Abstract Sustained-release Formulation of Valsartan using the Wet Granulation and PVP with HPMC Jea Il Cho Department of a Polymer Nano Science & Technology Graduate School Chonbuk National University Part 1. Characterization and Controlled-release of Solid Dispersed Valsartan by Hydroxypropyl methy...
Abstract Sustained-release Formulation of Valsartan using the Wet Granulation and PVP with HPMC Jea Il Cho Department of a Polymer Nano Science & Technology Graduate School Chonbuk National University Part 1. Characterization and Controlled-release of Solid Dispersed Valsartan by Hydroxypropyl methylcellulose/Eudragit L100 Valsartan, a selective angiotensin Ⅱ type 1 receptor(AT1R) antagonist, has high bioavailability. We prepared sustained-release drug by using spray dry. This solid dispersion was formulated by using the improvement of dissolution using eudragit L100, HPMC as a carrier for the solid dispersion and poloxamer as a surfactant. Characteriztion of valsartan solid dispersion was analyzed by SEM, DSC, XRD and FT-IR. SEM was used to obseve the surface of valsartan and solid dispersion. DSC and XRD were used to analyze the amorphous of solid dispersions. FT-IR was used to analyze the salt formation by hydrogen bond between valsartan and complex polymer. The in vitro tests was carried out to find character of dissolution of valsartan solid dispersion in intestinal juice and controlled experiment was carried out to compare valsartan solid disperion with conventional drugs(DiovanⓇ). In this study, we selectived the characterize of dissolution and found the controlled release of valsartan solid dispersion as the orally pharmaceutical formulation prepared by spray drying. Part 2. Sustaind-release Formulation of Valsartan Tablets using PVP and HPMC Valsartan, a selective angiotensin ⅠⅠ type 1 receptor (AT1R) antagonist, has high bioavailability. However, valsartan can causeas headaches, dizziness and vomiting. It is require to reduce drug initial burst by release of valsartan. Gastrointestinal retentive formulation was prepared by hydroxypropyl methylcellulose(HPMC) and polyvinylpyrrolidone(PVP) with mass ratio. As a swollen polymer, HPMC is widely known as hydrophilic carrier for the fabrication of orally controlled drug delivery system. Valsartan tablets were prepared by direct compression method with various mass ratio of polymer. The swelling test was performed to observe the different swelling property with various mass ratio of HPMC and PVP. The in vitro carried out to confirm whether valsartan tablet is soluble in intestinal juice(pH 6.8), and controlled study was carried out to compare valsartan tablet with conventional drug(DiovanⓇTab 80 mg). Also, we conducted in vitro test in order to confirm the controlled release of valsartan tablet with swelling properties of polymer. Accordingly, it is expected that the contact between tablet and simulated intestinal juice(pH 6.8) caused increase of retentive time and volume of tablets in stomach due to swelling of tablets. This studies showed sustained-release of valsartan tablet by swelling polymer, valsartan as orally pharmaceutical sustained-release formulation. Keywords : Solid dispersion, Valsartan, spray drying, controlled release, Diovan??, Swelling, Sustained-release Student ID Number : 200950609
Abstract Sustained-release Formulation of Valsartan using the Wet Granulation and PVP with HPMC Jea Il Cho Department of a Polymer Nano Science & Technology Graduate School Chonbuk National University Part 1. Characterization and Controlled-release of Solid Dispersed Valsartan by Hydroxypropyl methylcellulose/Eudragit L100 Valsartan, a selective angiotensin Ⅱ type 1 receptor(AT1R) antagonist, has high bioavailability. We prepared sustained-release drug by using spray dry. This solid dispersion was formulated by using the improvement of dissolution using eudragit L100, HPMC as a carrier for the solid dispersion and poloxamer as a surfactant. Characteriztion of valsartan solid dispersion was analyzed by SEM, DSC, XRD and FT-IR. SEM was used to obseve the surface of valsartan and solid dispersion. DSC and XRD were used to analyze the amorphous of solid dispersions. FT-IR was used to analyze the salt formation by hydrogen bond between valsartan and complex polymer. The in vitro tests was carried out to find character of dissolution of valsartan solid dispersion in intestinal juice and controlled experiment was carried out to compare valsartan solid disperion with conventional drugs(DiovanⓇ). In this study, we selectived the characterize of dissolution and found the controlled release of valsartan solid dispersion as the orally pharmaceutical formulation prepared by spray drying. Part 2. Sustaind-release Formulation of Valsartan Tablets using PVP and HPMC Valsartan, a selective angiotensin ⅠⅠ type 1 receptor (AT1R) antagonist, has high bioavailability. However, valsartan can causeas headaches, dizziness and vomiting. It is require to reduce drug initial burst by release of valsartan. Gastrointestinal retentive formulation was prepared by hydroxypropyl methylcellulose(HPMC) and polyvinylpyrrolidone(PVP) with mass ratio. As a swollen polymer, HPMC is widely known as hydrophilic carrier for the fabrication of orally controlled drug delivery system. Valsartan tablets were prepared by direct compression method with various mass ratio of polymer. The swelling test was performed to observe the different swelling property with various mass ratio of HPMC and PVP. The in vitro carried out to confirm whether valsartan tablet is soluble in intestinal juice(pH 6.8), and controlled study was carried out to compare valsartan tablet with conventional drug(DiovanⓇTab 80 mg). Also, we conducted in vitro test in order to confirm the controlled release of valsartan tablet with swelling properties of polymer. Accordingly, it is expected that the contact between tablet and simulated intestinal juice(pH 6.8) caused increase of retentive time and volume of tablets in stomach due to swelling of tablets. This studies showed sustained-release of valsartan tablet by swelling polymer, valsartan as orally pharmaceutical sustained-release formulation. Keywords : Solid dispersion, Valsartan, spray drying, controlled release, Diovan??, Swelling, Sustained-release Student ID Number : 200950609
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