Dry Plants Extracts Loaded on Fumed Silica for Direct Compression: Preformulation and Formulation

SANTIAGO DANIEL PALMA; HILARIO MANZO, RUBEN; ALBERTO ALLEMANDI, DANIEL

Pharmaceutical Development And Technology

Lugar: -; Año: 1999 vol. 4 p. 523 - 530

This paper describes the development of a method to load fumed silica with vegetal material (solid residue) from a liquid extract to obtain a solid loaded silica product (LSP) with satisfactory flow properties and compressibility to be processed by direct-compression technology. Extracts of Melissa officinalis L. (M.o.), Cardus marianus L. (C.m.), and Peumus boldus L. (P.b.) were used to load silica support. The release of boldine from LSP (P.b.) reached 100% in HCl 0.1 N solution and only approximately 70% in water. Some physical–mechanical properties of LSP (M.o. and C.m.) alone and LSP–excipient mixtures were determined. The densities (bulk and tap) of LSP were higher than those of fumed silica alone. Consequently, good flow properties of LSP products were observed. On the other hand, flowability, densities, and compactibility of directly compressible excipients (lactose, dicalcium phosphate dihydrate, and microcrystalline cellulose) were not adversely affected when mixed with LSPMelissa officinalis L. (M.o.), Cardus marianus L. (C.m.), and Peumus boldus L. (P.b.) were used to load silica support. The release of boldine from LSP (P.b.) reached 100% in HCl 0.1 N solution and only approximately 70% in water. Some physical–mechanical properties of LSP (M.o. and C.m.) alone and LSP–excipient mixtures were determined. The densities (bulk and tap) of LSP were higher than those of fumed silica alone. Consequently, good flow properties of LSP products were observed. On the other hand, flowability, densities, and compactibility of directly compressible excipients (lactose, dicalcium phosphate dihydrate, and microcrystalline cellulose) were not adversely affected when mixed with LSP(M.o.), Cardus marianus L. (C.m.), and Peumus boldus L. (P.b.) were used to load silica support. The release of boldine from LSP (P.b.) reached 100% in HCl 0.1 N solution and only approximately 70% in water. Some physical–mechanical properties of LSP (M.o. and C.m.) alone and LSP–excipient mixtures were determined. The densities (bulk and tap) of LSP were higher than those of fumed silica alone. Consequently, good flow properties of LSP products were observed. On the other hand, flowability, densities, and compactibility of directly compressible excipients (lactose, dicalcium phosphate dihydrate, and microcrystalline cellulose) were not adversely affected when mixed with LSP