# US 5,707,975 A · Oral formulations on an antifungal

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- Number: US 5,707,975 A
- Document ID: US5707975A
- Status: Granted
- Kind: A
- Application number: 08/604,950
- Filed: 1996-02-22
- Granted: 1998-01-13
- Earliest claimed: 1996-02-22
- Assignees: Janssen Pharmaceutica NV
- Inventors: Marc Karel Jozef Fran.cedilla.ois; Willy Maria Albert Carlo Dries
- Web page: https://patentgrep.com/patent/US5707975A

## CPC

- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 47/40: Cyclodextrins; Derivatives thereof
- A61K 47/6951: {using cyclodextrin (cyclodextrins used as simple excipients A61K47/40)}
- A61P 31/04: Antibacterial agents
- A61P 31/10: Antimycotics
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES

## Abstract

The present invention concerns a formulation for oral administration comprising an antifungal, a sufficient amount of a cyclodextrin or a derivative thereof, an aqueous acidic medium as bulk liquid carrier and an alcoholic co-solvent Addition of one or more pharmaceutically acceptable sweeteners and one or more pharmaceutically acceptable flavors thereto yields palatable oral formulations. A process of preparing such formulations and pharmaceutical dosage forms comprising said formulations.

## Claims

### Claim 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.

### Claim 2 (depends on 1)

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.

### Claim 3 (depends on 2)

A formulation according to claim 2 wherein the alcoholic co-solvent is propylene glycol.

### Claim 4 (depends on 3)

A formulation according to claim 3 having a pH of 2.0.+-.0.1.

### Claim 5 (depends on 4)

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.

### Claim 6 (depends on 1)

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.

### Claim 7 (depends on 1)

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.