{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,23]],"date-time":"2026-10-23T21:08:40Z","timestamp":1792789720754,"version":"4.5.0"},"reference-count":44,"publisher":"MDPI AG","issue":"19","license":[{"start":{"date-parts":[[2026,9,23]],"date-time":"2026-09-23T00:00:00Z","timestamp":1790121600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"National Research Foundation of Korea","award":["RS-2026-25474051"],"award-info":[{"award-number":["RS-2026-25474051"]}],"id":[{"id":"https:\/\/ror.org\/013aysd81","id-type":"ROR","asserted-by":"crossref"}]},{"award":["RS-2026-25474051"],"award-info":[{"award-number":["RS-2026-25474051"]}],"id":[{"id":"https:\/\/ror.org\/013aysd81","id-type":"ROR","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Tegoprazan (TPZ) is a promising potassium-competitive acid blocker, but its pH-dependent low solubility often leads to erratic oral absorption. Although several hydrophilic polymer-based amorphous solid dispersions have been attempted to enhance dissolution, they often suffer from thermodynamic instability or rely on complex, solvent-mediated manufacturing processes. Herein, to enhance dissolution and oral absorption, a crystalline drug-loaded melt granulation (MG) system using D-\u03b1-tocopheryl polyethylene glycol 1000 succinate (TPGS) was fabricated while maintaining stable physicochemical properties. MGs were prepared via a solvent-free, hot-melt process by optimizing the type of solid surfactant carrier, the ratio of drug to solid surfactant, and the type and ratio of flow-enhancing excipients. The optimized composition was TPZ:TPGS:microcrystalline cellulose = 1:2:4 (w\/w\/w). Solid-state analyses revealed that TPZ was uniformly dispersed within the granules while retaining its crystalline form. Compared to the raw drug, the MG showed remarkably faster and higher dissolution across both acidic and neutral media. Under long-term (25 \u00b0C\/60% RH) and accelerated storage conditions (40 \u00b0C\/75% RH) for 24 weeks, MG exhibited robust physicochemical stability, showing no drug degradation, changes in dissolution behavior, or crystalline alterations. Moreover, in a pharmacokinetic evaluation in Sprague\u2013Dawley rats, MG provided marked absorption enhancement, yielding over 1.8-fold increases in exposure compared to the raw material. Consequently, the crystalline drug-loaded TPGS-based MG represents a promising strategy for improving the oral delivery of TPZ.<\/jats:p>","DOI":"10.3390\/molecules31193382","type":"journal-article","created":{"date-parts":[[2026,9,23]],"date-time":"2026-09-23T10:17:26Z","timestamp":1790158646000},"page":"3382","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Enhanced Dissolution and Oral Bioavailability of Tegoprazan Using D-\u03b1-Tocopheryl Polyethylene Glycol 1000 Succinate-Based Melt Granulation System"],"prefix":"10.3390","volume":"31","author":[{"given":"Min Gyeong","family":"Jeong","sequence":"first","affiliation":[{"name":"College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 31116, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"},{"role":"conceptualization","vocabulary":"credit"},{"role":"investigation","vocabulary":"credit"},{"role":"writing-original-draft","vocabulary":"credit"}]},{"given":"Tae Hyoung","family":"Kim","sequence":"additional","affiliation":[{"name":"Department of MetaBioHealth, School of Medicine, Sungkyunkwan University, Suwon 16419, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"},{"role":"conceptualization","vocabulary":"credit"},{"role":"investigation","vocabulary":"credit"},{"role":"validation","vocabulary":"credit"},{"role":"data-curation","vocabulary":"credit"}]},{"ORCID":"https:\/\/orcid.org\/0009-0006-1868-8458","authenticated-orcid":false,"given":"In Gyu","family":"Yang","sequence":"additional","affiliation":[{"name":"Department of MetaBioHealth, School of Medicine, Sungkyunkwan University, Suwon 16419, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"},{"role":"investigation","vocabulary":"credit"},{"role":"validation","vocabulary":"credit"},{"role":"supervision","vocabulary":"credit"},{"role":"project-administration","vocabulary":"credit"}]},{"given":"Yeon Ju","family":"Baek","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 31116, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"},{"role":"methodology","vocabulary":"credit"},{"role":"data-curation","vocabulary":"credit"},{"role":"validation","vocabulary":"credit"},{"role":"formal-analysis","vocabulary":"credit"}]},{"given":"Min-Koo","family":"Choi","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 31116, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8878-2972","authenticated-orcid":false,"given":"Myung Joo","family":"Kang","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 31116, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"},{"role":"conceptualization","vocabulary":"credit"},{"role":"funding-acquisition","vocabulary":"credit"},{"role":"supervision","vocabulary":"credit"},{"role":"writing-review-editing","vocabulary":"credit"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4836-3551","authenticated-orcid":false,"given":"Ji Hoon","family":"Jeong","sequence":"additional","affiliation":[{"name":"Department of MetaBioHealth, School of Medicine, Sungkyunkwan University, Suwon 16419, Republic of Korea"},{"name":"School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea"}],"role":[{"vocabulary":"crossref","role":"author"},{"role":"writing-review-editing","vocabulary":"credit"},{"role":"investigation","vocabulary":"credit"},{"role":"validation","vocabulary":"credit"},{"role":"visualization","vocabulary":"credit"}]}],"member":"1968","published-online":{"date-parts":[[2026,9,23]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"751","DOI":"10.1111\/apt.15438","article-title":"Randomised clinical trial: Safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ-12420), a novel potassium-competitive acid blocker, in healthy male subjects","volume":"50","author":"Han","year":"2019","journal-title":"Aliment. 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