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9 protocols using explotab

1

Fenofibrate Formulation Development

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Fenofibrate was kindly donated from JPI Co. (Riyadh, Saudi Arabia). Polyvinylpyrrolidone, Kollidon® 12 and D-α-Tocopherol polyethylene glycol 1000 succinate, and Kolliphor® TPGS were obtained as a gift sample from BASF Co. (Ludwigshafen, Germany). Microcrystalline cellulose and Avicel® PH-102 were gained as a gift sample from DuPont Nutrition USA, Inc. (Wilmington, NC, USA). Lactose monohydrate and Granulac 200® were obtained from Meggle (Wasserburg, Germany). Colloidal silicon dioxide and Aerosil 200® were purchased from Evonik (Hanau-Wolfgang, Germany). Sodium stearyl fumarate, Pruv® and sodium starch glycolate, and Explotab® were obtained as a gift sample form JRS pharma (Rosenberg, Germany). Sodium dihydrogen phosphate dehydrate, disodium hydrogen phosphate dodecahydrate and sodium hydroxide were purchased from Merck (Darmstadt, Germany).
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2

Nebivolol Hydrochloride Formulation

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Nebivolol HCl (NEB) (2,2′-Azanediylbis(1-(6-fluorochroman-2-yl) ethanol) hydrochloride) was a kind gift from Menarini S.p.a. (L’Aquila, Italy). Beta-cyclodextrin (βCD) was from Sigma (St. Louis, MO, USA). Hydroxypropyl-βCD (HPβCD, average substitution degree 0.62) was kindly supplied by Roquette (Lestrem, France), and sulfobutylether-βCD (Dexolve®) (SBEβCD, average substitution degree 6.5) was a kind gift from Cyclolab Ltd. (Budapest, Hungary). Randomly substituted methyl-βCD (RAMEB, average substitution degree 1.8) was from Wacker Chemie (München, Germany). Explotab® (sodium starch glycolate) was from JRS Pharma (Rosenberg, Germany), and Mg stearate, polyvinylpyrrolidone (PVP) K90, mannitol and CaHPO4 were from Sigma (St. Louis, MO, USA). All other chemicals and solvents were of analytical reagent grade.
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3

Dry Granulation and Tablet Formulation

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Example 9

After crystallization, polymorph forms of Formula I compound, may be formulated by dry granulation using a roller compactor, followed by a tableting operation. Additional ingredients in the tablets may include microcrystalline cellulose (Avicel PH, FMC BioPolymer), lactose (FastFlo, Foremost Farms USA), sodium starch glycolate (EXPLOTAB, JRS Pharma), or magnesium stearate (Hyqual, Macron Fine Chemicals).

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4

Formulation of Polymorph Forms

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Example 9

After crystallization, polymorph forms of Formula I compound, may be formulated by dry granulation using a roller compactor, followed by a tableting operation. Additional ingredients in the tablets may include microcrystalline cellulose (Avicel® PH, FMC BioPolymer), lactose (FastFlo®, Foremost Farms USA), sodium starch glycolate (EXPLOTAB®, JRS Pharma), or magnesium stearate (Hyqual®, Macron Fine Chemicals).

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5

Niclosamide ASD Granules Formulation

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The niclosamide ASD granules were admixed with sodium bicarbonate (Spectrum chemical, New Brunswick, NJ, USA) and sodium starch glycolate (Explotab®, JRS Pharma, Patterson, NY, USA) in a 70/25/5 ratio. This mixture was filled into either Capsuline® (HPMCP/HPMC) (Dania Beach, FL, USA) or EudracapTM (HPMC/Eudragit® polymers) capsules, size 0. The Eudracaps were kindly donated by Evonik Corporation–North America (Piscataway, New Jersey, NJ, USA).
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6

Sustained-Release Metformin Pellet Formulation

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Pellets were fabricated with α-lactose monohydrate (Granulac 200®, Meggle Pharma, Wasserburg am Inn, Germany), MCC (Ceolus® PH-101, Asahi Kasei, Tokyo, Japan) or XPVP (Kollidon CL-M®, BASF, Ludwigshafen, Germany), and metformin hydrochloride (MET; Granules India, Hyderabad, India). The sustained release layering material consisted of ethylcellulose (EC) dispersion (Aquacoat® ECD, FMC Biopolymer, Philadelphia, PA, USA), triethyl citrate (Merck Schuchardt OHG, Hohenbrunn, Germany) as a plasticizer, and talc powder (Guangxi Longguang Talc Development Co., Ltd., Guilin, China) as an anti-adherent. MCC was also the tablet filler with sodium starch glycolate (Explotab®, JRS Pharma, Pirna, Germany). Purified water was used as the dissolution and disintegration media.
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7

Antioxidant-Enriched Pharmaceutical Excipients

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The ABTS•+ (2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (purity 98%), Trolox (6-hydroxy-2,5,7,8-tetramethyl-chroman-2-carboxylic acid), 97% absolute ethanol, D-mannitol, trifluoracetic acid (TFA, 99%), microcrystalline cellulose (MCC), Arabic gum, and sodium chloroacetate (SCA, 98%) were obtained from Sigma Aldrich (Saint Louis, MO, USA). High amylose corn starch (Hylon VII) was kindly provided by Ingredion (Westchester, IN, USA). Croscarmellose sodium (Solutab®, CMC, 98%) was purchased from Blanver (São Paulo, SP, Brazil). Explotab® and Prosolv® were obtained from JRS pharma (Patterson, NY, USA) and polyvinylpyrrolidone (PVP) from International Specialty Products (Wayne, WA, USA). The other chemicals were reagent grade.
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8

Formulation of Polymorph Compounds

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Example 9

After crystallization, polymorph forms of Formula I compound, may be formulated by dry granulation using a roller compactor, followed by a tableting operation. Additional ingredients in the tablets may include microcrystalline cellulose (Avicel® PH, FMC BioPolymer), lactose (FastFlo®, Foremost Farms USA), sodium starch glycolate (EXPLOTAB®, JRS Pharma), or magnesium stearate (Hyqual®, Macron Fine Chemicals).

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9

Formulation and Characterization of Nimodipine Cyclodextrin Complexes

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Nimodipine (Nim) was purchased from Fagron, Greece; and hydroxypropyl-β-cyclodextrin (HP-β-CD) and methyl-β-cyclodextrin (Me-β-CD) were provided from the Global Holding Group Co., Ltd., (Ningbo, China). All used chemicals and solvents were of analytical reagent grade.
F-MELT® was purchased from Fuji Chemical Industries Co., Ltd., Toyama, Japan; Disintequik™ ODT was purchased from Kerry Inc., Beloit, WI, USA; and PROSOLV® SMCC HD 90 and EXPLOTAB® were provided by JRS PHARMA GmbH & Co. KG, Rosenberg, Germany. LIGAMED® MF-2-V, used in the study, was produced by Peter Graven NV, Venlo, Limburg, The Netherlands.
A Mettler Toledo AT261 balance (with 0.01 mg sensitivity) was used for weighing the raw materials.
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