ascorbic-acid and ethenzamide

A rapidly disintegration tablet in the oral cavity was prepared using a glycine as a disintegrant. Effect of disintegrant on the disintegration behavior of the tablet in the oral cavity was evaluated. Wetting time prepared from carboxymethylcellulose (NS-300) having the hardness of 4 kg was 3 s. Tablet containing NS-300 showed fastest disintegration compared to other formulations. These results suggested that NS-300 possessed excellent wetting nature and resulted in the rapid disintegration of tablet. Ethenzamide and ascorbic acid were added to the formulation, and their disintegration behavior were evaluated. Ethenzamide did not affect the disintegration property, however, ascorbic acid prolonged disintegration time. It was suggested that the tablet formulation containing NS-300 and glycine was highly applicable to water-insoluble drug, such as ethenzamide.

Topics: Ascorbic Acid; Carboxymethylcellulose Sodium; Chemistry, Pharmaceutical; Excipients; Glycine; Hardness; Kinetics; Porosity; Salicylamides; Solubility; Tablets; Water

The purpose of this research was to evaluate the use of a rotating fluidized-bed granulator to produce acetaminophen granules with sufficient binding force between particles and good plasticity in tablets. Ethenzamide and ascorbic acid were used to compare the relationship between granulation and the sample wetness. It was revealed that a blade rotation rate of 300 rpm, inlet air flow rate of 42 m3/hr, and spraying pressure of 1.5 kg/cm3 produced tablets with the best properties. The granule and tablet properties of ethenzamide and ascorbic acid were compared to those of acetaminophen. These compounds showed different wetting behaviors with water and different compression behaviors. With an increase in medicament content, tablet hardness increased except for the ascorbic acid formulation. Capping and sticking were observed in acetaminophen and in ascorbic acid, respectively, and acetaminophen and ethenzamide showed prolonged disintegration time.

Topics: Acetaminophen; Analgesics, Non-Narcotic; Ascorbic Acid; Chemistry, Pharmaceutical; Drug Compounding; Hardness; Particle Size; Porosity; Powders; Salicylamides; Solubility; Tablets; Tensile Strength

Computer optimization technique was applied to the simultaneous optimization of wet granulation process by a high-speed mixer granulator. Four pharmaceutical properties, including yield, drug content uniformity, geometrical mean diameter of granules, and uniformity of granule size, were selected to evaluate the quality of the granules. In particular, dependence of drug content uniformity on granule size was investigated using two model drugs, ascorbic acid and ethenzamide. An appreciable dependence of ascorbic acid content on granule size was not observed in model formulations. On the other hand, ethenzamide was contained more in small-size granules, and its content was decreased with an increase in amounts of hydroxypropyl cellulose (HPC-L; used as a binder) and binder solution. These observations suggested that drug content uniformity is influenced not only by drug solubility in the binder solution, but also by the use of HPC-L. A simultaneous optimal point incorporating four pharmaceutical properties was obtained using the generalized distance function. The experimental values of the four response variables obtained in newly prepared granules were found to correspond well with the predicted values of both granules containing ascorbic acid and ethenzamide. These results suggested that computer optimization would benefit the wet granulation process even if drug content segregation was involved in the process. Further, data obtained from computer optimization, in particular the contour diagram, will be valuable in the process validation.

Topics: Ascorbic Acid; Cellulose; Chemistry, Pharmaceutical; Computer Simulation; Dosage Forms; Excipients; Humans; Particle Size; Regression Analysis; Salicylamides; Water

In this study, acetaminophen, ascorbic acid, and ethenzamide were selected as model drugs for tableting granules. Agitation and fluidized-bed granulation were carried out at three drug contents of 30, 50, and 70%. Compared with agitation granulation, granules made by fluidized-bed granulation showed superior compressibility with wide formulation allowance for drug type and amount. Fluidized-bed granulation resulted in less granule hardness and greater plastic deformability. The granules had considerable compactness and for tablets containing 70% ethenzamide, prolonged disintegration and dissolution times were noted. These are typical features of granules produced by fluidized-bed granulation.

Topics: Acetaminophen; Ascorbic Acid; Drug Compounding; Excipients; Hardness Tests; Microscopy, Electron, Scanning; Particle Size; Powders; Salicylamides; Solubility; Tablets