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

Lee, Su Chul; Kim, Myeongjoong; Kim, Dong-Hyun; Jeon, Eun-Ju; Lee, Eun Hee

doi:10.1007/s40005-022-00582-y

Cited by 2 publications

(5 citation statements)

References 36 publications

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“…25 This was also observed in the in vitro dissolution profile. 25 It is therefore necessary to evaluate the optimal IR and DR ratio for developing a novel MR formulation.…”

supporting

confidence: 52%

“…Furthermore, dexlansoprazole MR 30 mg is effective in treating symptomatic GERD in patients with moderate‐to‐very severe nocturnal heartburn 31 . However, despite these formulation modifications, certain limitations of PPIs remain to be addressed, including the slow onset of action attributable to the specific mechanism of action, which necessitate acid activation 25 . In addition, even high doses of dexlansoprazole MR fail to provide adequate control of night‐time pH > 4, which needs to be improved 32 .…”

Section: Discussionmentioning

confidence: 99%

“…31 However, despite these formulation modifications, certain limitations of PPIs remain to be addressed, including the slow onset of action attributable to the specific mechanism of action, which necessitate acid activation. 25 In addition, even high doses of dexlansoprazole MR fail to provide adequate control of night-time pH > 4, which needs to be improved. 32 It is consequently anticipated that tegoprazan can overcome the current limitations of modified PPIs, whilst conferring similar benefits based on a dual-release MR formulation consisting of a combination of IR and DR formulations.…”

Section: Discussionmentioning

confidence: 99%

“…Thus, a tegoprazan DR formulation was developed as an enteric‐coated pellet that releases active pharmaceutical ingredients in a pH‐dependent manner. In a preclinical study using cynomolgus monkeys, following the co‐administration of tegoprazan IR and DR, the drug plasma concentration reached a plateau after the initial dissolution of tegoprazan IR powder, and then slowly declined compared with the administration of tegoprazan IR alone 25 . This was also observed in the in vitro dissolution profile 25 .…”

Section: Introductionmentioning

confidence: 90%

“…In a preclinical study using cynomolgus monkeys, following the co‐administration of tegoprazan IR and DR, the drug plasma concentration reached a plateau after the initial dissolution of tegoprazan IR powder, and then slowly declined compared with the administration of tegoprazan IR alone 25 . This was also observed in the in vitro dissolution profile 25 . It is therefore necessary to evaluate the optimal IR and DR ratio for developing a novel MR formulation.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetic and pharmacodynamic exploration of various combinations of tegoprazan immediate and delayed‐release formulations

Park

Yang

Kim

et al. 2023

Brit J Clinical Pharma

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AimsThe new modified‐release formulation of tegoprazan, a novel potassium‐competitive acid blocker, is expected to improve the management of acid‐related disease, including nocturnal acid breakthrough, by prolonging the duration of acid suppression. This study aimed to explore the pharmacokinetics (PK) and pharmacodynamics (PD) of various combinations of tegoprazan with immediate‐release (IR) and delayed‐release (DR) formulations.MethodsA three‐cohort, open‐label, randomized, single‐dose, three‐treatment, six‐sequence, three‐period crossover study was conducted. Various combinations of tegoprazan IR and DR formulations (50, 75 or 100 mg) were administered orally once per period. The 24‐h intragastric pH was monitored before and after each administration. PK blood samples were collected for up to 48 h. PK and PD were compared among treatments.ResultsEighteen healthy Korean subjects completed the study. All treatment groups showed intragastric pH above 4 approximately 1 h following tegoprazan administration. Among the various combinations, the IR and DR combination at a 1:1 ratio induced greater gastric acid suppression (%Time pH ≥ 4) than IR alone in each dose group, both for 24 h (50 mg; 59% vs. 52%, P = .2188, 95% confidence interval [CI] −6.92–22.27, 100 mg; 85% vs. 70%, P < .05, 95% CI 8.92–22.19) and at night (50 mg; 27% vs. 16%, P = .1563, 95% CI −11.79–37.71, 100 mg; 77% vs. 49%, P < .05, 95% CI 16.14–42.98), with similar systemic exposure.ConclusionsThe combinatorial tegoprazan in the IR and DR 1:1 ratio formulation was found to induce stronger gastric acid suppression throughout the day and at night, compared to the conventional IR formulation.

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“…25 This was also observed in the in vitro dissolution profile. 25 It is therefore necessary to evaluate the optimal IR and DR ratio for developing a novel MR formulation.…”

supporting

confidence: 52%