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

2005; Elsevier BV; Volume: 26; Issue: 1 Linguagem: Inglês

10.1016/j.ejps.2005.05.002

1879-0720

Kotoe Ohta, Masayoshi Fuji, Takashi Takei, Masatoshi Chikazawa,

Drug Solubulity and Delivery Systems

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.