Ciclesonide contained pharmaceutical composition for application to mucosa

• US 6,767,901 B1
• Filed: 07/15/2002
• Issued: 07/27/2004
• Est. Priority Date: 10/20/1999
• Status: Expired due to Term

• Current Assignee: Covis Pharma GmbH (Apollo Global Management, Inc.)
• Original Assignee: Altana Pharma AG (Takeda Pharmaceutical Company Limited)
• Inventors: Nishibe, Yoshihisa, Nagano, Atsuhiro, Takanashi, Kazuya
• Primary Examiner(s): PAK, JOHN D
• Application Number:
  US10/110,629
• Time in Patent Office: 743 Days
• Field of Search: 514/172, 514/174, 514/826, 514/849, 514/853, 514/886, 514/946, 514/958, 514/975, 424/45, 424/46
• US Class Current: 514/174
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present invention provides a pharmaceutical composition for application to the mucosa to be used in drug therapy comprising a water-insoluble and/or water-low soluble substance, ciclesonide, and an aqueous medium, and having an osmotic pressure of less than 290 mOsm. This composition is superior over conventional pharmaceutical compositions for application to the mucosa, due to efficient and high ciclesonide retentivity and permeability to the submucosa or the blood at the mucosa.

Claims

1. An aqueous pharmaceutical composition for application to the mucosa, comprising one or more water-insoluble and/or water-low soluble substance, and ciclesonide, and having an osmotic pressure of 150 mOsm or less.

2. The pharmaceutical composition for application to the mucosa according to claim 1, wherein said osmotic pressure is 60 mOsm or less.

3. The pharmaceutical composition for application to the mucosa according to claim 1, wherein said osmotic pressure is 30 mOsm or less.

4. The pharmaceutical composition for application to the mucosa according to claim 1, wherein said osmotic pressure is 10 mOsm or less.

5. The pharmaceutical composition for application to the mucosa according to claim 1, further comprising an osmotic pressure-controlling agent.

6. The pharmaceutical composition for application to the mucosa according to claim 5, wherein said osmotic pressure-controlling agent is a salt.

7. The pharmaceutical composition for application to the mucosa according to claim 6, wherein said osmotic pressure-controlling agent is sodium chloride.

8. The pharmaceutical composition for application to the mucosa according to claim 5, wherein said osmotic pressure-controlling agent is a water-soluble sugar.

9. The pharmaceutical composition for application to the mucosa according to claim 8, wherein said osmotic pressure-controlling agent is glucose.

10. The pharmaceutical composition for application to the mucosa according to claim 1, wherein said water-insoluble and/or water-low soluble substance is a cellulose.

11. The pharmaceutical composition for application to the mucosa according to claim 10, wherein said cellulose is crystalline cellulose.

12. The pharmaceutical composition for application to the mucosa according to claim 1, wherein said one or more water-insoluble and/or water-low soluble substance is present as solid particles in an aqueous medium.

13. The pharmaceutical composition for application to the mucosa according to claim 1, wherein said one or more water-insoluble and/or water-low soluble substance is dispersed as solid particles in an aqueous medium.

14. The pharmaceutical composition for application to the mucosa according to claim 1, further comprising a water-soluble polymer substance.

15. The pharmaceutical composition for application to the mucosa according to claim 14, wherein said water-soluble polymer is one or more selected from the group consisting of alginic acid, propylene glycol, pectin, low methoxyl pectin guar gum, gum arabic, carrageenan, methyl cellulose, carboxymethyl cellulose sodium, xanthan gum, hydroxypropyl cellulose, and hydroxypropyl methyl cellulose.

16. The pharmaceutical composition for application to the mucosa according to claim 14, wherein said water-soluble polymer is carboxymethyl cellulose sodium.

17. The pharmaceutical composition for application to the mucosa according to claim 14, wherein said water-soluble polymer is xanthan gum.

18. The pharmaceutical composition for application to the mucosa according to claim 15, wherein said water-soluble polymer is hydroxypropyl methyl cellulose.

19. The pharmaceutical composition for application to the mucosa according to claim 14, wherein the combination of said water-insoluble substance and water-soluble polymer is crystalline cellulose carmellose sodium.

20. The pharmaceutical composition for application to the mucosa according to claim 1, further comprising a surfactant.

21. The pharmaceutical composition for application to the mucosa according to claim 20, wherein said surfactant is polysorbate 80.

22. The pharmaceutical composition ion to the mucosa according to claim 1, mucosa is nasal mucosa.