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Extended release delivery system of metoprolol succinate using hot-melt extrusion: effect of release modifier on methacrylic acid copolymer.
Drug Deliv Transl Res. 2018 12; 8(6):1679-1693.DD

Abstract

The current study reports on the manufacturing of extended release dosage forms of metoprolol succinate via hot-melt extrusion (HME) technology. Either Eudragit®S100 and Eudragit®L100 alone or in combination with release modifying agent Polyox™ WSR 303 and Eudragit®L100-55 were processed to obtain complete and faster release. Metoprolol succinate with similar solubility parameters to polymer was dispersed in polymer matrix and was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscopy (SEM). Stability of drug after extrusion was confirmed by thermogravimetric analysis and high-performance liquid chromatography. Physical characterization method exhibited that the drug was homogeneously dispersed in non-crystalline state in Eudragit®L100-55-based formulations whereas in semi-crystalline state in Polyox™ WSR 303. The drug release percentage was below 3 and 40% in 0.1 N HCL with Eudragit®L100-55- and Polyox™ WSR 303-containing formulations, respectively, and exhibited pH-dependent dissolution properties. The drug-release mechanism was anomalous with Polyox™ WSR 303 formulations whereas diffusion through pore formation was obtained with Eudragit®L100-55. Both Eudragit®L100-55 and Polyox™ WSR 303 changed the release mechanism and kinetics of drug release from thermally processed dosage forms. The optimized stable formulation is similar to the marketed formulation with F2 value of 72.36. Thus, it can be concluded that HME was exploited as an effective process for the preparation of controlled release matrix system based on pH-dependent polymer matrices Eudragit®S100 and Eudragit®L100.

Authors+Show Affiliations

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathelal Parekh Marg, Matunga (East), Mumbai, Maharashtra, 400019, India. sawant.uict@gmail.com.Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathelal Parekh Marg, Matunga (East), Mumbai, Maharashtra, 400019, India. Faculty of Pharmaceutics Department, H.K. College of Pharmacy, Relief Road, Oshiwara, Jogeshwari West, Mumbai, Maharashtra, 400102, India.Department of Pharmacy (Chemistry), School of Life Sciences, University of Sussex, Falmer-Brighton, BN1 9QJ, UK.Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathelal Parekh Marg, Matunga (East), Mumbai, Maharashtra, 400019, India.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

29948916

Citation

Sawant, Kiran P., et al. "Extended Release Delivery System of Metoprolol Succinate Using Hot-melt Extrusion: Effect of Release Modifier On Methacrylic Acid Copolymer." Drug Delivery and Translational Research, vol. 8, no. 6, 2018, pp. 1679-1693.
Sawant KP, Fule R, Maniruzzaman M, et al. Extended release delivery system of metoprolol succinate using hot-melt extrusion: effect of release modifier on methacrylic acid copolymer. Drug Deliv Transl Res. 2018;8(6):1679-1693.
Sawant, K. P., Fule, R., Maniruzzaman, M., & Amin, P. D. (2018). Extended release delivery system of metoprolol succinate using hot-melt extrusion: effect of release modifier on methacrylic acid copolymer. Drug Delivery and Translational Research, 8(6), 1679-1693. https://doi.org/10.1007/s13346-018-0545-1
Sawant KP, et al. Extended Release Delivery System of Metoprolol Succinate Using Hot-melt Extrusion: Effect of Release Modifier On Methacrylic Acid Copolymer. Drug Deliv Transl Res. 2018;8(6):1679-1693. PubMed PMID: 29948916.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Extended release delivery system of metoprolol succinate using hot-melt extrusion: effect of release modifier on methacrylic acid copolymer. AU - Sawant,Kiran P, AU - Fule,Ritesh, AU - Maniruzzaman,Mohammed, AU - Amin,Purnima D, PY - 2018/6/28/pubmed PY - 2019/6/14/medline PY - 2018/6/28/entrez KW - Eudragit®L100 KW - Eudragit®L100-55 KW - Eudragit®S100 KW - Extended release KW - Hot-melt extrusion KW - Metoprolol succinate KW - Polyox™ WSR 303 KW - Release-modifying agent SP - 1679 EP - 1693 JF - Drug delivery and translational research JO - Drug Deliv Transl Res VL - 8 IS - 6 N2 - The current study reports on the manufacturing of extended release dosage forms of metoprolol succinate via hot-melt extrusion (HME) technology. Either Eudragit®S100 and Eudragit®L100 alone or in combination with release modifying agent Polyox™ WSR 303 and Eudragit®L100-55 were processed to obtain complete and faster release. Metoprolol succinate with similar solubility parameters to polymer was dispersed in polymer matrix and was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscopy (SEM). Stability of drug after extrusion was confirmed by thermogravimetric analysis and high-performance liquid chromatography. Physical characterization method exhibited that the drug was homogeneously dispersed in non-crystalline state in Eudragit®L100-55-based formulations whereas in semi-crystalline state in Polyox™ WSR 303. The drug release percentage was below 3 and 40% in 0.1 N HCL with Eudragit®L100-55- and Polyox™ WSR 303-containing formulations, respectively, and exhibited pH-dependent dissolution properties. The drug-release mechanism was anomalous with Polyox™ WSR 303 formulations whereas diffusion through pore formation was obtained with Eudragit®L100-55. Both Eudragit®L100-55 and Polyox™ WSR 303 changed the release mechanism and kinetics of drug release from thermally processed dosage forms. The optimized stable formulation is similar to the marketed formulation with F2 value of 72.36. Thus, it can be concluded that HME was exploited as an effective process for the preparation of controlled release matrix system based on pH-dependent polymer matrices Eudragit®S100 and Eudragit®L100. SN - 2190-3948 UR - https://www.unboundmedicine.com/medline/citation/29948916/Extended_release_delivery_system_of_metoprolol_succinate_using_hot_melt_extrusion:_effect_of_release_modifier_on_methacrylic_acid_copolymer_ DB - PRIME DP - Unbound Medicine ER -