Powdery pharmaceutical composition for nasal administration

• US 4,613,500 A
• Filed: 03/09/1984
• Issued: 09/23/1986
• Est. Priority Date: 03/09/1983
• Status: Expired due to Term

• Current Assignee: Teijin Limited
• Original Assignee: Teijin Limited
• Inventors: Suzuki, Yoshiki, Sekine, Kunio, Nagai, Tsuneji, Nishimoto, Yuji, Nambu, Naoki
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/587,779
• Time in Patent Office: 928 Days
• Field of Search: 424/46, 424/85, 424/89, 424/92, 514/773, 514/774, 514/775, 514/776, 514/777, 514/778, 514/782, 514/951, 514/958, 514/213, 514/12-19
• US Class Current: 424/85.4
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system

Abstract

What is provided by this invention is a powdery pharmaceutical composition for nasal administration comprising physiologically active polypeptide or its derivative such as calcitonin, insulin, etc. and a water-absorbing and water-insoluble base. The pharmaceutical composition allows polypeptide or its derivative to be efficiently absorbed through the nasal macous membrane when it is nasally administered.

Claims

1. A method for nasal pharmaceutical administration which comprises the step of contacting the nasal mucosa with an intranasally effective amount of a powdery pharmaceutical composition for nasal adminstration consisting essentially of:

(A) a physiologically active polypeptide or its derivative selected from the group consisting of a peptide hormone, a physiologically active protein, an enzyme protein and a vaccine, and (B) a water-absorbing and water-insoluble base, wherein at least 90 wt % of the particles of said composition have an effective diameter ranging from 10 to 250 microns.

2. A method for nasal adminstration according to claim 1, wherein said base is a water-abosrbing and water-insoluble substance selected from the group consisting of cellulose, starche, protein, cross-linked vinyl polymer and gum.

3. A method for nasal administration according to claim 1, wherein said base is a water-absorbing and water-insoluble cellulose.

4. A method for nasal adminstration according to claim 3, wherein said water-absorbing and water-insoluble cellulose is selected from the group consisting of crystalline cellulose, cellulose, α

-cellulose, and cross-linked sodium carboxymethyl cellulose.

5. A method for nasal adminstration according to claim 3, wherein said water-absorbing and water-insoluble cellulose is crystalline cellulose.

6. A method for nasal adminstration according to claim 1, wherein said base is a water-abosrbing and water-insoluble cross-linked vinyl polymer.

7. A method for nasal administration according to claim 6, wherein said water-absorbing and water-insoluble cross-linked vinyl polymer is selected from the group consisting of cross-linked polyvinyl pryolidone and cross-linked carboxy vinyl polymer.

8. A method for nasal adminstration according to claim 1, wherein said water-absorbing and water-insoluble base is jointly used with a water-abosrbing and water-soluble base, wherein said water-absorbing and water-soluble base is employed in an amount of 0.1 to 60 wt % based on the weight of said water-absorbing and water-insoluble base.

9. A method for nasal administration according to claim 8, wherein said water-absorbing and water-soluble base is selected from the group consisting of a lower alkyl ether of cellulose, polyacrylate, polyethylene glycol and polyvinyl pyrolidone.

10. A method for nasal administration according to claim 1, wherein the physiologically active polypeptide or its derivative is a polypeptide or its derivative with a molecular weight of 1,000 to 300,000.

11. A method for nasal administration according to claim 1, wherein the physiologically active polypeptide or its derivative is a water-soluble polypeptide or its derivative.

12. A method for nasal administration according to claim 1, wherein the physiologically active polypeptide or its derivative is a peptide hormone.

13. A method for nasal adminstration according to claim 12, wherein the peptide hormone is selected from the group consisting of calcitonin, insulin, luteinizing hormone releasing hormone, desmopressin, vasopressin and oxytocin.

14. A method for nasal administration according to claim 1, wherein the physiologically active polypeptide or its derivative is a vaccine.

15. A method for nasal administration according to claim 14, wherein the vaccine is influenza vaccine or pertussis vaccine.

16. A method for nasal administation according to claim 1, wherein the physiologically active polypeptide or its derivative is a physiologically active protein.

17. A method for nasal administration according to claim 16, wherein the physiologically active protein is interferon.

18. A method for nasal adminstration according to claim 1, wherein said water-absorbing and water-insoluble base is employed in an amount of more than 10 times the weight of said polypeptide or its derivative.