Class experiment with student volunteers illustrating the influence of formulation on absorption of aspirin [proceedings].
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Aspirin↗
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Results for “Tablets, Enteric-Coated”
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[Influence of formulation of enteric coated tablets on the bioavailability of the drug. 5th Part: Bioavailability of Riboflavin enteric coated tablets (author's transl)].
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Biological Availability↗
An enteric-coated pancreatic enzyme preparation that works.
A new enteric-coated pancreatic enzyme preparation (microspheres) was compared with traditional enzyme tablets in six subjects with severe exocrine pancreatic insufficiency. The microspheres were found to be as effective as traditional enzyme supplements. In most patients in balance studies, the lowest fecal fat values were obtained with microsphere therapy in spite of a smaller amount of lipase administered (6015 vs 10,800-43,200 lipase units per meal). In contrast to enteric-coated tablets, microspheres can be recommended in the treatment of pancreatic steatorrhea.
Adult↗
Enteric-coated charcoal as a means of blinding studies comparing bismuth and H2-receptor antagonists.
Clinical trials comparing H2-receptor antagonists and bismuth-containing regimens in ulcer healing, ulcer relapse, or dyspepsia have not been double-blind, because bismuth darkens stools. This study was designed to determine whether enteric-coated charcoal could darken stools of subjects taking an H2-receptor antagonist without interfering with absorption of the drug. Twelve healthy volunteers participated in a randomized, double-blind, crossover trial of oral ranitidine (300 mg at bedtime) alone, ranitidine plus bismuth (30 ml Pepto-Bismol four times daily), and ranitidine plus enteric-coated charcoal (four tablets daily). Mean stool colors both with ranitidine plus charcoal and with ranitidine plus bismuth were significantly darker than with ranitidine alone, but were not significantly different from each other. Blood levels of ranitidine during the 10 h after its administration did not differ significantly among the three regimens. We conclude that enteric-coated charcoal can be used to blind clinical trials comparing an H2-receptor antagonist (e.g., ranitidine) and a bismuth regimen.
Administration, Oral↗
The effect of oral magnesium chloride therapy on the QTc and QUc intervals of the electrocardiogram.
The effect of magnesium, given orally as enteric-coated magnesium chloride tablets, on the ECG of 25 randomly selected patients was investigated. Each patient, who served as his own control, was given 4--6 tablets, each containing 0,5 g MgCl26H2O, at night for periods varying from 6 weeks to 2 years. Findings included (i) a statistically significant decrease in OTc and QUc intervals; (ii) a progressive shortening of QTc and QUc intervals with continuing therapy; (iii) reversion to normal of ECG abnormalities, especially of ST segments and T waves.
Administration, Oral↗
ISIS-3: a randomised comparison of streptokinase vs tissue plasminogen activator vs anistreplase and of aspirin plus heparin vs aspirin alone among 41,299 cases of suspected acute myocardial infarction. ISIS-3 (Third International Study of Infarct Survival) Collaborative Group.
41,299 patients entering 914 hospitals up to 24 h (median 4 h) after the onset of suspected acute myocardial infarction were randomised between streptokinase (SK: 1.5 MU infused over about 1 h), tissue plasminogen activator (tPA, duteplase: 0.60 MU/kg infused over about 4 h), or anisoylated plasminogen-streptokinase activator complex (APSAC), anistreplase: 30 U over about 3 min). All patients were to receive aspirin (162 mg/day enteric-coated), with the first tablet chewed for rapid and full antiplatelet effect. Half of all patients were randomly allocated subcutaneous calcium heparin (12,500 IU starting at 4 h and given twice daily for 7 days or until prior discharge) in addition to aspirin, and the other half were to receive aspirin alone. ASPIRIN PLUS HEPARIN VERSUS ASPIRIN ALONE--The addition of heparin to aspirin was associated with an excess of transfused or other major non-cerebral bleeds (1.0% aspirin plus heparin vs 0.8% aspirin alone; 2p < 0.01) and of definite or probable cerebral haemorrhage (0.56% vs 0.40%; 2p < 0.05), but with no significnat differences in total stroke (1.28% vs 1.18%). Reinfarctions were slightly less common among those allocated aspirin plus heparin (3.16% vs 3.47%; 2p = 0.09). There was no signficant difference in the pre-specified endpoint of 35-day mortality (2132 [10.3%] aspirin plus heparin vs 2189 [10.6%] aspirin alone). During the scheduled heparin treatment period there were slightly fewer deaths in the aspirin plus heparin group (days 0-7 in hospital: 1534 [7.4%] vs 1633 [7.9%]; 2 p = 0.06), with a slight convergence by day 35 (598 further deaths [3.1% of survivors] vs 556 [2.9%]). The pattern was similar to that observed in the GISSI-2 trial, so that in both trials combined there was a significant reduction in mortality during the scheduled treatment period (2071 [6.8%] vs 2239 [7.3%]; 2p < 0.01). This indicates avoidance of 5 deaths (SD 2) per 1000 patients allocated this high-dose subcutaneous heparin regimen in addition to aspirin, but some of any early benefit may be lost after heparin ceases, with no significant mortality advantage in days 0-35 (both trials: 3100 [10.0%] vs 3172 [10.2%]) or during follow-up to 6 months. SK VERSUS APSAC--APSAC was associated with significantly more reports of allergy causing persistent symptoms and of non-cerebral bleeds, but not of transfused bleeds or of reinfarctions. There was a slight excess of strokes with APSAC (1.04% SK vs 1.26% APSAC; 2p = 0.08), much of it appearing soon after treatment started (strokes during days 0-1: 0.50% SK vs 0.73% APSAC; 2p < 0.02) and being attributed to cerebral haemorrhage (0.24% SK vs 0.55% APSAC; 2p < 0.0001). No significant difference was observed in reinfarction (3.47% SK vs 3.55% APSAC). There was no significant mortality difference during days 0-35, either among all randomised patients (1455 [10.6%] SK vs 1448 [10.5%] APSAC) or among the pre-specified subset presenting within 0-6 h of pain onset and with ST elevation on the electrocardiogram in whom fibrinolytic treatment may have most to offer (861 [10.0%] SK vs 855 [9.9%] APSAC). No significant difference in 6-month survival was apparent overall or in the subset.(ABSTRACT TRUNCATED AT 400 WORDS)
Aged↗
Prospective comparison of patient tolerance to enteric-coated vs nonenteric-coated erythromycin.
Erythromycin base and its salts are frequently used in clinical practice. The most frequent side effects of oral erythromycin preparations are gastrointestinal. Various salts and enteric coatings have been developed without adequate comparison in regard to gastrointestinal side effects. The overall incidence of gastrointestinal side effects (abdominal pain and cramps, nausea, vomiting, diarrhea, and gas) of two common erythromycin base formulations, Erythromycin Base Filmtab (Abbott), a nonenteric-coated base tablet, and Eryc (Parke-Davis), a pelletized, encapsulated, enteric-coated base capsule, were compared in 368 adults at two dosage levels (1 g/d and 2 g/d). Minimal differences were found when target symptoms were compared by preparation coating. In contrast, subjects receiving erythromycin at the 2-g/d dosage level reported higher incidence rates for each of the target symptoms, regardless of product coating, than did those patients treated at the 1-g/d dosage level. Enteric coating of erythromycin base offers little protection from the common dose-related gastrointestinal adverse effects of oral erythromycin.
Administration, Oral↗
Prescribing and dispensing practices for oral iron tablets: a Canadian experience.
The formulation of an oral iron tablet may influence its therapeutic efficacy in correcting iron deficiency. In order to determine the oral iron preparations patients in a Canadian urban center were receiving, a questionnaire was circulated to family physicians, internists, surgeons, and obstetrician-gynecologists to determine their prescribing practices. A survey of pharmacies in the city was also conducted to determine which brand of each iron salt (sulfate, gluconate, fumarate) they dispensed for a generic oral iron prescription. Most physicians (74 percent) chose ferrous sulfate as their drug of first choice. The majority of prescribers would not specifically request either enteric-coated/slow-release or nonenteric-coated preparations as first or second choices (71 and 64 percent, respectively). Enteric-coated or slow-release preparations were specified by 10 and 19 percent of physicians as first and second choices, respectively. Most pharmacies (96 percent) dispensed an enteric-coated preparation of ferrous sulfate for a generic prescription. We believe that many patients are receiving iron tablets with altered release properties (enteric-coated/slow-release). These tablets may fail to provide the desired therapeutic benefit based on the known physiology of iron absorption.
Canada↗
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↗
[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↗
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↗
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↗
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↗
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↗
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↗
Comparison of two oral forms of erythromycin in the treatment of acute respiratory tract infections. A multicentre general practice study.
A total of 1244 patients with acute upper or lower respiratory tract infection were randomized to receive, twice daily for 7 days, either capsules of enteric-coated pellets of erythromycin base at a dose of 1 g/day or erythromycin ethylsuccinate tablets at a dose of 2 g/day in a single-blind, multicentre study. The efficacy of each formulation was similar, with about 90% of patients who had completed at least 5 days of treatment being reported as either cured or improved. Gastro-intestinal symptoms were the most commonly reported side-effects, being significantly more frequent in patients receiving erythromycin base. Gastro-intestinal intolerance was also the main reason for discontinuing either treatment, although it was a significantly more frequent reason in patients given erythromycin base. This study indicates that both formulations of erythromycin are highly effective for routine, empirical treatment of acute respiratory tract infections. Erythromycin base, however, appears to be less well tolerated than erythromycin ethylsuccinate.
Acute Disease↗
Gastrointestinal behavior of orally administered radiolabeled erythromycin pellets in man as determined by gamma scintigraphy.
The behavior of single 250-mg doses of a multiparticulate form of erythromycin base (ERYC(R)), each including five pellets radiolabeled with neutron-activated samarium-153, was observed by gamma scintigraphy in seven male subjects under fasting and nonfasting conditions. The residence time and locus of radiolabeled pellets within regions of the gastrointestinal tract were determined and were correlated with plasma concentrations of erythromycin at coincident time points. Administration of food 30 minutes postdosing reduced fasting plasma erythromycin Cmax and area under the plasma erythromycin versus time curve (AUC) values by 43% and 54%, respectively. Mean peak plasma concentration of erythromycin (Cmax) in the fasting state was 1.64 micrograms/mL versus 0.94 micrograms/mL in the nonfasting state. Total oral bioavailability, as determined by mean AUC (0-infinity) of the plasma erythromycin concentration versus time curve, was 7.6 hr/micrograms/mL in the fasted state, versus 3.5 hr/micrograms/mL in the nonfasting state. Mean time to peak plasma erythromycin concentration (tmax) in the fasting state was 3.3 hours, versus 2.3 hours in the nonfasting state. Plasma concentrations of erythromycin in both fasting and nonfasting states were within acceptable therapeutic ranges. Evidence provided by this study: 1) indicates that pellet erosion and absorption of active erythromycin base begins when the enteric-coated pellets reach the highly vascular mucosa of the jejunum and proximal ileum, and is essentially completed within the ileum, with a significant portion absorbed in the medial-to-distal ileum; 2) confirms that acceptable therapeutic plasma levels of erythromycin are attained in nonfasting subjects (Cmax = 0.94 microgram/mL) and that superior plasma erythromycin concentrations (Cmax = 1.64 micrograms/mL) are achieved by administration of the dose on an empty stomach 1 to 2 hours before or after meals; 3) corroborates other comparative studies reporting greater fasting bioavailability with this multiparticulate dosage form of erythromycin base than with reference single tablet or particle-in-tablet formulations; and 4) indicates that neutron activation of stable isotopes incorporated as a normal excipient in industrially-produced formulations provides an effective means for in vivo evaluation of dosage forms through gamma scintigraphy.
Administration, Oral↗
Gastrointestinal transit of nondisintegrating, nonerodible oral dosage forms in pigs.
Gastrointestinal (GI) transit data necessary as "baseline" or "control" information were collected using pigs as animal models preliminary to bioavailability studies of new sustained action formulations. Density and size effects of nondisintegrating dosage forms on GI transit were investigated. Initially, enteric-coated nondisintegrating magnesium hydroxide caplets (density, 1.5 g/ml; size, 19.6 x 9.5 mm; weight, 1.2 g) were utilized in seven pigs. Prolonged gastric residence (greater than 5 days) occurred in every case for this dosage form. Therefore, nondisintegrating caplets of three densities (1.25, 1.45, and 2.3 g/ml) and three different sizes (large, 20 x 10 mm; medium, 10 x 10 mm; small, 5 x 10 mm) were studied in two more pigs. Roentgenography was used to visualize passage of caplets through the GI tract. Heidelberg pH capsules (size, 8 x 20 mm; density, 1.61 g/ml) were also used in this study. Total GI transit times range from 2 to 33 days for 22 administrations of these nondisintegrating dosage forms. Pigs are found to not be an appropriate model for evaluating bioavailability of nondisintegrating controlled-release dosage forms because total GI transit time (especially gastric transit) is much too long.
Animals↗