# US 2010/0166853 A1 · Coated preparation

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- Number: US 2010/0166853 A1
- Document ID: US20100166853A1
- Status: Published application
- Kind: A1
- Application number: 12/452,587
- Filed: 2008-07-10
- Published: 2010-07-01
- Earliest claimed: 2007-07-12
- Assignees: Takeda Pharmaceutical Company Limited
- Inventors: Hiroto Bando; Yoshihiro Omachi; Kenichiro Kiyoshima
- Web page: https://patentgrep.com/patent/US20100166853A1

## CPC

- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 9/1676: {having a drug-free core with discrete complete coating layer containing drug (adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921)}
- A61K 9/2095: {Tabletting processes}
- A61K 9/5078: {with drug-free core}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- 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

The present invention provides a preparation containing pioglitazone or a salt thereof as an active ingredient, which shows high bioavailability of pioglitazone and less interindividual variation in blood drug concentration, as well as a preparation with suppressed color change during preservation. The preparation contains a core containing a pharmaceutically acceptable organic acid with water solubility at 20° C. of not less than 10 mg/mL and pKa1 (a negative common logarithm of the first acid dissociation constant Ka1) at 25° C. of not more than 5, and a coating layer containing pioglitazone or a salt thereof. The coating layer may further contain mannitol or trehalose.

## Claims

### Claim 1

A preparation comprising
a core comprising a pharmaceutically acceptable organic acid with water solubility at 20° C. of not less than 10 mg/mL and pKa1 (a negative common logarithm of the first acid dissociation constant Ka1) at 25° C. of not more than 5, and a coating layer comprising pioglitazone or a salt thereof.

### Claim 2 (depends on 1)

The preparation of claim 1, wherein the pharmaceutically acceptable organic acid is at least one kind selected from citric acid, tartaric acid, malic acid and ascorbic acid.

### Claim 3 (depends on 1)

The preparation of claim 1, wherein the pharmaceutically acceptable organic acid is citric acid.

### Claim 4 (depends on 1)

The preparation of claim 1, wherein the coating layer comprises mannitol or trehalose.

### Claim 5 (depends on 1)

The preparation of claim 1, wherein the pharmaceutically acceptable organic acid is citric acid crystal.

### Claim 6 (depends on 1)

The preparation of claim 1, wherein the weight ratio of pioglitazone and the pharmaceutically acceptable organic acid is 1:4 to 1:26.

### Claim 7 (depends on 1)

The preparation of claim 1, wherein the coating layer comprises cellulose or a cellulose derivative,

### Claim 8 (depends on 7)

The preparation of claim 7, wherein the cellulose derivative is low-substituted hydroxypropylcellulose.

### Claim 9 (depends on 1)

The preparation of claim 1, having a construct constituting the coating layer, which comprises a cellulose derivative as a skeleton and is maintained in an aqueous solvent.

### Claim 10 (depends on 9)

The preparation of claim 9, wherein the construct is present for at least 10 min in McIlvaine buffer (pH 3.0, 900 mL) under the conditions of the Paddle Method (50 rpm).

### Claim 11 (depends on 1)

The preparation of claim 1, wherein a construct constituting the coating layer, which comprises a cellulose derivative as a skeleton and is maintained in an aqueous solvent, wherein pioglitazone or a salt thereof is dissolved in an organic acid solution in the construct to afford an aqueous solution.

### Claim 12 (depends on 1)

The preparation of claim 1, which shows bioavailability exceeding 75% in a dog.

### Claim 13 (depends on 1)

The preparation of claim 1, wherein the pharmaceutically acceptable organic acid is at least one kind of crystals selected from citric acid, tartaric acid, malic acid and ascorbic acid.

### Claim 14 (depends on 7)

The preparation of claim 7, wherein the content of the cellulose or cellulose derivative in the coating layer is 0.5-70 parts by weight, per 100 parts by weight of the coating layer.