Irinotecan hydrochloride composition and preparation method thereof

A technology of irinotecan hydrochloride and composition, applied in the field of irinotecan hydrochloride composition and preparation thereof, can solve the problems of restricted use and many adverse reactions, and achieve the effects of improving stability, simple and convenient preparation, and prolonging circulation time

Active Publication Date: 2014-08-20
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the domestically marketed product is irinotecan hydrochloride injection, which has strong anticancer activity, but also has many adverse reactions. The common adverse reactions are ano

Method used

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  • Irinotecan hydrochloride composition and preparation method thereof
  • Irinotecan hydrochloride composition and preparation method thereof
  • Irinotecan hydrochloride composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation of irinotecan hydrochloride composition:

[0046] Dissolve 2g of soybean lecithin, 1g of cholesterol, and 0.5g of PEG-DSPE with 1.5ml of absolute ethanol sonically, inject it into 20ml of 300mM citric acid buffer (pH=3) preheated to 60°C, stir at high speed to obtain the primary product, and then Homogenize under high pressure 4 times at 20,000 psi, filter and sterilize, and dispense into vials of 2 ml / bottle to obtain a blank lipid nano-preparation (phospholipid concentration is 100 mg / ml).

[0047] Weigh 200mg of irinotecan hydrochloride (cpt-11), 9mg of lactic acid, and 450mg of sorbitol, add 20ml of water for injection to dissolve it ultrasonically, adjust the pH to 3-4 with hydrochloric acid (0.1M), and pack in 2ml / bottle in an anatomy , and then sterilized under high pressure at 121°C for 30 minutes to obtain irinotecan hydrochloride solution.

[0048] Prepare sodium carbonate solution (0.5M), filter and sterilize, then pack in 8ml / bottles into vi...

Embodiment 2

[0052] The preparation of irinotecan hydrochloride composition:

[0053] Weigh 2g of HSPC, 0.2g of cholesterol, 0.3g of PEG-DSPE, and 0.3g of RGD-PEG-DSPE and dissolve them in 2ml of absolute ethanol, inject them into 30ml of 300mM copper sulfate solution, stir at high speed, and then dissolve them with polycarbonate with a pore size of 100nm Extrude the membrane for 4 times, then replace the outer aqueous phase with sucrose solution (300mM) by ultrafiltration (molecular weight of the ultrafiltration tube: 10K), filter and sterilize, and divide into vials of 4ml / bottle to obtain the blank fat Quality nano-preparation (phospholipid concentration of 50mg / ml).

[0054] Weigh 200mg of irinotecan hydrochloride (cpt-11), 9mg of lactic acid, and 450mg of sorbitol, add 20ml of water for injection to dissolve it ultrasonically, adjust the pH to 3-4 with hydrochloric acid (0.1M), and pack in 2ml / bottle in an anatomy , and then sterilized under high pressure at 121°C for 30 minutes to o...

Embodiment 3

[0059] The preparation of irinotecan hydrochloride composition:

[0060] Weigh 2g of DSPC, 0.8g of cholesterol, 0.1g of FA-PEG-DSPE, and 0.2g of PEG-DSPE, dissolve them ultrasonically in 1.6ml of absolute ethanol, inject into 40ml of sbe-CD triethylamine solution (250mM), stir at high speed, and then The polycarbonate film of 100nm pore size was extruded 4 times, and the obtained preparation was dialyzed in normal saline for 24h, and after filtering and sterilizing, it was divided into vials at 4ml / bottle to obtain a blank lipid nano-preparation (the concentration of phospholipids was 50mg / ml).

[0061] Weigh 200mg of irinotecan hydrochloride (cpt-11), 9mg of lactic acid, and 450mg of sorbitol, add 20ml of water for injection to dissolve it ultrasonically, adjust the pH to 3-4 with hydrochloric acid (0.1M), and pack in 2ml / bottle in an anatomy , and then sterilized under high pressure at 121°C for 30 minutes to obtain irinotecan hydrochloride solution.

[0062] Prepare sodi...

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Abstract

The invention relates to an irinotecan hydrochloride composition, which comprises a blank lipid nano-preparation, an irinotecan hydrochloride solution and a pH adjustment solution. The blank lipid nano-preparation, the irinotecan hydrochloride solution and the pH adjustment solution have independent packaging respectively. Before clinical use, the three components are mixed and incubated, and are prepared into a clinical drug loaded nano-preparation through active drug loading. The composition provided by the invention adopts a three-bottle independent packaging design, and drugs are not loaded into the lipid nano-preparation in the storage process, so that the preparation is free of the easy drug leakage problem in existing preparations, and stability of the preparation is greatly improved. Before clinical use, the three components are mixed and incubated to be prepared into the drug loaded nano-preparation, which is simple and convenient for clinical use. The invention also relates to a preparation method for the irinotecan hydrochloride composition. The preparation process has the characteristics of simplicity and easy quality control, and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an irinotecan hydrochloride composition and a preparation method thereof. Background technique [0002] Irinotecan hydrochloride (1rinotecan, CPT-11) is a semi-synthetic water-soluble camptothecin derivative and an inhibitor of DNA topoisomerase I (Topo I). Irinotecan and its active metabolite SN-38 cause DNA single-strand breaks through the stable combination with the DNA-Topo-1 complex, resulting in irreversible damage to the DNA and death. Irinotecan is an effective drug for the treatment of metastatic colorectal cancer. It is still effective for fluorouracil-resistant cases and has a broad anti-tumor spectrum. Phase I and Phase II clinical research results show that the drug has a positive effect on chemotherapy-resistant tumors, such as non-small cell lung cancer, ovarian cancer and cervical cancer; Breast cancer, small cell lung cancer, skin cancer, ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4745A61K47/36A61K47/34A61K47/26A61K47/24A61P35/00
Inventor 李亚平陈伶俐樊继涛顾王文张志文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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