO 100K, Mw: 100000 g/mol, SentryTM Polyox ® WSR N10, Colorcon, Dartford Kent, United Kingdom), polyvinylpyrrolidone (Kollidon ® 12 PF, Mw: 2500 g/mol, BASF, Ludwigshafen, Germany), hydroxypropyl methylcellulose (Methocel ® E3, viscosity: 3 mPa.s, Colorcon, Dartford Kent, United Kingdom), hydroxypropyl cellulose (Klucel ® EF, Mw: 80000, Ashland, Covington, USA) and polyethylene glycol 4K (PEG 4K, Mw: 4000 g/mol, Fagron, Waregem, Belgium). All other chemicals were of analytical grade.
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7

Celecoxib Formulation Development

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Celecoxib (CCX, Mw = 381.37 g/mol) and magnesium stearate were purchased from Fagron Nordic A/S (Copenhagen, Denmark). Kollidon® 12PF (PVP12, Mw = 2000–3000 g/mol) and Kollidon® 17PF (PVP 17, Mw = 7000–11,000 g/mol) were kindly supplied by BASF (Ludwigshafen, Germany). Sodium chloride (NaCl, Mw = 58.44 g/mol) was purchased from Sigma-Aldrich (St. Louis, MO, USA). All chemicals were used as received.
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