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Development of a patient-centric formulation of tegoprazan, a novel potassium-competitive acid blocker, using modified-release drug-coated pellets

Authors
Lee, Su ChulKim, MyeongjoongKim, DonghyunJeon, Eun KyungLee, Eun Hee
Issue Date
9월-2022
Publisher
SPRINGERNATURE
Keywords
Drug-coated pellet; Modified release; Multiparticulate drug delivery system; Particle size; Tegoprazan
Citation
JOURNAL OF PHARMACEUTICAL INVESTIGATION, v.52, no.5, pp.623 - 638
Indexed
SCIE
SCOPUS
KCI
Journal Title
JOURNAL OF PHARMACEUTICAL INVESTIGATION
Volume
52
Number
5
Start Page
623
End Page
638
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/144089
DOI
10.1007/s40005-022-00582-y
ISSN
2093-5552
Abstract
Purpose The purpose of this study was to develop a patient-centric formulation of tegoprazan, a novel potassium-competitive acid blocker, using modified-release drug-coated pellets. Methods Tegoprazan tablets, sustained-release (SR) polymer-coated pellets, SR drug-coated pellets, enteric-coated (DR) pellets, SR polymer-coated pellets with an enteric coating (CR1), SR drug-coated pellets with an enteric coating (CR2), and tegoprazan immediate-release (IR) powder were prepared. Dual-release capsules were prepared by combining the IR powder with the CR1, CR2, and DR pellets (IR/CR1, IR/CR2, and IR/DR, respectively). In vitro dissolution tests were conducted to screen the formulations, and in vivo pharmacokinetic (PK) analysis was conducted using cynomolgus monkeys. Design of experiments was employed to optimize the formulation for the CR2 pellets. The effect of the particle size on the dissolution profile of the CR2 pellets was investigated using scanning electron microscopy. Results In vitro dissolution of the IR/CR1 capsule produced the desired pH- and time-dependent release profile, and in vivo PK analysis confirmed that drug absorption was well-controlled by this formulation. The IR/CR2 capsule exhibited a pH- and time-dependent release of tegoprazan that was similar to that of the IR/CR1 capsule. Small drug particles appeared to become embedded in the densely packed coating, thus dissolving more slowly than the medium and large drug particles. Conclusion Unlike the CR1 pellets, the CR2 pellets did not require an additional coating and curing process. The developed IR/CR2 capsule is also expected to prevent nocturnal acid breakthrough and thus improve patient compliance.
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약학대학 (약학과)
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