Claims
- 1. A formulation for oral administration comprising:
- (a) itraconazole or saperconazole;
- (b) a sufficient amount of a hydroxypropyl-.beta.-cyclodextrin having an M.S. in the range of 0.3 to 3 and containing less than 5% unsubstituted .beta.-cyclodextrin, to act as a solubilizer for the itraconazole or saperconazole;
- (c) an aqueous acidic medium as bulk liquid carrier;
- (d) from about 1% (v/v) to about 20% (v/v) of an alcoholic co-solvent selected from the group consisting of ethanol, propylene glycol and glycerol;
- (e) one or more pharmaceutically acceptable intense sweeteners plus one or more bulk sweeteners; and
- (f) one or more pharmaceutically acceptable flavors.
- 2. A formulation according to claim 1 wherein the cyclodextrin is hydroxypropyl-.beta.-cyclodextrin having an M.S. in the range of 0.35 to 0.50 and containing less than 1.5% unsubstituted .beta.-cyclodextrin.
- 3. A formulation according to claim 2 wherein the alcoholic co-solvent is propylene glycol.
- 4. A formulation according to claim 3 having a pH of 2.0.+-.0.1.
- 5. A formulation according to claim 4 wherein the intense sweetener is selected from the group consisting of saccharin, sodium or calcium saccharin and the bulk sweetener is selected from the group consisting of sorbitol, mannitol, fructose, sucrose, maltose, glucose, caramel or honey.
- 6. A formulation according to claim 1 comprising by weight or by volume based on the total volume of the formulation:
- (a) 4% (w/v) itraconazole;
- (b) 60% (w/v) hydroxypropyl-.beta.-cyclodextrin;
- (c) 10% (v/v) propylene glycol;
- (d) acid and base to adjust the pH of the composition within the range of 2.0.+-.0.1;
- (e) 0.08% (w/v) sodium saccharin;
- (f) up to 1% (w/v) of one or more flavours; and
- (g) water.
- 7. A formulation according to claim 1 comprising by weight or by volume based on the total volume of the formulation:
- (a) 1% (w/v) itraconazole or saperconazole;
- (b) 40% (w/v) hydroxypropyl-.beta.-cyclodextrin;
- (c) 10% (v/v) propyleneglycol;
- (d) acid or base to adjust the pH of the composition within the range of 2.0.+-.0.1;
- (e) 0.06% (w/v) sodium saccharin;
- (f) 19% (v/v) sorbitol (70%) non-crystallizing solution;
- (g) up to 1% (w/v) of one or more flavours;
- (h) 0.02% (w/v) of a carmel sweetener; and
- (i) water.
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is based upon PCT application Ser. No. PCT/EP 94/03169, filed Sep. 22, 1994, which claims priority from U.S. patent application Ser. No. 08/129,504, filed on Sep. 30, 1993 now abandoned.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/EP94/03169 |
9/22/1994 |
|
|
2/22/1996 |
2/22/1996 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO95/08993 |
4/6/1995 |
|
|
US Referenced Citations (11)
Foreign Referenced Citations (1)
Number |
Date |
Country |
9319061 |
Sep 1993 |
WOX |
Non-Patent Literature Citations (2)
Entry |
Hostetler et al., "Effect of Cyclodextrin on the Pharmacology of Antifungal Oral Azoles", Antimicrobial Agents And Chemotherapy, Feb. 1992, pp. 477-480. |
Pitha et al., "Preparation of drug:hydroxypropylcyclodextrin complexes by a method using ethanol or aqueous ammonium hydroxide as co-solubilizers", International Journal of Pharmaceutics, 80 (1992) 253-258. |