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33 protocols using eudragit l100 55

1

Polymeric Excipients for Controlled Drug Delivery

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Eudragit ® L100-55 (EL), Eudragit ® EPO (EE, after milling/sieving the supplied pellets), Eudragit ® RSPO (RS), and Eudragit ® RLPO (RL, after milling/sieving) were gifted by Evonik (Darmstadt, Germany) and Kollidon ® VA 64 (VA), Kollicoat ® IR, (IR), Kollidon ® SR (SR), Soluplus ® (SL) gifted by BASF (Ludwigshafen, Germany). Extruded polymers are denoted with subscript (ex). Lutrol ® F 127 (polyoxyethylene with polyoxypropylene copolymer) gift by BASF was used as a plasticizer for Eudragit ® L 100-55 only.
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2

Formulation and Evaluation of Delamanid Tablets

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Delamanid (DLM) was obtained from Gojira Fine Chemicals, LLC (Bedford Heights, OH) while Deltyba® tablets were manufactured by Otsuka Pharmaceutical Co., Ltd., (Tokyo, Japan). Hydroxypropyl methylcellulose phthalate (HPMCP, P-50 grade) was from Shin-Etsu Chemical Co., Ltd. (Tokyo, Japan). 1,2-Ethanedisulfonic acid dihydrate was supplied by Tokyo Chemical Industry Co. Ltd. (Tokyo, Japan). Croscarmellose sodium (Ac-Di-Sol®) and microcrystalline cellulose pH 101 were sourced from FMC Biopolymer (Newark, DE). Sodium starch glycolate was purchased from JRS Pharma (Posenberg, Germany). Silica, colloidal anhydrous (Aerosil® 200) and Eudragit® L 100-55 were provided by Evonik (Darmstadt, Germany). Magnesium stearate was procured from Spectrum (New Brunswick, NJ). Acryl-EZE® II was obtained from Colorcon (Harleysville, PA). Hydrochloric acid, dichloromethane (DCM), methanol (MeOH), acetone and phosphate salts, maleic acid, sodium hydroxide were supplied by Fisher-Scientific (Pittsburg, PA). Biorelevant simulated gastric and intestinal fluids, including FaSSIF/FaSSGF, FeSSIF-V2 and FEDGAS were purchased from Biorelevant (London, UK).
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3

Ketoconazole Oral Formulation Development

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The model drug ketoconazole was purchased from Fagron (Glinde, Germany). HPMCAS LG (glass transition temperature: 120°C) was gifted from Shin-Etsu (Tokyo, Japan), and Eudragit L100–55 (glass transition temperature: 120°C) was donated from Evonik (Darmstadt, Germany). PEG 3000 was obtained from Merck (Darmstadt, Germany). Vcaps Enteric® (consisting of HPMCAS) were donated by Capsugel (Morristown, NJ, USA).
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4

Formulation Development of Controlled-Release Theophylline

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Hydroxypropyl cellulose (HPC. SSL) was obtained from Nisso Chemical Europe (Dusseldorf, Germany). Theophylline was purchased from ACROS Organics. Polyvinylpyrrolidone (PVP, MW 40,000), triacetin and triethyl citrate (TEC) were purchased from Sigma-Aldrich (UK). Talc was purchased from Fluka Analytical (UK). Eudragit L100-55, RL, EPO and S100 were donated by Evonik Industries (Darmstadt, Germany).
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5

Synthesis and Characterization of DSPE-PCB Micelles

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DSPE-PCB micelle was synthesized following the previously reported method31 (link). Human recombinant insulin (Cat#: NC1063131) was purchased from Life Technologies Corporation. Polysorbate 80, porcine stomach mucin type II, streptozotocin (STZ), ZnCl2, HAuCl4, NaBH4, styrene, divinylbenzene, fluorescein-o’odemethacrylate, Poly(ethylene glycol) methyl ether methacylate (average Mn 500), SPMA (3-sulfopropyl methacrylate potassium salt) and MTTA ((2-(methacryloyloxy) ethyl) trimethylammonium chloride, betaine, lactulose, mannitol, Corning® Transwell polyester membrane cell culture inserts, Lactate dehydrogenase activity assay kit (Cat# MAK066) were purchased from Sigma-Aldrich. Eudragit L 100–55 was obtained from Evonik Industries. ZO-1 Monoclonal Antibody Alexa Fluor 488 was purchased from Invitrogen (Cata# MA3–39100-A488, Lot# UE288707), Mouse Magnetic Luminex® assays was purchased from R&D systems (Cata# LXSAMSM- 6, Lot# L131929).
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6

Ragweed Pollen Extraction and Characterization

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Raw ragweed pollens were purchased from Pharmallerga (Lisov, Czech Republic). BSA, glycofurol (tetraglycol), simulated gastric fluid (pH 1.2), simulated intestinal fluid (pH 6.8) were obtained from Sigma-Aldrich (MO, USA). Eudragit L100-55 was obtained from Evonik (NJ, USA). Pierce™ bicinchoninic acid (BCA) protein assay kit was purchased from Thermo Fisher Scientific (MA, USA). Acetone, potassium hydroxide, ortho-phosphoric acid, ethanol, sodium chloride (NaCl) were purchased from Fisher Scientific (PA, USA). Milli-Q water with a resistivity of 18.2 MΩ.cm was used in all the experiments.
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7

Hydrophilic Polymer-based Oral Drug Formulation

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Hydroxypropyl cellulose, HPC (Klucel® LF, Ashland, Kearny, NJ, USA); low viscosity hydroxypropyl cellulose, HPC SSL (Nisso HPC SSL, Nisso, Tokyo, Japan); methacrylic acid copolymer, EDR (Eudragit® L 100-55, Evonik, Essen, Germany); polyvinyl alcohol, PVA (Gohsenol® EG 03P, Mitsubishi Chemical, Tokyo, Japan); glycerol, GLY (Pharmagel, Milan, Italy); polyethylene glycol 400, PEG (Clariant Masterbatches, Milan, Italy); triethyl citrate, TEC (Sigma Aldrich, Milan, Italy); caffeine, CFF (ACEF, Milan, Italy); sodium starch glycolate, EXP (Explotab® CLV, JRS Pharma, Rosenberg, Germany); high-amylose maize starch, AMY (Amylo® N-460, Roquette Pharma, Lestrem, France); and polylactic acid filament (TreeD Filaments, Milan, Italy).
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8

Physico-Chemical Characterization of Polymeric Excipients

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The physico-chemical properties of the selected polymers are reported in Table 2. The chemical properties were obtained from the Handbook of Pharmaceutical Excipients, Fifth Edition (2006) [30 ]. Thermal properties were experimentally characterized using mDSC and TGA.
Hydroxypropylmethylcellulose phthalate (HPMCP-HP50, henceforth HP50) and hydroxypropylmethylcellulose acetate succinate fine grade (HPMCAS-LF, hence HAS) were obtained from Shin-Etsu (Tokyo, Japan). PVPVA (the copolymer of N-vinyl-2-pyrrolidone and vinyl acetate, henceforth PVA) was obtained from Ashland (Covington, KY, USA), and polyvinylpyrrolidone (PVPK30, hence PK30) was obtained from VWR (Radnor, PA USA). Soluplus (SOL, the copolymer of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer) was donated by BASF (Ludwigshafen am Rhein, Germany). Eudragit L100 (EUD, 1:1 copolymer of methacrylic acid, methyl methacrylate) and Eudragit L100-55 (EUD55, 1:1 copolymer of methacrylic acid, ethyl acrylate copolymer) were donated by Evonik (Essen, Germany). The solvents used were of analytical or HPLC grade.
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9

Lupin Pharmaceuticals LNS Formulation

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LNS was kindly gifted by Lupin Pharmaceuticals Ltd (Pune, India). K12 and F68 were kindly gifted by BASF SE (Ludwigshafen, Germany). Triethyl citrate was obtained from Fisher Scientific (Pittsburgh, PA, USA). Avicel® 102 and Ac-Di-Sol® Croscarmellose Sodium were generously gifted by FMC Biopolymers (Philadelphia, PA. USA). Aerosil® 200 and Eudragit® L 100-55 were gifted by Evonik (Evonik Industries, Germany). Magnesium stearate was purchased from Spectrum Laboratory Products Inc. (Gardena, CA, USA). Magnesium oxide USP light and Talc were purchased from PCCA (Houston, TX, USA). All other chemical reagents used for HPLC, dissolution, and coating were of analytical grade.
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10

Itraconazole Formulation Development

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Itraconazole (ITZ) was donated by Welding GmbH (Hamburg, Germany). Methacrylic acid -ethyl acrylate copolymer (Eudragit L100-55, EUD) was kindly donated by Evonik Industries AG (Germany), polyacrylic acid (Carbopol 981, CAR) was purchased from BF Goodrich (USA), while hypromellose acetate succinate (Shin-Etsu AQOAT) grade MG (HPMCAS-MG, HAS) was donated by Shin-Etsu Chemical Co. Ltd. (Japan). Figure 1 shows structure of the API and polymers used, while Table 1 presents their physicochemical characteristics. HAS starting material was a coarse powder and it was comminuted at 400 rpm for 30 minutes with a planetary ball mill PM 100 (Retsch, Germany) at room temperature prior to mixing with ITZ. Ethanol (98%, analytical grade) used for content uniformity experiments was purchased from Cooley distillery. 14 The total amount of powder, 0.5 g, was loaded into the stainless steel milling container with a volume of 25 ml and two stainless steel balls (15 mm in diameter) were used. The collected samples were stored in a desiccator over silica gel at 5 ˚C until use.
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