Pharmacodynamic comparison of two formulations of Acarbose 100-mg tablets

Lee, S.; Chung, Jae Yong; Hong, Kyoung Sup; Yang, Sihyung; Byun, S. Y.; Lim, Hyeong‐Seok; Shin, Sang Goo; Jang, In‐Jin; Yu, Kyung‐Sang

doi:10.1111/j.1365-2710.2012.01339.x

Cited by 18 publications

(40 citation statements)

References 9 publications

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“…However, given that tenapanor acts locally in the gut and has minimal systemic availability, it was not appropriate or possible to evaluate the effect of food on tenapanor activity based on pharmacokinetic parameters. Therefore, the effect of food intake had to be evaluated using pharmacodynamic parameters; a similar approach has been taken in clinical pharmacology studies of other agents that act in the gut . The need to use pharmacodynamic parameters rather than pharmacokinetic parameters has also been noted when testing the bioequivalence of drugs that are locally acting and have no or minimal systemic exposure .…”

Section: Discussionmentioning

confidence: 99%

Effect of Food Intake on the Pharmacodynamics of Tenapanor: A Phase 1 Study

Johansson

Knutsson

Leonsson-Zachrisson

et al. 2017

Clinical Pharm in Drug Dev

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Tenapanor (RDX5791/AZD1722) is a minimally systemic small‐molecule inhibitor of the sodium/hydrogen exchanger NHE3. Tenapanor acts in the gut to reduce absorption of sodium and phosphate. This phase 1 open‐label, 3‐way crossover study (NCT02226783) evaluated the effect of food on the pharmacodynamics of tenapanor. Eighteen volunteers completed a randomized sequence of three 4‐day treatments with tenapanor hydrochloride 15 mg twice daily: before food, after food, and while fasting. Participants received a diet standardized for sodium content. Stool sodium was significantly higher with tenapanor administration before versus after food (difference, +8.8 mmol/day, P = .006) or while fasting (+11.8 mmol/day, P = .0004). Differences in urinary sodium were not significant. Stool phosphorus was not significantly different with tenapanor before versus after food and significantly higher before food versus while fasting (+4.9 mmol/day, P = .006). Urinary phosphorus was significantly lower when tenapanor was administered before (−3.9 mmol/day, P = .0005) or after food (−3.7 mmol/day, P = .0009) versus while fasting. No serious adverse events were reported. These data suggest the effect of tenapanor on sodium absorption is most pronounced when administered before meals, whereas the effect on phosphate is similar whether administered before or after meals. This may support different timings of tenapanor administration with respect to food for sodium‐ and phosphate‐related indications.

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Section: Discussionmentioning

confidence: 99%

Effect of Food Intake on the Pharmacodynamics of Tenapanor: A Phase 1 Study

Johansson

Knutsson

Leonsson-Zachrisson

et al. 2017

Clinical Pharm in Drug Dev

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“…In addition, two studies of generic acarbose in Asian countries compared locally available generic versions with the brand name. Both were bioequivalence studies, although one found irregularities within the limits allowed by the Korean drug regulatory authority [38,39].…”

Section: Studies Of Non-fda-approved Generic Versionsmentioning

confidence: 97%

Modified Regulatory Pathways to Approve Generic Drugs in the US and a Systematic Review of Their Outcomes

Kesselheim

Fulchino

Isaman

et al. 2015

Drugs

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Pharmaceutical manufacturers sometimes raise scientific concerns related to potential generic versions of their drugs; however, in the six cases we reviewed, these companies did not follow up the pre-approval concerns they raised with any methodologically rigorous post-approval testing using clinical endpoints. Despite their pre-approval controversy, experience with these generic drugs provides reassurance of their clinical interchangeability. Systematized post-approval study of certain generic drug bioequivalence determinations is needed.

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“…Acarbose inhibits intestinal α-glycosidase, which decreases the digestion of ingested starch and disaccharides in the small intestine and reduces their oral absorption, resulting in decreased post-meal glucose levels (Lee et al 2012). PK endpoint method cannot be used to assess bioequivalence of acarbose tablet since its systemic exposure is negligible and the clinical efficacy is not correlated with its PK profile.…”

Section: Acarbose Tabletmentioning

confidence: 99%