orabase and ethenzamide

With the aim of directly predicting the functionality and mechanism of disintegrants during the disintegration and dissolution of tablets, we investigated an analysis method based on available surface area, which is the surface area of a drug in a formulation in direct contact with the external solvent during dissolution. We evaluated the following disintegrants in this study: sodium starch glycolate (Glycolys), crospovidone (Kollidon CL), carboxymethylcellulose calcium (CMC-Ca), low-substituted hydroxypropylcellulose (L-HPC), and croscarmellose sodium (Ac-Di-Sol). When disintegrant was added to a 50% ethenzamide tablet formulation, an increase in the dissolution rate dependent on disintegrant concentration was observed, according to the type of disintegrant. In addition, the available surface area also differed between disintegrants. For Glycolys, CMC-Ca, and Ac-Di-Sol, a rapid increase in available surface area and a large increase in maximum available surface area (Smax) were observed due to high swellability and wicking, even when the disintegrant concentration was only 1.0%. In contrast, for Kollidon CL and LH-21, a gradual increase in available surface area was observed, depending on the disintegrant concentration. To evaluate the disintegrant ability, Δtmax and ΔSmax were calculated by subtracting peak time (tmax) at 5.0% from that at 1.0% and subtracting Smax at 1.0% from that at 5.0%, respectively, and it was found that the water absorption ratio had strong negative correlations with Δtmax and ΔSmax. Therefore, this study demonstrates that analysis of only available surface area and parameters thereby obtained can directly provide useful information, especially about the disintegration ability of disintegrants.

Topics: Absorption; Carboxymethylcellulose Sodium; Cellulose; Excipients; Povidone; Salicylamides; Solubility; Starch; Surface Properties; Tablets; Water

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