| 摘要 |
Aqueous nanosphere suspension comprises nanospheres consisting of: (1) an amorphous lipophilic active ingredient (I) selected from dehydroepiandrosterone and its precursors and derivatives, pentacyclic triterpene acids, hydroxystilbenes, isoflavonoids and aminophenol derivatives; and (2) a surfactant (II). Aqueous nanosphere suspension comprises nanospheres with an average size of 10-1000 nm consisting of: (1) an amorphous lipophilic active ingredient (I) selected from dehydroepiandrosterone (DHEA) and its precursors and derivatives (other than cholesterol, plant sterols and their esters), pentacyclic triterpene acids, hydroxystilbenes, isoflavonoids and aminophenol derivatives of formula (III); and (2) a surfactant (II) capable, at its critical micelle concentration (cmc), of reducing the interfacial tension of a hexane/water system from 51 mN/m - 12 mN/m or less and/or reducing the surface tension of water to 50 mN/m or less. R = CONR1R2, COOR3 or SO2R3; R1 = H or (un)saturated 1-6C alkyl optionally substituted by OH; R2 = H or (un)saturated 12-30C alkyl or (poly)cycloalkyl optionally substituted by OH; and R3 = (un)saturated 12-30C alkyl or (poly)cycloalkyl optionally substituted by OH. Independent claims are also included for the following: (1) a process for producing the suspension, comprises: (i) dissolving (I) in a volatile water-miscible solvent at a concentration of 0.1-30 wt.%; (ii) stirring the solution into an aqueous phase, where the solution and/or the aqueous phase contains (II) at a concentration at least equal to its cmc; and (iii) evaporating the solvent and optionally part of the water; (2) a process for producing the suspension, comprises: (i) dissolving (I) in a volatile water-miscible solvent at a concentration of 0.1-30 wt.%; (ii) emulsifying the solution with an aqueous phase, where the solution and/or the aqueous phase contains (II) at a concentration at least equal to its cmc; and (iii) evaporating the solvent and optionally part of the water.
|
