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PubMed2000

Pharmacodynamics and kinetics of omeprazole MUPS 20 mg and pantoprazole 40 mg during repeated oral administration in Helicobacter pylori-negative subjects.

BACKGROUND: Omeprazole has become available in a tablet formulation, a Multiple Unit Pellet System (MUPS) containing a large number of small individually enteric-coated micropellets. AIM: To compare the acid-inhibitory effect of omeprazole MUPS 20 mg with pantoprazole 40 mg and to describe the pharmacokinetics of both drugs following administration on day 1 and day 6. METHODS: Randomized, two-way crossover study. Sixteen Helicobacter pylori-negative healthy subjects, whose gastric acidity fell below pH 4 for 70% of a 24-h baseline period were included. Intragastric pH was measured continuously. RESULTS: On day 1 both drugs significantly raised median 24-h gastric pH compared to baseline. Median pH and percentages of time above pH 3 and 4 on day 1 and day 6 of administration were not significantly different, with the exception of median daytime pH on day 6, which was significantly higher with omeprazole (4.65 vs. 4.05). AUC and Cmax of omeprazole were significantly increased on day 6. AUC and Cmax of pantoprazole were not significantly increased. CONCLUSIONS: No significant difference in acid-inhibitory effect on day 1. On day 6 median daytime pH was significantly higher with omeprazole MUPS, but the percentages of time spent above pH 3 and 4 were not significantly different. The significant increase in bioavailability of omeprazole may contribute to the increased effect on day 6.

2-Pyridinylmethylsulfinylbenzimidazoles↗

PubMed2004

Oral bioavailability and multiple dose tolerability of an antisense oligonucleotide tablet formulated with sodium caprate.

In vivo study was performed to determine the tolerability and pharmacokinetics of ISIS 104838, a phosphorothioate antisense oligonucleotide targetting human tumour necrosis factor alpha (TNF-alpha) mRNA, following multi-dose administration via intravenous and oral routes. Oral tablet formulations of ISIS 104838 were pre-formulated with the permeation enhancer, sodium caprate, in an enteric-coated solid dosage form. The average plasma bioavailability of ISIS 104838 was 1.4% relative to IV. The tissue distribution profile was similar following both routes of administration, with highest concentrations observed in the kidney followed by the liver, lymph nodes and spleen. Plasma bioavailability underestimated the tissue accumulation of ISIS 104838 observed 1 day after the last dose. Mean systemic tissue bioavailability ranged from 2.0 to 4.3%, relative to IV tissues, and was dependent on tissue type. No marked differences were noted in the pharmacokinetic parameters following multi-dosing either via intravenous or oral routes. All formulations administered were well tolerated. This paper reports the first evaluation of solid oral dosage forms comprising sodium caprate and an antisense oligonucleotide. Furthermore, this study demonstrates the oral delivery of ISIS 104838 from solid oral dose formulations, with the achievement of comparable tissue concentrations of the oligonucleotide to that of the intravenous treatment.

Administration, Oral↗

PubMed1976

A trial of micro-encapsulated and enteric-coated aspirin in rheumatoid arthritis.

In a trial of 48 patients with rheumatoid arthritis, enteric-coated aspirin (4.55 g daily( and micro-encapsulated aspirin (4.50 g daily) proved to be equally effective in reducing morning stiffness, relieving pain, increasing grip strength, reducing ESR, and reducing the need for additional analgesic tablets, compared with placebo. Reduction of joint tenderness was also found, but this was not statistically significant. Proximal interphalangeal joint circumference altered little during the trial. Tinnitus and deafness were commoner with enteric-coated aspirin, but gastric side-effects were similar. Of 39 patients completing the trial, there was an equal patient preference for enteric-coated aspirin and micro-encapsulated aspirin. Salicylate side-effects necessitated withdrawal of six patients from the trial and dose reduction in nine patients. It was concluded that the efficacy and side-effects in rheumatoid arthritis of both aspirin preparations were similar.

Administration, Oral↗

PubMed1975

[Comparative studies of oral "quick-release" and "slowrelease" iron preparations in the postabsorption serum iron concentration test].

In Heilmeyer's iron-loading test the iron preparation SA (Eryfer) proved greatly superior to a commercially available effervescent tablet (iron preparation SC), to an iron preparation in a sustained release from (iron preparation SD) and to an iron preparation in the form of enteric-coated pellets (iron preparation SE), in producing and maintaining an increased serum iron level. As compared to a sodium bicarbonate-free preparation (iron preparation SB) the iron preparation SA must be considered equivalent. The results of our investigations made with iron preparation SA are supported by experiences made by other authors with therapeutic application.

Administration, Oral↗

PubMed1984

Platelet aggregation and plasma levels of acetylsalicylic acid in stroke patients on long-term treatment with an enteric-coated aspirin formulation.

Enteric-coated formulations of acetylsalicylic acid (ASA) should be advantageous in prophylaxis after stroke because they cause fewer gastrointestinal side effects. However, the absorption of unchanged ASA and the effectiveness of these formulations have been questioned, which prompted the present investigation. Fourteen elderly stroke patients on long-term medication with enteric-coated ASA 1.5 g daily and four patients on placebo were studied. When tested with arachidonic acid platelet aggregation was completely inhibited in all ASA subjects whereas it was normal in the controls. Plasma samples, drawn every 1/2 h for 6 h after tablet intake, were analyzed by HPLC. The presence of ASA was short lasting with a mean peak concentration of 55 mumol/l reached after 2-3.5 h. Salicylic acid (SA) appeared later, having a mean peak value of 591 mumol/l after 2.5-6 h. Thus, absorption of ASA as well as inhibition of platelet aggregation were confirmed during long-term medication with enteric-coated ASA.

Aged↗

PubMed1979

Absorption of quinidine from an enteric-coated preparation.

The absorption of quinidine from single and multiple doses of an enteric-coated preparation (Systodin) was studied in seven healthy subjects, and was compared with the pharmacokinetics of intravenously administered quinidine and the results of in vitro dissolution tests of the tablets. Absorption of quinidine began after a variable delay, 2-8 h (mean 4.8) after fasting and 3-10 h (mean 6.1) after food. The rate of absorption varied both in and between individuals. It appeared to be lower when the drug was administered after food. Multiple doses after food gave a pattern of plasma concentration-time curves similar to that found on administration of single doses after food. The delay prior to absorption was prolonged at night. The ratio between the maximum and minimum concentration of quinidine during a dose interval varied from 1.3 to 3.2 (mean 2.0). Bioavailability of quinidine in fasting subjects ranged from 69 to 95% (mean 83); variation was greater when doses were administered after food. The release of quinidine from the enteric-coated preparation was pH dependent and was sustained at low pHs as may be found in the intestines. The results indicate that the absorption of quinidine from the enteric-coated formulation was dependent on the highly variable rate of gastric emptying and the pH of intestinal fluid, and it varied greatly both within and between individuals.

Adult↗

PubMed1979

Medical treatment of pancreatic insufficiency.

Treatment of exocrine pancreatic insufficiency with the use of eight tablets of pancreatin with meals consisting of 25 g of fat per meal will generally abolish azotorrhea. Although steatorrhea is not totally corrected, satisfactory nutritional status and relative relief of symptoms are usually achieved. For the occasional patient who continues to lose weight or remains symptomatic even after reduction of dietary fat, the addition of cimetidine to the standard pancreatin treatment will usually provide relief from the steatorrhea and alleviate troublesome diarrhea. In certain circumstances in which gastric pH is more than 4 for 1 hour after a meal, altering the dosage schedule to two tablets hourly may be effective in alleviating the steatorrhea. Conversely, in patients whose upper gastrointestinal tract is acidic for long periods postprandially (gastric pH less than 5, duodenal pH less than 4), Pancrease, an enteric-coated preparation, may be effective. In difficult cases in which symptoms and steatorrhea continue, special intraluminal studies need to be performed to ensure that intraluminal conditions are, in fact, present for certain dosage schedules to be effective or that intraluminal conditions have been altered by adjunctive therapy.

Celiac Disease↗

PubMed1998

Mebeverine decreases mass movements and stool frequency in lactulose-induced diarrhoea.

BACKGROUND: In spite of its frequent use in the treatment of irritable bowel disease little is known about mebeverine's mode of action in man. AIM: To examine mebeverine's effect on transit though the gut during lactulose-induced diarrhoea. METHODS: Nine healthy volunteers undertook a two-way randomized crossover study. Diarrhoea was induced using lactulose pre-treatment (20 m t.d.s., 4 days) and subjects received either mebeverine (135 mg t.d.s.) or no treatment. Transit of two enteric-coated capsules containing radiolabelled 8.4 mm tablets and 180-250 microM ion exchange resin were followed using gamma scintigraphy. Stool frequency and symptoms were assessed by diary cards. RESULTS: Mebeverine reduced mean daily stool frequency associated with lactulose ingestion from a median of 2.25 (interquartile range (IQR) 1.75-2.75) to 1.5 (IQR 1.25-2.25) movements. Mebeverine significantly reduced the number of mass movements observed in the colon during the 11 h of the study from 2 (2-2) to 1 (1-2), and the number of retrograde movements from 1 (0-2) to 0 (0-0) (P < 0.05). Mebeverine did not significantly alter the gastric emptying rate of the intact capsule (2.9 (1.9-3.2) to 2.8 (2.6-4.0) h) however it induced a small but significant acceleration in small intestinal transit of the capsule (1.6 (0.8-2.0) h to 1.0 (0.52-1.32) h, P=0.02). CONCLUSION: Mebeverine reduces the diarrhoeal effect of lactulose by decreasing the mass movements induced in the ascending colon. This effect may contribute to its clinical effect in irritable bowel syndrome.

Adolescent↗

PubMed1983

Plasma prednisolone studies in rheumatic patients.

Prednisolone concentration in plasma after a daily maintenance steroid dose was monitored in 83 patients with rheumatic diseases. Although no restrictions were imposed on the intake of food or drink, plasma drug levels tended to peak at 1 h after the ingestion of the standard tablets, whereas intestinal absorption of the enteric-coated preparation was found to be most unpredictable. A profound individual variation was observed in plasma prednisolone concentrations, and neither total nor unbound drug levels showed any consistent relationship with the size of the prednisolone dose or the control of the disease activity. The basal cortisol production was suppressed in one-third of the patients. There is no support from this study for the concept of an 'optimum therapeutic range' of plasma prednisolone for the treatment of rheumatic disease.

Adult↗

PubMed2004

"Soft tableting": a new concept to tablet pressure-sensitive materials.

The aim of this study was to confirm the hypothesis that tableting using excipients with greater elastic deformation results in improved performance of pressure-sensitive drugs relative to the excipients with low elastic deformation. Tableting with highly elastic deforming excipients and the resultant minimization of the process damage is referred to in this article as "soft tableting." Carrageenans, chitosans, and polyethylene oxides were tested as potentially useful tableting excipients. alpha-Amylase, amorphous indomethacin, theophylline monohydrate, and enteric-coated pellets were used as models for pressure-sensitive materials. Three-dimensional modeling of the tableting data and elastic recovery of the tablets were the tools for mechanical characterization. The crushing force of the tablets was analyzed. Inactivation of alpha-amylase was determined by using the starch iodine reaction method. Pseudopolymorphic and polymorphic changes were analyzed using Fourier transform (FT) Raman spectroscopy. The effects of pressure on the integrity of the pellets were tested by release studies and scanning electron microscopy. The process of tablet formation was characterized for potentially useful tableting excipients. The results were compared with the results of traditional excipients as microcrystalline cellulose (MCC), dicalcium phosphate dihydrate, and hydroxypropyl methylcellulose (HPMC). A ranking order for soft tableting was deduced from the mechanical properties. The tableting excipients were ranked according to their general plasticity (GP): GP(carrageenans)<GP(chitosans)<GP(MCC)<GP(HPMC)<GP(polyethylene oxides). This theoretical order of suitability has been experimentally proven to be valid for the pressure-sensitive materials. In conclusion, the new concept for soft tableting is valid.

Chemistry, Pharmaceutical↗

PubMed1980

The prevalence of duodenal lesions in patients with rheumatic diseases on chronic aspirin therapy.

Peroral endoscopy was performed in 56 patients with rheumatic disease who had been taking 8 or more aspirin tablets daily for more than 3 months yet who had no major gastrointestinal symptoms or history of peptic ulcer disease. Duodenal mucosal lesions were observed in 16 patients; 15 (27%) had erythema, 7 (13%) had erosions, and 2 (4%) had ulcers. The prevalence of duodenal lesions was the same in patients taking regular, buffered, or enteric-coated aspirin preparations. Patients with duodenal lesions were more likely to have associated gastric lesions.

Adult↗

PubMed1979

Incidence of gastric lesions in patients with rheumatic disease on chronic aspirin therapy.

Endoscopy was done in 82 patients with rheumatic disease who were receiving chronic aspirin therapy. Fifty-eight patients were taking at least eight aspirin tablets daily for 3 or more months; 24 patients were taking, in addition to the aspirin, a maximum of one other antiinflammatory, nonsteroidal medication. Endoscopy in 45 normal subjects not taking aspirin showed no ulcers or erosions and a 4% incidence of gastric erythema. In the 82 patients with rheumatic disease, 14 (17%) had gastric ulcers, 33 (40%) had gastric erosions, and 62 (76%) had gastric erythema. Regular aspirin and buffered aspirin users had an ulcer incidence of 23% and 31% respectively, compared with a 6% incidence in enteric-coated aspirin users (P less than 0.05). One third of all patients with gastric ulcer had no gastrointestinal symptoms. Patients taking chronic aspirin therapy for rheumatic diseases have a higher than suspected incidence of gastric ulcer and erosions. Gastric ulcer may exist without symptoms in such patients.

Adult↗

PubMed1995

The effect of aspirin on haemostatic activity in the treatment of chronic venous leg ulceration.

An increased rate of venous ulcer healing with the use of oral enteric-coated aspirin (300 mg) daily has been reported. Whether the effect of aspirin in this condition is related to its action on the haemostatic mechanism is unclear, and therefore this study aimed to assess the effect of aspirin on some haemostatic parameters in patients with chronic venous leg ulcers. A double-blind, randomized, placebo-controlled, parallel-group study of haemostatic activity and the effect of aspirin was implemented over a 4-month period. Twenty patients with venous leg ulcers, and 20 age- and sex-matched controls were studied. Patients received enteric-coated aspirin (300 mg) or placebo (one tablet) daily for 4 months, in addition to standardized local compressive bandaging (Setopress). Assessments made at recruitment, and at 2 and 4 months, included measurement of total ulcer surface area, haematological and biochemical screening, measurement of coagulation times, coagulation factor VIII:C (FVIII:C) and von Willebrand factor (vWF), and plasminogen activator inhibitor-1 (PAI-1) levels. Procoagulant activity was assessed by a computer-assisted technique, to determine the rate of thrombin production in vitro. Patients with venous ulcers had increased levels of fibrinogen (P < 0.01), FVIII:C (P < 0.05), vWF (P < 0.05) and PAI-1 antigen (P < 0.01) compared with controls. Shortening of the coagulation rate, shown by a reduction of the time to generate 50% maximal thrombin activity in seconds (T50), was seen in patients, in comparison with control subjects (P < 0.05). T50 was longer in patients receiving aspirin than those receiving placebo, reflecting prolongation of coagulation rate in the aspirin-treated group.(ABSTRACT TRUNCATED AT 250 WORDS)

Aspirin↗

PubMed2004

Management of acid-related disorders in patients with dysphagia.

Dysphagia affects a large and growing number of individuals in the United States, particularly the elderly and those who are neurologically impaired. Swallowing difficulties may be due to age-related changes in oropharyngeal and esophageal functioning as well as central nervous system diseases such as stroke, Parkinson disease, and dementia. Among institutionalized individuals, dysphagia is associated with increased morbidity and mortality. An appreciation of the physiology of swallowing and the pathophysiology of dysphagia is necessary for proper patient management. Careful history, physical examination, and evaluation of radiologic and endoscopic studies should differentiate oropharyngeal and esophageal etiologies of dysphagia and distinguish mechanical (anatomic) disorders from functional (motor) disorders. A significant percentage of patients with dysphagia have concomitant acid-related disorders that are managed best with proton pump inhibitor (PPI) therapy. Three of the currently available PPIs are manufactured as capsules containing enteric-coated granules that may be mixed with soft foods or fruit juices before oral administration to those with swallowing difficulties. In addition, omeprazole and lansoprazole may be administered via gastrostomy or nasogastric feeding tubes as suspensions in sodium bicarbonate. Novel dosage formulations of lansoprazole that may be appropriate for patients with dysphagia include the commercially manufactured lansoprazole strawberry-flavored enteric-coated granules for suspension and lansoprazole orally disintegrating tablets.

2-Pyridinylmethylsulfinylbenzimidazoles↗

PubMed1991

Pharmacokinetics of 2',3'-dideoxyinosine in patients with severe human immunodeficiency infection. II. The effects of different oral formulations and the presence of other medications.

2',3'-Dideoxyinosine (ddI) has shown activity against human immunodeficiency virus in phase I clinical trials. The drug is rapidly degraded by acid, however, thus raising questions as to the efficiency and reproducibility of its absorption after oral administration. This investigation studies the bioavailability of several oral dosage forms of ddI. When ddI was given to fasting patients as an oral solution with antacid, the bioavailability was 41% +/- 7% (mean +/- SEM). However, when given as buffered tablets, the bioavailability was considerably less (25% +/- 5%). The bioavailability increased slightly when the tablets were given with supplemental antacid (36% +/- 6%). Two enteric-coated preparations had reasonable bioavailability (36% +/- 5% and 26% +/- 5%), but the peak plasma level was much lower and occurred at a much later time than with the oral solution. When ddI was given as a premeasured powder containing sucrose and buffer to be reconstituted by the patient (the "sachet" preparation), the bioavailability was 29% +/- 6%. This was similar to that of the oral solution for this particular group of patients (30% +/- 7%). However, the bioavailability of the sachet was only 17% +/- 4% when administered with food. When the sachet was given to patients receiving ranitidine, no consistent change in bioavailability was noted. Also, no change in ddI pharmacokinetics was noted in patients receiving ganciclovir.

Acquired Immunodeficiency Syndrome↗

PubMed2001

Eosinophilic gastroenteritis treated with non-enteric-coated budesonide tablets.

A patient who presented with upper abdominal pain, nausea and ascites together with peripheral eosinophilia is described. Based on a surgical full-thickness biopsy of the antrum, the diagnosis of eosinophilic gastroenteritis was made. Treatment with prednisone resulted in a clinical response, but the prednisone dose could not be lowered below 5 mg. We preferred to treat the patient with corticosteroids with minimal systemic side effects. As there was gastric involvement, we could not give enteric-coated budesonide capsules. Therefore, we treated the patient with budesonide tablets, which were designed originally for use as a clysma but now are given orally. With this treatment regimen, the patient has been in remission for more than 2 years.

Adult↗

PubMed2000

Bioavailability of a new effervescent tablet of diclofenac.

OBJECTIVE: The bioavailability of a newly developed effervescent tablet containing 50 mg diclofenac Na (DIC-effervesc) was investigated and compared with an enteric-coated dragée (DIC-enteric). SUBJECTS AND METHOD: 24 healthy, male and informed volunteers (mean body weight 78.8 kg, mean age 31.9 years) received in a randomized cross-over design a single dose of 50 mg diclofenac as DIC-effervesc and DIC-enteric. A total of 19 blood samples were obtained before and up to 12 h after administration according to the different properties of the galenic formulation. Diclofenac was analyzed by a sensitive HPLC method with a lower limit of quantification of 20 ng/ml. The bioavailability was compared as ratios of the geometric means of AUC0-infinity and Cmax. RESULTS: DIC-effervesc shows no lag time, a tmax within 30 min and a double peak of Cmax in 15/24 subjects. The mean Cmax (arithm. mean +/- SD) for DIC-effervesc is 950+/-341 ng/ml (first Cmax) and for DIC-enteric 1364+/-335 ng/ml. The mean AUC0-infinity, (arithm. mean +/- SD) amounts to 1097+/-210 ng/ml x h for DIC-effervesc and 1262+/-220 ng/ml x h for DIC-enteric. Based on the point estimator and the 90% interval DIC-effervesc is bioequivalent in respect to amount absorbed (86.4%; 81.8 - 91.3%). DIC-effervesc was well tolerated. CONCLUSION: The new effervescent tablet of diclofenac Na shows a rapid absorption without lag time, the same amount of absorption and a slightly lower Cmax (caused by a double peak phenomenon) in comparison to the enteric-coated dragee. A rapid onset of therapeutic effect is postulated in acute pain disorders.

Adult↗

PubMed1979

The influence of food on the bioavailability of new formulations of erythromycin stearate and base.

1. The effect of food on the bioavailability of two new formulations of erythromycin, 1) erythromycin stearate, 500 mg (Erythrocin, 250 mg capsule-shaped tablets) and 2) erythromycin base, 500 mg (Eryc, 250 mg capsules containing enteric-coated pellets) was studied in 16 healthy subjects. 2. The study was a balanced, randomized Latin square design and was conducted on 4 days. The four treatments were erythromycin stearate immediately before (EB) and after EA) breakfast and erythromycin base immediately before (eB) and after (eA) breakfast. 3. The mean +/- s.d. maximal plasma erythromycin concentrations were 2.09 +/- 1.06, 0.37 +/- 0.40, 1.8+ +/- 1.15 and 1.91 +/- 1.57 micrograms/ml and the mean +/- s.d. times at which these occurred were 1.3 +/- 0.7, 2.3 +/- 0.9, 4.4 +/- 1.9 and 4.3 +/- 1.1 h for EB, EA, eB and eA respectively. 4. The mean +/- s.d. areas under the curves (0 to 8 h) were 4.99 +/- 2.41, 1.04 +/- 1.57, 4.93 +/- 2.98 and 4.98 +/- 3.14 for EB, EA, eB and eA respectively. 5. The bioavailability of erythromycin stearate was significantly reduced by the prior administration of food, whereas the absorption of the base was not inhibited by food.

Adult↗