Tablets In Terms Research Articles

Implementation of pre‐seasonal sublingual immunotherapy with a five‐grass pollen tablet during optimal dosage assessment

SummaryBackgroundThe optimal dose (300IR) of a five-grass pollen sublingual immunotherapy tablet in terms of efficacy was previously demonstrated from the first pollen season.ObjectiveHere, we aim to confirm whether this dose remained optimal during the peak of the pollen season by assessing the efficacy and quality of life data.MethodsA total of 628 subjects with grass pollen rhinoconjunctivitis were randomized in a double-blind, placebo-controlled, multi-centre, pan-European trial. Subjects received once-daily tablets (Stallergenes, Antony, France) of 100IR, 300IR, 500IR or placebo, starting 4 months before and throughout the 2005 grass pollen season. The pollen season was defined as the first day of 3 consecutive days with a grass pollen count above 30 grains/m3 of air, recorded using Hirst-type volumetric pollen traps, to the last day before 3 consecutive days with a pollen count below 30 grains/m3.ResultsThe grass pollen season lasted an average of 30 days, with a peak of 12 days. The mean treatment duration before the grass pollen season was similar in the four treatment groups (121.4±31.1 to 128.6±15.4 days in the safety population). Both the 300IR and 500IR groups had highly significant improvements in Rhinoconjunctivitis Total Symptom Score (RTSS) vs. placebo at the peak pollen season (P=0.0005 and 0.0014, respectively), which agreed with improvements in RTSS in the primary evaluations. The average RTSS scores were slightly elevated during the peak pollen season in all treatment groups. The overall Rhinoconjunctivitis Quality of Life Questionnaire score confirmed the optimal dosage 300IR at peak (P<0.0001) and at the end (P⩽0.0031) of the pollen season. All doses were well tolerated.ConclusionAt the peak pollen season, the efficacy and quality of life data for both 300IR and 500IR groups was significantly improved vs. the placebo group. These results confirm the conclusions of the primary evaluations and validate the use of 300IR tablets for clinical practice.

Development of tablets containing probiotics: Effects of formulation and processing parameters on bacterial viability

The probiotic products available in the market nowadays are mostly in the form of liquid or semisolid formulations which show low cell viability after oral administration, mainly because the bacteria do not survive the harsh conditions in the stomach. The development of suitable dry dosage forms enable higher bacterial survival and consequently is the main aim of the present study. An anticipated advantage is that due to the low water-activity lyophilized bacterial cells will preserve their viability. Further, by a proper selection of a tablet forming matrix, it is foreseen that the entrapped bacteria are protected against the low pH in the stomach. In this study, the effects on bacterial survival in tablets were investigated concerning compression force, matrix forming excipients such as hydroxypropyl methylcellulose phthalate (HPMCP) or other swelling agents. The results showed that the proportion of matrix forming excipients in tablets and the compression force affected the properties of probiotic tablets in terms of tensile strength and disintegration as well as the survival of the bacteria. The tensile strength of the tablets increased with increase of HPMCP content. Tablets manufactured with high compression force showed a slow disintegration time and high bacterial cell viability (more than 80%). Incorporation of sodium alginate in the tablets resulted in higher cell survival in simulated GI fluid (>90%) and a suitable disintegration time (approximately 5 h). By a proper design of the formulation, tablets with a fast disintegration time and a high preservation of bacterial cell viability were developed.

Influence of the formulation of an alumina powder on compaction

The compression of ceramic powders requires the addition of organic materials to insure tablet cohesion. For the compaction of formulated ceramic powders it is necessary to supply them energy. As a function of the formulation of ceramic powders, one can measure the specific energy acquired during the tablet compression. Recently, a technique used in powder metallurgy, High Velocity Compaction (HVC), has been studied to form ceramic compacts. This method brings special physical properties to tablets in terms of homogeneity compared to conventional uniaxial pressing. The properties of tablets prepared by the two processes are compared and discussed through a phenomenological model.

Development and evaluation of the tablets coated with the novel formulation termed thin-layer sugarless coated tablets

The purpose of this study was to develop and evaluate the thin-layer sugarless coated tablets containing Vitamin C, Vitamin E, Vitamin B 2, calcium pantothenate, and l-cysteine. As a result of the formulation study, three coating layers, 2% under coating (UC), 38% build-up coating (BC), and 5% syrup coating (SC) were necessary for sufficient impact toughness, elegant appearance, and improvement of appearance stability after storage at 25 °C/75% RH for 6 months under open conditions. We demonstrated that the thin-layer sugarless coated tablets are superior to the sugar-coated tablets in terms of small tablet size and stability of calcium pantothenate. It was due to the coating method, the continuous spray mist method, which can minimize the thicknesses of coating layers and the moisture content in the tablets. We also demonstrated that the thin-layer sugarless coated tablets are superior to the film-coated tablets in terms of masking ability of the unpleasant odor and the appearance, stability of the appearance, and low hygroscopicity. It was due to the dense, opaque, and stable coating layers mainly consist of erythritol. We revealed that thin-layer sugarless coated tablets have both advantages of film-coated tablets and sugar-coated tablets.

The determination of the mechanical properties of elongated tablets of varying cross section

The mechanical properties of elongated tablets of different thickness prepared at a range of pressures with surfaces that are flat or curved, have been determined by application of a flexure test. The strength of the tablets in terms of breaking load increases with an increase in the cross-sectional area of the tablets. To provide an improved method of comparing the strength of the tablets, the tensile strength of the specimens has been calculated from equations based on stress analysis. While an allowance for a change in thickness was provided by such a system there was a clear indication that the specimens tensile strength was still dependent on their dimensions. For equivalent central core thickness strength increased with the face curvature. This could be due to changes of the structure within the specimen during the formation process and there were clear indications that tablet porosities for equivalent compaction pressures were not equal. The differences could, however, be utilised to provide optimum conditions of curvature and central core thickness to give maximum tablet strength.

The efficacy and safety of a new ciprofloxacin suspension compared with co-amoxiclav tablets in the treatment of acute exacerbations of chronic bronchitis

A multinational, multicentre, randomized, prospective, parallel-group study compared treatment with ciprofloxacin administered as an oral suspension (500 mg twice daily for 7 days) with co-amoxiclav tablets (625 mg three times daily for 7 days) in patients suffering from acute exacerbations of chronic bronchitis (AECB). A total of 147 of 165 cases treated with ciprofloxacin (89·1%) and 146 of 162 cases treated with co-amoxiclav (90·1%) were classified as being clinical successes at the primary efficacy assessment 7 days after the end of therapy (assessed as reduced cough, improvement in dyspnoea, reduction in 24-h sputum volume or reduced purulence of sputum). Treatment equivalence was statistically confirmed; treatment difference: − 1·0%, 95% CI − 6·6% and 4·5%. Before treatment, 128 bacterial strains were isolated from 103 patients (60 ciprofloxacin and 68 co-amoxiclav). The most commonly isolated organism was Haemophilus influenzae (60 isolates), followed by Moraxella catarrhalis (12 isolates), Streptococcus pneumoniae (11 isolates) and Staphylococcus aureus (10 isolates). At day 14, 40 of 46 ciprofloxacin-treated patients (87·0%) and 46 of 55 co-amoxiclav-treated patients (83·6%) who were valid for bacteriological analysis were classified as being bacteriological successes (classed as eradication, eradication with colonization or presumed eradication; treatment difference: 3·3%, 95% CI − 8·3% and 14·9%). The adverse event profile was comparable between treatment groups. Most adverse events considered possibly or probably related to study drug were related to the gastrointestinal system and were of mild or moderate severity: nausea (13% ciprofloxacin, 10·6% co-amoxiclav), flatulence (10·3% ciprofloxacin, 3·9% co-amoxiclav), abdominal pain (7·6% ciprofloxacin, 7·3% co-amoxiclav) and diarrhoea (4·3% ciprofloxacin, 6·7% co-amoxiclav). We concluded that a 7-day course of ciprofloxacin suspension is equivalent to a 7-day course of co-amoxiclav tablets in terms of clinical and bacteriological efficacy and tolerability for the treatment of AECB. Thus, ciprofloxacin suspension may offer a suitable alternative treatment for AECB patients who have difficulty in swallowing, or who prefer liquid medications to tablets.

Ranitidine Effervescent and Famotidine Wafer in the Relief of Episodic Symptoms of Gastro-Oesophageal Reflux Disease

Background: The aim of this study was to measure the efficacy of 150-mg ranitidine effervescent tablets compared with 20-mg famotidine wafers in the management of patients presenting to primary care physicians with episodic symptoms of gastro-oesophageal reflux disease (GORD). Methods: The study was of a multicentre, open, randomized, parallel-group design in which 32 Norwegian general practitioners participated. After a pre-treatment demographic and symptom assessment, eligible patients were allocated to either ranitidine effervescent tablet or famotidine wafer. Patients were then provided with the study medication, a stopwatch, and a 2-week symptom diary card. Efficacy was primarily determined by the time to adequate symptom relief for the first symptom episode. Results: In total, 377 patients were recruited to the study; 187 patients received ranitidine effervescent, and 190 received famotidine wafer. More than 50% of the patients had daily GORD symptoms before recruitment. Median time to adequate symptom relief was 15 min in the ranitidine group and 18.5 min in the famotidine group (P = 0.005). Adequate symptom relief within 60 min was reported by 165 (92%) ranitidine patients and 156 (84%) famotidine patients (P=0.02). The number of non-responders after 60 min was twice as great in the famotidine group: 30 (16%) versus 15 (8%). A greater proportion of patients in the famotidine group liked taking the wafer formulation: 173 (94%) versus 126 (70%) (P = 0.001). Conclusion: There was a statistically significant difference in favour of 150-mg ranitidine effervescent tablets in terms of time to adequate symptom relief and the proportion of patients who achieved adequate symptom relief for the first episode. A greater proportion of patients in the famotidine group liked the type of formulation than in the ranitidine group.

ブプレノルフィン舌下錠の調製と臨床効果

We tried to improve buprenorphine (BN) sublingual tablets (previous tablets) prepared previously [Yakuzaigaku, 46: 134-139 (1986)] by focusing on shortening the disintegration time because the disintegration of these tablets sublingually in man is quite long (7-9 minutes). Five different tablets (100mg) containing 100μg of BN were prepared, and the qualitative characteristics, pharmacokinetic behavior and clinical effect of BN were compared with the previous tablets. In the quality tests, one of the new tablets comprising 78.1 mg of 0.128% BN powder, 19.9 mg of lactose, 1 mg of magnesium stearate and 1 mg of powdered acacia per tablet was superior to the other products in terms of both disintegration and dissolution. The mean sublingual disintegration times fos the placebo of the new tablet in five healthy volunteers and five patients were 3.0 and 3.6 minutes, respectively, values which were significantly shorter than those (7.5 and 6.5 minutes) for the previous tablet. The plasma concentration of BN or analgesic effect arising after sublingual administratation of the new tablet in one healthy volunteer and two patients were closely comparable with those following sublingual administration of the previous tablet. The new tablet is biologically and pharmacologically equivalent to the previous one and is superior to the previous tablet in terms of disintegration characteristics.

A large scale comparative study in general practice with nitroglycerin spray and tablet formulations in elderly patients with angina pectoris

In an 8-week comparative study, 410 patients were treated with nitroglycerin spray and 387 with conventional 500 mcg sublingual tablets. Data were analysed to compare the two treatments and to compare the results in older patients (greater than or equal to 65 y) with younger patients (less than 65 y). Spray was significantly superior to tablets in terms of number of patients helped, speed of pain relief and reduction in the number of attacks from pre-study levels. The occurrence of headache was significantly less in the spray group. There was no significant difference in the number or nature of adverse events but more spray patients reported taste disturbance. The clinical advantages seen in the entire population were maintained when the two age categories were considered separately. Further, 95% of patients found the spray convenient. The authors conclude that improved efficacy together with improved stability of the spray without loss of convenience makes Nitrolingual spray an acceptable alternative to tablets irrespective of patients' age.

KÜLTEPE TABLETLERİNİN ANADOLU TARİHİ VE KÜLTÜR TARİHİ BAKIMINDAN ÖNEMİ

This paper discusses the importance of Kultepe tablets in terms of the history of Anatolia and cultural history.

Slow-Release 5-Amino-Salicylic Acid (Pentasa®) for the Treatment of Active Crohn’s Disease

A double-blind, placebo-controlled trial of a slow-release preparation of 5-amino-salicylic acid (Pentasa) has been performed in 40 patients with active Crohn's disease. Over a 6-week period, Pentasa (1.5 g daily) was no different to the dummy tablet in terms of clinical activity (Harvey-Bradshaw Index) or laboratory indicators of inflammation. No serious adverse reactions occurred.

Cancer pain management with a controlled-release oral morphine preparation

An open-label pilot study was conducted to assess the efficacy and acceptability of a controlled-release oral morphine formulation, MS Contin tablets, when administered “by the clock” two to three times daily as a substitute for opioids given on request to patients with pain caused by advanced cancer. Initially, four-hourly doses of standard “immediate-release” oral morphine sulfate tablets were substituted for the patients' prior analgesic medication and titrated to individual needs. Forty of the 47 patients enrolled in the study were subsequently switched to an eight-hourly MS Contin regimen (three patients became too ill to continue the study, and four left the study during the immediate-release titration phase because of adverse reactions that may have been drug related). Small “rescue” doses of standard oral morphine were available to the patients, but they were taken infrequently. Twenty-one of the 37 patients maintained on the eighthourly schedule consented to be treated with, and were subsequently stabilized on, MS Contin administered every 12 hr, with a reduction of over 20% in their average daily morphine dose. Most of the patients rated the controlled-release medication superior to the standard oral morphine tablets in terms of both convenience and adequacy of relief.

Effect of Tablet Solubility and Hygroscopicity on Disintegrant Efficiency in Direct Compression Tablets In Terms of Dissolution

The effect of tablet composite solubility and hygroscopicity on the dissolution efficiency of three “super disintegrants”, sodium starch glycolate, crospovidone, and croscarmellose sodium, was investigated. Lactose, dicalcium phosphate dihydrate, and sorbitol, alone or in combination, provided varying degrees of solubility and hygroscopicity to the direct compression tablet formulations. To monitor in vitro dissolution, 1% p-aminobenzoic acid was added to the formulation as a tracer. The results indicate that hygroscopic ingredients decrease the effectiveness of super disintegrants in promoting in vitro dissolution. The greater the overall hygroscopicity of the tablet formulation, the larger the decrease in the efficiency of the super disintegrant. Composite tablet solubility did not influence the effectiveness of the super disintegrants. Super disintegrants that complied with the same compendial specifications, but were manufactured by different companies, behaved similarly in promoting tablet dissolution.

Biopharmaceutical studies on the clinical inequivalence of two carbutamide tablets.

Biopharmaceutical investigations were made to determine the reason for differences in therapeutic responses to two types of carbutamide tablets with the same carbutamide content. A two-way cross-over study in five healthy adult men on the serum concentration of carbutamide, measured by HPLC, showed differences between the tablets in terms of the mean serum concentration at 2 h (31.48 and 42.89 μg/ml, respectively) and Cmax (37.30 and 48.83 μg/ml, respectively). These findings were reflected in differences in therapeutic effects. Marked differences were also found between the tablets in in vitro tests, e.g., in disintegration time, hardness and dissolution rate. The findings were consistent with clinical findings only when a pre-incubation technique was employed in the in vitro dissolution test.

Studies on Swelling Behavior of HPMC based Matrix Tablets by the Application of Digital Imaging Technique

The widespread application of hydrogels in a number of applications like control of microfluidic flow, development of muscle-like actuators, filtration/separation and drug delivery makes it important to properly understand these materials. Understanding hydrogel properties is also important from the standpoint of their similarity to many biological tissues. The degree of swelling as well as the rate of swelling of the hydrogel was studied through experiments using digital photography. First of all the matrix was prepared by blending properly weighed HPMC, Theophylline and excipients in a laboratory mixture for 10 minutes followed by compression with 5 ton force for 30 seconds. The study was designed to evaluate the effect of hydrophobic materials on HPMC matrix tablets in terms of in vitro swelling study. Different viscosity grades of HPMC i.e. 6- cps, 15-cps and 50-cps were used to prepare tablets along with various hydrophobic materials. Among the hydrophobic materials stearic acid (SA), cetyl alcohol (CA), bees wax (BW), glyceryl monostearate (GMS), cetostearyl alcohol (CSA) and stearyl alcohol (STA) were used. It was found that presence of hydrophobic ingredients in the HPMC hydrogel matrix substantially reduces swelling of the matrix. In this work, the extent of swelling of HPMC matrix was evaluated by using digital photography and counting the pixels with Photoshop software. Finally, it was shown from the experiment that the rate and extent of drug release is mainly governed by swelling rate of different HPMC viscosity grade used and the nature of hydrophobic materials included into the matrix system. Key words: Swelling, Matrix, HPMC, Hydrogel, Photography. doi: 10.3329/dujps.v7i2.2174 Dhaka Univ. J. Pharm. Sci. 7(2): 169-175, 2008 (December)