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Preparation method of irinotecan hydrochloride injection

A technology of irinotecan hydrochloride and injection, which is applied in the field of medicine, can solve the problems such as easy precipitation of irinotecan hydrochloride, achieve stable product quality, avoid the reduction of curative effect, and have good safety effects

Pending Publication Date: 2019-06-21
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present invention aims to provide a preparation method of irinotecan hydrochloride injection, to solve the problem that irinotecan hydrochloride is easily precipitated in aqueous solution, and obtain stable product quality, simple and convenient preparation process, and facilitate commercial production

Method used

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  • Preparation method of irinotecan hydrochloride injection
  • Preparation method of irinotecan hydrochloride injection
  • Preparation method of irinotecan hydrochloride injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Comparative example 1 prescription quantity:

[0032] Element Dosage (200ml prescription) Irinotecan hydrochloride (calculated as trihydrate) 4.0g Sorbitol 9.0g phosphoric acid Appropriate amount, adjust the pH value to 3.0-3.8 Water for Injection Dilute to 200ml

[0033] Remarks: Use 2ml brown vials to fill 100 vials.

[0034] The preparation process takes 75%-85% of the full amount of water for injection at room temperature, sequentially adds the prescribed amount of sorbitol and irinotecan hydrochloride, heats and stirs at 70°C ± 5°C until completely dissolved, and cools to room temperature. Adjust the pH of the medicinal solution to 3.0-3.8 with phosphoric acid, and add water for injection to make up the volume. Filter through a 0.22μm microporous membrane, fill, stopper and cap. Sterilize at 121°C for 15 minutes.

[0035] Using HPLC detection, accelerated test data are as follows:

[0036]

[0037] Remarks: 1) ☆ stand...

Embodiment 2

[0053] Take 60% of the full amount of water for injection at room temperature, add the prescribed amount of lactic acid, sorbitol, and irinotecan hydrochloride in sequence, stir and heat to 70°C, and cool to room temperature after all are dissolved. Use a pH regulator to adjust the pH of the medicinal solution to 3.0-4.0, and add water for injection to make up the volume. Filter through a 0.22μm microporous membrane, fill, stopper and cap. Sterilize at 121°C for 15 minutes.

[0054] Using HPLC detection, accelerated test data are as follows:

[0055]

[0056]

[0057] Remarks: ☆ means light yellow clear liquid.

Embodiment 3

[0059] Take 50% of the full amount of water for injection at room temperature, add the prescribed amount of lactic acid, sorbitol, and irinotecan hydrochloride in sequence, stir and heat to 80°C, and cool to room temperature after completely dissolving. Use a pH regulator to adjust the pH of the medicinal solution to 3.0-4.0, and add water for injection to make up the volume. Filter through a 0.22μm microporous membrane, fill, stopper and cap. Sterilize at 121°C for 15 minutes.

[0060] Using HPLC detection, accelerated test data are as follows:

[0061]

[0062] Remarks: ☆ means light yellow clear liquid.

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Abstract

The invention provides a preparation method of an irinotecan hydrochloride injection. Each ml of the injection contains 20mg of irinotecan hydrochloride, 45mg of sorbitol, 0.9mg of lactic acid and thebalance of pH regulator and injection water. The preparation method includes: a), taking 50-70% of total volume of the injection water at room temperature, sequentially adding lactic acid, sorbitol and irinotecan hydrochloride of prescription volume sequentially, stirring, heating to 70-80 DEG C, and cooling to the room temperature after irinotecan hydrochloride is fully stirred and dissolved; b), using the pH regulator to adjust pH of medicine liquid to 3.0-4.0 (3.5 preferably), supplementing the injection water, and fixing volume to the total volume; c), filtering, filling, plugging and capping, sterilizing, and packaging to obtain the injection. Compared with the prior art, the preparation method has the advantages that the problem of separation-out of irinotecan hydrochloride in a solution is solved effectively, the injection is reliable in quality, and the preparation method is simple, convenient and suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of irinotecan hydrochloride injection. [0002] technical background [0003] Irinotecan hydrochloride is a water-soluble camptothecin derivative jointly developed by Japan Daiichi Sankyo Company and Yakult Honsha Company, molecular formula: C 33 h 38 N 4 o 6 .HCl.3H 2 O, molecular weight: 677.18, chemical name is (S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[ 3',4':6,7]indeno[1,2-b]quinolin-9-yl 1,4'-bipiperidine-1'-carboxylate hydrochloride trihydrate. Irinotecan (CPT-11) was approved by the US FDA in 1998 as a single drug for the treatment of patients with advanced colorectal cancer who have failed 5-FU-containing chemotherapy regimens. In 2000, it was approved by the FDA for the combined treatment with 5-FU and folinic acid in patients with advanced colorectal cancer who have not received chemotherapy before. [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/4745A61P35/00A61P1/00
Inventor 刘海成刘青荣先觉
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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