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Anti-cancer drug preparation taking Solutol HS 15 as solubilizer

A technology for anticancer drugs and preparations, applied in the field of medicine, can solve the problems of patient use risks, inconvenient clinical medication, interference with p-glycoprotein expression, etc.

Inactive Publication Date: 2010-12-22
BEIJING SL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method of use is cumbersome to operate, extremely inconvenient for clinical medication, and is prone to secondary pollution during the preparation process, which brings risks to patients.
It is also reported in literature that dissolving docetaxel in Tween 80-ethanol (50:50) mixed system was used, and most patients still had obvious allergic reactions in phase I clinical trials.
In addition, Tween 80 can interfere with the expression of p-glycoprotein, and it will interact instantaneously with some drugs used in combination, causing adverse reactions such as neutropenia, peripheral neuropathy, and hypersensitivity in clinical applications

Method used

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  • Anti-cancer drug preparation taking Solutol HS 15 as solubilizer
  • Anti-cancer drug preparation taking Solutol HS 15 as solubilizer
  • Anti-cancer drug preparation taking Solutol HS 15 as solubilizer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] prescription:

[0024] Paclitaxel: 2.0g

[0025] Polyethylene glycol-12-hydroxystearate: 200g

[0026] Glucose: 100g

[0027] Mannitol: 80g

[0028] PBS solution (pH 5.8): 1000ml

[0029] Method: Dissolve 2.0g paclitaxel in 200g Solutol HS 15 at a certain temperature, stir until clear to obtain solution 1, dissolve 100g glucose and 80g mannitol in an appropriate amount of PBS solution, stir until clear to obtain solution 2; 1. Mix solution 2, depyrogenate with activated carbon, adjust the volume of PBS solution to 1000ml, adjust the pH value to 5.5 with 0.1M NaOH or 0.1M HCL, filter and sterilize, aliquot and freeze-dry.

Embodiment 2

[0031] prescription:

[0032] Paclitaxel: 3.0g

[0033] Polyethylene glycol-12-hydroxystearate: 300g

[0034] Sucrose: 200g

[0035] Mannitol: 50g

[0036] Water for injection: up to 1000ml

[0037] Method: Dissolve 3.0g paclitaxel in 300g Solutol HS 15 at a certain temperature and stir until clear to obtain solution 1. Dissolve 200g sucrose and 50g mannitol in an appropriate amount of water for injection and stir until clear to obtain solution 2. 1. Mix solution 2, depyrogenate with activated carbon, adjust the volume to 1000ml with water for injection, adjust the pH value to 6.5 with 0.1M NaOH or 0.1M HCL, filter and sterilize, aliquot and freeze-dry.

Embodiment 3

[0039] prescription:

[0040] Paclitaxel: 4.0g

[0041] Polyethylene glycol-12-hydroxystearate: 400g

[0042] Trehalose: 200g

[0043] Lactose: 100g

[0044] VC: 0.5g

[0045] PBS solution (pH 5.0): up to 1000ml

[0046] Method: Dissolve 4.0g paclitaxel in 400g Solutol HS 15 at a certain temperature, stir until clear to obtain solution 1, dissolve 200g trehalose, 100g mannitol, and 0.5g VC in an appropriate amount of PBS solution, stir until clear to obtain a solution 2. Mix solution 1 and solution 2 evenly, depyrogenate with activated carbon, adjust the volume of PBS solution to 1000ml, adjust the pH value to 4.5 with 0.1M NaOH or 0.1M HCL, filter and sterilize, aliquot and freeze-dry.

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PUM

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Abstract

The invention discloses an injectable preparation of an anti-cancer drug, belonging to the technical field of medicines. The anti-cancer active ingredient in the preparation is paclitaxel or Docetaxol, and the dosage thereof is 0.01-10 percent (w / v); a solubilizer in the preparation is novel auxiliary polyethylene glycol-12-hydroxystearic acid (Solutol HS 15) with the characteristics of low hemolysis and low histamine release, and the dosage thereof is 5-50 percent (w / v). The preparation does not contain other surface active agent except Solutol HS 15. The preparation can eliminate or reduce anaphylactic reaction or haemocylolysis caused by Cremophor EL and Tween-80, has the characteristics of toxicity reduction, higher safety, certain slow release and targeting action, simple prescription constitution, simple and convenient process and low cost and has wide application prospect in the practice of preparing the anti-cancer drug.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an injectable preparation of paclitaxel and docetaxel containing antitumor active ingredients. The focus of the invention is to improve the water solubility of paclitaxel and docetaxel and reduce the toxicity, and the invented preparation also has a certain slow-release and targeting effect. Background technique [0002] 1. Model drug introduction: [0003] (1) Paclitaxel [0004] Paclitaxel is an active ingredient extracted from the bark of Taxus brevifolia by Wall et al. in 1963. It can also be artificially synthesized at present. Its chemical structure is a tetracyclic two terpenoids. In December 1992, the U.S. Food and Drug Administration (FDA) approved paclitaxel for the treatment of advanced ovarian cancer that was ineffective for other anticancer drugs. In 1994, the FDA approved paclitaxel for the treatment of advanced breast cancer. More than 40 countries including Ita...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/34A61K31/337A61P35/00A61K47/14
Inventor 邓硕吴彦卓刘迎徐明波
Owner BEIJING SL PHARMA
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