INHALANT COMPRISING MODIFIED SUPEROXIDE DISMUTASE

• US 20110262420A1
• Filed: 11/09/2009
• Published: 10/27/2011
• Est. Priority Date: 12/03/2008
• Status: Abandoned Application

• Current Assignee: Ltt Bio-Pharma Co., Ltd.
• Original Assignee: Ltt Bio-Pharma Co., Ltd.
• Inventors: Mizushima, Toru
• Application Number:
  US13/131,414
• Publication Number:
  US 20110262420A1
• Time in Patent Office: Days
• US Class Current: 424/94.4
• CPC Class Codes: A61K 38/446 Superoxide dismutase (1.15)
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/186 Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
• 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 47/544 Phospholipids
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61K 9/0078 for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

An inhalant containing a lecithinized superoxide dismutase (hereinafter referred to as PC-SOD) which effectively exerts the effect of superoxide dismutase (SOD) as an active ingredient, particularly for treatment of idiopathic (acute) or chronic interstitial pneumonia, is provided. The inhalant includes a PC-SOD represented by the following general formula (I):

SOD′(Q−B)_m  (I)

(wherein SOD′ is a residue of the superoxide dismutase; Q is a chemical crosslinking; B is a residue without a hydrogen atom of a hydroxyl group of lysolecithin having the hydroxyl group at the 2-position of glycerol; and m is the average number of bonds of lysolecithin to one molecule of superoxide dismutase and is an integer of 1 or more).

Claims

1. An inhalant comprising, as an active ingredient, a lecithinized superoxide dismutase represented by the following general formula (I):

SOD′

(Q−

B)_m 

 

(I)

wherein SOD′

is a residue of a superoxide dismutase;

Q is a chemical crosslinking;

B is a residue without a hydrogen atom of a hydroxyl group of lysolecithin having the hydroxyl group at a 2-position of glycerol; and

m is an average number of bonds of lysolecithin to one molecule of superoxide dismutase and is an integer of 1 or more.

2. The inhalant according to claim 1, wherein Q in the formula (I) is —

C—

(O)—

(CH₂)_n—

C(O)—

wherein n is an integer of 2 or more.

3. The inhalant according to claim 1, wherein the SOD′

is a residue of a human superoxide dismutase.

4. The inhalant according to claim 1, wherein the SOD′

is a residue of a modified superoxide dismutase, in which an amino acid at a 111-position of amino acid sequence of a human superoxide dismutase is converted into S-(2-hydroxyethylthio)cysteine.

5. The inhalant according to claim 3, wherein the superoxide dismutase is a superoxide dismutase containing copper and zinc at an active center.

6. The inhalant according claim 2, wherein n is an integer of 2 to 10.

7. The inhalant according to claim 1, wherein m is an integer of 1 to 12.

8. The inhalant according to claim 1, further comprising a stabilizing agent.

9. The inhalant according to claim 8, wherein the stabilizing agent is a sugar.

10. The inhalant according to claim 9, wherein the sugar is sucrose.

11. The inhalant according to claim 9, wherein the sucrose is sucrose processed by activated charcoal.

12. The inhalant according to claim 1, having a form of a fine powder formulation for inhalation.

13. The inhalant according to claim 1, having a form of an aqueous solution for inhalation or a suspension formulation for inhalation.

14. The inhalant according to claim 1, being intratracheally administered.

15. The inhalant according to claim 1, for use in treatment or prevention of interstitial pneumonia.

16. The inhalant according to claim 1, wherein interstitial pneumonia occurs as a side effect of antitumor drugs.