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At least 127 records · Page 7Linked to original sources

PubMed1997

Intragastric pH after oral administration of single doses of ranitidine effervescent tablets, omeprazole capsules and famotidine fast-dissolving tablets to fasting healthy volunteers.

BACKGROUND: The therapeutic effect of drugs inhibiting acid production on acid-related discomforts is related to both the onset and duration of action of the drug. The effects on gastric pH by single oral doses of some acid-inhibiting drugs were investigated by measuring daytime (morning to lunch) intragastric pH in healthy volunteers. METHODS: This randomized, single-dose, 4-way crossover study included 15 healthy fasting subjects. Effervescent ranitidine tablets 150 and 300 mg, fast-dissolving famotidine tablets 20 mg and capsules of omeprazole 20 mg were administered. Measurements of intragastric pH were performed every 4 s for 10 min prior to drug administration and during the following 4 h. RESULTS: The effervescent ranitidine tablets (150 or 300 mg) produced similar changes in intragastric pH: following an immediate increase to about pH 5, intragastric pH decreased slightly over the next 10-20 min. Thereafter pH increased steadily, reaching pH 4 after 20-40 min and pH 6 after about 70 min. After famotidine, pH 4 was reached after 80 min, significantly slower than ranitidine. After omeprazole, pH 3 was never reached. Ranitidine 150 and 300 mg showed significantly larger integrated pH responses over the 4-h observation period, compared to famotidine (P = 0.0288 and 0.0074) or omeprazole (P < 0.001). CONCLUSIONS: After single-dose administration to healthy fasting volunteers), ranitidine effervescent tablets showed a significantly more rapid onset of action and a significantly larger integrated pH response compared to either famotidine 20 mg fast-dissolving tablets or omeprazole 20 mg capsules.

Administration, Oral↗

PubMed2003

Characterization of excipient and tableting factors that influence folic acid dissolution, friability, and breaking strength of oil- and water-soluble multivitamin with minerals tablets.

The goal of this study is to characterize the formulation and processing factors that influence folic acid dissolution from oil- and water-soluble multivitamin with minerals tablet formulations for direct compression. The following parameters were studied: bulk filler solubility, soluble to insoluble bulk filler ratio, triturating agent (preblending carrier) solubility, disintegrant usage, compression pressure, and folic acid particle size. Folic acid particle size was determined by using light microscopy, and surface area was measured by using BET adsorption. The tablets were compressed on an instrumented Stokes B2 tablet press, and the friability, weight variation, and dissolution were measured according to USP methods, along with tablet breaking strength. In summary, we found the following factors to be critical to folic acid dissolution: bulk filler solubility (soluble fillers, such as maltose, increase folic acid dissolution); disintegrant amount (levels less than 0.4% (w/w) are ineffectual, whereas levels greater than 1.2% (w/w) did not further increase dissolution); and compression force (generally, maltose produce harder tablets). In addition, folic acid dissolution was less affected by changes in compaction pressure when a "super" disintegrant and maltose, as a bulk filler, were used. It was determined that the trituration agent did not play a significant role in folic acid dissolution. In the range of parameters studied, statistical analysis found no significant interactions between the parameters studied, which means they act independently in an additive manner. The results also show that no one factor is completely responsible for dissolution failure. Thus, it is the combination of formulation factors and processing conditions that collectively add up to produce dissolution failure; however, the use of a disintegrant and a soluble filler such as maltose can make a formulation more robust to the inevitable changes that can occur during commercial production.

Dietary Supplements↗

PubMed1978

The measurement of the adhesion of film coatings to tablet surfaces: the effect of tablet porosity, surface roughness and film thickness.

The effect of tablet porosity, surface roughness and film thickness on the adhesion of hydroxypropyl methyl cellulose films to placebo tablet substrates have been studied using a specially designed tensile tester (Fisher & Rowe, 4976). There were direct relations between measured adhesion and tablet porosity and also surface roughness and tablet porosity. The effect of film thickness on the measured adhesion is complex with an initial decrease with thicknesses up to 35 micron and then a gradual increase with thicknesses up to 140 micron dut to differences in the strees distribution within the film during testing. A knowledge of these effects is necessary if results from various sources are to be compared. The findings illustrate the potential capability of the extrapolation of measured adhesion results to zero porosity and zero thickness values in order to obtain a measure of the true or intrinsic adhesion at any film/tablet interface without the confusing elements of tablet porosity, surface roughness and residual stresses in the film.

Adhesiveness↗

PubMed1998

[Effect of tableting conditions on the sticking of tablet using ibuprofen].

Influence of tableting conditions on sticking was investigated using two formulations, the one formulation containing ibuprofen (formulation A) and the other being the standard formulation (formulation B). Sticking was observed on formulation A, and was not observed on formulation B. The degree of sticking was decreased with increase in compression pressure, and increased with compression speed. The shape of punch face was influenced the degree of sticking (sugar concave < bebel < flat). It was thought that sticking was observed when the adhesion between tablet and punch was larger than that among tableting granules. We investigated the pressure placed on a scraper (SCR), the adhesion between granules and metal, and boring hardness of tablet. The results showed that sticking was not observed when the SCR and/or the adhesion were small enough or boring hardness of tablet was high enough. Furthermore, it was suggested that boring hardness distribution would influence sticking.

Adhesiveness↗

PubMed2001

A comparison of the steady-state pharmacokinetics and safety of abacavir, lamivudine, and zidovudine taken as a triple combination tablet and as abacavir plus a lamivudine-zidovudine double combination tablet by HIV-1-infected adults.

STUDY OBJECTIVE: To investigate the steady-state pharmacokinetics of a triple combination tablet containing abacavir (ABC) 300 mg, lamivudine (3TC) 150 mg, and zidovudine (ZDV) 300 mg taken twice/day, and those of ABC 300 mg twice/day plus a double combination tablet containing 3TC 150 mg and ZDV 300 mg twice/day (ABC-COM). DESIGN: Open-label, crossover study. SETTING: Two hospital-based clinical research units. PATIENTS: Twelve men infected with human immunodeficiency virus-1. INTERVENTION: Steady-state pharmacokinetics of ABC, 3TC, and ZDV were assessed after dosing with ABC-COM and the triple combination tablet. MEASUREMENTS AND MAIN RESULTS: Steady-state pharmacokinetics of ABC, 3TC, and ZDV were similar for the triple combination tablet versus ABC-COM for the following: geometric mean (GM) area under the serum concentration-time curve, ABC 6.08 versus 5.87, 3TC 5.51 versus 5.53, and ZDV 1.38 versus 1.46 microg x hr/ml; GM maximum serum concentration (Cmax-ss), ABC 3.09 versus 3.19, 3TC 1.26 versus 1.40, and ZDV 1.19 versus 1.15 microg/ml; median time to Cmax-ss, ABC 0.75 versus 0.75, 3TC 1.50 versus 1.24, and ZDV 0.75 versus 0.75 hours; and GM oral clearance, ABC 51 versus 49, 3TC 27 versus 27, and ZDV 217 versus 206 L/hour. The GM half-lives of ABC and ZDV were similar for both treatments, 1.69 versus 1.58 and 2.30 versus 2.08 hours, respectively. CONCLUSION: Steady-state pharmacokinetics of ABC, 3TC, and ZDV were similar in patients who took them as ABC-COM or as a triple combination tablet.

Adult↗

PubMedDate not supplied

The application of solid dispersion technique in the preparation of therapeutic tablets. Part 1: Paracetamol, amylobarbitone, and caffeine tablets.

A trial was made to study the possibility of preparing high-quality therapeutic tablets by direct compression of the solidified drugcarrier melt via solid dispersion technique. Paracetamol-mannitol, amylobarbitone-urea and caffeine-nicotinamide systems were investigated. Phase diagrams of the first two systems were found to be of the simple eutectic type, while that of the third system was a peritectic type. Solubility studies were also carried out. Dissolution rate studies showed that the fused mannitol/paracetamol (80:20), urea/amylobarbitone (80:20) and nicotinamide/caffeine (50:50 and 70:30) solid dispersions exhibited better rates of dissolution than those of the pure drugs. Comparative studies were carried on with tablets prepared by direct compression of the drug-carrier solidified melt exhibiting the highest dissolution rate and by slugging the pure drug and the drug-carrier physical mixture of corresponding composition. The physical properties and dissolution rate data showed the superiority of the tablets prepared by the solid dispersion technique. The drug release from these tablets was 4.5, 7.6 and 3.7 times greater than that from tablets prepared from pure paracetamol, amylobarbitone and caffeine respectively.

Acetaminophen↗

PubMed1990

Pharmacokinetic comparison of a dextromethorphan-salbutamol combination tablet and a plain dextromethorphan tablet.

We compared in this double-blind crossover study the bioavailability of dextromethorphan from a dextromethorphan-salbutamol combination tablet (Redol comp) and from a plain dextromethorphan tablet (Extuson) by determining dextrorphan concentrations after single-dose oral administration in 10 healthy volunteers. The absorption of salbutamol from the combined preparation was also determined. The absorption of dextromethorphan was slightly faster from the plain dextromethorphan preparation. The peak concentration of dextrorphan was achieved at 1.5 h after Extuson and at 2 h after Redol comp (1,053.0 +/- 366.5 ng/ml and 901.5 +/- 210.9 ng/ml, NS). AUC0-12 values of dextrorphan were 4,315.6 +/- 295.0 (ng/ml)h after Extuson and 3,983.8 +/- 205.6 (ng/ml)h after Redol comp (p less than 0.05). Salbutamol was well absorbed from the combined preparation and the peak concentration was achieved at 3 h (6.57 +/- 2.95 ng/ml). Four subjects reported side-effects typical for salbutamol after the combination tablet. No side-effects were reported after the plain dextromethorphan tablet. On the basis of the present study, we conclude that the absorption of dextromethorphan from the preparations tested is almost equal and the dextromethorphan-salbutamol combination can be administered in tablet form for the treatment of cough.

Adult↗

PubMed1984

Bioavailability of nalidixic acid from uncoated tablets in humans--Part I: Correlation with the dissolution rates of the tablets.

Bioavailabilities of three commercially available tablets and two trial tablets of nalidixic acid were determined. The correlation between in vivo bioavailability parameters and in vitro dissolution rates derived by eight methods (oscillating basket I and II, beaker I, II, and III, rotating basket, paddle and rotating flask) is discussed. Nalidixic acid and its metabolite, 7-hydroxynalidixic acid, were determined in serum by HPLC with a strong anion-exchange resin column. All parameters for nalidixic acid bioavailability showed significant differences among the tablets tested. The relationship between Cmax and AUC was not linear but concave. However, Cmax decreased linearly in proportion to the delay of Tmax. The rank order of tablets according to bioavailabilities was just the same as the rank order obtained when comparing dissolution rates determined by any of the above methods, with the exception of one tablet which had a poor disintegrating ability. The parameters for the rate of bioavailability (Cmax and Tmax) showed good linearity with 1/T50 determined by all of the methods. However, AUC showed significant correlation with neither T50 nor 1/T50.

Adult↗

PubMed1982

[Use of paraformaldehyde tablets for bacterial count reduction, disinfection, cold sterilization, and sterile preservation of medical instruments. 3: On the use of paraformaldehyde tablets in medical institutions].

Paraformaldehyde tablets are very effective against a wide spectrum of organisms. They may be recommended for targeted degerming measures in medical practice. Their utilization requires the observance of the conditions necessary for their efficient use. The tablets should be employed only in containers which are as tight-fitting as possible (preferentially instrument cabinets, Heynemann cabinets, catheter boxes and plastic bags). Paraformaldehyde tablets are well suited for the reduction of the bacterial population and the storage of nonwrapped sterilized instruments. For this purpose, 1 tablet/dm3 is needed. The exposure time required for bacterial count reduction is no less than 3 h. Despite certain limitations, paraformaldehyde tablets may be used for disinfecting. The objects to be disinfected should be neither too contaminated nor too soiled. The minimum period of exposure is 5 h, and 10 tablets/dm3 are necessary. Cold sterilization requires 10 tablets/dm3, too; but the exposure time ranges from 15 to 24 h. This method (which must be considered an expedient) should be employed only if the respective device or instrument cannot be sterilized by other sterilizing techniques. In any case, 80% relative air humidity is a must in the devices in which paraformaldehyde tablets are used.

Bacteria↗

PubMed1997

A new generation starch product as excipient in pharmaceutical tablets. III. Parameters affecting controlled drug release from tablets based on high surface area retrograded pregelatinized potato starch.

This paper describes the general applicability of a new pregelatinized starch product in directly compressible controlled-release matrix systems. It was prepared by enzymatic degradation of potato starch followed by precipitation (retrogradation), filtration and washing with ethanol. The advantages of the material include ease of tablet preparation, the potential of a constant release rate (zero-order) for an extended period of time and the possibility to incorporate high percentages of drugs with different physicochemical properties. Constant release profiles are the result of solvent penetration into the tablet. For theophylline as test drug, constant release profiles could be realized up to a drug content of 75%. This illustrates the possibility to control the release of highly dosed drugs. Release rates from retrograded pregelatinized starch tablets can be enhanced or decreased to the desired profile by different parameters, like geometries of the tablet, compaction force and the incorporation of additional excipients. For procaine HCl it is demonstrated that larger tablets show slower release rates. The incorporation of soluble excipients like lactose and mannitol results for paracetamol in enhanced release rates. The delivery of bases and their salts can be modified by the incorporation of organic acid or alkaline excipients, as is demonstrated for lidocaine and procaine HCl.

Journal Article↗

PubMed1989

Comparison of the gastrointestinal side effects of naproxen formulated as plain tablets, enteric-coated tablets, or enteric-coated granules in capsules.

We studied the gastrointestinal side effects of three formulations of naproxen in 18 healthy male volunteers. In a Latin-square design crossover study, the subjects received 500 mg naproxen twice daily for 7 days as plain tablets, enteric-coated tablets, or enteric-coated granules in capsules. The 51Cr-EDTA absorption test was performed before and at the end of each drug period, to evaluate changes in the distal gut. The test dose was instilled distally in the duodenum to prevent lesions in the stomach from interfering with the evaluation. Upper endoscopy was performed at the same intervals, scoring changes in the middle and distal duodenum separately from findings in the stomach and duodenal bulb. The nature and severity of adverse effects were recorded for each treatment period. Non-parametric methods were used for statistical evaluation. All drugs induced a significant increase in 51Cr-EDTA absorption, but we did not detect any difference between the three formulations. All formulations were associated with a significant increase in all the endoscopic findings monitored. Enteric-coated tablets induced significantly less lesions than enteric-coated granules in the stomach and duodenal bulb, and an advantage over plain tablets was indicated. No difference was seen in the middle and distal duodenum. The proximal endoscopic scores were not correlated to those found in the middle and distal duodenum. Evaluation of the small and large bowel should probably be included in clinical studies of NSAIDs, but our findings suggest that the importance of transfer of mucosal lesions to the distal gut by enteric coating may have been overemphasized.

Adult↗

PubMed1994

[The effect of ranitidine and famotidine on the intragastric pH profile of healthy subjects. Randomized cross-over trial with ranitidine effervescent tablets (300 mg) versus famotidine film tablets (40 mg) ].

Influence of Ranitidine and Famotidine on the Intragastric pH-profile in Healthy Volunteers/Randomised cross-over study of ranitidine effervescent tablets (300 mg) versus famotidine film coated tablets (40 mg). A controlled cross-over trial was carried out to compare the duration of time until the onset of action and its intensity following administration of ranitidine (R, Sostril, CAS 76824-35-6) effervescent tablets (300 mg) and famotidine (F, CAS 76824-35-6) film coated tablets (40 mg). Twelve volunteers (4 female, 8 male) participated in the study. The efficacy of the test medications was assessed by pH-metry during 12 h. The evaluation of the measurements showed that a pH-value 3.5 was reached 100 s after administration of R and 3,392 s (56.5 min) after F (p < 0.01). The median pH-values were significantly higher after R during the first 2 h. The AUC-values (area under the curve; pH-time) for 1, 2 and 4 h were calculated by the trapezoid rule. The intake of R resulted in significantly higher areas than that of F. After reaching the pH-value of 3.5 this value remained stable during the complete period of measurement (R = 12 h, F = 11 h). The faster onset of pH-value elevation could correspond clinically with a faster onset of pain relief.

Adult↗

PubMed1998

Single- and multiple-dose pharmacokinetic comparison of a sustained-release tablet and conventional tablets of naproxen in healthy volunteers.

The pharmacokinetics of a new sustained-release tablet of naproxen (500 mg once daily) were compared with a conventional tablet (250 mg twice daily) after single- or multiple-dose oral administration in healthy volunteers using an open, randomized two-way crossover experimental design. Naproxen was well absorbed from the sustained-release tablet (approximately 97%) compared with the conventional tablet. Pharmacokinetic data showed that the sustained-release formulation reached significantly delayed mean peak plasma levels (Cmax) in both single- and multiple-dose studies and lower Cmax in a single-dose study than the conventional formulation. However, there were no statistically significant differences in other pharmacokinetic parameters, including area under the concentration-time curve (AUC), elimination half-life (t1/2), and elimination rate constant (Ke), in either single- or multiple-dose studies between the two treatments. In addition, there were no significant differences between formulations in Cmax, minimum plasma concentration (Cmin), and fluctuation index in the multiple-dose study.

Adult↗

PubMed2007

Modifying drug release and tablet properties of starch acetate tablets by dry powder agglomeration.

In this study three model drugs (N-acetyl-D-glucosamine (NAG), anhydrous caffeine, and propranolol hydrochloride) were agglomerated with starch acetate (SA) by mixing the binary powders on a stainless steel (SS) plate. Agglomeration was induced by triboelectrification of the particles during mixing, and it was evaluated as a method to achieve controlled drug release rate. These agglomerates, mixed with different amounts of a disintegrant, were compressed into tablets whose dissolution characteristics were determined. Triboelectric measurements showed that when the drugs were in contact with SS, charges of the opposite polarity were generated to SA (+) and caffeine and NAG (-) promoting adhesion. Instead, propranolol HCl was charged with the same polarity as SA. SEM micrographs showed that smaller caffeine particles, in spite of their larger negative charge, agglomerated less efficiently with SA than larger NAG particles. This emphasizes the importance of particle size in the agglomeration process. Propranolol HCl did not form agglomerates with SA since their particle sizes and charges were identical. As a result, agglomeration of powders prior to tablet compression allows for modification and control of the release rate of the drugs from the SA matrix tablets as well as the tensile strength of the tablets.

Acetylglucosamine↗

PubMed1976

Development of a stable sublingual nitroglycerin tablet II: formulation and evaluation of tablets containing povidone.

Stable and pharmaceutically elegant sublingual nitroglycerin tablets were formulated using povidone to retard volatilization of the drug. Formulation and processing variables were investigated to produce an acceptable product. A blend of two grades of povidone, of different degrees of cross-linkage and water solubility, provided stable tablets which exhibited rapid disintegration. Directly compressed sublingual tablets made in this study retained over 80% of the initial nitroglycerin when exposed to the atmosphere at room temperature for 2 months. The direct compression tablets are of good appearance and low friability, and the formulation is readily compressed without problems. An interesting relationship among the hardness, disintegration time, and compaction pressure is described.

Drug Compounding↗

PubMed1979

Comparative studies on eight dissolution method using 21 commercial chloramphenicol tablets and a nondisintegrating benzoic acid tablet.

Eight dissolution methods (beaker, rotating basket, oscillating basket, solubility simulator, rotating flask, and column) were evaluated using 21 commercial film-coated chloramphenicol (I) tablets and a nondisintegrating benzoic acid (II) tablet. The relative agitating intensities obtained from different dissolution methods were compared through the relative zero-order nondisintegrating tablet dissolution rate constants. Correlation coefficients between I dissolution rate parameters (lag time, T20, T50, and T80) were determined. Significant correlation was observed for the lag time among seven methods, and all pairwise regression lines passed through zero except one. The regression line slopes reflected the relative destructive force intensities produced by each dissolution method on the coated I tablet films. The seven dissolution methods could be classified into two main groups according to correlations of four dissolution rate parameters. The classification criterion agreed well with that based on the agitation method. However, dissolution methods may not be interchangeable even though they belong to the same dissolution method group.

Benzoates↗

PubMed1979

Comparative bioavailability of a microcrystalline theophylline tablet and uncoated aminophylline tablets.

The bioavailability of a rapidly dissolving tablet of theophylline and three brands of standard aminophylline tablets was estimated in a four way cross-over study involving 8 healthy adult volunteers. The relative extent of bioavailability as assessed by the measurement of the total area under the plasma concentration time curves showed no difference between the products (P greater than 0.05). Computed estimates of the rate of drug absorption were similar for all 4 products tested. The results indicate that the rapidly dissolving tablet offers no advantage in respect to rate and extent of absorption over conventional aminophylline tablets.

Aminophylline↗

PubMed1993

Calcium phosphates in pharmaceutical tableting. 2. Comparison of tableting properties.

Ten calcium phosphates suitable for direct compression (dibasic calcium phosphate dihydrate, dibasic calcium phosphate anhydrous and hydroxylapatite) were investigated with respect to their compressional behaviour. Except for Di-Cafos A all products gave tablets with sufficient to good mechanical strength. Nevertheless, there were differences between the products. All tablets prepared from the different products showed a high friability. This seems to be a problem of the calcium phosphates in general. On the other hand, the influence of magnesium stearate on the mechanical strength of the tablets was negligible for all products investigated. Moreover, a considerable effect of the particle size on the tensile strength of the tablets was found. The ejection forces and residual pressures were high in general, but critical only in the case of hydroxylapatites. Heckel plots were used to differentiate between plastic deformation and brittle fracture of the particles. In the case of calcium phosphates the slope of the Heckel plots indicated the hardness of the particles rather than their deformation behaviour.

Calcium Phosphates↗