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  • Polymethacrylates are synthetic cationic and anionic polymer

    2018-10-22

    Polymethacrylates are synthetic cationic and anionic polymers of dimethylaminoethyl methacrylates, methacrylic acid, and methacrylic buy Wortmannin esters in varying ratios. Several types are commercially available and may be obtained as the dry powder, aqueous dispersion, organic solution [1]. The most commonly used organic phase used was a (60:40) mixture of acetone and propan-2-ol. Polymethacrylates are primarily used as film-coating agents in tablet and capsule dosage forms. Films of different solubility can be produced by using different polymer grades. Table 1 outlines the solubility profile of each grade of Eudragit. Broadly polymethacrylates are used as film former, tablet binder and tablet diluents. Apart from the above applications, recent studies revealed that polymethacrylates have got widespread applications in formulation vis-à-vis taste masking, better permeation across skin, intestinal epithelium and corneal permeation, dissolution enhancement, bioavailability enhancement, enteric coating, sustain release, radioprotection, pH dependent release, colon targeting etc. Therefore polymethacrylates play a pivotal role in formulation and development of different type of dosage forms with versatile applications. Hence the objective of the present manuscript is to make a compilation review on research publications and patents on various applications of Eudragit. Polymethacrylates are known with various synonyms such as Acryl-EZE, Acryl-EZE MP, Eastacryl 30D; Eudragit; Kollicoat MAE 30 D; Kollicoat MAE 30 DP; polymeric methacrylates. This buy Wortmannin present review focused on various grades of Eudragit which is a trademark of GmbH & Co.K.G Darmastadt in Germany, first marketed in 1950s. polymerization of acrylic & methacrylic acids or their esters was adopted to obtain Eudragit e.g. butyl ester or dimethylaminoethyl ester. Chemical structure of Eudragit is shown in Fig. 1. Eudragit was included in USPNF, BP and PhEur. Dry powder polymer forms are stable at temperatures less than 30 °C. Dry powders are stable for at least 3 years if stored in a tightly closed container at less than 30 °C. Dispersions should be stored at temperatures between 5 and 25 °C and are stable for at least 18 months. Eudragits are generally regarded as nontoxic and nonirritant materials. A daily intake of 2 mg/kg body-weight in humans is regarded as essentially safe. It is included in the FDA Inactive Ingredients Guide (oral capsules and tablets), nonparenteral medicines licensed in the UK, Canadian list of acceptable nonmedicinal ingredients.
    Literature review
    Recent patents on eudragit based formulations Recent reviews on various patents published on Eudragit based formulation were collected. It was observed that Eudragit based formulation has been patented for diversified applications. They are used for colonic drug delivery, bitter taste masking, improved hardness, enhanced stability, improved bioavailability, prolonged drug release etc as shown in Table 9. Antoine et al. [97] prepared pectin beads cross linked with zinc or any divalent cation for colonic delivery of drugs. The beads were then coated with Eudragit- FS 30D, LE 30D and NE 30D. The use of zinc cations to crosslink the pectin is particularly preferred to provide a stable metallo-enzyme formulation for the lower intestinal or colonic delivery of such an enzyme. Choy et al. [98] patented hybrid of ursodeoxycholic acid-synthetic hydrotalcite-and Eudragit for bitter-taste-masking and improved body absorption rate with high solubility. Ursodeoxycholic acid is bitter in taste. The inventors found that a hybrid obtained by incorporating ursodeoxycholic acid between the layers of hydrotalcite, which is used as an antacid and a stomachic, and then coating with Eudragit, which is an enteric coating, blocks the bitter taste of ursodeoxycholic acid and simultaneously shows improvement of dissolution rate and high bioavailability. Shojaei et al. [99] patented on how the Eudragit L100-55 played a significant role in achieving desired hardness for tablets. The present invention relates to a pharmaceutical composition comprising a pharmaceutically active agent and a Eudragit L 100-55 which is useful to achieve the required release and desired compressibility. Tummala et al. [100] patented enhancement of bioavailability of the curcumin by complexing curcuminoid with Eudragit®. Chen et al. [101] prepared stable and sustain release solid dispersions of misoprostol with various grades of Eudragit RS series, Eudragit RL series, Eudragit S and Eudragit L. Periano [102] patented stable formulation of sennoside by granulation of senna extract (20% sennosides) with Eudragit L100 and then coated with Eudragit L 30 D 55. This product was stable for a long time and has good organoleptic properties (taste and odour). Christophe et al. [103] patented microgranules of ketoprofen using eudragit RL and RS for prolonged release. Aqueous dispersions of Eudragit RL and RS were used for the preparation of microgranules. Robert et al. [104] attempted to stabilize benzimidazole derivative proton pump inhibitors. The present invention provides a composition containing a benzimidazole derivative proton pump inhibitor and a polymeric base selected from the group consisting of cholestyramine-OH, Eudragit E-PO, chitosan, or a mixture thereof. The composition of the present innovation provides improved stability for the benzimidazole derivative proton pump inhibitor under naturally occurring humidity ranges so that degradation during storage and in the stomach is minimized. It can be easily manufactured by directly admixing the benzimidazole derivative proton pump inhibitor with the polymeric base.