Development of a simple method for the preparation of a silica gel based controlled delivery system with a high drug content.

Silica gel was used as core particles to design a simple preparation for controlled delivery system with a high drug content. Drug loading was carried out by immersing the silica gel in a pre-heated drug solution or suspension. HPLC, SEM, DSC, PXRD analysis and N2 adsorption studies evaluated the drug-loading process. In the next step, the drug-loaded silica gel was coated with hydroxypropyl methylcellulose (HPMC) and an aqueous dispersion of ethylcellulose (Aquacoat) to control the drug release. The release profile was determined using a dissolution test. The results showed that silica gel could adsorb great quantities of the drug, up to about 450 mg/g, by repetition of the loading process. Evaluation of the drug-loading process indicates that drug deposition in the pores occurs during the loading process and the drug-loading efficacy is strongly related to the drug solubility. On the other hand, the dissolution test showed that the drug release could be controlled by polymer coating the drug-loaded silica gel. An HPMC undercoating effectively suppresses the drug release, as it smoothes the drug-loaded core surface and aids in the formation of a continuous Aquacoat coating film. The floating property was also observed during the dissolution test.

Effect of geometric structure of flow promoting agents on the flow properties of pharmaceutical powder mixture.

PURPOSE: The object of this work was to investigate the mechanism of how the surface geometric structure of flow agents affects on the flowability of pharmaceutical powder mixtures. METHODS: Nonporous and porous silicas were mixed with directly compressible fillers as flow promoting agents. The geometric structure of flow agents was investigated by gas adsorption and laser diffraction analysis. Flowability was evaluated with Carr's index measurement. Adhesion force between fillers and flow agents was determined using atomic force microscopy. RESULTS: Flowability was improved with the addition of both nonporous and porous flow agents. In the case of nonporous flow agents, effect to promote flowability decreased with the increase of particle diameter, whereas porous flow agents highly improved flowability independent of particle diameter. Atomic force microscopy measurement found that the adhesion force between a porous agent and filler was smaller than that between a nonporous agent and filler. CONCLUSIONS: Enhancement of flowability varies depending on the geometric structure of flow agents. Porous flow agents improve flow properties more than nonporous agents, because porosity is highly contributed to reduction of adhesion force between particles.