Formulations for poorly soluble drugs comprising hydrophilic polymers.

Abstract:

The present invention provides a drug delivery system comprising nanoparticles or microparticles of a water poorly sol. drug dispersed in a polymeric bead contg. essentially only of hydrophilic polymers (i.e., without hydrophobic polymers). The present invention further provides a method of producing the drug delivery system of the invention. Thus, a 4% sodium alginate soln. was prepd. by mixing 16 g of sodium alginate and 400 g water together with 0.4 g of Bronopol (preservative) at about 37° until complete dissoln. A crosslinking agent was prepd. by dissolving 14.8 g of calcium chloride dihydrate in 1000 g water. An oil-in-water emulsion (20% oil phase, 80% aq. phase) was prepd. contg. 3% surfactant (mixt. of Tween 20 and Span 20, HLB = 10) and 3.3584 g of simvastatine powder (a poorly sol. drug) in 80.0 g toluene. To a mixt. of 95.1 g of 4% sodium alginate soln. and 3.8 g of silica used to prevent shrinking upon drying, was added 95.1 g of the o/w emulsion and stirred together until homogeneous mixt. was achieved. The alginate-emulsion mixt. was introduced into encapsulator and jetted into 100 mM CaCl2 crosslinking soln. to obtain simvastatine beads. [on SciFinder(R)]

Notes:

CAPLUS AN 2005:732592(Patent)