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Results for “Gastrointestinal Transit”

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At least 145 records · Page 8Linked to original sources

PubMed1991

Variation in gastrointestinal transit of pharmaceutical dosage forms in healthy subjects.

The variability in the gastrointestinal transit of a multiple-unit and single-unit dosage form was investigated following a light breakfast in six, healthy, male volunteers after repeated weekly administration. The dosage forms were labeled with gamma-emitting radionuclides and the transit of the formulations was monitored on 4 separate study days using the technique of dual-isotope gamma scintigraphy. Gastric emptying times and small intestinal transit times were calculated and compared statistically within and between subjects using the standard deviation and coefficient of variance. The variability in gastric emptying of single- and multiple-unit systems was large; the intrasubject variation being less than the intersubject. There was less variation in small intestinal transit times for the single- and multiple-unit formulations than in gastric emptying, intrasubject variation again being less than intersubject variation.

Adult↗

PubMed1997

High-resolution monitoring of the gastrointestinal transit of a magnetically marked capsule.

The purpose of this study was to demonstrate that it is possible to continuously monitor the gastrointestinal transit of magnetically marked, solid, oral dosage forms with multichannel biomagnetic measuring equipment and by magnetic source imaging (MSI) methods. For the investigations presented, a sucrose pellet was coated with powdered magnetite (Fe3O4) in poly(methyl methacrylate). Then, the pellet was enclosed in a capsule prepared from silicone rubber and magnetized to obtain a net magnetic dipole moment. After ingestion of the capsule, its magnetic field distribution over the abdomen was recorded for several time intervals with a 37-channel superconducting quantum interference device (SQUID) magnetometer. At each time point, the position of the capsule within the gastrointestinal tract was calculated from the measured field distribution, assuming a magnetic dipole model. The data presented here demonstrate that with this noninvasive method of magnetic marker monitoring it is possible to investigate the gastrointestinal transit of a solid oral dosage form with a temporal resolution in the order of milliseconds and a spatial resolution within a range of millimeters.

Capsules↗

PubMed2006

5-aminosalicylic acid release from a new controlled-release mesalazine formulation during gastrointestinal transit in healthy volunteers.

BACKGROUND: Mesalazine (5-aminosalicylic acid, 5-ASA) containing formulations represent a cornerstone in the treatment of inflammatory bowel diseases. A novel formulation with an Eudragit L/S mixture coating has been developed to provide selective release of 5-ASA to the ileo-caecal region and the colon. AIM: To determine the release of 5-ASA during the gastrointestinal transit. METHODS: A single oral dose of mesalazine EC 500 mg gastroresistant tablets (Asamax) was administered to eight healthy male volunteers. Gastrointestinal transit and tablet disintegration were monitored by scintigraphy. 5-ASA release was verified by assessing plasma pharmacokinetics. RESULTS: Initial tablet disintegration was observed 5.65 +/- 0.86 h after dosing, corresponding to the detection of 5-ASA in plasma. This occurred in the ileo-caecal region in three subjects and the ascending colon in the remaining five. The relative percentage of 5-ASA absorption was more pronounced in the ascending colon (41 +/- 27.4%) than the ileo-caecal region (6.6 +/- 9.2%). CONCLUSION: This mesalazine EC gastroresistant tablets release locally active 5-ASA specifically in the ileo-caecal region and the ascending colon.

Administration, Oral↗

PubMed1993

Absorption, gastrointestinal transit, and tablet erosion of felodipine extended-release (ER) tablets.

The gastrointestinal transit and tablet erosion of felodipine extended release (ER) tablets 10 mg were studied by gamma scintigraphy in eight healthy young males after administration under fasting and nonfasting conditions. Plasma concentrations of felodipine were also measured. Gastric emptying after administration together with food (mean, 3.2 hr) was slower in all subjects compared to emptying under fasting conditions (mean, 0.6 hr). The mean small intestinal transit times for the two study conditions did not differ significantly (5.1 and 4.7 hr, respectively). Tablets did not leave the colon in any subject within 14 hr after administration. Felodipine was shown to be absorbed in the colon, although the major part of the dose was absorbed in the small intestine. The absorption rate of felodipine was related to erosion of the hydrophilic matrix tablet. Tablet erosion and hence drug absorption were slower in the more distal parts of the gastrointestinal tract. Administration together with food did not significantly affect tablet erosion.

Adult↗

PubMed1985

Intrathecal morphine slows gastrointestinal transit in rats.

Intrathecal (i.th.) (by direct lumbar puncture) and intraperitoneal (i.p.) administration of morphine (30-100 micrograms/rat) caused a dose-related inhibition of gastrointestinal transit in the rat. Pretreatment with i.th. naloxone (5 micrograms at -5 min) reversed the effects of i.th., but not i.p., morphine. These results suggest that the spinal cord appears to be a target site for the inhibitory effects of morphine on gastrointestinal transit in the rat.

Animals↗

PubMed1990

Gastrointestinal transit and release of mesalazine tablets in patients with inflammatory bowel disease.

Gastrointestinal transit and release of a delayed-release, enteric-coated tablet of mesalazine (Claversal) were studied in 13 patients with Crohn's disease and ulcerative colitis. The tablets disintegrated a mean of 3.2 h after leaving the stomach, resulting in drug dispersion in the distal small intestine or proximal colon. Tablet disintegration closely correlated with onset of drug absorption. Peak mean concentrations of mesalazine and its main metabolite, Ac-5-ASA, were 0.5 microgram/ml and 1.0 microgram/ml, respectively, and occurred 3 to 4 h after gastric emptying. The plasma levels correlated with scintigraph images of tablet disintegration. It is concluded that the tablets effectively deliver mesalazine to the terminal ileum and proximal colon in patients with inflammatory bowel disease.

Aminosalicylic Acids↗

PubMed1991

Fecal output, gastrointestinal transit time, frequency of evacuation and apparent excretion rate of dietary fiber in young men given diets containing different levels of dietary fiber.

Five healthy young male subjects were given meals containing different levels of dietary fiber (DF) for one week each, and the effects on the fecal output, gastrointestinal transit time, frequency of evacuation, and apparent excretion rate of dietary fiber in feces were studied. The experiments were conducted twice by varying the subjects and the DF levels. The following results were obtained. 1) With an increase in the intake of DF, feces increased significantly in both wet weight and volume. The fecal specific gravity did not show any clear-cut relation with the intake level of DF. 2) The gastrointestinal transit time tended to shorten in each DF period compared to the DF-free period. However, it did not shorten with an increase in the intake level of DF. 3) Frequency of evacuation tended to be high in any of the DF periods compared to the DF-free period. However, the differences in the intake level of DF produced no changes in the frequency. 4) The DF content in feces increased significantly with an increase in the intake of DF, indicating that the larger the fecal output, the larger the fecal DF content. The apparent mean excretion rate of DF in feces remained in the range of 60-75% throughout the two experimental phases. Residues in feces other than DF increased with an increase in the DF intake. 5) The results obtained here indicate that the DF intake of at least 20 g per day produces 140-150 g of fecal output which can be easily excreted daily by a normal adult person.

Adult↗

PubMed2001

Evaluation of absorption kinetics of orally administered theophylline in rats based on gastrointestinal transit monitoring by gamma scintigraphy.

The gastrointestinal (GI) transit and absorption of orally administered theophylline, a highly absorbable drug without presystemic elimination, were investigated under fasted and fed conditions using three rats in a crossover study. To evaluate the GI transit rate for each segment in vivo, a noninvasive technique, gamma scintigraphy, was employed using a nonabsorbable compound, (99m)Tc-labeled diethylenetriamine pentaacetic acid (DTPA). Using a gamma scintigraphic technique it is possible to simultaneously evaluate the GI transit and absorption of orally administered drug in the same individual. Theophylline was simultaneously administered along with [(99m)Tc]DTPA to animals in the fasted and fed states. Each GI transit pattern, simulated using the GI transit-kinetic model with a lag time factor, was well fitted to the experimental data. Gastric emptying rate varied in each study, even under the same experimental condition. The GI transit pattern for each segment was highly variable, especially in animals in the fed state. This inconsistency in transit pattern was mainly due to the variability in gastric emptying, which was much slower in animals in the fed compared with the fasted state. However, in spite of a large variability of GI transit kinetics, the plasma concentration-time curves of theophylline were well predicted by the GI transit-absorption model using the individual GI transit parameters obtained in the study. The absorption rate of theophylline was considerably reduced in animals in the fed state, because of the reduction of gastric emptying rate. Analysis using GI transit-absorption model and gamma scintigraphic technique made it possible to estimate the variable absorption kinetics regulated by GI transit with huge variability.

Administration, Oral↗

PubMed1983

Ketazocines and morphine: effects on gastrointestinal transit after central and peripheral administration.

The mu agonist, morphine, and the prototype kappa agonists, ketocyclazocine and ethylketocyclazocine (EK), were studied for their effects on gastrointestinal transit. Following s.c. administration, both morphine (0.3-3 mg/kg) and ketocyclazocine (0.3-10 mg/kg) antagonized transit of an opaque marker through the small intestines of mice. Morphine (0.1-1 microgram) was also effective after intracerebroventricular (icv) administration in mice whereas ketocyclazocine (0.3-30 micrograms) was not. Similarly, while both morphine (0.3-5 mg/kg) and EK (0.6-10 mg/kg) slowed transit after s.c. injection to rats, only morphine (1-10 micrograms), but not EK (0.3-300 micrograms), was active following icv administration. Icv infusion of the mu benzomorphan, phenazocine (10-100 micrograms), slowed transit in a dose-related manner. These results indicate that there may be an anatomically distinct distribution of receptors for benzomorphan kappa agonists in both the mouse and rat, with these opiate receptors not being located near the lateral cerebral ventricles. The difference in efficacy between morphine and ketazocines in slowing gastrointestinal transit after icv administration to rodents suggests that (a) inactivity in this endpoint is a characteristic of benzomorphan kappa compounds and (b) the model may serve as a useful screen when establishing in vivo profiles of kappa agonists in mice and rats.

Animals↗

PubMed1985

Gastrointestinal transit of an osmotic tablet drug delivery system.

The gastrointestinal transit of a radiolabelled osmotic tablet drug delivery system has been monitored in groups of young and elderly healthy subjects, using gamma scintigraphy. The gastric emptying and small intestinal transit times were similar for both groups of subjects. The units were observed to move through the gastrointestinal tract at about the same rate as the released contents, arriving at the caecum on average 7 h after dosing. The data suggest that tablet adhesion to the mucosal surface is unlikely to be the mechanism responsible for the side effects reported for the indomethacin formulation Osmosin.

Adult↗

PubMed1989

Gastrointestinal transit of undigestible solids measured by metal detector EAS II.

A new method was developed to measure gastrointestinal transit: a metal particle is followed on its way through the gastrointestinal tract by means of a portable metal detector. Deviation of measured localization of the metal particle from the exact site was 0.5-1.0 cm depending on its size and distance from the search probe. A metal sphere of 6 mm diameter can be located accurately in the body at a distance of 2-12 cm from the abdominal surface. Emptying of a metal particle from the stomach, its arrival at the caecal area and its passage through the colon into the rectum can be registered and hence, gastric residence time, small intestinal transit and transit through different parts of the colon were determined. Gastric residence time at the interdigestive phase was (mean +/- SD) 67 +/- 52 min in 20 persons with a range of 9-185 min. When gastric emptying was recorded by pH sensitive radiotelemetering capsule in 10 persons, correlation of both methods was r = 0.99. Small intestinal transit averaged 110 +/- 56 min in six healthy volunteers when breakfast was eaten after the marker had left the stomach. It was delayed to 218 +/- 34 min (P less than 0.01) when fasting was continued. Large intestinal transit of the metal marker was compared to whole body transit of radio-opaque ('Hinton') markers. In nine normal persons, 70% of the Hinton markers were excreted together with the metal particle. It is concluded that this new method is suitable for studying a large variety of physiological, pathophysiological and pharmacological questions concerning gastrointestinal transit.(ABSTRACT TRUNCATED AT 250 WORDS)

Digestive System Physiological Phenomena↗

PubMed1993

Effect of sodium acid pyrophosphate on ranitidine bioavailability and gastrointestinal transit time.

During development of a ranitidine effervescent oral solution dosage form, a marked decrease was observed in the extent of ranitidine absorption relative to the conventional oral tablet. Two studies were conducted in healthy volunteers to confirm the involvement of an excipient, SAPP (sodium acid pyrophosphate), and the mechanism of interaction, altered gastrointestinal transit. The first study (n = 12) involved single-dose crossover comparisons of (A) 150 mg ranitidine with 1132 mg SAPP versus (B) 150 mg ranitidine and (C) 150 mg ranitidine with all the effervescent tablet excipients except SAPP versus (D) a 150-mg ranitidine effervescent tablet, all administered as oral solutions. Serum ranitidine AUC, Cmax, and tmax were compared using two one-sided t test 90% confidence intervals (CI). Comparing treatments A to B and D to C, all 90% CI were below the 80-120% range, indicating significantly less extensive ranitidine absorption (54% based on AUC) from the oral solutions containing SAPP. The second study (n = 12) was a single-dose crossover comparing 50 microCi 111 InCl solutions with and without 1132 mg SAPP. Gastrointestinal transit times, determined by scintigraphic imaging, were compared between treatments. Gastric emptying time was unchanged, but small intestinal transit time was decreased to 56% in the presence of SAPP. More rapid small intestinal transit associated with an excipient of a solution dosage form apparently resulted in a decreased extent of ranitidine absorption. This observation contradicts the conventional wisdom that oral solutions are unlikely to fall short of bioequivalence relative to solid oral formulations.

Adult↗

PubMed1985

Gastrointestinal transit times of cathartics combined with charcoal.

Oral activated charcoal usually is administered in toxic ingestions along with a cathartic. A study was done in volunteers to determine the rapidity of gastrointestinal transit when activated charcoal was administered with various cathartics. A control of activated charcoal was compared to the gastrointestinal transit times of activated charcoal plus the cathartics magnesium citrate, magnesium sulfate, or sorbitol. Activated charcoal alone produced a mean transit time of 23.5 hours; magnesium citrate catharsis occurred in 4.2 hours, magnesium sulfate catharsis occurred in 9.3 hours, and sorbitol catharsis occurred in 0.9 hours. Sorbitol clearly was the most rapidly acting cathartic.

Administration, Oral↗

PubMed2006

Effects of mu, kappa or delta opioids administered by pellet or pump on oral Salmonella infection and gastrointestinal transit.

Our laboratory has shown previously that subcutaneously implanted, slow-release morphine pellets markedly enhanced susceptibility to oral infection with Salmonella typhimurium. Further, morphine, kappa and delta opioid receptor agonists infused via osmotic minipumps were immunosuppressive. The present study compared morphine pellets to morphine pumps and also examined the differential effects of morphine versus U50,488H (kappa agonist), deltorphin II (delta2 agonist), and (D-Pen2, D-Pen5)-enkephalin (DPDPE, delta1 agonist), administered via Alzet minipumps, on oral Salmonella infection and on gastrointestinal transit. The results show that all morphine-pelleted mice (26/26) had a marked increase in Salmonella burden in the Peyer's Patches, mesenteric lymph nodes and spleen. In comparison, only 8/20 mice receiving morphine by minipump at doses ranging from 1 to 25 mg/kg/day had any culturable Salmonella in their organs and the number of bacteria was very low. The level of Salmonella colonization correlated with blood morphine levels and gut transit measured using an intragastric charcoal meal. Morphine pellets inhibited gut transit by 38%, while mice receiving morphine by minipump at doses of 1 to 25 mg/kg/day showed only a dose-dependent 7% to 17% inhibition. Mice receiving various doses of U50,488H or DPDPE had no culturable Salmonella in the three sites. Deltorphin II given by minipump resulted in a moderate level of Salmonella in the spleen. Deltorphin II and U50,488H (0.1 to 10 mg/kg/day) did not suppress gut transit. The present studies indicate that a predominantly mu opioid receptor agonist, morphine, given by slow-release pellet, potentiated Salmonella infection and inhibited gastrointestinal transit. In contrast, morphine in pumps slightly inhibited intestinal transit, but did not sensitize to Salmonella infection. A delta1 opioid receptor agonist did not sensitize to infection, and a delta2 and a kappa opioid receptor agonist had minimal effects on either parameter.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗

PubMed1981

Limits of predicting gastrointestinal transit time from other measures of bowel function.

The two aims of these experiments were first, to examine the relationships between mean daily stool weight, mean weight per stool, frequency of defecation, dye transit time, dietary fiber intake, and transit time of small radiopaque pellets, and second, to determine the ability of these measures of bowel function, singly or in combination, to predict gastrointestinal transit time of the pellets. Variables were observed simultaneously in 13 healthy women consuming controlled low and high cellulose diets. All except one of the correlation coefficients between the measures of bowel function were significant. Stepwise regression analysis retained log stool weight, fiber and dye transit to predict log of the mean transit time of all pellets (R2 = 71.3); the same three variables were selected to predict log of the transit time of 80% of the pellets (R2 = 59.4). Mean daily stool weight explained about 50% of the variation for both measures of transit, while dye transit and dietary fiber explained the rest. Log transformation of either stool weight or pellet transit time or both variables improved the prediction of about 10%. These results suggest that prediction of pellet gastrointestinal transit time from other measures of bowel function may be limited and is influenced significantly by the fiber level of the diet.

Adult↗

PubMed1994

Diarrhea associated with intestinal inflammation increases the potency of mu and delta opioids on the inhibition of gastrointestinal transit in mice.

The aim of the study was to determine the effects of intestinal inflammation induced by croton oil on the antitransit action of systemically administered receptor-specific opioids. Our hypothesis was that inflammation would "sensitize" opioid receptors in peripheral and/or central terminals of myenteric and submucous plexus neurons and enhance the effects of exogenously administered opioids. Diarrhea was induced by p.o. administration of croton oil and was demonstrated by weight loss and increased gastrointestinal transit. Histologically, an increased number of clear vesicles in the cytoplasm of jejunal epithelial cells and enlarged spaces filled with fine granular material in the extravascular compartment were observed. Subcutaneous morphine and fentanyl produced dose-related inhibitions of gastrointestinal transit in saline-treated controls with ED50 values of 1.24 +/- 0.06 and 0.036 +/- 0.010 mg/kg, respectively. In animals with diarrhea, dose-response curves were parallel and shifted to the left with a significant decrease in ED50 values of 2.95 times for morphine and 1.89 for fentanyl. The effects of the delta agonist Tyr-D-Pen-Gly-Phe-D-Pen, but those of U50,488H [trans-3,4-dichloro-N-methyl-N-(2-(1-pyrrolydynil)cyclohexyl) benzeneazetamine] also were increased significantly during diarrhea associated with inflammation. Naloxone (0.1 mg/kg), MR-2266 [(-)-a-5,9-diethyl-2'-hydroxy-2-(3-furylmethyl)-6,7-benzomorphan] (3 mg/kg) and naltrindole (1 mg/kg) antagonized the effects of the receptor-specific opioid agonists used in the study. Our results show that the potency of s.c. mu and delta opioids is increased during inflammation of the gut and that the effect is mediated by the same type of opioid receptors present in the noninflamed tissue. These results support the view that a sensitization of opioid receptors occurs during acute inflammation of the gut.

Amino Acid Sequence↗

PubMed1993

Gastrointestinal transit is not impaired by regional loss of myenteric neurons in rat jejunum.

Chronic absence of myenteric neurons from a 5-cm segment of rat jejunum causes alterations in myoelectric activity. Spike potentials characteristic of phase III activity of the migrating motor complex (MMC) are present; however, the number of propagating spike potentials through the myenterically denervated region is reduced. The objective of this study was to examine the effect of the regional loss of myenteric neurons on gastrointestinal transit of a solid marker in the fasted rat. The rate of gastric emptying was not affected by the absence of the myenteric plexus in a 5-cm segment of the jejunum. However, 15 days after either myenteric denervation or vehicle treatment of a segment of jejunum, a more cephalad distribution and decreased rate of intestinal propulsion of the solid marker was observed in the small intestine. This delay in small intestinal transit observed at 15 days was not seen at 48 and 120 days. The decrease in transit at 15 days can be attributed to the handling of the bowel during the surgical procedure. The mouth-to-cecum transit time (MCT) was also not affected by chronic absence of the myenteric plexus. Furthermore, the MCT indicated that bacterial overgrowth, a common manifestation when gut motility is disrupted, did not occur in the small intestine after the experimental destruction of the myenteric plexus. The results of this study indicate that the regional loss of the myenteric plexus does not impair gastrointestinal transit in the fasted rat.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

PubMed1987

Gastrointestinal transit of an enteric-coated delayed-release 5-aminosalicylic acid tablet.

Gastrointestinal transit of an enteric-coated, delayed-release 5-aminosalicylic acid tablet radiolabelled with indium-111 has been monitored in a preliminary study with eight healthy subjects using gamma scintigraphy. Gastric emptying of the tablet was delayed by the presence of food in the stomach. Disintegration occurred about 5 hours after the tablet left the stomach. There was close agreement between the tablet disintegration times and the initial detection of drug in the blood. The site of disintegration could be established in most instances; approximately 80% of the doses resulted in drug dispersion within the ascending colon. The coated tablets provide an effective means of drug delivery to the proximal colon.

Adult↗