Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “TABLETS”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 1,099 records · Page 61Linked to original sources
PubMed1996

[The relative bioavailability of paracetamol in suppositories in comparison to tablets].

Relative Bioavailability Studies on Paracetamol in Suppositories as Compared to Tablets. Relative bioavailabilities of 250 mg paracetamol (CAS 103-90-2) in ben-u-ron 125 mg and ben-u-ron 250 mg suppositories were determined in comparison with that of cut-in-half Benuron tablets 500 mg in an open intraindividual 3-period-changeover-study in 18 healthy volunteers. Plasma concentrations of paracetamol were analyzed by means of a specific and sensitive HPLC-method with UV-detection. For the assessment of the bioavailability AUC, Cmax, tmax and HVD (half value duration) were used as pharmacokinetic characteristics. Relative bioavailability of paracetamol was 102% for 125 mg and 93% for 250 mg suppositories, compared with that of cut-in-half 500 mg tablets. Mean maximum paracetamol plasma concentrations (Cmax) were determined as 2.1 micrograms/ml (CV = 31%; (CV = Coefficient of Variation), 2.0 micrograms/ml (CV = 27%) and 3.5 micrograms/ml (CV = 27%) after administration of 125 mg and 250 mg suppositories and 500 mg cut-in-half tablets, respectively. These maximum concentrations were achieved 2.2 +/- 0.7, 1.8 +/- 0.7 and 0.6 +/- 0.3 h (tmax) after administration of the respective preparations. The corresponding HVD-values were 3.8 +/- 1.0, 3.5 +/- 0.9 and 1.8 +/- 0.8 h, respectively. Extent of bioavailability of paracetamol (dose: 250 mg) following administration of 125 mg as well as 250 mg suppositories in comparison with 500 mg tablets was shown to be equivalent. The results obtained in this study confirm the adequate bioavailability of both suppositories compared with tablets. On the other hand both suppository preparations were assessed as being bioequivalent concerning AUC and Cmax.

Acetaminophen↗
PubMed1997

Pharmacokinetics of the controlled-release nisoldipine coat-core tablet formulation.

UNLABELLED: The pharmacokinetics, safety, and tolerability of the novel once-daily "coat-core" formulation of the calcium antagonist nisoldipine were investigated in 4 randomized nonblind studies A-D in 52 healthy volunteers. Immediate-release or intravenous formulations were administered as reference in 3 studies. The objective of the present studies was to select the optimum controlled-release formulation (A), compare it to the immediate-release tablet at steady-state (B), determine the absolute bioavailability (C), and investigate bioequivalence after a small change in composition (D). Comparative pharmacokinetic properties: Mean residence time and apparent terminal half-life of nisoldipine in the coat-core formulation were significantly increased in comparison to administration via the intravenous route or the oral immediate-release formulation. Concentration profiles could be described with a 3-segment input model. Steady-state conditions were established with the second dose of nisoldipine coat-core and accumulation from first dose to steady-state accounted for 46% as expected due to the contribution of AUC beyond 24 h. At steady-state the coat-core formulation produced a plateau-shaped profile of nisoldipine plasma concentrations throughout the 24 h dosing interval and the peak-trough fluctuation was reduced by approximately 4-fold, compared to the immediate-release tablet in a b.i.d. regimen. While the absolute bioavailability of the drug in the coat-core tablet was 5.5%, its relative bioavailability was greater by 1.5-fold compared to the immediate-release tablet. This can be attributed to release of drug in the colon where the contribution of the gut wall to presystemic metabolism is reduced resulting in an increase in bioavailability as compared to stomach and small intestine. The intersubject variability of nisoldipine coat-core pharmacokinetics was comparable to that of the immediate-release tablet. The within-subject (intraindividual) variability was considerably smaller. Based on its pharmacokinetic profile the side chain-hydroxylated metabolite M 9 is not expected to contribute significantly to the antihypertensive effect of nisoldipine coat-core. In vitro/in vivo correlation: There was a rank order correlation between in vitro release rate of 3 different nisoldipine coat-core formulations and their noncompartmental pharmacokinetic parameters, a decrease in dissolution rate leading to increased bioavailability in vivo. Likewise, the mean dissolution times in vitro and in vivo were correlated in rank order. A linear (level A) correlation could be established within approximately 0-6 hours (in vitro) corresponding to 0-12 hours in vivo. The change in slope of the correlation curve after approximately 12 hours (in vivo) most likely reflects changes in both rate and extent of nisoldipine absorption in different sections of the gastrointestinal tract. SAFETY: In the present studies the drug was safe and well tolerated, adverse events related to peripheral vasodilatation being less frequent with the coat-core tablet compared to intravenous or immediate-release formulations.

Adult↗
PubMedDate not supplied

Determination of reserpine and rescinnamine in Rauwolfia serpentina powders and tablets: collaborative study.

A liquid chromatographic (LC) method for determining reserpine and rescinnamine in Rauwolfia serpentine powders and tablets, which uses fluorescence detection, was subjected to a collaborative study. The procedure for extraction and purification is a simplified version of that used in the current official method for analysis of these products. LC separations are performed on a normal-phase column. The mobile phase is methanol to which a small volume of an aqueous solution of 1-pentanesulfonic acid sodium salt can be added to achieve desired elution characteristics. Reserpine and rescinnamine elute at approximately the same time but can be individually quantitated by appropriate settings of the fluorescence detector. Reserpine is determined at an excitation wavelength of 280 nm and an emission wavelength of 360 nm, because rescinnamine is completely non-fluorescent at these wavelengths. Rescinnamine is determined at an excitation wavelength of 330 nm and an emission wavelength of 435 nm, because reserpine is completely nonfluorescent at these wavelengths. The following materials were used for the study: one sample of United States Pharmacopeia (USP) standard R. serpentine powder, one tablet type labeled as containing 100 mg R. serpentine and 2 tablet types labeled as containing 50 mg R. serpentine. For each of the 4 materials, 2 pairs of blind duplicates were prepared. Three materials were analyzed in duplicate by 8 laboratories. One of the 2 tablets labeled to contain 50 mg R. serpentine was analyzed only by 7 of 8 participating laboratories. Average combined content of reserpine and rescinnamine was 0.144% for the USP raw material and 0.132, 0.135, and 0.137% for the 3 commercial tablets. Reproducibility relative standard deviation values were 5.72, 5.93, 8.61, and 3.48% and repeatability relative standard deviation values were 2.57, 4.87, 3.19, and 1.99% for the 4 samples. The Associate Referee conducted a study to determine recoveries of reserpine plus rescinnamine by this method from mixtures simulating sample extracts. Average recovery of 15 determinations was 100.1%, with a relative standard deviation of 1.3%. The LC method for determination of reserpine and rescinnamine in R. serpentine powders and tablets has been adopted first action by AOAC INTERNATIONAL.

Chromatography, Liquid↗
PubMed2007

Lower weight gain with the orally disintegrating olanzapine than with standard tablets in first-episode never treated psychotic patients.

OBJECTIVE: A post-hoc analysis of the data from a randomised clinical trial involving prescription of antipsychotic treatment to never treated first-onset psychotic patients was used to compare the weight change after 6-week olanzapine treatment (standard tablets vs. orally disintegrating formulation). METHOD: In the subgroup of 38 patients randomised to olanzapine, standard olanzapine tablets were non-randomly and consecutively prescribed to the first 19 patients, with the orally disintegrating formulation being prescribed to the following 19 patients. RESULTS: After 6-week treatment with olanzapine, a significant higher increase in weight was noted in those patients on standard tablets (mean weight increase 6.3 +/- 1.9 Kg) as compared to those on orally disintegrating olanzapine (mean weight increase 3.3 +/- 3.2 Kg) (F = 7.7; p = 0.009). BMI increase was also significantly higher in the olanzapine tablet group (mean increase of 2.1 Kg/m(2) as compared with 1.1 Kg/m(2) in the orally disintegrating group) (F = 4.7; p = 0.036). Substantial weight gain (SWG) (> or =7% increase from baseline weight) was noted in 84.2% (n = 16) of the olanzapine tablet patients and in 31.6% (n = 6) of the orally disintegrating olanzapine patients, with the olanzapine tablet group showing a significant increase in the mean percentage of weight gain (F = 4.0; p = 0.014). CONCLUSIONS: Partial sublingual absorption occurring with orally disintegrating olanzapine may bypass gastrointestinal metabolisation and hence lead to differences in metabolite versus parent compound ratios. However, the need arises to replicate the present study with a longer follow-up.

Administration, Oral↗
PubMed1995

Effect of food on the oral bioavailability of isosorbide-5-mononitrate administered as an extended-release tablet.

We evaluated the effect of a high-fat breakfast and gastric emptying rate on the oral bioavailability of a isosoribide-5-mononitrate (5-ISMN) controlled-release tablet formulation (IMDUR 60-mg tablets, Astra Hässle AB, Mölndal, Sweden) relative to an oral solution in 18 healthy men. Gastric emptying was monitored by radiotelemetry using the Heidelberg capsule technique. After administration of the 5-ISMN 60-mg solution, absorption was rapid with mean peak plasma 5-ISMN concentrations of 1533 ng/mL achieved in less than 1 hour. In contrast, after administration of IMDUR 60-mg tablets, the drug was more slowly absorbed, reaching mean peak plasma concentrations of 541 ng/mL in 3 to 4 hours. The bioavailability of 5-ISMN from IMDUR tablets under fasted conditions was approximately 78% relative to the solution; and, in the presence of food, the bioavailability was slightly increased to 86% (P = .057). The mean gastric residence time of IMDUR tablets under fasted conditions was 68 minutes, and in the presence of food was increased to 478 minutes, with 9 of the 18 subjects having gastric emptying delayed for at least 600 minutes. We conclude that in the presence of food, gastric emptying time is considerably increased causing a delay in drug absorption and a slight increase in the bioavailability of 5-ISMN from this controlled-release tablet formulation, however this effect is not clinically relevant.

Administration, Oral↗
PubMed1983

Plasma concentration of disopyramide given as capsules and controlled release tablets.

Steady state plasma levels and clinical effects of disopyramide have been compared following administration of standard capsules and controlled release (CR) tablets. Nineteen patients (29-70 years) with atrial or ventricular arrhythmias were treated for two weeks with disopyramide capsules 200 mg t.i.d. and then with CR tablets 300 mg b.i.d. for 14 weeks. After treatment either with capsules or CR tablets, plasma concentrations of disopyramide and its metabolite N-deisopropyldisopyramide were similar within 1 dosage interval. Maximum and minimum concentrations of the parent drug were 10.1 +/- 0.9 mumol/l (mean +/- SEM) and 5.7 +/- 0.5 mumol/l with CR tablets, and 10.2 +/- 0.5 mumol/l and 5.6 +/- 0.5 mumol/l with standard capsules. The bioavailability of disopyramide was the same after capsules and CR tablets. Disopyramide, independent of the formulation, produced good antiarrhythmic effects. The side-effects reported on questioning were mainly of the anti-cholinergic type and there was no significant difference between the formulations with respect to their incidence, type or severity. Of 16 patients who stated a preference for one of the dosage forms, 11 prefered the CR tablets. The study confirms the good antiarrhythmic effect of disopyramide and shows that the CR preparation permits twice daily administration of disopyramide.

Adult↗
PubMed1998

Double-blind placebo controlled trial of dextrose tablets and nicotine patch in smoking cessation.

In a placebo-controlled double-blind trial 308 smokers were individually randomly allocated to one of four groups: 1) 3 g dextrose tablets and 15 mg nicotine transdermal patch; 2) dextrose and placebo patch; 3) placebo tablets and nicotine patch; 4) placebo tablets and placebo patch. Patients were scheduled to attend weekly smokers clinic sessions starting 1 week before the quit date and continue for 4 weeks after that date. The primary outcome variable was biochemically verified abstinence at the final session, four weeks after the scheduled quit date. The proportion of smokers abstinent in the four groups was as follows: 49% - dextrose plus active patch; 44% - dextrose plus placebo patch; 36% - placebo tablet plus active patch; 30% - placebo tablet plus placebo patch. The difference between the dextrose and placebo tablets (13%) was statistically significant (P < 0.01, one-tailed); the difference between the active and placebo patches (6%) was not. There was no significant difference between the effect of the dextrose when accompanied by active versus placebo patches. There was no significant effect of dextrose on weight. The results suggest that dextrose supplementation to the diet may be a cheap and simple aid to giving up smoking. Further research is now needed to establish its long-term efficacy.

Adolescent↗
PubMed1998

Lack of bioequivalence of a generic mefloquine tablet with the standard product.

OBJECTIVE: To assess the bioequivalence between a generic tablet of mefloquine (Mephaquin = M1) with the reference tablet (Lariam = M2) in healthy volunteers. METHODS: This open label, randomized two-way crossover study was performed in a single centre. Following an overnight fast, eighteen healthy volunteers received a single oral dose of 750 mg mefloquine either in the form of three M1 lactabs or three M2 tablets. Serial blood samples were collected up to 8 weeks after drug administration. Plasma samples were analysed for mefloquine and its carboxylic acid metabolite using liquid chromatography and subsequent tandem mass spectrometry (LC-MS/MS). The pharmacokinetic parameters of mefloquine and its metabolite were estimated by non-compartmental methods. RESULTS: The pharmacokinetics of mefloquine after administration of M1 and M2 tablets were significantly different as reflected by the respective mean values of maximum plasma concentration (Cmax 656 vs 1018 ng x ml(-1)), time to reach maximum concentration (tmax 46 vs 13 h) and area under the plasma concentration-time curve (AUC0-->infinity 338 vs 432 microg x h x ml(-1)). No significant differences existed between the elimination half-lives of the two formulations (394 vs 396 h). The relative bioavailability (M1 vs M2) was 0.78 and ranged from 0.38 to 1.37. Bioequivalence could not be demonstrated for log-transformed data of AUC0-->infinity or AUC0-->last within a predefined range of 80-125% and for Cmax within a range of 70-143%. CONCLUSIONS: The observed differences in Cmax, tmax and AUC are consistent with a slower rate and lower extent of mefloquine absorption after administration of M1. Statistical evaluation of these kinetic data showed that the M1 tablet is not bioequivalent to the M2 tablet. Clinical consequences of this finding cannot be excluded.

Administration, Oral↗
PubMed1994

A prospective randomized clinical trial comparing a new oral sustained-release ritodrine with conventional tablets.

OBJECTIVES: Evaluation of maternal metabolic and cardiovascular responses to treatment with the new sustained-release oral ritodrine as compared with the conventional tablets. METHOD: Thirty-two pregnant patients who had successful intravenous tocolysis were randomly assigned to treatment with either ritodrine tablets or sustained-release capsules. After 5 days of the randomly determined first oral treatment each patient was shifted to the alternate ritodrine formulation for a further 5-day course. Each patient underwent metabolic and non-invasive hemodynamic evaluation. RESULTS: Echocardiographic parameters during treatment with ritodrine tablets were not significantly different from during sustained-release capsules. Mean systolic blood pressure increased significantly during peak drug activity in patients treated with ritodrine tablets and not during treatment with the sustained-release form. Fasting plasma glucose levels were higher in patients on conventional tablets therapy than in patients on sustained-release ritodrine therapy (88.9 +/- 9 mg/dl vs. 78.7 +/- 8 mg/dl, P < 0.05) while levels following a 50-g oral glucose challenge test did not differ significantly (135 +/- 32 mg/dl vs. 124.5 +/- 27 mg/dl) CONCLUSIONS: Because of fewer metabolic and cardiovascular side-effects, the new oral therapy offers some advantages over the presently available tablets.

Administration, Oral↗
PubMed2002

The effect of tablet moistening on labor induction with intravaginal misoprostol: a randomized trial.

OBJECTIVE: To estimate whether a dosage of 50 microg of misoprostol tablets moistened with 3% acetic acid and administered intravaginally is more efficacious for labor induction than a similar dosage regimen using dry tablets. METHODS: A total of 177 women who presented with an indication for cervical ripening and labor induction were randomly assigned to one of two treatment groups: 1) intravaginal misoprostol in dry tablet form, or 2) intravaginal misoprostol moistened with 1 mL of 3% acetic acid solution. The primary outcome assessed was the interval from start of induction to vaginal delivery. To detect at least a 3.5-hour difference in the primary outcome with 80% power, 87 subjects were required in each group. RESULTS: Among 162 patients evaluated, 80 were allocated to the misoprostol dry group and 82 to the misoprostol moistened group. No significant difference was noted for the mean +/- standard deviation interval to vaginal delivery: 1130 +/- 636 minutes for the group who received dry tablets and 1004 +/- 636 minutes for those who received moistened misoprostol tablets (P =.25). Additionally, no statistically significant differences were noted between the groups with respect to need for oxytocin, proportion of patients delivered after a single dose, intrapartum complications (including tachysystole and uterine hyperstimulation), mode of delivery, or perinatal outcomes. CONCLUSION: Tablet moistening with 3% acetic acid solution does not seem to improve the efficacy of intravaginally administered misoprostol for labor induction.

Acetic Acid↗
PubMed2001

Effect of encapsulation on absorption of sumatriptan tablets: data from healthy volunteers and patients during a migraine.

BACKGROUND: Some comparative trials of selective serotonin 1B/ID-agonists in migraine have reported -15% lower efficacy for sumatriptan tablets than that reported in placebo-controlled trials. OBJECTIVE: This study was designed to test the hypothesis that the encapsulation methods used to mask active drug may delay absorption of sumatriptan from dosing to 2 hours after dosing (the traditional end point in clinical trials of migraine treatment), an effect that may be enhanced by migraine-associated gastric stasis. METHODS: Two randomized, open-label, 2-way crossover trials were conducted to evaluate the absorption and bioequivalence of conventional 50-mg sumatriptan tablets and encapsulated 50-mg sumatriptan tablets in supine, fasted, healthy volunteers (Glaxo Wellcome protocol SUM40270) and supine patients experiencing a migraine (Glaxo Wellcome protocol SUM40268). Absorption was assessed by calculating the area under the plasma concentration-time curve from dosing to 2 hours after dosing (AUC2) and the times to first measurable plasma concentration, 10 ng/mL, 20 ng/mL, and maximum plasma concentration. Data for the AUC from time zero to infinity and maximum plasma concentration were used to assess standard bioequivalence, which is considered to occur when the 90% CIs for the geometric mean treatment ratios (test/reference) fall between 0.8 and 1.25. RESULTS: Study 1 included 26 healthy subjects (73% men, 27% women; mean age, 39.1 years), and study 2 included 30 patients with migraine (67% women, 33% men; mean age, 42.7 years). Sumatriptan absorption was delayed with the encapsulated tablet compared with the conventional tablet 0 to 2 hours after dosing, particularly during a migraine. AUC2 values with encapsulated sumatriptan compared with the conventional tablet were 21% lower in healthy volunteers (ratio of capsule/tablet, 0.79; 90% CI, 0.588-1.050) and 27% lower in patients experiencing a migraine (ratio of capsule/tablet, 0.73; 90% CI, 0.519-1.023). Standard bioequivalence was demonstrated in both healthy volunteers and patients experiencing a migraine. CONCLUSIONS: Encapsulation delayed absorption of sumatriptan 0 to 2 hours after dosing, particularly during a migraine. This delay in absorption of the encapsulated form may account for the lower efficacy of sumatriptan in some comparative studies.

Adult↗
PubMedDate not supplied

Evaluation of the safety, tolerability, and efficacy of meloxicam tablets in patients with osteoarthritis.

This 12-week, open-label, multicenter study assessed the safety, tolerability, and efficacy of the tablet formulation of meloxicam 15 mg, a new, nonsteroidal antiinflammatory drug (NSAID), in patients with confirmed osteoarthritis (OA) of the hip or knee. Meloxicam differs from established NSAIDs in its preferential activity against cyclooxygenase type 2 compared with cyclooxygenase type 1. One hundred thirty-nine patients were given meloxicam tablets 15 mg once daily. Data were analyzed using an intent-to-treat analysis. Assessments of global tolerability at the end of the study showed meloxicam tablets to be well or very well tolerated by 83% of patients, with only 4% rating the tablets poorly. This finding was supported by the low incidence of adverse events. Only 11% of patients discontinued therapy due to gastrointestinal adverse events, and no serious gastrointestinal adverse events related to meloxicam 15-mg tablets occurred during treatment. Efficacy results showed significant improvement from baseline, with 41% of patients experiencing mild or no pain by the end of the study. In conclusion, the tablet formulation of meloxicam 15 mg is well tolerated and effective in patients with moderate-to-severe, clinical confirmed OA of the hip or knee.

Adult↗
PubMed1994

Controlled drug release of highly water-soluble pentoxifylline from time-limit disintegration-type wax matrix tablets.

A pulsatile drug release system with a dry-coated tablet containing pentoxifylline was investigated for controlling drug release in the gastrointestinal tract. The system consisted of a core tablet with disintegrator and outer layer, which obtained compression from the ground mixtures of pentoxifylline and behenic acid. Drug release from a dry-coated tablet was investigated at 37 degrees C in JPXII 2nd fluid at pH 6.8. The drug release from the outer layer was fitted to the Cobby model. The drug release from the wax matrix increased significantly after tablet distintegration; therefore, the drug release profiles showed typical sigmoidal curves. The disintegration time depended on the weight fraction of the core tablet, and the drug release rate after disintegration increased with increasing drug concentration in the core tablet. The relationship between the time required for 50% drug release and the disintegration time was linear, indicating that the drug release rate was controlled by regulating the disintegration time.

Delayed-Action Preparations↗
PubMed2001

Comparison of deltamethrin tablet formulation with liquid deltamethrin and permethrin for bednet treatment in The Gambia.

The study aim was to compare three formulations, tablet deltamethrin, liquid deltamethrin and liquid permethrin, for their impact on vector behaviour and persistence. Product acceptance, perceived side-effects and user's perceptions of effectiveness were also investigated. At the beginning of the 1998 rainy season, 255 nets in a Gambian village were dipped in one of the three insecticides. Chemical residue analysis immediately after dipping showed that the target doses were reached for the liquid insecticides, but tablet deltamethrin deposited significantly less. Insecticide persistence at 5 months, however, was highest for the tablet formulation. Susceptibility tests established that Anophelines in this area were sensitive to both insecticides. All three formulations appeared effective as very few live Anophelines, or other mosquitoes, were caught under the treated nets. This conclusion was supported by the bioassay data with both deltamethrin formulations giving over 90% mortality soon after dipping and at 3 months, and at 5 months 70.8 and 79.6% were obtained for deltametrin liquid and tablet, respectively. Permethrin appeared less effective at all times (72.4, 86.8, 59.0%). There were no serious side-effects reported by the villagers following dipping. All three treatments were perceived as effective by the majority (92%) of users and most (93%) wanted to use the insecticide again. Deltamethrin tablets thus appear as good as permethrin for treating bednets in The Gambia. In addition, a tablet formulation is considerable easier to pack and distribute.

Animals↗
PubMed2002

Zolmitriptan orally disintegrating tablet is effective in the acute treatment of migraine.

A new formulation of zolmitriptan has been developed that dissolves on the tongue without the need for additional fluid intake. In this double-blind, parallel study, 471 patients were randomized to receive the zolmitriptan orally disintegrating tablet 2.5 mg (n=231) or matching placebo (n=240) to treat a single moderate or severe migraine. Headache relief following zolmitriptan 2.5 mg (63%) was significantly greater than with placebo (22%) at 2 h post-dose (primary endpoint; P < 0.0001). The zolmitriptan orally disintegrating tablet was also significantly more effective than placebo for 1-, 2- and 4-h pain-free response (8% vs. 3%, P=0.0207, 27% vs. 7%, P < 0.0001, and 37% vs. 11%, P < 0.0001, respectively). Of those patients stating a preference, 70% of patients preferred the orally disintegrating tablet to a conventional tablet. Zolmitriptan orally disintegrating tablets are an effective and convenient alternative to a conventional tablet, allowing migraine attacks to be treated anytime a migraine strikes, which can facilitate earlier treatment.

Administration, Oral↗
PubMed2002

[Application of quantifying scoring systems for the determination of changes in the mucosa of the upper gastrointestinal tract. A comparative study of a diclofenac effervescent tablet with conventional diclofenac preparations and acetylsalicylic acid after repeated administration].

UNLABELLED: Application of Quantifying Scoring Systems for the Determination of Changes of the Mucosa of the Upper Gastrointestinal Tract/A comparative study of a diclofenac effervescent tablet with conventional diclofenac preparations and acetylsalicylic acid after repeated administration. BACKGROUND AND AIM: A new diclofenac effervescent tablet (DIC-BT) was developed in order to circumvent the high variable delay in delivery of the drug in enteric coated tablets of diclofenac (CAS 15307-86-5). The gastrointestinal side effects of the effervescent tablet were investigated in comparison to two other galenic principles of DIC preparations (DIC entero coated dragees = DIC-mrD) and dispersible tablets (DIC-DispT) and to acetylic salicylic acid (ASA (CAS 50-78-2). For the assessment of gastrointestinal side effects, two score systems were used simultaneously. The Lanza-scores were compared with our HEU-criteria system (Haemorrhage, Erosion, Ulceration) to find out if the pattern and the localisation of the lesions differ between the drugs tested. METHODS: In a single-blind, randomised, controlled, parallel study design healthy volunteers (27 females, 33 males; mean age 26.9 years, mean b.w. 72.5 kg, Helicobacter pylori antibody negative) were treated by 150 mg/d DIC or 1500 mg ASA (as positive control group) for 7 days. DIC-BT (n = 20 subjects), DIC enteric coated dragees (DIC-mrD) (n = 20), DIC-Dispers tablets (DIC-DispT) (n = 10) and ASA (n = 10) were administered t.i.d. The effects were investigated by videoendoscopy with chromoscopy before and after treatment. Mucosa lesions were assessed according to the Lanza-scores and HEU-criteria system. The results were calculated as pre-post comparison and assessed as paired test between treatment groups. RESULTS: DIC preparations caused mostly erosions and scarcely haemorrhages, but different from ASA only few combined lesions of haemorrhages and lesions in Corpus ventriculi and Bulbus duodeni. The number of mucosal lesions was different with regard to the region (Antrum ventriculi > Corpus ventriculi > Bulbus duodeni). The spreading with Helicobacter pylori (histological assessment at the end of study) varied between 20% and 50% (7/20 subjects in DIC-BT and DIC-msrD, respectively, 5/10 in DIC-dispT group, 2/10 subjects in the ASA group). Based on the HEU-criteria, erosions were seen in 9/20 subjects in DIC-BT, 10/20 subjects in DIC-mrD, 4/10 in DIC-DispT, and 3/10 subjects in ASA group, respectively, the combination of haemorrhages and erosions is seen in 2/20 subjects in DIC-BT, 6/20 in DIC-mrD, 4/10 subjects in DIC-DispT, and in 7/10 subjects in the ASA group, respectively. The difference is significantly between DIC-BT and ASA (p < 0.05) to the sum of all lesions in stomach. Based on Lanza-scores (score values > 2), (a) erosions were seen in 7/20 subjects in DIC-BT, 15/20 subjects in DIC-mrD, 7/10 in DIC-DispT, and 9/10 subjects in ASA group; (b) haemorrhages were seen in 0/20 subjects in DIC-BT, 5/20 subjects in DIC-mrD, 2/10 in DIC-DispT, and 4/10 subjects in ASA group, (c) combined type in 3/20 subjects in DIC-BT, 8/20 subjects in DIC-mrD, 5/10 in DIC-DispT, and 8/10 subjects in ASA group, respectively. Independent of the scoring systems, the difference was significant between DIC-BT and DIC-mrD, as well as between all DIC preparations and ASA. At the end of the study Helicobacter pylori infections were observed by biopsy in 20-50% of volunteers (DIC-BT and DIC-mrD in 7/20 subjects, each, and DIC-DispT in 5/10, and ASA in 2/10 subjects, respectively) and between Dic-BT and ASA (p < 0.05) for all categories. CONCLUSION: Mucosal lesions induced by DIC-BT were significantly less than by DIC-mrD and DIC-DispT. The effect was confirmed by both scoring systems, i.e. Lanza scores and HEU-criteria system. Using the HEU-criteria the pattern and the localization of the lesions could be characterized. There were remarkable differences between the effects of DIC and ASA. The assessment of gastrointestinal side effects using the HEU-criteria was superior to Lanza-scores because there was no bias according to the type of lesion and the type of drug.

Adult↗
PubMed2003

Pharmaceutical applications of shellac: moisture-protective and taste-masking coatings and extended-release matrix tablets.

Shellac is a natural polymer, which is used as enteric coating material in pharmaceutical applications. The major objective of the present study was to investigate the potential of shellac for other purposes, namely to provide moisture-protective and taste-masking coatings as well as extended-release matrix tablets. The efficiency of shellac to achieve moisture protection and taste masking was compared with that of hydroxypropyl methylcellulose (HPMC), which is most frequently used for these purposes. Shellac-coated tablets showed lower water uptake rates than HPMC-coated systems at the same coating level. The stability of acetylsalicylic acid was higher in tablets coated with shellac compared with HPMC-coated systems, irrespective of the storage humidity. Therefore, lower shellac coating levels were required to achieve the same degree of drug protection. Shellac coatings effectively masked the unpleasant taste of acetaminophen tablets. Compared to HPMC, again lower coating levels were required to achieve similar effects. The resulting drug release in simulated gastric fluid was not significantly altered by the thin shellac coatings, which rapidly ruptured due to the swelling of the coated tablet core. In addition, shellac was found to be a suitable matrix former for extended-release tablets. The latter could be prepared by direct compression or via wet granulation using ethanolic or ammoniated aqueous shellac binder solutions. The resulting drug-release patterns could effectively be altered by varying different formulation and processing parameters.

Acetaminophen↗
PubMed1996

Nutritional effect of calcium supplementation by skim milk powder or calcium tablets on total nutrient intake in postmenopausal women.

The effect of different types of calcium supplements on total nutrient intake has not been studied. The effect of dietary calcium supplementation (calcium tablets or skim milk powder) on nutrient intake in 64 postmenopausal women was studied in a 4-y longitudinal study consisting of 2 y of intervention and 2 y of follow-up. Subjects also received advice on how to reduce their consumption of high-fat and cholesterol-rich foods. Analysis of 4-d weighed diet records at 1 y showed that calcium intakes from the milk-powder supplement (1618 +/- 213 mg) and calcium tablets (1718 +/- 257 mg) were above recommended dietary intakes (RDI), and dietary fat intake and plasma cholesterol were significantly reduced compared with baseline values. The subjects supplemented with milk powder had higher intakes of several nutrients, including protein and zinc, compared with the subjects given calcium tablets. A greater proportion of subjects using the milk-powder supplement achieved > or = 70% of the RDI for zinc compared with tablet-supplemented subjects during the intervention study. Subjects were advised to continue with supplementation at the end of the intervention study. Thirty-nine subjects were available for follow-up. The mean (+/- SD) calcium intake for the milk-powder group (942 +/- 434 mg) was below the RDI and significantly lower than that of the calcium-tablet group (1346 +/- 512 mg). These data suggest that advice on dietary calcium supplementation and fat reduction had a beneficial effect on the nutrient intakes of postmenopausal women but compliance outside of a control trial by women taking calcium tablets was higher than that by women taking milk powder. Thus, strategies to encourage women to increase calcium intake can be introduced without significant deleterious effects on other aspects of the diet.

Administration, Oral↗