Clopidogrel bisulfate and rosuvastatin calcium were purchased from Dr. Reddy’s Laboratory Ltd. (Hyderabad, India) and TEVA Pharmaceutical Industries Ltd. (Petah Tikva, Israel), respectively. Low-substituted hydroxypropyl cellulose (L-HPC) was obtained from Shin-Etsu Chemical (Tokyo, Japan). Copovidone, crospovidone, and sodium lauryl sulfate were purchased from BASF (Ludwigshafen, Germany). Lactose monohydrate (Meggle Pharma, Wasserburg, Germany), colloidal silicon dioxide (Evonik, Essen, Germany), talc (Nippon Talc, Osaka, Japan), magnesium stearate (Mallinckrodt Pharmaceuticals, Staines, UK), carnauba wax (SS Pharm Co., Ansan, South Korea), sodium stearyl fumarate (JRS Pharma, Rosenberg, Germany), glyceryl behenate (Gattefosse, Saint-Priest, France), titanium dioxide (Kronos Inc., Chelmsford, MA, USA), sodium starch glycolate (DFE Pharma, Goch, Germany), and croscarmellose sodium (FMC Co., Philadelphia, PA, USA) were also purchased from the corresponding companies as indicated in parentheses. All other chemicals and reagents were of analytical grade.
Copovidone
Manufactured by BASF
Sourced in Germany
Copovidone is a polymeric excipient used in the formulation of various pharmaceutical and cosmetic products. It is a copolymer of vinylpyrrolidone and vinyl acetate, and serves as a binder, disintegrant, and film-forming agent. Copovidone is primarily used in the manufacture of solid dosage forms, such as tablets and capsules, to improve the physical and chemical properties of the final product.
Automatically generated - may contain errors
Lab products found in correlation
Soluplus, by BASF (2 mentions)
Sodium lauryl sulfate, by BASF (1 mentions)
Colloidal silicon dioxide, by Evonik (1 mentions)
Sodium stearyl fumarate, by JRS Pharma (1 mentions)
Glyceryl behenate, by Gattefosse (1 mentions)
Low substituted hydroxypropyl cellulose l hpc, by Shin-Etsu Chemical (1 mentions)
Magnesium stearate, by Mallinckrodt (1 mentions)
Crospovidone, by BASF (1 mentions)
Cremophor elp, by BASF (1 mentions)
Poloxamer 407, by BASF (1 mentions)
Poloxamer 188, by BASF (1 mentions)
Pvp k30, by BASF (1 mentions)
Transcutol hp, by Gattefosse (1 mentions)
Polyethylene glycol peg 400, by Samchun (1 mentions)
Polyvinylpyrrolidone pvp k90, by BASF (1 mentions)
Dimethyl sulfoxide (dmso), by Thermo Fisher Scientific (1 mentions)
Eudragit l 100 55 el 100 55, by Evonik (1 mentions)
Sodium taurocholate, by Thermo Fisher Scientific (1 mentions)
Lecithin, by Thermo Fisher Scientific (1 mentions)
Hpmcas lg, by Shin-Etsu Chemical (1 mentions)
6 protocols using copovidone
1
Formulation and Evaluation of Clopidogrel-Rosuvastatin Tablet
2
Formulation and Evaluation of Saquinavir
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Saquinavir was purchased from Vivagen Co., Ltd. (Seongnam, Korea). Capryol™ 90, Labrasol®, propylene glycol, Tween® 80, Labrafac® CM 10, and urethane (ethyl carbamate) were obtained from Daejung Chemicals & Metal Co., Ltd. (Siheung, Korea). Cremophor® ELP, polyvinylpyrrolidone (PVP) K90, PVP K30, hydroxypropyl methylcellulose (HPMC) 2910, poloxamer 407, poloxamer 188, copovidone, and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) were purchased from BASF (Cleveland, OH, USA). Polyethylene glycol (PEG) 400 was provided by Samchun Pure Chemical (Pyeongtaek, Korea). Transcutol® HP was obtained from Gattefosse (Lyon, France). Male specific pathogen-free/vial antibody-free outbred Sprague-Dawley (SD) rats (275–300 g) were purchased from Orient Bio Inc. (Seongnam, Korea). All solvents used in the experiments were of high-performance liquid chromatography (HPLC) grade.
3
Gram-scale Synthesis of PROTAC ARCC-4
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The PROTAC ARCC-4 was synthesized in-house in our laboratories. Based on previously gathered knowledge on the development of AR-targeting PROTACs, we could design a new synthetic route towards a gram-scale synthesis of the desired PROTAC ARCC-4 (for experimental details, see Supplementary Materials ) [32 (link),33 (link),34 (link)]. The obtained material was used in all the subsequent experiments conducted in this study.
HPMCAS (L Grade) was obtained from Shin-Etsu Chemical (Tokyo, Japan), Eudragit® L 100-55 (EL 100-55) from Evonik (Darmstadt, Germany), Copovidone from BASF (Ludwigshafen, Germany), and HPMC HME 15 LV was sent from DuPont Pharma & Nutrition (Luzern, Switzerland). HPC-SSL was kindly donated by Nippon Soda Co., Ltd. (Tokyo, Japan). Silsol 6035 was received from Grace GmbH (Worms, Germany). Propylencarbonat (PC) was purchased from Carl Roth GmbH (Karlsruhe, Germany), and N-Methyl-2-Pyrollidon (NMP) was obtained from VWR International S.A.S. (Rosny-sous-Bois, France). Dimethyl sulfoxide (DMSO, ≥99.9%) was purchased from Fisher Scientific (Geel, Belgium). Di-sodium hydrogen phosphate dihydrate and sodium dihydrogen phosphate dihydrate were obtained from Th. Geyer (Renningen, Germany).
HPMCAS (L Grade) was obtained from Shin-Etsu Chemical (Tokyo, Japan), Eudragit® L 100-55 (EL 100-55) from Evonik (Darmstadt, Germany), Copovidone from BASF (Ludwigshafen, Germany), and HPMC HME 15 LV was sent from DuPont Pharma & Nutrition (Luzern, Switzerland). HPC-SSL was kindly donated by Nippon Soda Co., Ltd. (Tokyo, Japan). Silsol 6035 was received from Grace GmbH (Worms, Germany). Propylencarbonat (PC) was purchased from Carl Roth GmbH (Karlsruhe, Germany), and N-Methyl-2-Pyrollidon (NMP) was obtained from VWR International S.A.S. (Rosny-sous-Bois, France). Dimethyl sulfoxide (DMSO, ≥99.9%) was purchased from Fisher Scientific (Geel, Belgium). Di-sodium hydrogen phosphate dihydrate and sodium dihydrogen phosphate dihydrate were obtained from Th. Geyer (Renningen, Germany).
4
Celecoxib Solubility Enhancement via Polymer Blends
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Polyvinyl alcohol (PVA, Parteck MXP®) was kindly donated by Merck (Darmstadt, Germany). HPMCAS LG (hydroxypropylmethylcellulose acetate succinate) was provided by Shin-Etsu Chemical (Tokyo, Japan). Copovidone, Kolliphor P188 and Kolliphor P407 were donated by BASF (Ludwigshafen, Germany). HPC-SSL was obtained from Nisso Chemical Europe (Düsseldorf, Germany) and Eudragit L100-55 was obtained from Evonik (Darmstadt, Germany). Celecoxib (CXB) was obtained from Swapnroop Drugs & Pharmaceuticals (Aurangabad, India) (Figure 1 ). Lecithin and sodium taurocholate were purchased from Alfa Aesar (Haverhill, MA, USA). FaSSIF-V2 medium was prepared according to Denninger et al. [30 (link)], in henceforth will be referred to as FaSSIF.
5
Amorphous Solid Dispersion of A-1396076
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A-1396076 was prepared and dosed as an amorphous solid dispersion (ASD) containing A-1396076, vitamin E TGPS (BASF, Florham Park, NJ), and copovidone (BASF, Florham Park, NJ) at a ratio of 15/20/65 by weight. Briefly, vitamin E TPGS and copovidone were dissolved in methanol and dichloromethane in a rotating round bottom flask until clear solution obtained. A-1396076 was added to the solution and rotation continued until all components dissolved. Solvent was evaporated at 40C until majority of solvent was gone then allowed to further dry for 90 min prior to being placed into a vacuum oven to dry overnight. For in vivo studies, ASD containing A-1396076 was suspended in 0.2% hydroxymethylcellulose (Sigma-Aldrich, St. Louis, MO) and administered at the indicated doses. Indicated doses refer to the amount of A-1396076 dosed rather than total ASD amount. ASD with vitamin E TPGS and copovidone without A-1396076 was used as a vehicle control in all animal studies.
6
Pharmaceutical Compound Synthesis Protocol
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Telmisartan was purchased from Molekula Limited (Darlington, UK) and sulfamerazine from Sigma-Aldrich (Steinheim, Germany). HPLC-grade tetrahydrofuran (THF) was purchased from Sigma-Aldrich (Steinheim, Germany). Copovidone and Soluplus were purchased from BASF (Ludwigshafen, Germany).
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