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Eudragit l100

Manufactured by Evonik
Sourced in Germany, United States

Eudragit L100 is a pharmaceutical-grade polymer used in the formulation of enteric coatings. It is a methacrylic acid-methyl methacrylate copolymer that is soluble in intestinal fluids at a pH above 6.0. This allows it to protect sensitive active pharmaceutical ingredients from the acidic environment of the stomach and release them in the intestine.

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51 protocols using eudragit l100

1

Liposome-mediated delivery of anti-diabetic compound

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LG powder was provided by Agrisan Company (Larciano, Pistoia, Italy). The liposome components Soy lecithin and Eudragit® L100 were purchased from Evonik Industries AG (Essen, Germany). Streptozotocin (STZ; cat. S0130) was purchased from Sigma Aldrich-Merck (St. Louis, MO, USA). RIPA lysis buffer (cat. sc-24948A) was obtained from Santa Cruz Biotechnology (Dallas, TX, USA), while the phosphatase and proteinase inhibitor cocktails were obtained from Roche Applied Science (Indianapolis, IN, USA). Micro BCA Protein Assay (cat. 23235) and β-mercaptoethanol (cat. J66742) was purchased from Thermo Fisher Scientific (Waltham, MA, USA). SDS (cat. A02263) and non-fat milk (cat. A0830) powders were obtained from PanReac AppliChem (Milano, Italy). Clarity western enhanced chemiluminescence substrate (cat. 1705061) was purchased from Bio-Rad Laboratories, Inc. (Hercules, CA, USA). The specifics of the primary and secondary antibodies used are reported in Table 1.
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2

Formulation development of amorphous solid dispersions

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PCM (lot 1511337) was purchased by Purifarma (São Paulo, Brazil), and MTL (lot FN 81700006) was provided by Purifarma (Anápolis, Brazil). Plasdone® K-29/32 (poly (vinylpyrrolidone-co-vinyl acetate) (PVPVA), lot 002177615) was donated by Ashland Specialty Ingredients (Covington, LA, USA), Eudragit® L100 (EUL, methacrylic acid-methyl methacrylate copolymer, lot B111003013) was provided by Evonik (Essen, Germany), Soluplus® (SOL, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol copolymer, lot 84414368E0) was a gift from BASF (Ludwigshafen, Germany), and Parteck® MXP (PVA, polyvinyl alcohol, lot F1952064) was donated by Merck (Darmstadt, Germany).
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3

Oregano Oil and Modified Starches Formulation

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Oregano essential oil of Greek origin (EO, 85.89% carvacrol) from Oreganum vulgare (Heracleoticum) was gifted by Ecopharm Hellas, Kilkis, Greece. Arabic gum (AG, Spraygum AB) was from Nexira, France. Maltodextrin (MD, Glucidex 21), modified starches (MS, Clearam® CH 2020, food grade acetylate di-starch adipate, E1422) and Cleargum® (food grades sodium octenyl succinate starch, E1450 of high CO 01 and low CO 03 viscosity) were all from Roquette Italia, gifted by Interallis Chemicals, Greece. For practical reasons and to link with their chemistry, the starches were coded: Clearam® as ADA; Cleargum® as SOS (SOS1 grade for high and SOS3 for low viscosity). Eudragit® L100 was from Evonik (Darmstadt, Germany) kindly gifted by ChemiX SA, Greece. The chemical structures of the two chemically different modified starches are shown in Figure 1.
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4

Eudragit L100-based Compound Formulation

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Example 8

4.5 g Eudragit L100 (Evonik Germany) was weighed, and added to anhydrous ethanol (J.T. Baker) under stirring. After it was completely dissolved, 3.0 g of the compound HMS5552 was added. Stirring was continued after adding sufficient amount of anhydrous ethanol to obtain 50 ml solution in a yellow to orange color.

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5

Eudragit L100-based Drug Formulation

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Example 5

1.5 g Eudragit L100 (Evonik Germany) was weighed, and added to anhydrous ethanol (J.T. Baker) under stirring. After it was completely dissolved, 6 g of the compound HMS5552 was added. Stirring was continued after adding sufficient amount of anhydrous ethanol to obtain 50 ml solution in a yellow to orange color.

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6

Eudragit L100-based Solid Dispersion Formulation

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Example 3

3.75 g Eudragit L100 (Evonik Germany) was weighed, and added to anhydrous ethanol (J.T.Baker) under stirring. After it was completely dissolved, 3.75 g of the compound HMS5552 was added. Stirring was continued after adding sufficient amount of anhydrous ethanol to obtain 50 ml solution.

Unit formula
Formula compositionamount/mg% (w/w)
Glimepiride1.000.40
HMS5552 solid dispersion*200.0080.00
Microcrystalline cellulose29.0011.60
Hydroxypropyl cellulose7.503.00
Croscarmellose sodium7.503.00
Sodium dodecyl sulfate2.501.00
Magnesium stearate2.501.00
Total weight of a tablet core250.00100.00
Opadry7.503.00
Total weight of a coated tablet257.50
*200.00 mg of the HMS5552 solid dispersion contained 100 mg of HMS5552.

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7

Eudragit L100-Based Solid Dispersion Formulation

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Example 7

3.0 g Eudragit L100 (Evonik Germany) was weighed, and added to anhydrous ethanol (J.T.Baker) under stirring. After it was completely dissolved, 4.5 g of the compound HMS5552 was added. Stirring was continued after adding sufficient amount of anhydrous ethanol to obtain 50 ml solution.

Unit formula
Formula compositionamount/mg% (w/w)
Repaglinide2.000.80
HMS5552 solid dispersion*100.0040.00
Microcrystalline cellulose128.0051.20
Hydroxypropyl cellulose7.503.00
Croscarmellose sodium7.503.00
Sodium dodecyl sulfate2.501.00
Magnesium stearate2.501.00
Total weight of a tablet core250.00100.00
Opadry7.503.00
Total weight of a coated tablet257.50
*100.00 mg of the HMS5552 solid dispersion contained 50 mg of HMS5552.

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8

Eudragit L100-Based Solid Dispersion of HMS5552

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Example 6

0.75 g Eudragit L100 (Evonik Germany) was weighed, and added to anhydrous ethanol (J.T.Baker) under stirring. After it was completely dissolved, 6.75 g of the compound HMS5552 was added. Stirring was continued after adding sufficient amount of anhydrous ethanol to obtain 50 ml solution.

Unit formula
Formula compositionamount/mg% (w/w)
Repaglinide1.000.40
HMS5552 solid dispersion*150.0060.00
Microcrystalline cellulose79.0031.60
Hydroxypropyl cellulose7.503.00
Croscarmellose sodium7.503.00
Sodium dodecyl sulfate2.501.00
Magnesium stearate2.501.00
Total weight of a tablet core250.00100.00
Opadry7.503.00
Total weight of a coated tablet257.50
*150.00 mg of the HMS5552 solid dispersion contained 75 mg of HMS5552.

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9

Budesonide-loaded Eudragit Formulation

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The Budesonide (BUD) was a gift sample from Symbiotec Pharma Lab, Indore, India. The Poloxamer 188 (PXM) was obtained from BASF, Ahmedabad, India. Polyvinylpyrrolidone K30 (PVP K30), Croscarmellose sodium (CCS), Sodium Starch Glycolate (SSG), Lactose monohydrate, and Dibutyl phthalate (DBP) were purchased from S. D. Fine Chem. Ltd., Mumbai, India. Eudragit S100 and Eudragit L100 were purchased from Evonik Industries, Mumbai, India. All other reagents and chemicals used in this research were of analytical grade.
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10

Formulation and Characterization of Polymeric Nanocarriers

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Eudragit L100 (methacrylic acid-methyl methacrylate copolymer (1 :1)) powder (Mw= 125000 g/mol) and Eudragit E100 (dimethylaminoethyl methacrylate, butyl methacrylate, and methyl methacrylate tri-copolymer with a ratio of 2 :1 :1) pellets (Mw=47000 g/mol) were obtained from Evonik Röhm GmbH (Darmstadt, Germany). Sodium hydroxide was purchased from Sigma Aldrich (Sweden) and hydrochloric acid (35%) from VWR Chemicals (France). Sodium chloride was obtained from Laurylab (Brindas, France). Branched polyethylenimine (PEI, Mw=25000 g/mol, Mn∼10000) was purchased from Aldrich Chemistry (Germany), polyvinyl alcohol (Mw=200000 g/mol) from Merck KGaA (Darmstadt, Germany) and polyacrylic acid 40% wt. (Mw=30000 g/mol) from Aldrich Chemical Company (Milwaukee, USA). Dextran 40 (Mw=40000 g/mol) was a product of AppliChem GmbH (Darmstadt, Germany) and Pluronic F68 was purchased from Molekula Group (Shaftesbury, Dorset, Great Britain). Amino-dextran was prepared according to Mouaziz et al. [35] (link) and using hexamethylenediamine from Merck (Germany) and Dextran-T40 from Amersham Biosciences (Germany)(Table 1).
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