The influence of gastric motility on the intraluminal behavior of fosamprenavir

Braeckmans, Marlies; Brouwers, Joachim; Masuy, Imke; Servais, Cécile; Tack, Jan; Augustijns, Patrick

doi:10.1016/j.ejps.2019.105117

Cited by 13 publications

(6 citation statements)

References 18 publications

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“…In a follow-up study, incomplete mixing was confirmed upon oral administration of paromomycin (250 mg tablet); gastric motility appeared to play a critical role in determining the degree to which the administered drug and the residual gastric volume mixed: the drug was more homogenously distributed in the stomach when it was administered during a period of gastric contractile activity (phase II of the MMC) as in the absence of gastric contractile activity (phase I of the MMC) 41 . Variability in PK caused by the cyclic motility pattern was confirmed with an immediate release tablet of fosamprenavir 42 . The intragastric disintegration of the tablet was faster and less variable after administration during phase II of the MMC, resulting in faster and less variable absorption of amprenavir.…”

Section: Discussionmentioning

confidence: 84%

An Assessment of Occasional Bio-Inequivalence for BCS1 and BCS3 Drugs: What are the Underlying Reasons?

Butler

Augustijns

2022

Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 84%

An Assessment of Occasional Bio-Inequivalence for BCS1 and BCS3 Drugs: What are the Underlying Reasons?

Butler

Augustijns

2022

Journal of Pharmaceutical Sciences

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“…The used high-resolution manometry catheters have 36 pressure sensors, enabling monitoring of regional pressure events. With this technique, a drug can be administered during a specific phase of the migrating motor complex-a cyclical pattern of GI contractile activity [31][32][33].…”

Section: Description Of the Methodsmentioning

confidence: 99%

Application of In Vivo Imaging Techniques and Diagnostic Tools in Oral Drug Delivery Research

et al. 2022

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Drug absorption following oral administration is determined by complex and dynamic interactions between gastrointestinal (GI) physiology, the drug, and its formulation. Since many of these interactions are not fully understood, the COST action on “Understanding Gastrointestinal Absorption-related Processes (UNGAP)” was initiated in 2017, with the aim to improve the current comprehension of intestinal drug absorption and foster future developments in this field. In this regard, in vivo techniques used for the characterization of human GI physiology and the intraluminal behavior of orally administered dosage forms in the GI tract are fundamental to gaining deeper mechanistic understanding of the interplay between human GI physiology and drug product performance. In this review, the potential applications, advantages, and limitations of the most important in vivo techniques relevant to oral biopharmaceutics are presented from the perspectives of different research fields.

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“…24,25 Another factor that influences systemic absorption is the time of tablet intake relative to the occurrence of gastric contractions. 26 When strong and frequent gastric contractions (migrating motor complex phase 3) onset shortly after the formulation reaches the stomach, sulindac might quickly transfer to the small intestine where improved dissolution and subsequent absorption is enabled (Fig. 1).…”

Section: Time-dependent Systemic and Caecal Disposition Of Sulindacmentioning

confidence: 99%

Insight into the Colonic Disposition of Sulindac in Humans

Lemmens

Brouwers

Snoeys

et al. 2021

Journal of Pharmaceutical Sciences

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NSAIDs such as celecoxib and sulindac play a critical role in the treatment of colorectal cancer, yet it is not understood how sufficiently high concentrations are reached in colonic tissue. We previously demonstrated that an incomplete small intestinal absorption of celecoxib enables gut driven drug accumulation in caecal tissue, which is most likely needed for inducing remission. However, a multistage dissolution experiment suggested a more extensive absorption of sulindac relative to celecoxib, though still incomplete. To study whether caecal accumulation of sulindac is solely plasma driven or also gut driven, we performed an exploratory clinical study in healthy volunteers. After intake of a tablet of sulindac (200 mg; Arthrocine), two colonoscopies (1.0e2.5 h, and 6.0e7.5 h after drug intake) were performed to assess concentrations of sulindac and metabolites in plasma, caecal tissue and caecal contents. We observed that sulindac, even without the use of a colon-targeted delivery strategy, can arrive at the colonic lumen due to incomplete absorption and biliary excretion, and that the microbiota can catalyse the production of sulindac sulfide, which then accumulates in a high and local manner in the colonic tissue. These data can be relevant for drug development in the treatment of colorectal adenomas and cancer.

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The influence of gastric motility on the intraluminal behavior of fosamprenavir

Cited by 13 publications

References 18 publications

An Assessment of Occasional Bio-Inequivalence for BCS1 and BCS3 Drugs: What are the Underlying Reasons?

An Assessment of Occasional Bio-Inequivalence for BCS1 and BCS3 Drugs: What are the Underlying Reasons?

Application of In Vivo Imaging Techniques and Diagnostic Tools in Oral Drug Delivery Research

Insight into the Colonic Disposition of Sulindac in Humans

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