Crude drugs are usually supplied in the form of powder or flakes, which have various shapes and undesirable properties such as poor fluidity and adhesiveness. Those inherent properties often bring difficulty in handling and quality control in the manufacturing process of drug products. Therefore, the granulation of crude drug powders is considered to be meaningful for not only convenience of taking a granulated dosage form but also sequential tableting operation. We studied the granulation conditions of crude drug powders by the fluidized bed granulation method. Powdered Senna Leaf was selected as a model crude drug. The powders were pre-granulated with distilled water and sequentially granulated with 10% (w/v) hydroxy propyl cellulose (HPC) and dried until their temperature reacted 45°Cin the granulator. The properties of granules—size distribution, mean diameter, angle of repose, bulk density, strength and compressibility—were examined, and the correlation between those properties and volume of distilled water and HPC solution was analyzed by multiple regression analysis. The properties of crude drug granules were strongly affected by the volumes of distilled water and HPC solution. The relationship between various parameters mentioned above were shown as correlative equations. The regression analyses of them would give useful information for the preparation of granules that show desirable properties once the granulation operation has been experimentally done.

We reported previously the granulation of Powdered Senna Leaf by the fluidized bed granulation method (J. Pharm. Sci. Technol., Jpn., 66, 457-463, 2006). In this study, we investigated the effect of physical properties of the granules on tableting in terms of hydroxy propyl cellulose (HPC) binder solution, tensile strength, friability, disintegration and dissolution rate. The relationships among those properties were analyzed by multiple regression analysis and given by correlative equations. They would give useful information for the manufacturing of crude drug tablets that show desirable properties once the granulation and tableting operation have been experimentally done.

A rapidly disintegrating tablet is known to be a form that can be swallowed easily because it is deformed by sputum in the human oral cavity. In this study, the tablet was prepared by the dry granulation and compression method using powdered cellulose (PC) as the main excipient. Powdered cellulose is expected to be good for not only compressibility but also disintegration due to its swelling property. It also has the advantage of lower cost compared with other excipients such as microcrystalline cellulose. Batches containing some model drugs, PC, lactose (Lac) and L-HPC as excipients were compacted to flakes by a Roller Compactor, then the flakes were crushed and sieved to granules. The granules were mixed with sucrose fatty acid esters (SE) as a lubricant and AEROSIL (AERO) as a fluidized ingredient then compressed to tablets by a rotary tableting machine. The tablets were evaluated mainly by tensile strength and disintegration time. Consequently, the rapidly disintegrating tablets containing PC were successfully prepared by the dry granulation and compression method. Fluidity of the granules and tensile strength of the tablets were improved by using 0.1% AERO. As the amounts of SE were increased, the tensile strength became lower and the disintegration time became longer, but from the pressure transmission ratio, the optimal amounts were 1-2%. PC had very good compressibility and disintegrated more rapidly after blending with L-HPC than using L-HPC alone. Although the evaluations on sensory test worsened as the amounts of PC increased, it was improved by using saccharides such as Lac. Optimal proportions of PC, Lac and L-HPC could be determined by Artificial Neural Network.