# US 4,985,242 A · Intranasally applicable powdery pharmaceutical composition

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- Number: US 4,985,242 A
- Document ID: US4985242A
- Status: Granted
- Kind: A
- Application number: 07/132,447
- Filed: 1987-12-14
- Granted: 1991-01-15
- Earliest claimed: 1985-02-25
- Assignees: Teljin Limited
- Inventors: Kunio Sekine; Daisuke Araki; Yoshiki Suzuki
- Web page: https://patentgrep.com/patent/US4985242A

## CPC

- A61K 9/0043: {Nose}
- A61K 47/186: {Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide}
- 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)

## Abstract

An intranasally applicable powdery pharmaceutical composition comprising a polypeptide having a physiological activity, a quaternary ammonium compound, and a lower alkyl ether of cellulose. This powdery pharmaceutical composition has an excellent preservability and chemical stability of the polypeptides and, when the powdery composition is administered to the nasal cavity in the form of a spray, the polypeptides are effectively absorbed through the nasal mucosa.

## Claims

### Claim 1

An intranasally applicable powdery pharmaceutical composition comprising a pharmaceutically effective amount of a polypeptide having a physiological activity and about 0.001% to 12% by weight, based on the total weight of the composition, of at least one quaternary ammonium compound selected from the group consisting of benzalkonium chloride, benzethonium chloride, cetyl trimethyl ammonium bromide, and dodecyl dimethyl ammonium bromide in at least one lower alkyl ether of cellulose selected from the group consisting of hydroxypropyl cellulose, methyl cellulose, hydroxyethyl cellulose and hydroxpropylmethyl cellulose.

### Claim 2 (depends on 1)

A powdery pharmaceutical composition as claimed in claim 1, wherein the polypeptide has a molecular weight of 300 to 300,000.

### Claim 3 (depends on 1)

A powdery pharmaceutical composition as claimed in claim 1, wherein the polypeptide is at least one member selected from the group consisting of peptide hormones, physiologically active proteins, zymoproteins, and vaccines.

### Claim 4 (depends on 3)

A powdery pharmaceutical composition as claimed in claim 3, wherein the peptide hormones include calcitonin, insulin luteinzing hormone-releasing hormones, desmopressin, vasopressin, oxytocin, and inteferons.

### Claim 5 (depends on 1)

A powdery pharmaceutical composition as claimed in claim 1, wherein the quaternary ammonium compound is benzalkonium chloride or benzethonium chloride.

### Claim 6 (depends on 1)

A powdery pharmaceutical composition as claimed in claim 1, wherein the lower alkyl ether of cellulse is hydroxypropyl cellulose.

### Claim 7 (depends on 1)

A powdery pharmaceutical composition as claimed in claim 1, wherein the quaternary ammonium compound is included therein in an amount of about 0.025% to 1% by weight based on the total weight of the composition.

### Claim 8 (depends on 1)

A powdery pharmaceutical composition of claim 1, wherein the composition is prepared by mixing (i) a lyophilized mixture of the polypeptide having a physiological activity, a portion or total amount of the quaternary ammonium compound, and a portion of the lower alkyl ether of cellulose, (ii) the remainder of the lower alkyl ether of cellulose, and, optionally (iii) the quaternary ammonium.

### Claim 9 (depends on 8)

A powdery pharmaceutical composition as claimed in claim 8, wherein the amount of the component (ii) is 0.01% to 10% by weight of the total amount of the lower alkyl ether of cellulose in the composition.

### Claim 10 (depends on 1)

A powdery pharmaceutical composition as claimed in claim 1, wherein at least about 90% by weight of the powder particles of the pharmaceutical composition has an effective particle diameter of about 10 to 250 .mu.m.

### Claim 11 (depends on 1)

A powdery pharmaceutical preparation in unit dosage form for application to the mucosa of the nasal cavity comprising the powdery pharmaceutical composition of claim 1.

### Claim 12 (depends on 11)

A powdery pharmaceutical preparation as claimed in claim 11, wherein the pharmaceutical composition is included in a capsule.