# US 2010/0168140 A1 · Easily Absorbable Oral Preparations of Xanthine Derivatives

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- Number: US 2010/0168140 A1
- Document ID: US20100168140A1
- Status: Published application
- Kind: A1
- Application number: 12/086,550
- Filed: 2006-12-14
- Published: 2010-07-01
- Earliest claimed: 2005-12-14
- Assignees: Kyowa Hakko Kogyo Co., Ltd.
- Inventors: Makoto Kigoshi; Hideki Kato; Noboru Aoki
- Web page: https://patentgrep.com/patent/US20100168140A1

## CPC

- A61K 9/1617: {Organic compounds, e.g. phospholipids, fats}
- 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)}
- A61K 9/1611: {Inorganic compounds}
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/4858: {Organic compounds}
- A61K 31/52: Purines, e.g. adenine
- A61K 31/522: having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
- A61P 11/08: Bronchodilators
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 13/12: of the kidneys
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

An object of the present invention is to provide an easily absorbable oral preparation containing a xanthine derivative or a pharmaceutically acceptable salt thereof and a fatty acid or a fatty acid derivative for the purpose of providing an easily absorbable oral preparation containing the xanthine derivative of which absorbability has been enhanced by dissolving the xanthine derivative that shows adenosine A1 receptor antagonistic activity and has diuretic activity, kidney-protecting activity, bronchodilating activity, cerebral function-improving activity, anti-dementia activity or the like in a solvent.

## Claims

### Claim 1

An easily absorbable oral preparation which comprises a xanthine derivative represented by formula (I):
(wherein R1 and R2 are the same or different and represent substituted or unsubstituted lower alkyl, and Q represents hydrogen or hydroxy) or a pharmaceutically acceptable salt thereof and a fatty acid or a fatty acid derivative.

### Claim 2 (depends on 1)

The easily absorbable oral preparation according to claim 1, wherein the fatty acid or the fatty acid derivative is acetic acid, propionic acid, a saturated or unsaturated fatty acid having 4 to 22 carbon atoms, a saturated or unsaturated fatty acid in which the hydrogen atom of alkyl or alkenyl moiety having 3 to 21 carbon atoms is substituted by hydroxy or O(C2H4O)XH (wherein X represents 0 to 100) or a derivative thereof.

### Claim 3 (depends on 1)

The easily absorbable oral preparation according to claim 1, wherein the fatty acid or the fatty acid derivative is a fatty acid derivative represented by formula (II):
{wherein R3 represents methyl; ethyl; alkyl, alkenyl or alkadienyl having 3 to 21 carbon atoms; or alkyl, alkenyl or alkadienyl having 3 to 21 carbon atoms substituted by hydroxy or O(C2H4O)XH (wherein X represents 0 to 100), and R4 represents hydrogen; methyl; ethyl; alkyl, alkenyl or alkadienyl having 3 to 21 carbon atoms; formula (III):
[wherein R5 and R6 are the same or different and represent hydrogen; methyl; ethyl; alkyl, alkenyl or alkadienyl having 3 to 21 carbon atoms; or (C2H4O)YCOR7 (wherein R7 represents hydrogen; methyl; ethyl; alkyl, alkenyl or alkadienyl having 3 to 21 carbon atoms; or alkyl, alkenyl or alkadienyl having 3 to 21 carbon atoms substituted by hydroxy or O(C2H4O)ZH (wherein Z represents 0 to 100), and Y represents 0 to 100), and m represents 0 to 100]; formula (IV):
(wherein R5 and R6 have the same meanings as defined above respectively, and n represents 0 to 100); formula (V):
[wherein R5 and R6 have the same meanings as defined above respectively, and R8 represents hydrogen; methyl; ethyl; alkyl, alkenyl or alkadienyl having 3 to 21 carbon atoms; or (C2H4O)WH (wherein W represents 0 to 100)]; or formula (VI):
(wherein R5, R6 and R8 have the same meanings as defined above respectively)}.

### Claim 4 (depends on 3)

The easily absorbable oral preparation according to claim 3, wherein R3 is methyl; alkyl, alkenyl or alkadienyl having 11, 13, 15, 17 or 19 carbon atoms; or alkyl, alkenyl or alkadienyl having 11, 13, 15, 17 or 19 carbon atoms substituted by hydroxy or O(C2H4O)XH (wherein X represents 0 to 100).

### Claim 5 (depends on 3)

The easily absorbable oral preparation according to claim 3, wherein R3 is methyl, cis-8-heptadecenyl, or cis-8-heptadecenyl or heptadecyl in which a carbon atom at position 11 is substituted by hydroxy or O(C2H4O)XH (wherein X represents 0 to 100).

### Claim 6 (depends on 3)

The easily absorbable oral preparation according to claim 3, wherein R4 is formula (III), (IV), (V) or (VI), R5 and R6 are the same or different and are hydrogen or (C2H4O)YCOR7, at least one of R5 and R6 being (C2H4O)YCOR7, and R7 is hydrogen; alkyl, alkenyl or alkadienyl having 15 to 21 carbon atoms; or alkyl, alkenyl or alkadienyl having 15 to 21 carbon atoms substituted by hydroxy or O(C2H4O)ZH (wherein Z represents 0 to 100).

### Claim 7 (depends on 3)

The easily absorbable oral preparation according to claim 3, wherein R4 is formula (III), (IV) or (V), and R5 and R6 are the same or different and are hydrogen; or alkyl, alkenyl or alkadienyl having 15 to 21 carbon atoms.

### Claim 8 (depends on 1)

The easily absorbable oral preparation according to claim 1, wherein the fatty acid or the fatty acid derivative is a fatty acid or a fatty acid derivative which is available either as vinegar or olive oil.

### Claim 9 (depends on 1)

The easily absorbable oral preparation according to claim 1, wherein the fatty acid or the fatty acid derivative is one or more selected from acetic acid, octadecaenoic acid, hydroxyoctadecanoic acid, hydroxyoctadecaenoic acid and derivatives thereof.

### Claim 10 (depends on 1)

The easily absorbable oral preparation according to claim 1, wherein the fatty acid or the fatty acid derivative is one or more selected from acetic acid, oleic acid, monooleic acid sorbitan, trioleic acid sorbitan and polyoxyethylene sorbitan monooleate.

### Claim 11 (depends on 1)

The easily absorbable oral preparation according to claim 1, wherein the fatty acid or the fatty acid derivative is acetic acid or oleic acid.

### Claim 12 (depends on 1)

The easily absorbable oral preparation according to claim 1, which further comprises a fatty acid or a fatty acid derivative which is available as any of Wittepzol™H5, Wittepzol™H15, Wittepzol™ S51, Wittepzol™ S55, Gelucire™ and Suppocire™.

### Claim 13 (depends on 1)

The easily absorbable oral preparation according to claim 1, which further comprises one or more selected from microcrystalline cellulose, hydrated silicon dioxide, light silicic anhydride, aluminum silicate, calcium silicate and magnesium methasilicate aluminate.