Scintigraphic assessment of the intragastric distribution and gastric emptying of an encapsulated drug: the effect of feeding and of a proton pump inhibitor

Atherton, John C.; Washington, N.; Bracewell, Melanie A.; Sutton, Lee; Greaves, Jane; Perkins, Alan C.; Hawkey, Chris J.; Spiller, Robin C.

doi:10.1111/j.1365-2036.1994.tb00320.x

Cited by 18 publications

(4 citation statements)

References 10 publications

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“…It has also been suggested that bismuth be administered with meals to enhance it distribution throughout the stomach 59 83 84. The recent clinical trials in China have administered bismuth 30 min before meals.…”

Section: Understanding the Variation In Outcome With Triple Therapy Pmentioning

confidence: 99%

Role of bismuth in improvingHelicobacter pylorieradication with triple therapy

Dore

Lü

Graham

2016

Gut

214

248

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In most regions of the world, antimicrobial resistance has increased to the point where empirical standard triple therapy for Helicobacter pylorieradication is no longer recommended. The treatment outcome in a population is calculated as the sum of the treatment success in the subpopulation with susceptible infections plus treatment success in the subpopulation with resistant infections. The addition of bismuth (i.e., 14-day triple therapy plus bismuth) can improve cure rates despite a high prevalence of antimicrobial resistance. The major bismuth effect is to add an additional 30%-40% to the success with resistant infections. The overall result is therefore dependent on the prevalence of resistance and the treatment success in the subpopulation with resistant infections (eg, with proton-pump inhibitor-amoxicillin dual therapy). Here, we explore the contribution of each component and the mechanisms of how bismuth might enhance the effectiveness of triple therapy. We also discuss the limitations of this approach and provide suggestions how triple therapy plus bismuth might be further improved.

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Section: Understanding the Variation In Outcome With Triple Therapy Pmentioning

confidence: 99%

Role of bismuth in improvingHelicobacter pylorieradication with triple therapy

Dore

Lü

Graham

2016

Gut

214

248

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“…Moreover, in the above study, drugs were given on an empty stomach. Since a meal markedly prolongs gastric residence time of the drug and improves its intragastric distribution to the body and fundus [177], postprandial dosing seems a more suitable strategy for improving topical delivery and mixing (thanks to increased antral motility) of antimicrobials [177,178], provided that binding to or inactivation by food does not occur. An additional finding that would suggest postprandial dosing is that eating is associated with desquamation of gastric surface cells and discharge of mucus [179], possibly exposing the organisms to higher concentrations of the antimicrobial agent, or exposing a higher percentage of the organisms to it.…”

Section: Bowel Preparation For Colorectal Surgerymentioning

confidence: 99%

Rifaximin, a Poorly Absorbed Antibiotic: Pharmacology and Clinical Potential

2005

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Rifaximin (4-deoxy-4′-methylpyrido[1′,2′-1,2]imidazo- [5,4-c]-rifamycin SV) is a synthetic antibiotic designed to modify the parent compound, rifamycin, in order to achieve low gastrointestinal (GI) absorption while retaining good antibacterial activity. Both experimental and clinical pharmacology clearly show that this compound is a nonsystemic antibiotic with a broad spectrum of antibacterial action covering Gram-positive and Gram-negative organisms, both aerobes and anaerobes. Being virtually nonabsorbed, its bioavailability within the GI tract is rather high with intraluminal and fecal drug concentrations that largely exceed the minimal inhibitory concentration values observed in vitro against a wide range of pathogenic organisms. The GI tract represents, therefore, the primary therapeutic target and GI infections the main indication. The appreciation of the pathogenic role of gut bacteria in several organic and functional GI diseases has increasingly broadened its clinical use, which is now extended to hepatic encephalopathy, small intestine bacterial overgrowth, inflammatory bowel disease and colonic diverticular disease. Potential indications include the irritable bowel syndrome and chronic constipation, Clostridium difficile infection and bowel preparation before colorectal surgery. Because of its antibacterial activity against the microorganism and the lack of strains with primary resistance, some preliminary studies have explored the rifaximin potential for Helicobacter pylori eradication. Oral administration of this drug, by getting rid of enteric bacteria, could also be employed to achieve selective bowel decontamination in acute pancreatitis, liver cirrhosis (thus preventing spontaneous bacterial peritonitis) and nonsteroidal anti-inflammatory drug (NSAID) use (lessening in that way NSAID enteropathy). This antibiotic has, therefore, little value outside the enteric area and this will minimize both antimicrobial resistance and systemic adverse events. Indeed, the drug proved to be safe in all patient populations, including young children. Although rifaximin has stood the test of time, it still attracts the attention of both basic scientists and clinicians. As a matter of fact, with the advancement of the knowledge on microbial-gut interactions in health and disease novel indications and new drug regimens are being explored. Besides widening the clinical use, the research on rifaximin is also focused on the synthesis of new derivatives and on the development of original formulations designed to expand the spectrum of its clinical use.

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“…Moreover, in the above study, drugs were given on an empty stomach. Since a meal markedly prolongs drug gastric residence time and improves its intragastric distribution to the body and fundus [58], postprandial dosing seems a more suitable strategy for improving topical delivery and mixing (thanks to increased antral motility) of antimicrobials [58, 59], provided binding to or inactivation by food does not occur. An additional finding that would suggest postprandial dosing is that eating is associated with desquamation of gastric surface cells and discharge of mucus [60], possibly exposing the organisms to higher concentrations of the antimicrobial agent, or may expose a higher percentage of the organisms to it.…”

Section: In Vivo Helicobacter Pylori Eradication Trialsmentioning

confidence: 99%

Eradication of <i>Helicobacter pylori</i>: Are Rifaximin-Based Regimens Effective?

Gasbarrini

Pelosini

et al. 2006

Digestion

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Rifaximin is a non-absorbed semisynthetic rifamycin derivative with a broad spectrum of antibacterial activity including Gram-positive and Gram-negative bacteria, both aerobes and anaerobes. Although originally developed for the treatment of infectious diarrhea, the appreciation of the pathogenic role of gut bacteria in several organic and functional gastrointestinal diseases has increasingly broadened its clinical use. Being the antibiotic active against Helicobacter pylori, even towards clarithromycin-resistant strain, and being the primary resistance very rare, several investigations explored its potential use for eradication of the microorganism. Rifaximin alone proved to be effective, but even the highest dose (1,200 mg daily) gave a cure rate of only 30%. Dual and triple therapies were also studied, with the better results obtained with rifaximin-clarithromycin and rifaximin-clarithromycin-esomeprazole combinations. However, the eradication rates (60–70%) obtained with these regimens were still below the standard set by the Maastricht Consensus guidelines. Although rifaximin-based eradication therapies are promising, new antimicrobial combinations (with and without proton pump inhibitors) need to be explored in well-designed clinical trials including a large cohort of H. pylori-infected patients. The remarkable safety of rifaximin will allow high-dose regimens of longer duration (e.g. 10 or 14 days) to be tested with confidence in the hope of achieving better eradication rates. A drawback of rifaximin could be its inability to reach sufficiently high concentrations in the gastric mucus layer under and within which H. pylori is commonly located and this would likely affect eradication rate. Taking these considerations into account, bioadhesive rifaximin formulations able to better and persistently cover gastric mucosa, or combination with mucolytic agents, such as pronase or acetylcysteine, need to be evaluated in order to better define the place of this antibiotic in our therapeutic armamentarium.

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Scintigraphic assessment of the intragastric distribution and gastric emptying of an encapsulated drug: the effect of feeding and of a proton pump inhibitor

Cited by 18 publications

References 10 publications

Role of bismuth in improvingHelicobacter pylorieradication with triple therapy

Role of bismuth in improvingHelicobacter pylorieradication with triple therapy

Rifaximin, a Poorly Absorbed Antibiotic: Pharmacology and Clinical Potential

Eradication of <i>Helicobacter pylori</i>: Are Rifaximin-Based Regimens Effective?

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