# US 9,040,017 B2 · Liver-receptor imaging injection, dispensing method and pharmaceutical composition thereof

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- Number: US 9,040,017 B2
- Document ID: US9040017B2
- Status: Granted
- Kind: B2
- Application number: 13/243,225
- Filed: 2011-09-23
- Published: 2012-05-03
- Granted: 2015-05-26
- Earliest claimed: 2010-10-29
- Assignees: Institute of Nuclear Energy Research Atomic Energy Council, Executive Yuan
- Applicants: Mei-Hui Wang; Wuu-Jyh Lin; Hung-Man Yu; Chuan-Yi Chien; Ping-Yen Wang
- Inventors: Mei-Hui Wang; Wuu-Jyh Lin; Hung-Man Yu; Chuan-Yi Chien; Ping-Yen Wang
- Web page: https://patentgrep.com/patent/US9040017B2

## CPC

- A61K 51/0491: {Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers}
- A61K 51/0406: {Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines}
- A61K 51/0497: {conjugates with a carrier being an organic compounds}
- A61K 51/065: {conjugates with carriers being macromolecules}
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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 is related to a pharmaceutical composition for a liver-receptor imaging injection, the pharmaceutical composition including a bi-functional compound which has a ASGPR specificity, wherein the bi-functional compound includes a backbone of alpha-amino acid (or the derivatives thereof) and a poly-galactosamine chain (or a poly-lactose chain) connected to the alpha-amino acid. Thereby, the pharmaceutical composition can quantify potential of liver storage ability and evaluate severity of the course of liver disease. A liver-receptor imaging injection using the same and the one-step dispensing method thereof are also provided to improve defects of iodine-labeled and overcome disadvantages of the reduced labeling-yield and the instability after autoclave sterilization.

## Claims

### Claim 1

A pharmaceutical composition, wherein the pharmaceutical composition is a precursor capable of being labeled with a radionuclide for a liver receptor imaging injection, comprising:
a bi-functional compound having a structure of formula,
D-{A-(B)n}k
wherein A is lysine or the derivative thereof, B is lactose or a derivative thereof, D is aspartic acid or a derivative thereof, n is 1, and k is 1;
a citrate of about 10 to about 100 mg; and
a citric acid of about 10 to about 100 mg.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the derivative of D is Nα-(trifluoroacetaminohexanoyl)-L-aspartic acid.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1, wherein the derivative of A is ε-benzyloxycarbonyl-N,N-bis(carboxymethyl)-L-lysine.

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1, wherein the citrate is trisodium citrate.

### Claim 5 (depends on 1)

The pharmaceutical composition of claim 1, wherein the citric acid and the citrate remain at pH of about 4 in an aquatic condition.

### Claim 6 (depends on 1)

The pharmaceutical composition of claim 1, wherein the pharmaceutical composition further comprises mannitol and is a lyophilized dosage form.

### Claim 7 (depends on 1)

The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is a lyophilized dosage form.

### Claim 8 (depends on 1)

A method for preparing a liver-receptor imaging injection, comprising steps of:
storing the pharmaceutical composition of claim 1 and a radionuclide in a first container and a second container respectively; and
adding the radionuclide in the second container into the first container to react about 10 to 30 minutes to obtain the liver-receptor imaging injection.

### Claim 9 (depends on 8)

The method of claim 8, wherein the pharmaceutical composition further comprises mannitol and is a lyophilized dosage form.

### Claim 10 (depends on 8)

The method of claim 8, wherein the radionuclide in the second container is added into the first container to react about 10 to 30 minutes at room temperature.

### Claim 11 (depends on 8)

The method of claim 8, wherein the radionuclide is DTPA-chelated In-111.