| 摘要 |
Compsn. for intravenous admin. of a staurosporin deriv. (S) which is sparingly soluble in water comprises: (a) (S) as above; (b) ≥ 1 pure phospholipid of formula (I) or its salt; (c) a triglyceride of formula (II); (d) a partial fatty acid ester (III) of polyoxyethylene sorbitan; (e) water for intravenous injection; and (f) opt. water-soluble adjuvants for injection compsns. R1 = 10-20C acyl; R2 = H or 10-20C acyl; R3 = H, 2-(trimethylamino-1-ethyl, 2-amino-1-ethyl, 1-4C alkyl, 1-5C alkyl (substd. by COOH or OH, or by COOH and OH or NH2), inositol or glyceryl; R4-R6 = 8-24C acyl (sic). Also claimed are: (A) the prodn. of a compsn. contg. (S) as above comprising: (i) mixing a liposome dispersion contg. (I) and opt. (e) with a homogeneous oil phase of (II) and (c); and (ii) forming a clear dispersion by high pressure homogenisation; and either: (iiia) adding water and opt. (e); (iiib) filtering and opt dialysing; or (iii') filtering, dialysing and drying, opt with (e); and (iii'') reconstitution to an injectable dispersion; (B) the nanoemulsion concentrate or dry compsn. obtd. using process (A); (C) a nanoemulsion contg. (S) for therapy; and (D) a nanoemulsion contg. N-benzoyl staurosporin (S1) for use in tumour therapy. |
