EUDRAGIT - Rofarma

1 EUDRAGIT . Acrylic Polymers for solid Oral Dosage Forms EUDRAGIT Technical Formulation Proof of GMP Advanced 1 Products 2 Support 3. Development 4 Concept 5 Services 6 Drug Delivery Evonik. Power to create. When it comes to targeted drug release profiles, EUDRAGIT . is the pharmaceutical industry's preferred choice of product. The range of EUDRAGIT Poly(meth)acrylate-based products provides full flexibility for your solid oral dosage forms. EUDRAGIT Polymers . Pharmaceutical Properties The basis of our offerings are masking to increase patient A distinction is made between 2. Poly(meth)acrylates; inso- our Poly(meth)acrylates for compliance. The range of our 1. Poly(meth)acrylates; soluble luble but permeable in digestive pharmaceutical applications, product portfolio provides full in digestive fluids by salt forma- fluids EUDRAGIT RL and RS.

2 Which are known worldwide flexibility for your targeted tion EUDRAGIT L, S, FS and E polymers with alkaline and in the industry under the trade drug release profiles by offering polymers with acidic or alkaline EUDRAGIT NE polymers with name EUDRAGIT . These po- best performance for enteric, groups enable pH-dependent neutral groups enable con- lymers allow the active in your protective or sustained-release release of the active ingredient. trolled time release of the active solid dosage form to perform properties. Applications: from simple taste ingredient by pH-independent during the passage of the human masking through gastric resis- swelling. body. The flexibility to combine EUDRAGIT polymers are tance to controlled drug release Applications: delayed and the different polymers enables copolymers derived from esters in all sections of the intestine sustained drug release you to achieve the desired drug of acrylic and methacrylic acid, release profile by releasing the whose physicochemical proper- drug at the right place and at ties are determined by functio- the right time and, if necessary, nal groups (R).

3 EUDRAGIT . over a desired period of time. polymers are available in a wide Other important functions are range of different physical forms protection from external influ- (aqueous dispersion, organic ences (moisture) or taste/odor solution granules and powders). Methacrylic copolymers Functional group: carboxylic acid R = COOH (anionic) Aminoalkyl methacrylate copolymers EUDRAGIT L 100/S 100/L 100-55 (powders) Functional group: dimethyl aminoethyl EUDRAGIT L 30 D-55 / FS 30 D R = COOCH2 CH2 N(CH3)2 (cationic). (aqueous dispersion 30%) EUDRAGIT E 100 (granules). EUDRAGIT L 12,5 / S 12,5 EUDRAGIT E 12,5 (organic solution ). (organic solution ). Gastroresistant and EUDRAGIT E PO (powder). enterosoluble Gastrosoluble and enteroresistent CH3(H) CH3.

4 I I. --- C CH2 C CH2--- I I. COO-Alkyl R. Ammonioalkyl Methacrylate copolymers methacrylate copolymers Functional group: trimethylammonioethyl Functional group: neutral esters R = COOCH2 CH2N+(CH3)3CI- (neutral). R = COOCH3 or COOC4H9 (neutral). EUDRAGIT RL 100 (granules). EUDRAGIT NE 30 D / 40 D / NM 30 D EUDRAGIT RL PO / RS PO (powders). (aqueous dispersion 30% / EUDRAGIT RL 30 D / RS 30 D. 40% polymer content) (aqueous dispersion 30%). EUDRAGIT RL 12,5 / RS 12,5. (organic solution ). Insoluble, permeable; Insoluble, permeable or dispersable;. pH-independent pH-independent 2 3. Enteric Formulations EUDRAGIT offers valuable Gastroresistance and advantages for your enteric GI Targeting coatings: If you need to protect your active product portfolio of anionic pH-dependent drug release from the gastric fluid and would EUDRAGIT grades which like to improve drug effective- dissolve at rising pH values.

5 Targeted drug release in the gastrointestinal tract. Moreover, with the following technical Protection of actives sensitive ness EUDRAGIT L and S In addition, the different colon is required for local treat- the gastroresistance of the advantages: to gastric fluid polymers are your preferred grades can be combined with ment of intestinal disorders such coating ensures that the oral aqueous processing choice of coating polymers. each other, making it possible as Crohn's disease, ulcerative dosage form is patient compliant. highly flexible coatings Protection of gastric mucosa They enable targeting specific to adjust the dissolution pH, colitis or intestinal cancer. It is The preferred coating is suitable for multiparticulate from aggressive actives areas of the intestine.

6 Pharma and thus to achieve the required also required for drugs that are EUDRAGIT FS 30 D, which tablet preparation Polymers offers a broad GI targeting for the drug. poorly soluble in the upper combines release in the colon Increase in drug effectiveness Good storage stability GI and colon targeting 350. 300. 250. EUDRAGIT Polymer Availability Dissolution Properties L 30 D-55 30 % Aqueous Dispersion 200. Dissolution rate [mg/min g]. Dissolution above pH L 100-55 Powder 150. L 100 Powder 100. Dissolution above pH EUDRAGIT L 30 D-55. L 12,5 % Organic Solution 50 EUDRAGIT L 12,5. S 100 Powder EUDRAGIT L/S 12,5 (1:1). 0. S 12,5 % Organic Solution Dissolution above pH EUDRAGIT FS 30 D. 5 6 7 8. FS 30 D 30 % Aqueous Dispersion pH-value EUDRAGIT S 12,5.

7 Take your active to the right place. When it is a long way to the target and still the target has to be hit exactly, EUDRAGIT offers the right solution. 4 5. Protective Formulations Our protective polymers are melt extrusion process. During interacts with the anionic active suitable for aqueous or organic the melt extrusion process the which provides excellent taste coatings and can be applied in a cationic EUDRAGIT E polymer masking properties. Moisture Protection and Odor/Taste Masking Do you need to protect your EUDRAGIT E polymers help making it an extremely eco- Take advantage of protective active from moisture or light and would like to increase patient you to seal sensitive actives and increase patient compliance by nomical application.

8 Pharma Polymers offer various cationic EUDRAGIT coatings: compliance? masking tastes and odors. EUDRAGIT E grades for Even thin layers of EUDRAGIT protective coatings. pH-dependent drug release provide the desired effect, Protection of sensitive actives Taste and odor masking Moisture protection EUDRAGIT Polymer Availability Dissolution Properties Economical application E 100 Granules Soluble in gastric fluid up to pH Improved passage of the dosage form E 12,5 % Organic Solution Swellable and permeable above pH Smooth and glossy surfaces, good color coating E PO Powder EUDRAGIT offers a strong protection of sensitive contents and improved patient compliance. 6 7. Sustained-Release Formulations Time-Controlled Drug Release Matrix tablets Multiparticular tablets Whether you need your drug profile.

9 Drug delivery can be allow custom-tailored release There are two EUDRAGIT serves as a matrix EUDRAGIT is employed as a to release over a specific period controlled throughout the entire profiles to achieve the desired formulation options: within which the active ingre- coating material, usually for the of time or would like to benefit gastrointestinal tract to increase drug delivery performance. dient is embedded. The matrix coating of pellets or particles from the advantages of multi- the therapeutic effect and EUDRAGIT NE and NM grades structure is obtained by direct that are filled into capsules or particulate or matrix formula- patient compliance. Different are neutral ester dispersions compression, granulation, or compressed into tablets.

10 These tions EUDRAGIT can help polymer combinations of which do not require addition melt extrusion. EUDRAGIT pellets or particles act as diffusion you achieve your desired release EUDRAGIT RL and RS grades of plasticizer. NM 30 D is particularly suitable cells in the digestive tract and for granulation processes in the release a constant drug quantity manufacture of matrix tablets. per unit of time (multi-unit dosage forms). EUDRAGIT Polymer Availability Dissolution Properties RL 100 Granules RL PO Powder Insoluble High permeability RL 30 D 30 % Aqueous Dispersion pH-independent swelling Benefit from EUDRAGIT coatings RL 12,5 % Organic Solution with sustained release: RS 100 Granules RS PO Powder Insoluble Time-controlled release of active ingredients RS 30 D 30 % Aqueous Dispersion Low permeability pH-independent swelling Therapeutically customized release profiles RS 12,5 % Organic Solution H igher patient compliance due to reduced number NE 30 D 30 % Aqueous Dispersion Insoluble, low permeability pH-independent swelling of doses to be taken NE 40 D 40 % Aqueous Dispersion No plasticizer required Highly flexible Cost-effective processing NM 30 D 30 % Aqueous Dispersion Controlled release: EUDRAGIT enables formulations which allow customer-tailored release profiles and releases over a specific period of time.