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24 protocols using kollicoat ir

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 of Amorphous Solid Dispersions

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TMP (water solubility ≈ 50 ng/mL; agglomerated particles (sieved fraction <355 μm) consisting of sub-micrometric size crystals with Dv90 < 1 μm); Chiesi Farmaceutici S.p.A., Parma, I); low viscosity hydroxypropyl cellulose (NISSO HPC SSL, Nisso Chemical Europe GmbH, Duesseldorf, D; HPC); hydroxypropyl methyl cellulose acetate succinate (AQUOT-LG®; Shin-Etsu, Tokyo, J; HPMCAS); polyethylene oxide (Sentry Polyox™ WSR N10 LEO NF, Dupont, Paris, F; PEO); low viscosity polyvinyl alcohol (Gohsenol® EG 03P, Mitsubishi Chemicals, Tokyo, J; PVA); polyvinyl alcohol-polyethylene glycol graft copolymer (Kollicoat® IR, BASF, Ludwigshafen, D; KIR); polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer (Soluplus®, BASF, Ludwigshafen, D; SLP); polyvinylpyrrolidone (Kollidon® VA 64, BASF, Ludwigshafen, D; KVA); glycerol (Pharmagel, Milan, I; GLY); polyethylene glycols with different molecular weights (Clariant Masterbatches, Milan, I;, PEG 400 and PEG 8000, respectively); Dextrates (EMDEX®, JRS Pharma, Rosenberg, D; EMD); Isomalt (GalenIQ™ 810, Beneo-Palatinit GmbH, Mannheim, D; GIQ); Potato dextrins (Tackidex®, Roquette, Lestrem, F; TCK); Cetrimonium bromide (VWR International, Milan, I; CTAB).
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3

Modular Capsular Drug Delivery System

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Main polymeric components: hydroxypropyl cellulose (HPC, Klucel ® LF, Aqualon, US-NJ); hydroxypropyl methyl cellulose (HPMC; Affinisol™ 15cP, Dow, US-CA); hydroxypropyl methyl cellulose acetate succinate (HPMCAS; AQUOT-LG, Shin-Etsu, J); polyvinyl alcohol of different molecular weight (PVA 03 and PVA 05; Gohsenol™ EG 03PW and 05P, Nippon Gohsei, J); polyvinyl alcohol-polyethylene glycol graft copolymer (KIR; Kollicoat ® IR, BASF, D). Plasticizers: glycerol (GLY; Pharmagel, I); polyethylene glycol (PEG; PEG 400, 1500 and 8000, Clariant Masterbatches, I). Dietary ingredient tracer: caffeine (CFF; A.C.E.F., I). The delivery platform consisted in capsular devices having separate inner compartments with different volume and composition of the walls, obtained following assembly of modular units. The compartments are intended to breakup in succession and release their contents, leading to multiplepulse release profiles. Additional external capsule shells able to enclose single-and two-compartment capsular devices already assembled were also conceived in the form of matching modular units. The opening behavior of compartments and external shells would depend on the composition and thickness of the walls.
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4

Extraction and Characterization of KPD

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KPD was extracted by maceration method as described previously [6] (link). Briefly, fresh rhizomes of K. parviflora were blended and extracted successively by macerating with 95% ethanol for 48 h, followed by extracting with dichloromethane. The dichloromethane-soluble part was filtered and then evaporated. The dried residue from the dichloromethane extract was further treated by vacuum condition in order to remove residual dichloromethane and then a yellowish gummy of KPD was obtained.
Polyvinyl alcohol polyethylene glycol graft copolymer (Kollicoat® IR, referred to as PVA-co-PEG) and polyethyleneglycol-polyvinyl acetate-polyvinylcaprolactame grafted copolymer (Soluplus®, referred to as PCL-PVAc-PEG) were a gift form BASF (Thai) Co., Ltd. (Bangkok, Thailand). Polyvinylpyrrolidone K30 (referred to as PVP), hydroxypropyl methylcellulose K4M (referred to as HPMC) and polyethylene glycol 4000 (referred to as PEG) were purchased form P.C. Drug Center (Bangkok, Thailand). Other chemicals were of pharmaceutical grade or analytical grade and used without further purification.
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5

Printing Substrates with Hydrophilic Polymers

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Four hydrophilic polymers were investigated as single film-forming agents or polymer blends for printing substrates preparation: (1) hydroxypropyl cellulose (HPC, Klucel® GF, Ashland™, Wilmington, DE, USA), (2) polyethylene glycol–polyvinyl alcohol graft copolymer (PVA-PEG, Kollicoat® IR, BASF, Ludwigshafen, Germany), (3) maltodextrin (MDX, Glucidex IT6, Roquette, Lestrem, France) and (4) sodium alginate (SA, Fisher Scientific, Waltham, MA, USA), as well as three commercially available wafer edible sheets (Easy Bake, UK, Edible print supplies, Birstall, The United Kingdom). Ink formulation contained caffeine anhydrous (CAF, Sigma-Aldrich Chemie GmbH, Munich, Germany) as the selected model drug, dissolved in the 7:3 mixture of ethanol (≥99.8%, Honeywell, Charlotte, NC, USA) and glycerol, 85% (w/w) (Ph. Eur.).
Simulated salivary fluid pH 6.75 [18 (link)] prepared with sodium chloride, potassium phosphate monobasic, disodium hydrogen phosphate, hydrochloric acid (Sigma-Aldrich Chemie GmbH, Munich, Germany) and purified water (Ph. Eur.) was used as drug release media.
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6

Besifloxacin-based Ophthalmic Formulations

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Besifloxacin (99.93%, MW 430.301 g/mol, Log P 0.54, water solubility: 0.143 mg/mL) was purchased from Jinan Shengqi Pharmaceutical Co., Ltd. (Jinan China). Povacoat® (POVA) was donated from DAIDO Takeshima Nishiyodogawa-Ku, Osaka, Japan). Polysorbate 80, cetylpyridinium chloride (CPC), benzalkonium chloride (BAC), benzyldimethylhexadecylammonium chloride 16-BAC), and chitosan (CS) were purchased from Sigma-Aldrich (St. Louis, MO, USA). Poloxamer 188 (P188), Poloxamer 407 (P407), Poloxamer HS 15 (HS 15), tocopherol polyethylene glycol succinate (TPGS), and Kollicoat® IR (KLT) were purchased from BASF (Ludwigshafen am Rhein, Germany). Triethylamine, phosphoric acid, acetonitrile, and phosphate buffer solution pH 7.0 (Certipur®) were purchased from Merck (Darmstadt, Germany). The product Besivance® (0.6% ophthalmic suspension) (Bausch & Lomb Incorporated, Bridgewater, NJ, USA) was obtained from a local market. Milli-Q® Integral 10 ultrapure water (Merck KGaA, Darmstadt, Germany) was used for analytical purposes.
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7

Formulation of Haloperidol Solid Dispersions

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Polyvinylpyrrolidone-vinyl acetate copolymer (Kollidon ® VA64) and polyvinyl alcohol-polyethylene glycol graft copolymer (Kollicoat ® IR) were donated by BASF Corp. (Tarrytown, NY). Hydroxypropyl methylcellulose HME 15 cP (HPMC HME 15 cP; Affinisol ™ 15 cP) and hydroxypropyl methylcellulose acetate succinate (HPMCAS MG; Aqoat ® AS-MG) were received as gifts from, respectively, DOW Chemical Co. (Midland, MI) and Shin-Estu Chemical (Totowa, NJ). Haloperidol was purchased from VWR (Radnor, PA). All materials were used as received.
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8

3D Printing of Polymer Filaments for Controlled Drug Release

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Polylactic acid (PLA) filament (L-PLA natural, ø 1.75 mm; MakerBot ® Industries, US-NY); polyvinyl alcohol (PVA) filament (natural, ø 1.75 mm; German RepRap, D); hydroxypropyl methyl cellulose (HPMC; Affinisol™ 15cP, Dow, US-CA); hydroxypropyl methyl cellulose acetate succinate (HPMCAS; AQUOT-LG, Shin-Etsu, J); polyvinyl alcohol-polyethylene glycol graft copolymer (KIR; Kollicoat ® IR, BASF, D); glycerol (GLY; Pharmagel, I); polyethylene glycol (PEG; PEG 400 and 8000, Clariant Masterbatches, I); triethyl citrate (TEC; Sigma Aldrich, D); acetaminophen (AAP; Rhodia, I); blue and yellow dye-containing formulations (Kollicoat ® IR Brilliant Blue and Kollicoat ® IR yellow, BASF, D).
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9

Formulation Ingredients for Topical Applications

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Niacinamide 99.5% (nicotinamide, NAC), hexadecyltrimethylammonium bromide 98.0%, benzalkonium chloride 95.0%, alkyltrimethylammonium bromide 95.0%, dodecylamine 98.0%, cetylpyridinium chloride 98.0%, sodium dodecyl sulfate (SDS) 98.5%, Tween®80 (polysorbate 80), Tween®20 (polysorbate 20), Span®20 (sorbitan laurate), phosphate-buffered saline (PBS pH 7.4) powder, and Strat-M® Membrane (25 mm) were purchased from Sigma-Aldrich Inc. (St. Louis, MO, USA). TEGOSOFT® CT was obtained from Evonik (Essen, Germany). Butylene glycol 99.0% (BG), dipropylene glycol 97.0% (DPG), and propylene glycol 99.0% (PG) were purchased from Samchun Pure Chemical Co., Ltd. (Pyeongtaek, Korea). Polyethylene glycol 400 was purchased from Junsei Chemical Co., Ltd. (Tokyo, Japan). Polyoxyethylene (1 6 0) and polyoxylpropylene (30) glycol (Kolliphor® P188), polyoxyethylene (1 9 6) and polyoxylpropylene (67) glycol (Kolliphor® P407), Polyethylene glycol 6000 (PEG6000), polyvinyl alcohol-polyethylene glycol graft copolymer (Kollicoat® IR), polyvinylpyrrolidone (Kollidon® K12), macrogol 15 hydroxystearate (Kolliphor® HS 15), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®), and D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) were obtained from BASF (Ludwigshafen, Germany). PVP/VA S-630 was obtained from ISP Technologies Inc. (Wayne, NJ, USA).
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10

Indomethacin Formulation Development

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Indomethacin with a purity of more than 99% was purchased from Aladdin Chemical Reagent Corporation, Shanghai, China; Kollicoat IR was obtained from BASF, Port Ludwig, Germany; hydroxypropyl methylcellulose E5 (HPMC) was obtained from Sunhere Pharmaceutical Excipients Chemical Reagent Corporation, Anhui, Huainan, China; Hexadecyl trimethyl ammonium Bromide (CTAB), tetraethyl orthosilicate (TEOS), and 3-aminopropyltriethoxysilane (APTES) were supplied by Yu Wang Chemical Reagent Corporation, Shangdong, Yucheng, China. The IR 820 was provided by Aladdin Chemical Reagent Corporation. Other chemical agents were obtained from Yu Wang Chemical Reagent Corporation, and solvents were of reagent grade and used without further purification.
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