Se ha denunciado esta presentación.
Se está descargando tu SlideShare. ×

Enteric Polymers - SlideShare

Anuncio
Anuncio
Anuncio
Anuncio
Anuncio
Anuncio
Anuncio
Anuncio
Anuncio
Anuncio
Anuncio
Anuncio
Próximo SlideShare
Paavan  Polymers
Paavan Polymers
Cargando en…3
×

Eche un vistazo a continuación

1 de 15 Anuncio

Enteric Polymers - SlideShare

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

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

Anuncio
Anuncio

Más Contenido Relacionado

Similares a Enteric Polymers - SlideShare (20)

Más reciente (20)

Anuncio

Enteric Polymers - SlideShare

  1. 1. ENTERIC POLYMERS RAMESHWAR K. KHILLARE M.S Pharm. Pharmaceutics NIPER-Ahmedabad 1 Drug + Polymer formulation
  2. 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 2
  3. 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) 3
  4. 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 4
  5. 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 5
  6. 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 6
  7. 7. Table: methacrylate grade manufacturer company other than Evonik industry 7 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. 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) 8
  9. 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® 9
  10. 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 10
  11. 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 11
  12. 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 12
  13. 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 13
  14. 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 14
  15. 15. 15

×