# US 9,750,735 B2 · Pharmaceutical composition containing palonosetron

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- Number: US 9,750,735 B2
- Document ID: US9750735B2
- Status: Granted
- Kind: B2
- Application number: 15/107,503
- Filed: 2014-12-22
- Published: 2016-11-03
- Granted: 2017-09-05
- Earliest claimed: 2013-12-23
- Assignees: Samyang Biopharmaceuticals Corporation
- Applicants: Samyang Biopharmaceuticals Corporation
- Inventors: Hye-Jeong Yoon; Sang-Jun Lee
- Web page: https://patentgrep.com/patent/US9750735B2

## CPC

- A61K 31/473: ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- 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
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- 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)

## Abstract

Provided are a pharmaceutical composition with improved stability including palonosetron, a preparation method thereof, and a pharmaceutical package including the pharmaceutical composition.

## Claims

### Claim 1

A pharmaceutical package, comprising:
a pharmaceutically acceptable container, and
a pharmaceutical composition comprising:
palonosetron or pharmaceutically acceptable salts thereof in the container as an active ingredient at a concentration of 0.01 to 0.5 mg/ml;
a pharmaceutically acceptable aqueous carrier;
a buffering agent, an isotonic agent, or a mixture thereof,
wherein the pharmaceutically acceptable container is a transparent borosilicate glass container, and the glass is a low-expansion borosilicate glass, satisfying ASTM type 1, class A, USP type 1 Powdered Glass, USP Arsenic, EP type 1 Glass Grains (Test B) and EP Arsenic conditions, and
wherein the pH of the pharmaceutical composition is 4 to 6,
wherein the pharmaceutical composition is free of EDTA or a salt thereof,
wherein a total content of heavy metals is maintained to be equal to or less than 50 ppm during a storage period, and
wherein the pharmaceutical composition has storage stability of maintaining the content of palonosetron or a pharmaceutically acceptable salt thereof at 95% by weight to 100% by weight based on the initial content thereof when the pharmaceutical composition is stored at 25 ° C. for 24 months.

### Claim 2 (depends on 1)

The pharmaceutical package of claim 1, wherein the pharmaceutically acceptable container is a glass tubing vial.

### Claim 3 (depends on 1)

The pharmaceutical package of claim 1, wherein the glass satisfies the following conditions:
1) a strain point of less than 510° C.,
2) an annealing point of 550 to 570° C.,
3) a softening point of 800 to 900° C.,
4) a linear coefficient of expansion (0-300 ° C.) of 30×10−7 to 40×10−7, and
5) a density of 2.2 to 2.3 g/cm3.

### Claim 4 (depends on 1)

The pharmaceutical package of claim 1, wherein the glass comprises SiO2≧80%, Al2O3≦5%, Na2O+K2O≦5%, CaO+MgO<0.2%, B2O3≧10% and Fe2O3<0.1%, and does not comprises BaO, ZnO, MnO2, TiO2, and SO3.

### Claim 5 (depends on 1)

The pharmaceutical package of claim 1, wherein the glass container has element extraction data of the following table:
Glass type
Si
Al
Na
K
Ca
Mg
Fe
Ba
Zn
Ti
SiO2
4.8
<0.01
1.1
<0.03
0.13
0.07
<0.012
<0.008
<0.01
<0.005
(unit: ppm, after autoclave in high-purity water at 121° C. for 60 min in a 20-mL container) .