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Novel solid preparation containing block copolymer and anthracycline anticancer agent and process for producing the same

A technology of solid preparations and anticancer agents, applied in the field of anthracycline anticancer agents, capable of solving problems not specifically described

Inactive Publication Date: 2005-08-24
樱井靖久 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the publication does not specifically describe clinically applicable injectable solid dosage forms
The problems of the method of producing the above-mentioned aqueous solution include the processes of ultrasonic irradiation and dialysis which are not easily carried out industrially, and the use of an organic solvent such as dimethylformamide to dissolve the retarded copolymer and doxorubicin in the precipitated retarded copolymer, and isopropyl ether etc.

Method used

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  • Novel solid preparation containing block copolymer and anthracycline anticancer agent and process for producing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] 1000 mg of the retarded copolymer obtained according to the reference example described below, and 18.5 g of sodium bicarbonate were added to 20 ml of the injection solvent, stirred and dissolved at 60 to 70°C, and then the solution was cooled to room temperature. 200mg of doxorubicin hydrochloride and 1000mg of sucrose were separately stirred and dissolved in 40ml of injection solvent. The two solutions were mixed, and the pH was controlled at 6 with sodium hydroxide and hydrochloric acid, and then the total amount was controlled to 100 ml with the injection solvent. The solution was filtered through a membrane filter with a pore size of 0.45 μm, and then filtered and sterilized through a membrane filter with a pore size of 0.2 μm. The solution was filled into vials of 5 ml each, lyophilized, and then the vials were sealed to produce a solid preparation for injection. 5 ml of injection solvent was added to the formulation to re-dissolve the formulation to obtain an aqueous...

Embodiment 2

[0077]1000 mg of the retarding copolymer (same as in Example 1), and 8.8 g of sodium hydroxide were added to 20 ml of injection solvent, stirred and dissolved at 60 to 70°C, and then the solution was cooled to room temperature. 200 mg of doxorubicin hydrochloride and 800 mg of trehalose were stirred and dissolved in 40 ml of injection solvent. The two solutions were mixed, and the pH was controlled at 6 with sodium hydroxide and hydrochloric acid, and then the total amount was controlled to 100 ml with the injection solvent. The solution was filtered through a membrane filter with a pore size of 0.45 μm, and then filtered and sterilized through a membrane filter with a pore size of 0.2 μm. The solution was filled into vials of 5 ml each, lyophilized, and then the vials were sealed to produce a solid preparation for injection. 5 ml of injection solvent was added to the formulation to re-dissolve the formulation to obtain an aqueous solution of the retarding copolymer-doxorubicin co...

Embodiment 3

[0079] 1000 mg of the retarding copolymer (same as in Example 1), and 18.5 g of sodium bicarbonate were added to 20 ml of injection solvent, stirred and dissolved at 60 to 70°C, and then the solution was cooled to room temperature. 200 mg of doxorubicin hydrochloride and 1000 mg of maltose were stirred and dissolved in 40 ml of injection solvent. The two solutions were mixed, and the pH was controlled at 6 with sodium hydroxide and hydrochloric acid, and then the total amount was controlled to 100 ml with the injection solvent. The solution was filtered through a membrane filter with a pore size of 0.45 μm, and then filtered and sterilized through a membrane filter with a pore size of 0.2 μm. The solution was filled into vials of 5 ml each, lyophilized, and then the vials were sealed to produce a solid preparation for injection. 5 ml of injection solvent was added to the formulation to re-dissolve the formulation to obtain an aqueous solution of the retarding copolymer-doxorubicin...

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Abstract

There has been required a clinically applicable solid preparation for injection which contains a block copolymer composed of a hydrophilic polymer structure moiety and a hydrophobic polyamino acid structure moiety and an anthracycline anticancer agent. It is intended to provide a clinically applicable solid preparation for injection which contains a block copolymer composed of a hydrophilic polymer structure moiety and a hydrophobic polyamino acid structure moiety, an anthracycline anticancer agent, a saccharide and a base.

Description

Invention field [0001] The present invention relates to a solid preparation for injection, which comprises a retarding copolymer composed of a hydrophilic polymer structural part and a hydrophobic polyamino acid structural part, and is an anthracycline anticancer agent as a malignant tumor therapeutic agent. The invention also relates to a production method of the preparation. Background technique [0002] Some of the known preparations contain anthracycline anticancer agents in polymer micelles formed by retarding copolymers, which are composed of hydrophilic polymer structural parts that have polyethylene oxide Alkanes are obtained as a main chain and a polyamino acid structure part with fat-soluble substituents on the side chain. [0003] For example, JP-A No. 7-69900 describes an aqueous solution of micelle formulations, which contains a retarding copolymer composed of polyethylene oxide and polyaspartic acid through adriamycin residues and Combined with doxorubicin. [0004]...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/08A61K9/107A61K9/51A61K31/704A61K47/04A61K47/12A61K47/26A61K47/34A61P35/00
CPCA61K47/48315A61K31/704A61K47/48215A61K9/1075A61K47/60A61K47/645A61P35/00A61K9/14A61K47/34A61K9/08
Inventor 本山顺
Owner 樱井靖久
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