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Results for “Tablets, Enteric-Coated”

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At least 19 recordsLinked to original sources
PubMed1977

Enzyme replacement therapy of exocrine pancreatic insufficiency in man. Relations between in vitro enzyme activities and in vivo potency in commercial pancreatic extracts.

I assayed 16 commercially available pancreatic extracts (representing capsules, tablets and enteric-coated tablets) for enzyme activities and the relation between the in vitro activities and in vivo potency evaluated in man. Lipase activity ranged from 10 to 3600 units per unit, with 11 preparations containing less than 600 units per unit. The preparations with the highest lipase activities were llozyme, 3600, Kuzyme HP, 2330, Festal, 2073, Cotazym, 2014, and Viokase, 1636 units. Lipase activity in vitro correlated with potency in vivo for tablets and capsules, with tablets and capsules being effective in reducing steatorrhea by 56.1 +/- 9 per cent and 48.6 +/- 10 per cent (mean +/- S.E.M.) respectively, P less than 0.001. Enteric-coated tablets were less effective (20 +/- 13 per cent reduction, P greater than 0.02). The longer the gastric pH remained greater than or equal to 4 (r = 0.915, P less than 0.01) and the higher the average duodenal pH (r = 0.966, P less than 0.01), the more marked the reduction in steatorrhea.

Administration, Oral↗
PubMed1976

Gastric acid inactivation of erythromycin stearate in solid dosage forms.

The effect of hydrochloric acid at pH 1.2-3.2 ON ERYTHROMYCIN STEARATE AND COMMERCIAL DOSAGE FORMS OF ERYTHROMYCIN STEARATE WAS STUDIED. Under all conditions examined, erythromycin was readily dissolved from the stearate as hydrochloride, and rapidly lost its biological activity in solution. The inclusion of pepsin in the test systems did not affect the results. Although formulation differences somewhat affected the rate of destruction, acid lability was exhibited by all products examined, except enteric-coated tablets. Amounts of acid considered to be normal in the fasting stomach contents of adults during the time likely for a dose to remain in the stomach caused 70-90% destruction within 15 min after the shells started to rupture. Amounts of hydrochloric acid appreciably less than 1 mEq, representing abnormally small quantities even in the fasting state, caused destruction ranging from 30 to 70% of the doses in 15 min. These results are not reconcilable with published statements that the sensitivity of erythromycin to gastric acid is overcome by providing the antibiotic in the form of stearate salt.

Capsules↗
PubMed1976

Aspirin-induced gastritis and gastrointestinal bleeding.

Aspirin-induced gastritis and gastrointestinal hemorrhage were reviewed and discussed on the basis of currently available literature. Acute hemorrhagic gastritis occurs in from 50% to 70% of all patients taking aspirin, is not directly related to dose size, and can be severe enough to cause death in a few cases. No tolerance appears to ever develop. The mechanism that causes this bleeding is not definite, but the back diffusion of H+ ions accross the gastric barrier seems to bear primary responsibility, with physical erosion, prolonged platelet bleeding, and the effect of low pH values also being possible explanations. There appears to be less acid present in the stomach when bleeding occurs, but this is a masking effect of the aspirin that causes increased absorption of the H+ ions. Factors important in determining pharmaceutical formulation are method of administration, particle size of the aspirin, duration of contact between the drug and the mucosa, presence of buffers in the drug to raise the gastric pH, dissolution rate of the drug in the stomach, and ionization characteristics of the drug itself. Gastrointestinal blood loss caused by aspirin can be minimized by administering the drug in one of these forms:--a dilute solution of acetylsalicylate;--an intravenously injected solution;--a very rapidly dissolving and rapidly absorbed tablet;--a solution with sufficiently large amounts of antacid added;--a fine-grain, highly buffered aspirin tablet;--an enteric-coated tablet that does not dissolve in the stomach; or--an aspirin substitute such as acetaminophen.

Administration, Oral↗
PubMed1979

Relative systemic availability of sulfapyridine from commercial enteric-coated and uncoated sulfasalazine tablets.

The absorption of sulfapyridine after a single 2.0-Gm oral dose of sulfasalazine, the drug of choice in the treatment of inflammatory bowel disease, as commercial uncoated and enteric-coated and uncoated tablets was evaluated in four healthy male adults. The peak plasma concentration of sulfapyridine after the enteric-coated tablets occurred at 20 hours on the average (compared to 14 hours for the uncoated tablets) and was only 50% of that attained from the uncoated tablets (P less than 0.05). The low relative extent of systemic availability of sulfapyridine from the enteric-coated tablets (65.5 +/- 6.3 per cent, mean +/- S.E.) compared to uncoated tablets may be due to absorption rate-dependent presystemic metabolism, since the relative extent of sulfapyridine absorption was 92.7 +/- 6.2 per cent compared to uncoated tablets. These findings suggest that enteric-coated and uncoated tablets of sulfasalazine are not bioequivalent. It remains to be determined whether the clinical efficacy of sulfasalazine from enteric-coated tablets is affected.

Adult↗
PubMed1978

Influence of food on the absorption of acetylsalicylic acid from enteric-coated dosage forms.

The absorption of acetylsalicylic acid (ASA) from two different enteric-coated dosage forms, tablets (Premaspin) and granules (Reumyl), was studied in healthy volunteers under fasting and non-fasting conditions by following the plasma concentration and urine recovery of salicylates after single doses of ASA 1 g. Conventional tablets (Aspirin) were used as the reference. Under fasting conditions the absorption of ASA from the two different enteric-coated preparations was complete. Taken with food the enteric-coated tablets gave much lower plasma concentrations than under fasting conditions, and absorption was not complete in all subjects. In contrast, absorption from the enteric-coated granules was not influenced by the intake of food. It was concluded that enteric-coated granules of ASA permit more reproducible absorption than enteric-coated tablets.

Adult↗
PubMed1977

Comparative effects of antacids, cimetidine and enteric coating on the therapeutic response to oral enzymes in severe pancreatic insufficiency.

To provide a rational basis for pancreatic enzyme replacement therapy, we evaluated, in six patients with advanced pancreatic insufficiency, the effects of various treatment regimens on fecal fat and nitrogen balance and on duodenal recovery of ingested pancreatic enzymes after a solid test meal. The combination of cimetidine (an H2-receptor antagonist) and pancreatin, each given by mouth, produced significantly higher postprandial duodenal recoveries and concentrations of trypsin and lipase (P less than 0.05). Steatorrhea was reduced in all patients and abolished in four of the six. In the dosages used, neither enteric-coated enzymes nor supplemental neutralizing antacids were more effective than pancreatin alone in decreasing steatorrhea or improving duodenal enzyme delivery. Cimetidine may be a useful adjunct to oral pancreatic extract therapy in some patients with severe pancreatic insufficiency who fail to respond to pancreatic enzyme replacement alone.

Administration, Oral↗
PubMed1979

A pharmacokinetic study of doxapram in patients and volunteers.

1. Following intravenous bolus injections or brief infusions in healthy volunteers, plasma concentrations of doxapram declined in a multi-exponential fashion. The mean half-life from 4-12 h was 3.4 h (range 2.4-4.1h), the mean apparent volume of distribution was 1.5 1 kg-1 and the whole body clearance was 370 ml min-1. 2. Enteric-coated capsules of doxapram base were absorbed rapidly after an initial delay, and the systemic availability was about 60%. 3. Doxapram is extensively metabolized and less than 5% of an i.v. dose was excreted unchanged in the urine in 24 h. A metabolite (AHR 5955) was present in plasma in amounts comparable to the parent compound and had a similar half-life. 4. The disposition of doxapram appears to be similar in healthy volunteers and patients with respiratory failure. 5. The previously held belief that plasma concentrations fall rapidly when an infusion is stopped is only true following short duration infusions. The pharmacokinetic properties of doxapram are such that steady-state plasma concentrations will not be achieved for many hours with the recommended constant rate infusion régime.

Administration, Oral↗
PubMed1976

Ferrous sulphate.

Explore the source record for details and available documents.

Child, Preschool↗
PubMed1975

[On the influence of a special preparation of oxytetracycline and sodiumbituminosulfonates on amount and composition of skin surface lipids in acne vulgaris (author's transl)].

Two groups of 27 and 23 patients with acne vulgaris were first treated for a period of one week with 1 g oxytetracycline a day p.o. In a second treatment period of 6 weeks the first group received 100 mg oxytetracycline a day p.o. and the second group a combination of 100 mg oxytetracycline and 1.2 g sodiumbituminosulfonates a day p.o. In the third treatment period, similarly continued for 6 weeks, the method was reversed. Gastric juice-insoluble preparations were used for the investigation. All criteria for a double-blind study were considered. Amount and composition of the skin surface lipids were analysed before beginning the treatment, at the end of the 2nd and at the end of the 3rd treatment period. The combination of both agents in gastric juice-insoluble preparations suppresses to a great extent the known effects brought about by the substances separately, namely the reduction in free fatty acids and the decrease in the skin surface lipids. The findings also show that the reduction of the free fatty acids was in a limited time observed only in patients treated with 100 mg oxytetracycline a day p.o. if they had been treated in the beginning of this therapy with a higher dosage of tetracycline.

Acne Vulgaris↗
PubMed1976

[Galenical possibilities and problems in protraction of drug effects (author's transl)].

In recent years, dosage forms with sustained release have obtained a significant importance. The technological possibilities for manufacturing are described as coating, embedding and matrix procedures. The range of auxiliary substances, which are responsible for the retardation of drug activity, reaches from lipophilic compounds as lipoids, fatty alcohols and compounds which are forming hydrogels as cellulose derivatives and natural polysaccharides to synthetic polymers derived from acrylic acid. The formulation of the dosage forms requires particular care in respect to the amount of initial and maintenance doses. On account of technological processes, for example during manufacturing of tablets, under certain circumstances the liberation rate is altered. In vitro test methods allow comparisons only then when the results can be counter-checked by in vitro experiments. The release of drug follows different mechanisms, which are described, entirely or in part, to be reactions following the time law of zero or first order. In special cases, a linear correlation is observed as a function of square root of time. The calculation of given special equations for events within the dosage form is feasible from blood-level values.

Biological Availability↗