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PubMed1976

Effect of variation in compaction force on properties of six direct compression tablet formulations.

The effect of variation in compaction force on six direct compression tablet matrixes was investigated. An instrumented tablet press allowed direct measurement of applied and ejection forces. Hardness, apparent tablet density, and disintegration times also were determined. The disintegration time of spray-dried lactose tablets was essentially independent of compaction force. However, in the other systems investigated, the properties studied showed varying types of dependence on compaction pressure. A direct compression formula was developed and exhibits a decrease in disintegration time as compaction force is increased.

Chemistry, Pharmaceutical↗
PubMed1977

Prediction of tableting problems such as capping and sticking: theoretical calculations.

Tabletability factors were developed through the use of an automated tabletability tester, and the applicability of these factors to actual manufacturing procedures was tested by the large-scale manufacturing of tablets. Use of this approach does not require knowledge of the tablet's physical properties, e.g., moisture content, porosity, particle size, fluidity, and angle of repose.

Drug Compounding↗
PubMed1977

Comparative bioavaiability of four commercial quinidine sulfate tablets.

A comparative bioavailability study was performed using four commercially available, chemically equivalent brands of quinidine sulfate tablets. Two 200-mg tablets were administered to 11 different subjects following a completely randomized crossover design. Serum levels, urinary excretion data, and derived pharmacokinetic parameters were compared statistically. There were no statistical differences in the extent of quinidine absorption from the four brands of tablets as evidenced by the cumulative urinary excretion values and the areas under the serum level-time curves. Significant differences in the mean serum levels at 0.5 and 1 hr and differences in the peak times and absorption rate constants indicate that there was a difference in the absorption rate between Treatments A and D and C and D. A significant difference in the peak times also was noted for Treatments B and C. When mean disintegration times for the four tablet formulations were compared with their values for ka, tmax and mean serum levels at 0.5 and 1 hr, rank-order correlations were observed. A considerable degree of variability in quinidine elimination was noted, with half-life values ranging from 2.71 to 8.12 hr (mean half-life of 5.36 hr).

Adult↗
PubMed1977

Polymer sorption of nitroglycerin and stability of molded nitroglycerin tablets in unit-dose packaging.

The sorption of nitroglycerin by thermoplastic polymers and the stability of molded nitroglycerin tablets in strip packaging were studied. The polymers investigated varied greatly in their affinity for nitroglycerin, the order of decreasing affinity being: vinyls greater than low density polyethylene greater than ionomers greater than high density polyethylene. With the proper choice of packaging, molded nitroglycerin tablets stabilized with povidone maintained acceptable potency for up to 2 years at 26 degrees when strip packaged in unit doses. Chemical decomposition (hydrolysis) of nitroglycerin also was investigated. Povidone accelerated the decomposition of nitroglycerin; at high temperature, decomposition was a significant factor in tablet stability for tablets containing povidone.

Adsorption↗
PubMed1977

Drug migration during drying of tablet granulations II: effect of binder solution viscosity and drying temperature.

The effect of binder solution viscosity and drying temperature on the integranular migration of propoxyphene hydrochloride was studied. Wet granulations containing the drug were prepared using binder solutions with viscosities ranging from 1 to 1000 cps. Temperature studies were conducted using granulations prepared with a 3-cps binder solution and dried at 40, 50, 60, 70, and 80 degrees. Drug migration decreased with increased binder solution viscosity, and insignificant migration occurred in granulations prepared with binder solutions having apparent viscosities above 90 cps. No significant effect on intergranular drug migration was observed within the drying temperature range studied. Tablets compressed from a granulation in which drug migration was high showed a greater tablet-to-tablet drug content variation than a granulation with lower migration, even though each dried granulation was thoroughly mixed before tableting.

Calcium Phosphates↗
PubMed1977

Determination of time course of tablet disintegration I: numerical method.

A method is described for determining the time course of tabled disintegration. It involves a numerical analysis of the experimental dissolution profile of a tablet and the dissolution characteristics of the primary drug particles in the tablet. The disintegration profile is determined for an acetaminophen tablet to demonstrate the application of the method. Tablet dissolution is simulated with the disintegration-dissolution model, and the interrelationship between the two fundamental processes is studied theoretically by varying the parameters describing the two processes.

Acetaminophen↗
PubMed1978

Determination of time course of tablet disintegration II: Method using continuous functions.

An analysis of the disintegration-dissolution sequence of drug release from a tablet leads to a mathematical expression relating disintegration to the dissolution profile of the tablet and the dissolution rate of the primary drug particles in the tablet. The equation describing the disintegration of an acetaminophen tablet is determined to demonstrate the application of the theory.

Acetaminophen↗
PubMed1980

Cost evaluation of alternative pharmaceutical tableting processes by simulation.

A simulation model and a subsequent computer program were developed as experimentation methods for evaluating tableting processes with respect to cost. These methods also allow estimation of the various times involved in a tableting operation (e.g., the processing time). The model was programmed in FORTRAN using the GASP IV simulation language. After verification of the program, experiments were run that involved comparing different levels of specific input variables to determine which variable had an effect on the cost-time relationships of a particular processing method. Among the possible input variables chosen for evaluation were the drying method, the type of tableting machine, the batch size, the labor rate, and the operation of the equipment in the process. An analysis of variance was made, and three separate regression equations were developed that described the relationship between the input variables and the dependent variables of processing cost and time. Graphs were developed from the regression equations by manipulating them through series of different independent variables. These graphs then were used in determining minimum costs and times, breakeven points, and rates of change, as well as in simple evaluation of processes through graphic representation. By using the simulation program to run experiments and then by analyzing them, results can be obtained to help in making intelligent decisions about the cost-time relationships of a particular tableting procedure before it is implemented.

Chemistry, Pharmaceutical↗
PubMed1981

Kinetics of aspirin, salicylic acid, and salicyluric acid following oral administration of aspirin as a tablet and two buffered solutions.

Twelve fasting normal volunteers received three aspirin dosage forms in a single-dose, complete crossover study; the plasma and urine levels of aspirin, salicylic acid, and salicyluric acid were measured for 10 hr. The three dosage forms were an unbuffered tablet, an effervescent solution with 16 mEq of buffer, and an effervescent solution with 34 mEq of buffer. Significant differences in the absorption rate were observed, with the solution having 16 mEQ of buffer being fastest, the solution having 34 mEq of buffer being intermediate, and the tablet being slowest. These differences are attributed to gastric emptying rates and tablet dissolution. Urine pH and renal clearance for all three acid compounds are influenced by the buffer during the first 2 hr following dosing but not later. Area under the curve comparisons suggest that approximately 20% more aspirin reaches the general circulation intact following the tablet but that the total amount of salicylate absorbed is not different. Further studies are required to select the optimal buffer content to provide rapid absorption with minimal sodium dose and urine alkalinization.

Absorption↗
PubMed1981

Simultaneous high-performance liquid chromatographic determination of theophylline, ephedrine hydrochloride, and phenobarbital in tablets.

A rapid reversed-phase high-performance liquid chromatographic (HPLC) method was developed for the simultaneous assay of theophylline, ephedrine hydrochloride, and phenobarbital in a tablet matrix. A methanolic extract of the powdered sample containing salicylamide as the internal standard was injected into the chromatograph. The HPLC system used methanol-0.007 M monobasic potassium phosphate (37:63, pH 2.3) as the mobile phase. Detection was at 254 nm, and quantitation was based on the drug-internal standard peak area ratio. This ratio was linear over a concentration range of 20.9-83.5 microgram of theophylline, 4-15.9 microgram of ephedrine hydrochloride, and 1.3-5.1 microgram of phenobarbital. Overall recoveries (+/- SD) from three synthetic tablets were: theophylline, 99.8 +/- 1.3%; ephedrine hydrochloride, 100.2 +/- 0.6%; and phenobarbital, 99.4 +/- 0.7%. The method was compared to the compendial method and also was applied to the assay of commercial tablets containing these three active ingredients. The proposed method is applicable to the assay of individual tablets.

Chromatography, High Pressure Liquid↗
PubMed1983

Comparison of granule strength and tablet tensile strength.

The granule strength (crushing load) of lactose granulated with 1-9% povidone was measured initially and at intervals during a 1-year period. The granule strengths of dibasic calcium phosphate dihydrate granulated with various concentrations of starch and povidone were measured. The axial and radial tensile strengths of tablets compressed from these granules were determined and related to concentration of binder and granule strength. The effect of compressional force on the integrity of granules in a tablet matrix is shown in scanning electron photomicrographs of the fractured tablets which had undergone a diametral compression test. It appears that the compressional force and the concentration of binder contribute more than granule strength to tablet tensile strength.

Hardness↗
PubMed1983

Influence of food on aspirin absorption from tablets and buffered solutions.

After a standard meal, 12 normal volunteers received three aspirin dosage forms in a single-dose, complete crossover study. The three dosage forms were an unbuffered tablet, an effervescent solution with 16 meq of buffer, and an effervescent solution with 34 meq of buffer. Plasma and urine aspirin, salicylic acid, and salicyluric acid were measured for 10 hr. Significant differences in the absorption kinetics of aspirin were observed, with aspirin from the two solutions being absorbed faster than from the tablet. Urine pH and renal clearance for all three acid compounds were influenced by the buffer during the first 2 hr only. Area under the curve (AUC) and urine accumulation comparisons suggest that 15-20% more aspirin reaches the general circulation after the tablet, but that the total salicylate absorbed is not different. Comparison with an earlier study indicates the solution with 34 meq of buffer is virtually unaffected by the presence of the meal while the solution with 16 meq buffer and the tablet are more slowly absorbed in the nonfasted state.

Adult↗
PubMed1985

Steady-state bioavailability of dexbrompheniramine and pseudoephedrine from a repeat-action combination tablet.

The steady-state bioavailabilities of dexbrompheniramine and pseudoephedrine were evaluated following multiple-dose administrations of a repeat-action combination tablet containing 6 mg of dexbrompheniramine maleate with 120 mg of pseudoephedrine sulfate every 12 h for 7 d compared with reference standards. The reference standards used in this study were concomitant administration of conventional 2-mg dexbrompheniramine maleate tablets every 4 h and 120-mg pseudoephedrine sulfate repeat-action tablets every 12 h, each for 7 d. Twelve healthy adult male volunteers completed this randomized two-way crossover study. Blood samples for subsequent assay were obtained at frequent time intervals throughout each 7-d dosing phase. Sensitive and specific gas-liquid chromatographic methods were used for the determination of dexbrompheniramine and pseudoephedrine in plasma. Based on the plasma levels, the times to reach steady state were determined. In addition, the major bioavailability parameters (Cmin, Cmax, tmax, and AUC) for days 6 and 7 of dosing were determined and statistically evaluated. The results of this study demonstrate that, at steady state, the repeat-action combination tablet and concomitant administration of the reference standards are bioequivalent.

Biological Availability↗
PubMed1985

Effect of food and tablet age on relative bioavailability and pharmacodynamics of two tolbutamide products.

Relative bioavailability and pharmacodynamics of tolbutamide from two different commercially available tablet products have been evaluated in healthy subjects in a single-dose crossover study. "Fresh" tablets and tablets aged by exposure to 98% relative humidity for 3 d at ambient temperature were studied. Aging was found to differentially affect both the rate and extent of absorption for the two products. Differences were reflected by log AUC (generic product AUC 10% lower than the product of the innovator, p = 0.047), peak concentration (generic product 27% lower than the product of the innovator, p = 0.0001), mean absorption time (generic product 119% longer than the product of the innovator, p = 0.0008), and mean residence time (generic product 17% longer than the product of the innovator, p = 0.011). Aged product from the innovator produced statistically significantly higher serum tolbutamide concentrations for the first 8 h postdose and a greater glucose depression than aged generic product. Administration of unaged tablets with food produced differences in the rate of absorption, manifested in time-to-peak (generic product 69% later than the product of the innovator, p = 0.006), peak concentration (generic product 18% lower than the product of the innovator, p = 0.001), and mean absorption time (generic product 104% greater than the product of the innovator, p = 0.007), which resulted in statistically significantly higher tolbutamide concentrations for the product of the innovator than for the generic product for the first 3 h postdose.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1985

Bioequivalence of carbamazepine chewable and conventional tablets: single-dose and steady-state studies.

Single-dose and steady-state studies were carried out on separate occasions to examine the bioequivalence of the newly formulated carbamazepine chewable tablet. In the single-dose study, the plasma levels resulting from 2 X 200-mg conventional tablets (CT), 4 X 100-mg chewable tablets swallowed whole (SW), and 4 X 100-mg chewable tablets chewed before swallowing (CHEW) were compared. A randomized 3 X 3 Latin-square design balanced for residual effects, with a 3-week washout period, was used (n = 6). Plasma samples were analyzed by a specific GC method for carbamazepine. The following parameters were used for evaluation: AUC, Cmax, tmax, and t1/2. None of the parameters were significantly different except Cmax and t1/2 values for CHEW and CT. The Cmax was 25% higher and t1/2 was 11% shorter for CHEW than CT. The impact of differences in the peak plasma levels at steady state were examined by pharmacokinetic projection (400 mg b.i.d.) based on the single-dose data and with simulated induction equal to a 50% reduction in t1/2. The projected steady-state CT and CHEW plasma concentrations were similar, with a difference of only 4%. The results demonstrate the bioequivalence of the dosage forms with respect to the extent of absorption, and similar steady-state concentrations of carbamazepine in plasma can be expected. To test the conclusion from the projected study, a separate bioequivalence study to compare CHEW relative to CT was performed at steady state in normal volunteers (200 mg b.i.d.).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1987

Relationship between planar and all-surface rate constants for drugs formulated in nondisintegrating cylindrical slow-release tablets.

The release of drug through the planar surface of a nondisintegrating tablet with an insoluble matrix has been described mathematically using the Higuchi release rate constant (kH). The release of drug through a similar all-surface tablet has been described by using a cubic equation and the all-surface rate constant (kr). Using sodium salicylate and quinidine sulfate as model drugs, the relationship between kH and kr was verified for cylindrical slow-release tablets. Accordingly, the rate constant obtained from a single exposed planar surface can be used to predict the rate constant (kr) when all surfaces of the tablet are exposed to dissolution fluid.

Delayed-Action Preparations↗
PubMed1987

Relative bioavailability of rimantadine HCl tablet and syrup formulations in healthy subjects.

Twenty healthy male subjects completed an open-label randomized crossover design to assess the bioavailability of 100 mg of rimantadine HCl in tablet and syrup forms relative to an oral solution. Blood samples were drawn and rimantadine plasma concentrations were determined by a GC-MS method. The maximum plasma concentration (Cmax), the time to Cmax (tmax), the area under the plasma concentration-time curve (AUC), and k were compared among treatments using an analysis of variance and the Hauck-Anderson test for bioequivalence. The Hauck-Anderson test was satisfied when the syrup and solution were compared. The relative bioavailability of the syrup was 96%. Both Cmax and AUC were significantly (p less than 0.05) increased (23 and 17%, respectively) when the tablet was compared with the solution. The relative bioavailability of the tablet was 117%. This outcome was unusual and could not be explained. However, this was not anticipated to be of clinical consequence since the majority of the safety and efficacy of rimantadine HCl was established using a tablet.

Adamantane↗
PubMed1990

In vitro dissolution and in vivo bioavailability of commercial levothyroxine sodium tablets in the hypothyroid dog model.

The objective of this study was to determine whether a correlation exists between the rate of in vitro dissolution and bioavailability of levothyroxine sodium (T4) tablets. Dissolution versus time profiles for Synthroid, the Flint brand of levothyroxine sodium, and two competitors' tablets (brands A and B) were generated using an official dissolution apparatus (USP), and 0.05 M phosphate buffer (pH 7.4) as the medium. These tablets were also utilized in single-dose crossover bioavailability studies in the hypothyroid dog model (n = 6). The average areas under the serum T4 concentration versus time curve from 0 to 8 h (AUC) for Synthroid, brand A, and brand B were 8.22, 6.32, and 8.70 ng-h/mL per dose (micrograms per kg body weight), respectively. Respective peak serum concentrations (Cmax) for each tablet formulation were 1.26, 1.07, and 1.36 ng/mL per dose. The corresponding dissolution rates, expressed as t50%, were 20.5, 3.06, and 14.1 min, respectively. Data analysis indicated no correlation between dissolution kinetic parameters and the bioavailability parameters AUC and Cmax. However, a linear relationship was observed between dissolution kinetics and both the time to reach maximal serum concentration (tmax) and the observed absorption rate constant (ka).

Animals↗