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Intragastric pH

Jari Rubbens, Joachim Brouwers, Jan Tack, Patrick Augustijns
This study investigated the impact of relevant gastrointestinal conditions on the intraluminal dissolution, supersaturation and precipitation behavior of the weakly basic drug indinavir. The influence of (i) concomitant PPI intake and (ii) the nutritional state on the gastrointestinal behavior of indinavir was assessed in order to identify the underlying mechanisms responsible for previously reported interactions. Five healthy volunteers were recruited into a cross-over study containing the following arms: fasted state, fed state and fasted state with concomitant proton pump inhibitor (PPI) use...
September 28, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Hisatsugu Noda, Seiji Noguchi, Takashi Yoshimine, Shigeki Goji, Kazunori Adachi, Yasuhiro Tamura, Shinya Izawa, Masahide Ebi, Sayuri Yamamoto, Naotaka Ogasawara, Yasushi Funaki, Makoto Sasaki, Kunio Kasugai
BACKGROUND AND AIMS: In Japan, 7-day triple therapy for Helicobacter pylori including clarithromycin (CAM) was approved in 2000. However, antibiotic resistance subsequently reduced this rate to an unacceptable level (70%). Vonoprazan, an orally bioavailable potassium-competitive acid blocker (P-CAB), was approved in Japan in 2014. This could improve eradication rates by increasing the intragastric pH, thus increasing bacterial antibiotic susceptibility. This study compared the efficacy of 7-day triple therapies that included CAM and vonoprazan or proton pump inhibitor (PPI)...
September 2016: Journal of Gastrointestinal and Liver Diseases: JGLD
David R Mitchell, Mohammad H Derakhshan, Angela A Wirz, Clare Orange, Stuart A Ballantyne, James J Going, Kenneth E L McColl
OBJECTIVE: Gastric acid secretory capacity in different anatomical regions, including the postprandial acid pocket, was assessed in Helicobacter pylori positive and negative volunteers in a Western population. DESIGN: We studied 31 H. pylori positive and 28 H. pylori negative volunteers, matched for age, gender and body mass index. Jumbo biopsies were taken at 11 predetermined locations from the gastro-oesophageal junction and stomach. Combined high-resolution pH metry (12 sensors) and manometry (36 sensors) was performed for 20 min fasted and 90 min postprandially...
September 23, 2016: Gut
Felix Schneider, Michael Grimm, Mirko Koziolek, Christiane Modeß, Anne Dokter, Tarek Roustom, Werner Siegmund, Werner Weitschies
In the present study temperature, pH and pressure profiles of nine healthy human volunteers were investigated after ingestion of the SmartPill® under conditions simulating the fasted state treatment in bioavailability and bioequivalence studies. In a previously published study the same subjects received the SmartPill® under fed conditions as recommended by the FDA. Since large non-digestible objects are mainly emptied during phase III of the interdigestive migrating motor complex, the gastric residence time of the SmartPill® was found to be clearly shorter under fasting conditions...
September 14, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Morten Würtz, Erik L Grove
Aspirin and P2Y12 receptor antagonists are widely used across the spectrum of cardiovascular diseases. Upper gastrointestinal complications, including ulcer and bleeding, are relatively common during antiplatelet treatment and, therefore, concomitant proton pump inhibitor (PPI) treatment is often prescribed.PPIs provide gastroprotection by changing the intragastric milieu, essentially by raising intragastric pH. In recent years, it has been heavily discussed whether PPIs may reduce the cardiovascular protection by aspirin and, even more so, clopidogrel...
September 15, 2016: Advances in Experimental Medicine and Biology
Adam Chwiesko, Radoslaw Charkiewicz, Jacek Niklinski, Wojciech Luczaj, Elzbieta Skrzydlewska, Robert Milewski, Andrzej Baniukiewicz, Eugeniusz Wroblewski, Mariusz Rosolowski, Andrzej Dabrowski
AIM: We aimed to identify the best method of omeprazole (OME) application with respect to intragastric pH, cytochrome CYP2C19 genotype and phenotype. METHODS: Fifty patients with NVUGIB were prospectively enrolled, after achievement of endoscopic hemostasis, were randomized to 40-mg IV OME bolus injection bid or 80-mg IV bolus injection + 8-mg/h continuous IV infusion for 72 hours. The intragastric pH was recorded for 72 hours. The CYP2C19 variant alleles (*2, *3, *17) were analysed, the serum concentrations of OME and 5-hydroxy-OME were determined...
August 12, 2016: Journal of Digestive Diseases
Vijayalakshmi S Pratha, Thomas McGraw, William Tobin
Proton pump inhibitors (PPIs) effectively block gastric acid secretion and are the treatment of choice for heartburn. PPIs differ, however, in onset of action and bioavailability. In this single-center, open-label, three-way crossover study, onset of action of immediate-release omeprazole 20 mg/sodium bicarbonate 1100 mg (IR-OME) and delayed-release (DR) lansoprazole 15 mg was evaluated in 63 healthy fasting adults. Subjects were randomized to once daily IR-OME, or DR-lansoprazole, or no treatment for 7 days...
June 2016: Pharmacology Research & Perspectives
Yan Tang, Yingtao Wu, Ziyi Huang, Weiwei Dong, Ying Deng, Fengjiao Wang, Ming Li, Jieli Yuan
OBJECTIVE: The use of probiotics to alleviate chemotherapy-induced intestinal mucositis is supported by clinical consensus. However, no studies to date, to our knowledge, have systematically analyzed the effects of a probiotic mixture on chemotherapy-induced mucositis or assessed changes in the intestinal microbiota after probiotic treatment. The aim of this study was to report the effects of a probiotic mixture, DM#1, on intestinal mucositis and dysbiosis of rats treated with 5-fluorouracil (5-FU)...
May 20, 2016: Nutrition
WonGun Kwack, YunJeong Lim, ChiYeon Lim, David Y Graham
Objective. The eradication rate of Helicobacter pylori (H. pylori) following standard triple therapy has declined over the past few decades. This study has determined whether high dose dual therapy (PPI and amoxicillin) is adequate for eradicating H. pylori in Korea. Methods. This was an open-labeled study of H. pylori infected treatment-naive patients. Subjects received dual therapy for 14 days: ilaprazole 40 mg tablets given twice a day and amoxicillin 750 mg tablets given 4 times a day. At the end of the therapy, the subjects visited the clinic to confirm compliance and monitor for any side effects...
2016: Gastroenterology Research and Practice
Li-Sheng Li, Yun-Mei Luo, Juan Liu, Yu Zhang, Xiao-Xia Fu, Dan-Li Yang
It has been reported that icariin (ICA) increased contents of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) by improving expression of endothelial nitric oxide synthase (eNOS) and inhibition of phosphodiesterase type 5 (PDE5). In addition, dysfunction of the NO/cGMP pathway may play a crucial role in the pathogenesis of pulmonary hypertension (PH). In this study, the potential protective effects of ICA on PH induced by monocrotaline (MCT, 50 mg/kg) singly subcutaneous injection were investigated and the possible mechanisms involved in NO/cGMP pathway were explored in male Sprague Dawley rats...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
A Ormeci, Z Emrence, B Baran, O M Soyer, S Gokturk, S Evirgen, F Akyuz, C Karaca, F Besisik, S Kaymakoglu, D Ustek, K Demir
Proton pump inhibitors (PPI) metabolism and pharmacokinetics are regulated by cytochrome P450 enzymes in the liver. Cytochrome P450 2C19 (CYP2C19) polymorphism plays an import role in the metabolism of PPIs. The three possible genotypes for CYP2C19 each has a distinct effect on the pharmacodynamics of PPIs. Homozygote extensive metabolizers (HomEM) are the most frequent genotype and have two wild-types (non-mutant) (*1/*1) alleles. HomEM is associated with increased enzyme activity, which increases the rate of PPI metabolism...
May 2016: European Review for Medical and Pharmacological Sciences
N F Rinsma, F A Mauritz, L W E van Heurn, C E J Sloots, P D Siersema, R H J Houwen, D C van der Zee, A A M Masclee, J M Conchillo, M Y A Van Herwaarden-Lindeboom
BACKGROUND: Laparoscopic antireflux surgery (LARS) is a well-established treatment option for children with proton pomp inhibitor (PPI)-resistant gastroesophageal reflux disease (GERD). Besides preventing reflux of gastric fluid and solid content, LARS may also impair the ability of the stomach to vent intragastric air (i.e. gastric belching) and induce gas-related complications, such as bloating and/or hyperflatulence. Furthermore, it was previously hypothesized that LARS induces a behavioral type of belching, not originating from the stomach, called supragastric belching...
October 2016: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
Arumugam Ramamoorthy Vijayakumar, Epison Prabu Daniel, Raju Ilavarasan, S Venkataraman, S Vijayakumar
BACKGROUND: Several synthetic drugs are useful in the treatment of peptic ulcer, but almost of these drugs are used in prolonging time, it may cause several adverse reactions. However, the herbal medicines are more potent to the treatment and minimize the side effects. OBJECTIVE: To evaluate the methanol extract of Jatropha gossypiifolia Linn. (MEJG) for gastro protective activity against Wistar rats. MATERIALS AND METHODS: Anti-ulcer potency of MEJG (100 and 200 mg/kg, b...
March 2016: Pharmacognosy Research
Hongyun Wang, Liwei Lang, Ning Ou, Ruihua Shi, Haitang Hu, Pei Hu, Ji Jiang
BACKGROUND AND OBJECTIVES: Ilaprazole is a novel proton pump inhibitor that provides effective and long lasting inhibition of intragastric acid secretion. The objectives of this study were to investigate the pharmacokinetics, pharmacodynamics, and safety of intravenous ilaprazole after multiple administrations in healthy Chinese subjects. METHODS: This was an open-label and multiple-dose clinical study. Ten healthy Chinese subjects received 10 mg ilaprazole infusion once daily for 5 days...
June 2016: Clinical Drug Investigation
E Gould, C Clements, A Reed, L Giori, J M Steiner, J A Lidbury, J S Suchodolski, M Brand, T Moyers, L Emery, M K Tolbert
BACKGROUND: Chronic proton pump inhibitor administration has been associated with electrolyte and cobalamin deficiency, disrupted bone homeostasis, hypergastrinemia, and rebound acid hypersecretion in humans. It is unknown if this occurs in cats. OBJECTIVES: Prolonged oral omeprazole results in altered bone mineral density or content, serum calcium, magnesium, cobalamin, and gastrin concentrations in healthy cats. ANIMALS: Six healthy adult DSH cats...
May 2016: Journal of Veterinary Internal Medicine
G S Dzhulay, E V Sekareva
AIM: To estimate esophageal and gastric pH values on an empty stomach and after stimulation of gastric secretion and gastric and duodenal motor-evacuatory activity in patients with gastroesophageal reflux disease (GERD) associated with pathological refluxes, such as gastroesophageal reflux (GER) and duodenogastroesophageal reflux (DGER). SUBJECTS AND METHODS: The observational cross-sectional study was conducted to investigate and compare the parameters of intraesophageal and intragastric pH metry and peripheral electrogastroenterography in 103 GERD patients with endoscopically positive distal reflux esophagitis in GER and DGER...
2016: Terapevticheskiĭ Arkhiv
Hongyun Wang, Ning Ou, Liwei Lang, Ruihua Shi, Pei Hu, Ji Jiang
1. Ilaprazole is a novel proton pump inhibitor and this is the first study to investigate the pharmacokinetics, pharmacodynamics and safety of intravenous ilaprazole in healthy volunteers. 2. In this open-label, single-dose, randomized and four-period crossover study, 16 healthy Chinese subjects received ilaprazole 5, 10 or 20 mg intravenously, or 10 mg orally. Serial blood and urine samples were collected and intragastric pH was recorded within 24 h. The percentage time of intragastric pH > 6 was the major index...
March 21, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
T Kagami, S Sahara, H Ichikawa, T Uotani, M Yamade, M Sugimoto, Y Hamaya, M Iwaizumi, S Osawa, K Sugimoto, H Miyajima, T Furuta
BACKGROUND: Acid inhibitory effects of proton pump inhibitors (PPIs) are influenced by CYP2C19 genotype. In contrast, the potent acid inhibition of vonoprazan is not influenced by CYP2C19 genotype. AIM: To compare the acid inhibitory effects of vonoprazan and esomeprazole in relation to CYP2C19 genotype. METHODS: Twenty-eight healthy Japanese volunteers [7 CYP2C19 poor metabolisers (PMs), 11 intermediate metabolisers (IMs) and 10 rapid metabolisers (RMs)] received four different regimens in a randomised crossover manner: (i) vonoprazan 20 mg twice daily (b...
May 2016: Alimentary Pharmacology & Therapeutics
Huayi Suo, Xin Zhao, Yu Qian, Peng Sun, Kai Zhu, Jian Li, Baozhong Sun
The purpose of the study was to determine the inhibitory effects of Lactobacillus fermentum Suo (LF-Suo) on HCl/ethanol induced gastric injury in ICR (Institute for Cancer Research) mice and explain the mechanism of these effects through the molecular biology activities of LF-Suo. The studied mice were divided into four groups: healthy, injured, LF-Suo-L and LF-Suo-H group. After the LF-Suo intragastric administration, the gastric injury area was reduced compared to the injured group. The serum MOT (motilin), SP (substance P), ET (endothelin) levels of LF-Suo treated mice were lower, and SS (somatostatin), VIP (vasoactive intestinal peptide) levels were higher than the injured group mice...
March 2016: Nutrients
Christos Soukoulis, Ian D Fisk, Torsten Bohn, Lucien Hoffmann
In the present work, the intragastric structuring ability of o/w emulsions either stabilised (1-4%, w/w of sodium alginate (SA)) or structured with sheared ionic gel (1-3%, w/w of SA crosslinked with Ca(2+)) in the absence (saliva and gastric phases constituted of deionised water) or presence of in vitro pre-absorptive conditions (physiological simulated saliva and gastric fluids) was investigated. Visualisation of the morphological aspects of the gastric chymes, in the absence of multivalent counterions, demonstrated that SA stabilised systems underwent a remarkable swelling in the pH range of 2-3, whilst at the same pH range, ionic SA gel structured systems maintained their major structure configuration...
April 20, 2016: Carbohydrate Polymers
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