Ursodeoxycholic acid-containing medicament in a liquid adminstration form

• US 5,534,505 A
• Filed: 08/25/1994
• Issued: 07/09/1996
• Est. Priority Date: 08/30/1993
• Status: Expired due to Term

• Current Assignee: Medichemie AG (CSL Limited)
• Original Assignee: Medichemie AG (CSL Limited)
• Inventors: Widauer, Josef O.
• Primary Examiner(s): Dees, Jose G.
• Assistant Examiner(s): KEYS, ROSALYND ANN
• Application Number:
  US08/296,355
• Time in Patent Office: 684 Days
• Field of Search: 514/169, 514/937, 514/944, 514/951, 514/974
• US Class Current: 514/169
• CPC Class Codes: A61K 31/575 substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• CPC Class Codes: 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
• CPC Class Codes: A61P 1/16 for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

The active agent ursodeoxycholic acid has proved therapeutically active in infants, inter alia for the treatment of cholestatic hepatic diseases. A problem when administering this active agent, a bile acid, to infants is its extreme bitterness. As a result of the present invention a taste-acceptable, liquid administration form for ursodeoxycholic acid with an adequately high active agent concentration is described. The liquid to be ingested is a suspension prepared accompanied by the addition of a swelling and/or thickening agent, which contains the active agent mainly in fine crystalline form as the disperse phase and only in a much smaller proportion dissolved in the aqueous dispersant. A remaining residual bitterness can be additionally masked by the addition of β-cyclodextrin or suitable taste correcting agents.

Claims

1. Medicament in a liquid administration form containing ursodeoxycholic acid as the active agent, particularly for the treatment of cholestatic hepatic diseases in infants, characterized in that the liquid to be taken is a suspension prepared by the addition of a swelling or thickening agent which said suspension contains the active agent mainly in a finely crystalline form in the disperse phase and only in a much smaller proportion dissolved in the aqueous dispersant.

2. Medicament according to claim 1, characterized in that over 99% of the fine crystalline active agent has a nucleus size smaller than 90 μ

m.

3. Medicament according to claim 1, characterized in that demineralized water is used as the aqueous dispersant.

4. Medicament according to claim 1, characterized in that the swelling or thickening agent is a microcrystalline cellulose, which is dispersible in water and which contains a proportion of sodium carboxymethyl cellulose as a protective colloid and is present in a quantity range of 0.005 to 0.03 g/ml.

5. Medicament according to claim 1, characterized in that the suspension additionally contains β

-cyclodextrin as a taste masking agent for the active agent dissolved in the dispersant.

6. Medicament according to claim 1, characterized in that the suspension additionally contains as preservatives methylparaben and/or propylparaben and/or benzoic acid.

7. Medicament according to claim 6, characterized in that the suspension additionally contains propylene glycol as a solubilizer for the preservatives.

8. Medicament according to claim 1, characterized in that the suspension additionally contains saccharose as a sweetener and/or flavoring agents.

9. Medicament according to claim 1, characterized in that the suspension contains a sugar substitute.

10. Medicament according to claim 1, characterized in that the suspension has a pH-value adjusted to between 2.5 and 8.