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At least 1,297 records · Page 72Linked to original sources
PubMed2005

Patients' preference for administration of endocrine treatments by injection or tablets: results from a study of women with breast cancer.

BACKGROUND: Endocrine therapies for advanced breast cancer include tablets and intramuscular injections. When treatments have similar efficacy and tolerability profiles, addressing preferences about routes of administration is important. PATIENTS AND METHODS: Two hundred and eight women>2 years post-breast cancer diagnosis were interviewed about their preferences for daily tablets or monthly intramuscular injections. Health-care professionals treating the women estimated patients' preferences. RESULTS: Sixty-three per cent of patients preferred tablets, 24.5% preferred the injection and 12.5% had no preference. The most cited reasons for tablet preference were convenience and dislike of needles; for injection preference, adherence and convenience. Variables associated with preferences were body mass index, educational level, attitudes towards injections and efficacy perceptions. Estimates about patients' preferences by health-care professionals varied widely. When asked to imagine scenarios where injections produced fewer hot flushes, or where two injections monthly improved efficacy, injection preference increased to 60.6% and 74.5%, respectively. Disturbingly, approximately 50% of patients admitted they sometimes forgot or chose not to take their current oral medication. CONCLUSIONS: The majority of breast cancer patients preferred hormone therapy via daily tablets rather than monthly injections. Information about side-effects or improved efficacy altered these preferences. Adherence to treatment cannot be assumed; patients' preferences about drug administration may influence this.

Administration, Oral↗
PubMed1983

Comparison of colloidal bismuth subcitrate tablets and liquid in duodenal ulcer healing.

A double-blind trial using 51 outpatients was aimed at comparing the effectiveness of colloidal bismuth subcitrate (C.B.S.) in tablet and liquid form in the healing of duodenal ulcer. Criteria of entry included endoscopically proven duodenal ulcer, duration of symptoms greater than 4 weeks, and the absence of other major systemic disease. Patients were given either C.B.S. tablets (1 four times daily) or C.B.S. liquid (5 ml four times daily) for 4 weeks. Ulcer symptoms and their relief were recorded by patients, along with data on cigarette, alcohol, and drug intake. Endoscopy was performed after 4 weeks to assess healing. By 4 weeks, 18 of 26 patients taking tablets (69%) and 19 out of 25 patients taking liquid (76%), had healed (p = 0.82). Symptomatic improvement was similar with both tablets and liquid. Smoking and analgesic ingestion did not influence healing rate. We conclude that C.B.S. tablets and liquid are equally effective in healing duodenal ulcer.

Adult↗
PubMed2007

The tablet formulation of lopinavir/ritonavir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect.

Lopinavir, an HIV protease inhibitor, is coformulated with ritonavir to enhance the bioavailability and pharmacokinetics of lopinavir. The original solid oral formulation of lopinavir/ritonavir, a soft-gelatin capsule (SGC), requires refrigerated storage, is taken as 6 capsules daily at the recommended adult dose, and is administered with food to maximize the bioavailability of lopinavir. Melt extrusion technology was used to produce a tablet formulation reducing the number of dosage units administered per day and simplifying storage requirements. Three studies assessed the bioavailability of tablet doses of lopinavir/ritonavir at 800/200 mg or 400/100 mg under different meal conditions compared with equal doses of the SGC after a moderate-fat meal. The tablet was bioequivalent to the SGC after a moderate-fat meal with respect to lopinavir and ritonavir areas under the concentration-time curve. Compared with the SGC formulation, the tablet formulation resulted in more consistent lopinavir and ritonavir exposures within and across studies and across meal conditions. The diminished food effect and decreased variability of the tablet are likely to result in more consistent lopinavir and ritonavir exposures, minimizing the likelihood of extreme high or low values compared with the SGC.

Adult↗
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↗
PubMed1989

Pharmacokinetics of a 5-aminosalicylic acid enteric-coated tablet and suppository dosage form.

An Eudragit-L coated oral 5-aminosalicylic acid (5-ASA; mesalazine) product (Mesasal), has been formulated to deliver 5-ASA to the distal small intestine and colon for the treatment of inflammatory bowel disease. The purpose of this study was to compare the pharmacokinetic profile of this product to sulphasalazine (SASP; Salazopyrin) and to assess the pharmacokinetics of a suppository 5-ASA dosage form. Twelve healthy volunteers randomly received four single doses of 5-ASA delivering formulations not less than 1 week apart. (a) Mesasal tablets, 2 x 250 mg, fasting; (b) Mesasal tablets, 2 x 250 mg, fed; (c) Salazopyrin tablets, 3 x 500 mg (corresponding to 576 mg 5-ASA), fasting; and (d) Mesasal suppository, 1 x 500 mg, fasting. Plasma 5-ASA and acetyl-5-ASA (Ac-5-ASA) concentrations were followed for 48 h and urine and faecal concentrations for 72 h. Mesasal tablets (fasting) produced a greater area under the concentration-time curve (AUC), peak and time to peak for both plasma 5-ASA and Ac-5-ASA than Salazopyrin. Median urinary recovery values were 21.7% for Salazopyrin and 35.5% for Mesasal (fasting) (P less than 0.01). This means that the systemic absorption was higher after Mesasal than after Salazopyrin. The total faecal recovery values were 38.3 and 26.5%, respectively (NS). Except for a delay of 1.5-.3 h in the time to peak of 5-ASA and Ac-5-ASA plasma levels, the pharmacokinetics of Mesasal tablets were essentially the same in fasting or fed subjects. Suppository administration of 5-ASA resulted in a low median urinary recovery of 10.8%.

Adult↗
PubMed2004

A novel option for dosing of proton pump inhibitors: dispersion of lansoprazole orally disintegrating tablet in water via oral syringe.

BACKGROUND: A new formulation of lansoprazole, the lansoprazole orally disintegrating tablet, rapidly disintegrates in water eliminating the need for swallowing whole pills. AIM: To assess the effect that dispersing the lansoprazole orally disintegrating tablet in water would have on lansoprazole pharmacokinetics. METHODS: Forty healthy adult men and women (18-43 years) received two single 15 mg lansoprazole orally disintegrating tablet doses separated by 3 days (one administered directly onto the tongue without water and one dispersed in water and administered orally via syringe) in a randomized, crossover fashion. Serial plasma samples were determined from 0 to 12 h for each dose. Ratios of central values for peak plasma exposure (C(max)) and mean overall extent of exposure (area under the plasma concentration) were used to compare the bioavailability. RESULTS: The two dosing regimens were bioequivalent, with the point estimate for area under the plasma concentration equalling 1.080 (confidence interval 1.012-1.152) and the point estimate for C(max) equalling 1.082 (confidence interval 0.961-1.218). CONCLUSIONS: Dispersing the 15 mg lansoprazole orally disintegrating tablet in water and administering the dose orally via syringe is bioequivalent to the 15 mg intact lansoprazole orally disintegrating tablet with respect to lansoprazole area under the plasma concentration and C(max). This dosing route provides an additional, convenient dosing option for lansoprazole.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2004

Mesalazine (5-aminosalicylic acid) micropellets show similar efficacy and tolerability to mesalazine tablets in patients with ulcerative colitis--results from a randomized-controlled trial.

BACKGROUND: Formulations containing 5-aminosalicylic acid, such as mesalazine, are the gold standard of treatment for mild-to-moderate ulcerative colitis. Current oral regimens require the use of large tablets and frequent dosing to reach the recommended treatment dose. Mesalazine micropellets were designed to allow less frequent dosing in an easier to swallow formulation. AIM: To compare the efficacy of mesalazine micropellets with the tablet formulation in patients with mild-to-moderate ulcerative colitis. METHODS: This phase 2, double-blind, active-controlled, parallel-group, multiple dose clinical trial randomized 362 patients to either mesalazine micropellets or tablets, at a dosage of 3 g/day. The primary efficacy end-point was the incidence of clinical remission within 8 weeks, defined as the sum of clinical activity index components 1-4 (CAI(C1-4)) < or = 2. RESULTS: CAI(C1-4) decreased significantly in both treatment groups within 8 weeks. The micropellet formulation showed confirmatory non-inferiority with statistical significance compared with the tablet formulation, with regard to the incidence of clinical remission (odds ratio in according-to-protocol population 1.008; 95% CI: 0.623-1.632). There was no significant difference in the incidence of adverse events. CONCLUSIONS: The mesalazine micropellet formulation is as effective as tablets in patients with mild-to-moderate ulcerative colitis, enabling a larger dose to be taken comfortably and conveniently, thereby potentially improving patient compliance, treatment response and quality of life.

Administration, Oral↗
PubMed1986

A comparison of the clinical and bronchodilating effects of plain and slow-release tablets of terbutaline at steady state.

The clinical efficacy, the bronchodilating effect and the side effects of two oral forms of terbutaline were compared in a double-blind, cross-over study involving ten patients with chronic reversible airways obstruction. The administration of plain-tablets, containing 2.5 mg terbutaline sulphate, three times daily at 6 h intervals was compared to the administration of slow-release (SR) tablets, containing 5 mg terbutaline sulphate, every 12 h. Each course of treatment lasted for 7 days. Treatment with SR-tablets resulted in significantly higher lung function values in the morning (PEFR at home and FEV1 at the lung function laboratory on day 7). There were no significant differences between the two forms with regard to symptom score, extra use of rimiterol aerosol, heart rate or blood pressure. The plasma terbutaline concentration in the morning of the seventh treatment day was significantly higher during SR-tablet treatment. The plasma terbutaline concentration curve showed a smaller peak/trough ratio for the SR-tablets.

Administration, Oral↗
PubMed1995

Oxytocin and desamino-oxytocin tablets are not stable under simulated tropical conditions.

OBJECTIVES: This study is part of a programme on reduction of postpartum haemorrhage. Buccal oxytocin and desamino-oxytocin administration with a favourable effect on both blood loss and maternal morbidity and mortality were regarded as possible treatments for use in tropical countries. The stability of buccal oxytocin and desamino-oxytocin under tropical conditions was unknown and therefore tested in this study. STUDY METHODS: The 'experimental shelf lives' of buccal oxytocin and desamino-oxytocin were examined by exposing the tablets to seven artificially controlled conditions. Samples were analysed by high performance liquid chromatography to determine the content of oxytocin and desamino-oxytocin at nine different times during the period of 1 year. RESULTS: Oxytocin and desamino-oxytocin are fairly stable under refrigeration. Instability for both drugs was detectable after 20 weeks' storage under humid conditions, independent of temperature. Desamino-oxytocin is more sensitive to light exposure; its concentration declines to 55.6% of the stated amount after 1 year of exposure to light compared to 85% in the case of oxytocin. Oxytocin packaged as supplied by the manufacturer were stable for 21 weeks when exposed to simulated humid (75% relative humidity) conditions. At 40 degrees C and 25% relative humidity there is no difference in stability between tablets in sealed aluminium packs as supplied by the manufacturer and unpackaged tablets. CONCLUSIONS: Tropical conditions make oxytocin and desamino-oxytocin tablets unstable, with humidity as the most adverse factor. The oxytocin tablets were partially protected from the harmful effect of humidity by sealed aluminium package.

Drug Packaging↗
PubMed1982

A time-related study of intake pattern of fluoride tablets among Swedish preschoolchildren and parental attitudes.

The principal aim of this study was to investigate sodium fluoride tablet consumption and its variability over a particular period. Information was collected from questionnaires sent in 1975 and 1980 to all parents of children born in Lund, Sweden, in 1967 and 1972 and still resident in this city, where drinking water contains 0.2 parts/10(6) F. The results showed that 69% of the children born in 1967 (n = 373) had taken tablets at some time during the period 1/2-7 years of age and that 13% had consumed tablets regularly for minimum 5 1/2 years. The corresponding figures for children born in 1972 (n = 474) were 51% and 12%, respectively. Sporadic consumers were responsible for the main difference (15%) between the two populations. A selection of parents from the 1975 and 1980 materials was made with respect to duration of consumption and level of parental education. The frequency of non-users had increased mostly among families with a higher parental education. For those parents who had not given their children tablets or had ceased to do so, the 1980 inquiry was enlarged with questions about reasons for this. The item marked most frequently (56%) implied that fluoride may be dangerous to swallow. Another 13% responded that they had not been recommended to give their children tablets. However, topical use of fluoride in toothpaste during preschool age and in mouthrinses from 6 years of age is, according to the present study, well accepted.

Adult↗
PubMed1989

Dental fluorosis among participants in a non-supervised fluoride tablet program.

The aim of the present study was to describe the intraoral pattern of dental fluorosis among fluoride tablet consumers. One hundred and forty-two children, of whom 56 had participated in a fluoride tablet program of 0.5/1.0 mg NaF per day were examined blindly for possible fluoride-induced enamel changes. A low prevalence of dental fluorosis was found among non-participants. The later in life the tooth was formed, the higher was the prevalence. The subjects who had participated in the fluoride tablet program showed a significantly higher prevalence of fluorosis. They could be divided into three groups: Group 1 exhibited a tooth prevalence pattern not statistically different from that of the non-participants, group 2 showed dental fluorosis in almost all teeth except in those formed before the start of the tablet program. In group 3 the early and the late formed teeth showed very little fluorosis while those formed in the few years just after the initiation of the fluoride tablet intake were affected by fluorosis.

Child↗
PubMed1980

Some effects of bone meal and NaF tablets on the composition of saliva.

Whole saliva was collected from dental students while: 1) chewing paraffin, 2) sucking bone meal tablets, and 3) sucking NaF tablets. Initial pH, content of ionized and total calcium and content of fluoride in saliva were measured. As compared to paraffin stimulated saliva, the sucking of bone meal tablets caused a decrease in salivary pH, ionized calcium and fluoride. Sucking NaF tablets caused a fall in initial pH and an increase in total calcium, while the amount of ionized calcium remained unchanged. The content of fluoride was high in saliva during sucking of NaF tablets.

Biological Products↗
PubMed2004

Durable efficacy of metformin/glibenclamide combination tablets (Glucovance) during 52 weeks of open-label treatment in type 2 diabetic patients with hyperglycaemia despite previous sulphonylurea monotherapy.

Oral anti-diabetic combinations that address insulin resistance and beta-cell dysfunction (e.g. metformin and glibenclamide) represent a rational therapeutic option for patients uncontrolled on monotherapy. A 52-week, open-label extension to a double-blind study evaluated metformin-glibenclamide combination tablets (Glucovance) in 477 patients with hyperglycaemia despite sulphonylurea therapy. Reductions in HbA1C were maintained, with a mean reduction of -1.7% after 52 weeks, compared with the baseline value for the double-blind trial. Eighty-five patients receiving 4 x 500 mg/2.5 mg tablets daily displayed a marked improvement in HbA1c following up-titration to a regimen of 2 x 500 mg/2.5 mg + 3 x 500 mg/5 mg tablets. Lipid profiles improved significantly. The combination tablets were well tolerated: 11.1% of patients reported hypoglycaemic symptoms (all either mild or moderate severity). No patient withdrew or required pharmacologic intervention for hypoglycaemia. Metformin-glibenclamide combination tablets are an effective and well-tolerated therapeutic option for intensifying oral anti-diabetic therapy.

Administration, Oral↗
PubMed2006

Beta-cell response to metformin-glibenclamide combination tablets (Glucovance) in patients with type 2 diabetes.

This exploratory double-blind, randomised, 20-week study evaluated the mechanism of action of metformin-glibenclamide combination tablets (Glucovance) vs. metformin and glibenclamide in 50 type 2 diabetes patients inadequately controlled by diet and exercise. A glycaemic target of HbA1C 7.0% was used. Final HbA(1C), fasting glucose and post-oral glucose tolerance test (OGTT) glucose were similar between groups, although average doses of metformin and glibenclamide from combination tablets (708 and 3.5 mg) were lower than monotherapy doses (1500 and 6.6 mg). Second-phase insulin during a hyperglycaemic clamp increased by 93% with combination tablets, 36% with metformin and 46% with glibenclamide. The insulin response post-OGTT was more rapid with the combination tablets vs. glibenclamide. First-phase insulin responses improved modestly in all groups, possibly due to reduced glucotoxicity. Changes in insulin sensitivity were minor. Larger beta-cell responses between combination tablets and glibenclamide may reflect more rapid glibenclamide absorption.

Adult↗
PubMed1984

Absorption of acetylsalicylic acid from enteric-coated tablets in relation to gastric emptying and in-vivo disintegration.

The absorption of acetylsalicylic (ASA) acid from enteric coated tablets was studied in relation to gastric emptying and in-vivo disintegration. ASA tablets labelled with 51Cr were given to six healthy subjects under fasting and non-fasting conditions. The position and disintegration of the 51Cr-labelled tablets was followed by external radiation measurement and the amount of salicylic acid in blood and urine was analysed. The absorption of ASA from the studied enteric coated tablets was usually correlated with gastric emptying and in-vivo disintegration. However in some cases the absorption can be delayed between 10-20 h even if gastric emptying and disintegration of the tablet have occurred.

Aspirin↗
PubMed1985

The effect of some excipients on the physical properties of a paracetamol tablet formulation.

The effects of the addition of the excipients sorbitol, sodium lauryl sulphate and Aerosil on the physical properties of a paracetamol tablet formulation have been evaluated. Increase in the concentration of sorbitol and sodium lauryl sulphate caused a decrease in the hardness with a corresponding increase in the friability, disintegration and dissolution rates of the tablets. The mode of incorporation of the excipient, Aerosil, greatly influenced the physical properties of the paracetamol tablets. When added internally, the tablets' strength decreased while the friability, disintegration and dissolution rates increased. However, when Aerosil was added externally, the strength of the tablets increased while their friability, disintegration and dissolution rates decreased.

Acetaminophen↗
PubMed1988

Oesophageal transit of small tablets.

Oesophageal transit has been studied in six asymptomatic subjects aged 29-80 years. Using gamma scintigraphy, the transit of a liquid and five small tablets was monitored in each subject. All the subjects exhibited normal liquid swallowing, with 50% oesophageal clearance times of less than 5 s. In three subjects all the tablets passed through the oesophagus within 6 s, but transit was prolonged in 60% of the swallows in the other subjects. Tablet hold up occurred more frequently in the elderly. An additional drink of water cleared all lodged tablets into the stomach. To minimize possible mucosal irritation, the taking of even small tablets should be followed by an additional drink of water.

Adult↗
PubMed1989

Effects of the mechanical energy of multi-tableting compression on the polymorphic transformations of chlorpropamide.

The effects of the mechanical energy of tableting compression on the polymorphic transformation of chlorpropamide have been examined. A single-punch eccentric tableting machine with a load cell and a non-contact displacement transducer were used to measure compression stress, distance and energy. An amount of 100 mg of the stable form A or the meta-stable form C of the drug was loaded into the press and the sample compressed with a compression stress of 196 MPa at room temperature (20 degrees C). The compression cycle was repeated from 1 to 30 times. The powder X-ray diffraction profiles of the deagglomerated compressed sample powder were measured to calculate the polymorphic content. The results on forms A and C suggested that both forms were transformed into each other in the solid state by mechanical energy during tableting. The contents of forms A and C reached equilibrium at a constant value above 100 J g-1 of compression energy after more than 10 cycles. After 30 tableting cycles of forms A and C, the contents of A, C and the non-crystalline solid were almost constant at about 45, 25 and 30%, respectively. The compression energies were estimated to be about 500-600 J g-1. From the results it seems that the transformation mechanism of forms A and C during tableting were as follows. The crystal form of A or C was converted to a non-crystalline solid by the mechanical energy, and the solid was then transformed into form A or C.

Chemical Phenomena↗