{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,12,17]],"date-time":"2025-12-17T08:55:28Z","timestamp":1765961728907,"version":"build-2065373602"},"reference-count":57,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2023,11,30]],"date-time":"2023-11-30T00:00:00Z","timestamp":1701302400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Basic Science Research Program through the National Research Foundation of Korea","award":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"],"award-info":[{"award-number":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"]}]},{"name":"National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT)","award":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"],"award-info":[{"award-number":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"]}]},{"DOI":"10.13039\/501100003052","name":"Technology Innovation Program","doi-asserted-by":"publisher","award":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"],"award-info":[{"award-number":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"]}],"id":[{"id":"10.13039\/501100003052","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Ministry of Trade, Industry and Energy (MOTIE, Korea)","award":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"],"award-info":[{"award-number":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"]}]},{"name":"BUSAN TECHNO PARK grant funded by the Busan Metropolitan City","award":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"],"award-info":[{"award-number":["2016R1A6A1A03007648","2022R1C1C1010130","RS-2023-00234996"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>In this study, an amorphous solid dispersion containing the poorly water-soluble drug, bisacodyl, was prepared by hot-melt extrusion to enhance its therapeutic efficacy. First, the miscibility and interaction between the drug and polymer were investigated as pre-formulation strategies using various analytical approaches to obtain information for selecting a suitable polymer. Based on the calculation of the Hansen solubility parameter and the identification of the single glass transition temperature (Tg), the miscibility between bisacodyl and all the investigated polymers was confirmed. Additionally, the drug\u2013polymer molecular interaction was identified based on the comprehensive results of dynamic vapor sorption (DVS), Fourier transform infrared spectroscopy (FT-IR), Raman spectroscopy, and a comparison of the predicted and experimental values of Tg. In particular, the hydroxypropyl methylcellulose (HPMC)-based solid dispersions, which exhibited large deviation between the calculated and experimental values of Tg and superior physical stability after DVS experiments, were selected as the most appropriate solubilized bisacodyl formulations due to the excellent inhibitory effects on precipitation based on the results of the non-sink dissolution test. Furthermore, it was shown that the enteric-coated tablets containing HPMC\u2013bisacodyl at a 1:4 ratio (w\/w) had significantly improved in vivo therapeutic laxative efficacy compared to preparations containing un-solubilized raw bisacodyl in constipation-induced rabbits. Therefore, it was concluded that the pre-formulation strategy, using several analyses and approaches, was successfully applied in this study to investigate the miscibility and interaction of drug\u2013polymer systems, hence resulting in the manufacture of favorable solid dispersions with favorable in vitro and in vivo performances using hot-melt extrusion processes.<\/jats:p>","DOI":"10.3390\/pharmaceutics15122704","type":"journal-article","created":{"date-parts":[[2023,11,30]],"date-time":"2023-11-30T09:37:54Z","timestamp":1701337074000},"page":"2704","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":8,"title":["Preparation of Hot-Melt-Extruded Solid Dispersion Based on Pre-Formulation Strategies and Its Enhanced Therapeutic Efficacy"],"prefix":"10.3390","volume":"15","author":[{"given":"Seon-Kwang","family":"Lee","sequence":"first","affiliation":[{"name":"College of Pharmacy, Pusan National University, 63 Busandaehak-ro, Geumjeong-gu, Busan 46241, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eun-Sol","family":"Ha","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, 63 Busandaehak-ro, Geumjeong-gu, Busan 46241, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Heejun","family":"Park","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Duksung Women\u2019s University, 33, Samyangro 144-gil, Dobong-gu, Seoul 01369, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5163-0262","authenticated-orcid":false,"given":"Kyu-Tae","family":"Kang","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Duksung Women\u2019s University, 33, Samyangro 144-gil, Dobong-gu, Seoul 01369, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ji-Su","family":"Jeong","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, 63 Busandaehak-ro, Geumjeong-gu, Busan 46241, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jeong-Soo","family":"Kim","sequence":"additional","affiliation":[{"name":"Dong-A ST Co., Ltd., Giheung-gu, Yongin 17073, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9538-0565","authenticated-orcid":false,"given":"In-hwan","family":"Baek","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Kyungsung University, 309, Suyeong-ro, Nam-gu, Busan 48434, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Min-Soo","family":"Kim","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Pusan National University, 63 Busandaehak-ro, Geumjeong-gu, Busan 46241, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2023,11,30]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"641","DOI":"10.1007\/s40005-015-0218-8","article-title":"Enhancement of dissolution and bioavailability of ezetimibe by amorphous solid dispersion nanoparticles fabricated using supercritical antisolvent process","volume":"45","author":"Ha","year":"2015","journal-title":"J. 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