eudragit it's role as an excipient

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EUDRAGIT It’s role as an excipient

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Content: Polymer : Overview Eudragit : Introduction Types of Eudragit Eudragit for conventional film coating Eudragit for modified release

application

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Polymer Greek Word – Many parts It is made of many simpler

parts/units. Simple compound from which

polymer are made called monomer. They are formed by a process called

polymerization.

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Types of polymer Natural

Polysaccharides Proteins Nucleic acids

Synthetic

Elastomer Fibers Plastics

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Classification of Polymer Homopolymer : represented as : -[A-A-A-A-A-A]- Copolymer : represented as : -[A-B-A-B-A-B]-

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Formation of Polymers They are formed by a process called

as a Polymerization.

Polymer are formed by two ways –a. Chain reaction polymerizationb. Step reaction polymerization

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Use of polymer Film coating of solid dosage form Capsule Gels Disperse system Transdermal drug delivery system Controlled drug delivery system.

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Eudragit Eudragit was developed by Rohm & Haas Gmbh in Darmstadt in 1953.

Eudragit polymers are copolymers derived from esters of acrylic and methacrylic acid.

Physicochemical properties of Eudragit is determined by functional groups.

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Acrylate and Acrylic acid are a type of vinyl polymer.

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Types of Eudragit There is two types of Eudragit1. pH-dependent: e.g. Eudragit L,S,E2. pH-independent: e.g. Eudragit RS,RL,NE

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Eudragit for conventional film coating Eudragit E is methacrylate amino

ester copolymer.

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Due to presence of amine these are basic in nature.

Due to this polymer is dissolve in acidic medium below pH 4.

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EUDRAGIT Polymer

Availability Dissolution Properties

E 100 Granules Soluble in gastric fluidup to pH 5.0 .Swellable and permeableabove pH 5.0

E 12.5 12.5 % Organic Solution

E PO Powder

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Advantage of Eudragit E coatings:

pH-dependent drug release. Protection of sensitive actives. e.g. Antibiotics. Taste and odor masking -Due to pH difference. Moisture protection e.g. Aspirin Improved passage of the dosage form Smooth and glossy surfaces, good color

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Eudragit for modified release application In which RL,RS,NE are used for timed

release or sustained release formulation.

Eudragit L,S are used for enteric and colon targeted drug delivery.

Eudragit RL,RS,NE are pH independent while Eudragit L,S are pH dependent.

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Time-Controlled Drug Release Eudragit RL,RS are Copolymers of acrylate

and methacrylates with quaternary ammonium group.

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These are totally esterified with no free carboxylic acid group.

It is neutral in characters and are insoluble over the entire physiological pH range.

Amine salts are typical ionic compound Water are able to dissolve ionic

compound appreciably.

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Due to presence of this group Eudragit RL,RS are permeable to water.

Vary the quantity of quaternary ammonium group, permeability also vary in the RL,RS.

Type of Type of EudragitEudragit

nn1 1 :n:n2 2 :n:n33 USP NF USP NF DesignationDesignation

RLRL 1 :2 :0.21 :2 :0.2 Type AType A

RSRS 1 :2 :0.11 :2 :0.1 Type BType B18

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After permeation of the fluid of surrounding medium it causes Dissolution of drug in the fluid entering the dosage forms.

Diffusion of drug solution in the opposite direction across films

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EUDRAGIT Polymer

Availability Dissolution Properties

RL 100 GranulesInsoluble , High permeability.

pH-independent swelling

RL PO Powder

RL 30 D 30 % Aqueous Dispersion

RL 12.5 12.5 % Organic Solution

RS 100 GranulesInsoluble, Low permeability.

pH-independent swelling

RS PO Powder

RS 30 D 30 % Aqueous Dispersion

RS 12.5 12.5 % Organic Solution

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Eudragit NE is an aqueous dispersion of a neutral copolymer consisting of polymethacrylic acid esters.

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Low permeability. pH independent swelling. Highly flexible. -It can be easily combined with

other type of polymer. No plasticizer is required. - Due to low glass transition

temperature of polymer.(< 8 °C )

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Type of Type of EudragitEudragit

nn1 1 :n:n2 2

NE 30 DNE 30 D 2:1 2:1

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EUDRAGIT Polymer

Availability Dissolution Properties

NE 30 D 30 % Aqueous Dispersion

Insoluble, low permeabilitypH-independent swelling

NE 40 D 40 % Aqueous Dispersion

NM 30 D 30 % Aqueous Dispersion 23

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Advantage of Eudragit RL,RS,NE coatings Time-controlled release of active

ingredients Therapeutically customized release

profiles Higher patient compliance due to

reduced number of doses to be taken Cost-effective processing

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Eudragit L and S are anionic polymers of methacrylic acid and methacrylates with a -COOH group.

RR11 RR22 TypeType

HH CC22HH55 L30DL30D

CHCH33 CHCH33 L100L100

CHCH33 CHCH33 S100S100

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Eudragit L and S contains ionizable carboxylic groups.

In low pH environments of the stomach the carboxylic group remain unionized and polymer coating remains insoluble.

In the intestine, the pH increases above 5 and allows carboxylic group to ionize.

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Eudragit L is mainly used for drug release in the intestine.

While, Eudragit S is mainly used for drug release in the colon.

TypeType nn11: n: n22 USP NF USP NF DesignationDesignation

LL 1:11:1 Type AType A

SS 1:21:2 Type BType B27

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In Eudragit L methacrylic acid content is 46-50.6, producing acid to ester ratio 1:1.

Eudragit S has methacrylic acid content is 27-30.6, producing acid to ester ratio 1:2.

Due to this Eudragit L dissolved at pH above 5.5-6 and Eudragit S dissolved at pH above 7.

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EUDRAGIT FS 30 D is a 30% (w/w) aqueous dispersion of a copolymer produced by the polymerization of methacrylic acid, methyl acrylate & methyl methacrylate.

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Eudragit FS 30 D has acid to ester ratio is 1:10.

Due to this Eudragit FS 30 D dissolved at pH above 7.

This leads to drug release very late in the intestinal tract.

Most commonly used for colon targeted drug delivery.

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Application of EUDRAGIT L & S coatings: pH-dependent drug release Protection of actives sensitive to gastric

fluid - e.g. : antibiotics ( Streptomycin ,

Gentamycin ( Septopal) , Erythromycin) Protection of gastric mucosa from

aggressive actives - e.g. : Salicylate Increase in drug effectiveness GI and colon targeting - e.g. : Intestinal antiseptic and mesalazine

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EUDRAGIT Polymer

Availability Dissolution Properties

L 30 D-55 30 % Aqueous Dispersion

Dissolution above pH 5.5L 100-55 Powder

L 100 Powder Dissolution above pH 6.0

L 12.5 12.5 % Organic Solution

S 100 Powder

Dissolution above pH 7.0

S 12.5 12.5 % Organic Solution

FS 30 D 30 % Aqueous Dispersion

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DrugDrug Trade Trade NameName

FormulatioFormulationn

Mesalazine Mesalazine Asacol Asacol Eudragit-S Eudragit-S coated coated tablets tablets ((dissolves at dissolves at pH 7)pH 7)

Mesalazine Mesalazine SalofacSalofac Eudragit-L Eudragit-L coated coated tablets tablets (dissolves at (dissolves at pH 6)pH 6)

MesalazineMesalazine ClaversalClaversal

MesazalMesazal

CalitoflakCalitoflak

Eudragit-L Eudragit-L coated coated tablets tablets

Budesonide Budesonide EntocortEntocort Eudragit-L Eudragit-L coated coated beads beads

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References Hogan JE . Film – coating materials and

their properties. In : Cole G editor. Pharmaceutical coating technology. Special ed. New York : informa health care ;2008 .p.7-19

Wang J, Ghebre – Sellassic I . Aqueous polymeric Dispersion as Film Formers . In : Lieberman HA , Rieger MM , Banker GS editor. Pharmaceutical dosage Forms : Disperse system , Volume -3. 2nd ed. New York : Marcel Dekker, Inc.p.135-136

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Agyilirah GA , Banker GS. Polymer for enteric coating application. In : Tarcha PJ, editor. Polymer for controlled Drug delivery. Boston: CRC press; 2000 .p. 41-44 , 58-60.

Shukla AJ . Polymethacrylate . In : Wade A , Weller PJ editor. Handbook of Pharmaceutical Excipients . 2nd ed. Washington : American pharmaceutical association ; 1994.p. 362-366

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Sinko PJ . Biomaterials . In : Sinko PJ editor. Martin’s Physical and Pharmaceutical Science . 5thed. Philadelphia : Lippincott Williams and Wilkins ;2006.p.7-19

Morrison RT , Boyd RN .Macromolecules. In : Morrison RT , Boyd RN editor. Organic chemistry . 6thed. New Delhi: Prentice – Hall of India ;2006.p.1077-1093

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