1.Eudragit is the brand name for a diverse range of polymethacrylate-based copolymers. It includes anionic, cationic, and neutral copolymers based on methacrylic acid and methacrylic/acrylic esters or their derivatives.
2.Applications of different grades of Eudragit in colon-specific/enteric-coated/sustained release drug delivery and taste masking.
3.Eudragits are non-biodegradable, non-absorbable, and nontoxic.
4.Anionic Eudragit L dissolves at pH > 6 and is used for enteric coating, while Eudragit S, soluble at pH > 7 is used for colon targeting. Eudragit RL and RS, having quaternary ammonium groups, are water insoluble, but swellable/permeable polymers which are suitable for the sustained release film coating applications. Cationic Eudragit E, insoluble at pH less than 5, can prevent drug release in saliva and finds application in taste masking.
5.Eudragit is the brand name for a diverse range of copolymers based on polymethacrylates principally marketed by Evonik Industries, Germany. Eudragit was first introduced by Rohm & Hass GmbH, Darmstadt in 1953 as an alkaline soluble drug coating material resistant to stomach acid. It is used for functional pharmaceutical coatings, matrix formers in common granulation techniques as well as in direct compression.
5. Eudragit Nomenclature, Eudragit Abbreviation, Eudragit E, L, S, RL, RS, Cellulose acetate phthalate, HPMC phthalate, HPMC acetate succinate, PVAP
2. 1. Methacrylate derivates
• Eudragit® L 100
• Eudragit® L 100-55
• Eudragit® L 30 D-55
• Eudragit® L 12.5
• Eudragit® S 100
• Eudragit® S 12.5
• Eudragit® R 12.5
• Eudragit® FS 30 D
2. Cellulose derivatives
• Cellulose Acetate Phthalate (CAP), Aquacoat® CPD
• Hypromellose phthalate (HPMCP)
• Hypromellose acetate succinate (HPMC-AS), Aquot®, AquaSolve®
3. Polyvinyl acetate derivatives
• Polyvinyl acetate phthalate (PVAP), Opadry® Enteric
Enteric polymers
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3. 1. Polymethacrylate derivatives
Eudragit- Brand name of methacrylate derivatives , Manufacturer Company- Evonik industries
Eudragit® is trademark of Rohm GmbH & Co. KG. Darmstadt in Germany, first marketed in 1950s
Eudragit Trade name codes of different Eudragit polymer
Sr. No Code Availability Eudragit® grade
1 100 a Solid (Granules) Eudragit® L 100-55
Eudragit® RL 100
Eudragit® RS 100
Eudragit® L 100
Eudragit® S 100
2 PO Powder Eudragit® RL PO
Eudragit® RS PO
Eudragit® E PO
3 30 D a Aqueous dispersion Eudragit® L 30 D-55
Eudragit® RL 30 D
Eudragit® RS 30 D
Eudragit® NE 30 D
4 12.5 a Organic solution Eudragit® L 12.5
Eudragit® S 12.5
Eudragit® RL 12.5 P
Eudragit® E 12.5
a-Polymer dry weight
content in percentage
P-Indicate Plasticizer
(1.25%)
Indicate Soluble at pH 5.5
NE-neutral Eudragit grade
Eudragit® L 12.5 = 12.5%
Solution in isopropanol to
acetone(60:40)
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4. 1.Eudragit E Grade
The ratio of
(2-dimethylaminoethyl)
methacrylate to butyl
methacrylate to methyl
methacrylate is 2:1:1
4.Eudragit RL Grade &
Eudragit RS grade
The ratio of ethyl acrylate to
methyl methacrylate to triethyl
ammonioethyl methacrylate
chloride is 1:2:0.2 for RL
Grade and 1:2:0.1 for RS grade
2.Eudragit L Grade
The ratio of
methacrylic acid to
ethyl acrylate or methyl
methacrylate is 1:1
3.Eudragit S Grade
The ratio of
methacrylic acid to
methyl methacrylate is
copolymer 1:2
Eudragit Polymers are grade on the basis of its proportion of different Polymethacrylate
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5. Stomach pH 1-5
Eudragit® E 100
Eudragit® E 12.5
Eudragit® E PO
DELAYED RELEASE
Duodenum pH >5.5
Eudragit® L 100-55
Eudragit® L 30 D-55
Jejunum pH >6
Eudragit® L 100
Eudragit® L 12.5
IMMEDIATE RELEASE
Ileum and Colon pH>7
Eudragit® S 100
Eudragit® S 12.5
Eudragit® FS 30 D
Highly Permeable
Eudragit® RL PO
Eudragit® RL 100
Eudragit® RL 30 D
Eudragit® RL 12.5
Low Permeable
Eudragit® RS PO
Eudragit® RS 100
Eudragit® RS 30 D
Eudragit® RS 12.5
Swellable, Permeable
Eudragit® NE 30 D
Eudragit® NE 40 D
Eudragit® NM 30 D
SUSTAINED RELEASE
Eudragit® polymer for oral solid dosage formulations
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6. Chemical name Trade name
Poly(butyl methacrylate, (2-dimethylaminoethyl) methacrylate,
methyl methacrylate) 1:2:1
Eudragit E 100, Eudragit E 12.5
Eudragit E PO
Poly(ethyl acrylate, methyl methacrylate) 2:1 Eudragit NE 30 D, Eudragit NE 40 D
Eudragit NM 30 D
Poly(methacrylic acid, methyl methacrylate) 1:1 Eudragit L 100, Eudragit L 12.5
Eudragit L 12.5 P
Poly(methacrylic acid, ethyl acrylate) 1:1 Eudragit L 30 D-55
Eudragit L 100-55
Poly(methacrylic acid, methyl methacrylate) 1:2 Eudragit S 100, Eudragit S 12.5
Eudragit S 12.5 P
Poly(methyl acrylate, methyl methacrylate, methacrylic acid)
7:3:1
Eudragit FS 30D
Poly(ethyl acrylate, methyl methacrylate, trimethyl
ammonioethyl methacrylate chloride) 1:2:0.2
Eudragit RL 100, Eudragit RL PO
Eudragit RL 30 D, Eudragit RL 12.5
Poly(ethyl acrylate, methyl methacrylate, trimethyl
ammonioethyl methacrylate chloride) 1:2:0.1
Eudragit RS 100, Eudragit RS PO
Eudragit RS 30 D, Eudragit RS 12.5
Evonik industries manufactured different grade of polymethacrylates polymer
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7. Table: methacrylate grade manufacturer company other than Evonik industry
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Chemical Name Grade Availability Solubility Manufacturer
company
Poly(methacrylic
acid, ethyl acrylate)
1 : 1
Acryl-EZE Powder Soluble at pH
above 5.5
Colorcon Inc.
Acryl-EZE 93A Powder Soluble at pH
above 5.5
Colorcon Inc.
Acryl-EZE MP Powder Soluble at pH
above 5.5
Colorcon Inc.
Eastacryl 30 D Aqueous
dispersion
Soluble at pH
above 5.5
Eastman Chemical
Kollicoat MAE
30 DP
Aqueous
dispersion
Soluble at pH
above 5.5
BASF Fine
Chemicals
Kollicoat MAE
100 P
Powder Soluble at pH
above 5.5
BASF Fine
Chemicals
8. Properties of Polymethacrylates
Polymethacrylates are categorized by varying ratios of dimethylaminoethyl methacrylates, methacrylic acid,
and methacrylic acid esters.
1.Cationic
Immediate release
e.g. Eudragit E series
Sustained release Eudragit except NE series of Eudragit
e.g. Eudragit RL and RS series
2.Anionic
Delayed release
e.g. Eudragit L and S series
Kollicoat MAE 30 DP and 30 D
3.Non ionic
Sustained release
e.g. Eudragit® NE 30 D
Eudragit® NE 40 D
Eudragit® NM 30 D
Molecular weights of
Polymethacrylates
30,000–278,000 g/mole
pH range where soluble
o >5.5 (L 100-55, L 30 D-55)
o >6.0 (L 100, L 12.5)
o >7.0 (S 100, S 12.5 )
o Insoluble (RL)
o Insoluble (RS)
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9. 2. Cellulose derivatives
A. Cellulose Acetate Phthalate
Properties
Available in Powder, Granule and flake form
Soluble at pH above 6
Molecular weight is 48,000 g/mol
Practically insoluble in water & alcohols and Freely soluble in acetone, soluble in diethylene glycol
Soluble in ketones, esters, ether alcohols, and in solvent mixtures.
Hygroscopic 7–8% at 75% RH
Application
used as an enteric film coating material
Manufacturer company
Colorcon Inc. USA , Cellulose acetate phthalate-CPD®
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10. B. Hypromellose phthalate (HPMCP)
Application
used as an enteric coating material for tablets or granules.
Tablets coated with HPMCP disintegrate more rapidly than tablets coated with CAP.
Properties
Available in Powder, Granule and flake form
Soluble at pH above 5 (HP-50) and above 5.5 (HP-55, HP-55S)
Hygroscopic
Practically insoluble in water and dehydrated alcohol
Readily soluble in a mixture of acetone and methanol or ethanol
HPMCP is more stable than CAP
HPMCP has three grades
Grade Mol wt.
HP-50 84000
HP-55 78000
HP-55S 132000
Manufacturer company
Shin-Etsu, Tokyo Japan
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11. C. Hypromellose Acetate Succinate (HPMC-AS) Aquot®
Application
used as a film coating as well as an enteric coating
Properties
Available in Powder or granules forms
Hygroscopic
Divided into subclasses based upon pH at which polymer dissolves
L (low): pH ≥ 5.5
M (medium):pH ≥ 6.0
H (high): pH ≥ 6.8
And also classified predominant size
Cohesive fine powder, F
Free-flowing granules, G
Practically insoluble in ethanol, hexane and unbuffered water.
mixture of ethanol and dichloromethane produced clear or turbid solution
Manufacturer company
Shin-Etsu, Tokyo Japan
Examples of HPMC-AS
Aqoat® MF- medium and
fine grade
Aqoat® MG-medium and
granule grade
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12. Polyvinyl acetate derivatives
Polyvinyl Acetate Phthalate (PVAP) Opadry®
Application
Used as viscosity-modifying agent
as enteric coatings
as core sealing of tablets prior to a sugar-coating process
Properties
Soluble at pH above 6
Soluble in ethanol and methanol, sparingly soluble in acetone and isopropanol;
practically insoluble in chloroform, dichloromethane and water
polyvinyl acetate phthalate undergoes less hydrolysis than other commonly
used enteric coating polymers.
Manufacturer company
Colorcon Inc. USA
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13. Merits of enteric polymers
Gastric resistance
pH-controlled drug release
Gastrointestinal targeting
Colon delivery
Protection of acid-sensitive actives
Protection of gastric mucosa from aggressive actives
Increased drug effectiveness
Excellent storage stability
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14. 1. Raymond C Rowe, Paul J sheskey and Marian E Quinn Handbook of Pharmaceutical
Excipients. Edition 6th.
2. https://healthcare.evonik.com/en/drugdelivery/oral-drug-delivery/oral-
excipients/eudragit-portfolio,Evonik industries.
3. Ashlee D. Brunaugh Hugh D. C. Smyth Robert O. Williams III, Essential
Pharmaceutics,AAPS Introductions in the Pharmaceutical Sciences.
4. Ann Newman Seventh Street Development Group Lafayette, Indiana, USA, wiley,
Pharmaceutical Amorphous Solid Dispersions.
References
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