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8 protocols using prosolv smcc 90

1

Controlled Release Matrix Formulations

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Hypromellose (Methocel™ K4M Premium CR, Colorcon GmbH Germany) and/or glyceryl behenate (Compritol® 888 ATO, Gattefossé France) were used as the controlled release agents forming matrix system. Prosolv® SMCC 90 (JRS PHARMA, GmbH & Co. KG, Germany) was used as a co-processed dry binder and magnesium stearate (Acros Organics, USA) was used as a lubricant. Tramadol hydrochloride and pentoxifylline (both European Pharmacopoeia Reference Standard, Sigma Aldrich Chemie GmbH, Germany) were chosen as the model highly water soluble drug and non-ionizing drug, respectively. Ethanol (96% v/v, 0.81 g/cm3) according to specification ph. eur. (Lach-Ner s.r.o., Neratovice, Czech Republic) was used to prepare the alcoholic dissolution medium (20 and 40% v/v).
For the preparation of dissolution media and standard solution of Tramadol hydrochloride or pentoxifylline, redistilled water and chemicals of analytical grade (Lach-Ner s.r.o., Neratovice, Czech Republic) were used.
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2

Amlodipine Besylate Tablet Formulation

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Amlodipine besylate was supplied by Daewon Pharmaceutical Co., Ltd. (Seoul, Korea). Silicified microcrystalline cellulose (Prosolv SMCC® 90) and croscarmellose sodium (CCM-Na) were purchased from JRS PHARMA GmbH & Co. KG (Rosenberg, Germany). Polyvinylpyrrolidone (PVP K25) was purchased from BASF AG (Ludwigshafen, Germany). Magnesium stearate (St-Mg) was purchased from Sigma-Aldrich Co. (St. Louis, MO, USA). All other reagents were of analytical or HPLC grade and were used as received.
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3

Detailed Methods for Diazepam and TPA023B Administration in Mice and Dogs

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Diazepam was obtained from Sigma. TPA023B (6,2′-difluoro-5′-[3-(1-hydroxy-1-methylethyl)imidazo[1,2-b][1,2,4]triazin-7-yl]biphenyl-2-carbonitrile) was synthesized by ANAWA, purity was >95%. For oral (p.o.) and intraperitoneal (i.p.) administration to mice, Diazepam and TPA023B were suspended in 0.9% saline/1% Tween80. For electrophysiological experiments and radioligand binding, TPA023B was dissolved in DMSO and diluted with extracellular solution to 0.001–1 µM (final DMSO concentration ≤0.12%). For experiments in dogs, TPA023B was packed into tablets containing 20 mg TPA023B, 38 mg Prosolv® SMCC90 (JRS Pharma) and 2 mg Ac-Di-Sol® (FMC). Placebo tablets were of the same weight, size, color and composition but contained 2.4 mg Quinoline Yellow (E104) instead of 20 mg TPA023B. Quinoline Yellow was added to ensure the same color of TPA023B and placebo tablets. GRP and BNP were obtained from Tocris. For intrathecal (i.t.) administration into mice, both peptides were dissolved in distilled water and diluted in extracellular solution to 1–10 nmoles per 10 µl. For topical application, TPA023B (0.3 µM 100 µl) was suspended in acetone/olive oil (4:1 v/v) and applied on the shaved nape of the neck once daily.
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4

Enteric-coated multiparticulate capsules

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Paracetamol and tramadol HCl (both supplied by Janssen Pharma) were chosen as model drugs. Methacrylic acid–methyl methacrylate copolymers (Eudragit S100 and L100) were from Evonik Industries (Essen, Germany). Hypromellose acetate succinate (MF and HF grades) were obtained from Shin-Etsu Chemical (Tokyo, Japan). Silicified microcrystalline cellulose (Prosolv sMCC90, JRS Pharma, Rosenberg, Germany), anhydrous lactose (SuperTab 24AN, DFE Pharma, Goch, Germany) anhydrous dibasic calcium phosphate (DI-CAFOS A 60, Budenheim, Budenheim, Germany), and Triethyl Citrate (RoFarma Italia, Gaggiano, Italy) were used as received. Isopropanol (Carlo Erba, Cornaredo, Italy) and Yellow Eosin (Carlo Erba, IT) were of standard chemical grades. Gelatin capsules were purchased from ACEF (Fiorenzuola D’Arda, Italy), while HPMC cps (size 0), DRcaps® (size 2 and size 0), and Vcaps® Enteric capsules (size 0) were obtained from Lonza (Lonza Capsules & Health Ingredients, Basel, Switzerland).
Throughout the text, the following abbreviations are used: paracetamol (AAP), tramadol HCl (Tram), Eudragit S100 (EuS100), Eudragit L100 (EuL100), hypromellose acetate succinate MF (HPMC AS-MF), hypromellose acetate succinate HF (HPMC AS-HF), Triethyl Citrate (TEC), Prosolv sMCC90 (SMCC), SuperTab 24AN (LAC), DI-CAFOS A 60 (DCP), and Isopropanol (Iso).
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5

Controlled Release Tramadol HCl Matrices

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Kollidon® SR (BASF SE, Ludwigshafen, Germany) and/or glyceryl behenate (Compritol® 888 ATO, Gattefossé, Saint-Priest, France) were used as the controlled release agents forming the matrix systems. Prosolv® SMCC 90 (JRS PHARMA, GmbH & Co. KG, Herzogenaurach, Germany) was used as a dry binder and Kolliwax (BASF SE, Ludwigshafen, Germany) was used as a lubricant. Tramadol hydrochloride (TH) (Sigma Aldrich Chemie GmbH, Darmstadt, Germany) was chosen as a model highly water-soluble drug. The commercial PVA filament (PrimaCreator, Malmö, Sweden) and the filament prepared from HPMC (AffinisolTM, DuPont, Wilmington, DE, USA) by hot melt extrusion were used for the 3DP coating of the matrix tablets.
Redistilled water and chemicals of analytical grade (HCl, NaCl–Lach-Ner s.r.o., Neratovice, Czech Republic) were used for the preparation of the dissolution media and of the standard solution of tramadol hydrochloride. For the preparation of the alcoholic dissolution medium (40% v/v), ethanol p. a. (Lach-Ner s.r.o., Neratovice, Czech Republic) was used.
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6

Polyelectrolyte-Based Matrix System for Tramadol and Salicylic Acid

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ι-carrageenan (Merck KG&A, Darmstadt, Germany) and chitosan of a medium molecular weight and an 85% degree of deacetylation (JBICHEM, Shanghai, China) were used as the agents to form the polyelectrolyte-based matrix system. Silicified microcrystalline cellulose (Prosolv® SMCC 90; JRS PHARMA GmbH & Co. KG, Rosenberg, Germany) or calcium sulfate dihydrate (Compactrol®; JRS PHARMA GmbH & Co. KG, Germany) were used as a dry binder, and sodium stearyl fumarate (Pruv®; JRS PHARMA GmbH & Co. KG, Germany) was used as a lubricant. Tramadol hydrochloride (Sigma Aldrich Chemie GmbH, Taufkirchen, Germany) was chosen as a model highly water-soluble drug, and salicylic acid (NOVACYL SAS, Écully, France) as a model slightly water-soluble drug. Mucin from porcine stomach Type II was purchased from Merck (Merck KG&A, Darmstadt, Germany) and used as a model substrate for adhesion testing.
Redistilled water and chemicals of an analytical grade (HCl, NaCl, NaOH, and KH2PO4; Lach-Ner s.r.o., Neratovice, Czech Republic) were used for the preparations of the dissolution media and the standard solution of the model drugs.
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7

Formulation and Evaluation of Papaverine Tablets

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Papaverine hydrochloride (PAP) was the product of Farm-Impex Sp. J., Poland. Polyvinylpyrrolidone K 10 (PVP 10), microcrystalline cellulose (Avicel PH 101, Avicel PH 102), α-lactose (lactose), crospovidone CL (Kollidon CL), magnesium stearate (MS), and mannitol were produced by Sigma-Aldrich Chemmie Gmbh, Germany. Croscarmellose sodium (AcDiSol) was the product of BioPolymer, Belgium and gelatinized starch (CPharmGel) was the product of CargillBenelux BV, Netherlands. The manufactured mixture called Prosolv EasyTab SP (Prosolv) containing microcrystalline cellulose, colloidal silicon dioxide, sodium starch glycolate, and sodium stearyl fumarate was produced by JRS Pharma Gmbh & CO KG, Germany. The manufactured mixture called Prosolv SMCC 90 containing microcrystalline cellulose and colloidal silicon dioxide (CMSi), and manufactured by JRS Pharma Gmbh & CO KG, Germany, was also used. All other reagents and solvents were of analytical grade, distilled water was freshly distilled.
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8

Tramadol Hydrochloride Tablet Formulation

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Silicified microcrystalline cellulose Prosolv ® SMCC 90 was supplied by JRS Pharma, GmbH+Co.kG (Germany), Disintequik ™ MCC 25 by Kerry (USA), hypromellose (Methocel ™ K4M Premium CR, Methocel ™ K100M Premium CR) by the firm Colorcon GmbH (Germany). Magnesium stearate was obtained from Acros Organics (USA). Tramadol hydrochloride was from Sigma-Aldrich (Czech Republic).
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