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Method capable of increasing solubility of paclitaxel

A paclitaxel and solubility technology, applied in the field of significantly improving the solubility of paclitaxel and increasing the solubility of paclitaxel, can solve problems such as restricting the application of paclitaxel, and achieve the effect of improving the solubility

Inactive Publication Date: 2015-10-21
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because polyoxyethylene castor oil can cause severe allergic reactions, nephrotoxicity, neurotoxicity and cardiac toxicity and other adverse reactions, it largely limits the application of paclitaxel

Method used

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  • Method capable of increasing solubility of paclitaxel
  • Method capable of increasing solubility of paclitaxel
  • Method capable of increasing solubility of paclitaxel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Paclitaxel 20mg (relative excess) was added to 500 μL of absolute ethanol, and dissolved to form a paclitaxel ethanol solution; in addition, 85 mg of glycyrrhizic acid was ultrasonically dissolved in 9.5 ml of distilled water to prepare a glycyrrhizic acid aqueous solution. Under the condition of ultrasound at 360W power, add paclitaxel ethanol solution dropwise into glycyrrhizic acid aqueous solution through a syringe, adjust the pH of the solution to 4, ultrasonicate for 30min, seal and place in an incubation shaker at 25°C, shake 48h to reach dissolution equilibrium. After the finally obtained sample is filtered through a 0.45 μm microporous membrane, take 0.1 mL and add 0.9 mL of methanol, dilute 10 times (in case precipitation occurs), and take a certain amount into high performance liquid chromatography to detect the paclitaxel concentration to determine its solubility.

Embodiment 2

[0027] Paclitaxel 20mg (relative excess) was added to 750 μL of absolute ethanol, and dissolved to form a paclitaxel ethanol solution; in addition, 85 mg of glycyrrhizic acid was dissolved in 9.25 ml of distilled water by ultrasonic to prepare a glycyrrhizic acid aqueous solution. Under ultrasonic conditions with a power of 360W, the ethanol solution of paclitaxel was added dropwise into the aqueous solution of glycyrrhizic acid in a syringe to form a solvent-like solution, and the pH of the solution was adjusted to 4, ultrasonicated for 30 minutes, sealed and placed at 25°C for incubation and shaking. Bed, shaken for 48h to achieve dissolution equilibrium. After the finally obtained sample is filtered through a 0.45 μm microporous membrane, take 0.1 mL and add 0.9 mL of methanol, dilute 10 times (in case precipitation occurs), and take a certain amount into high performance liquid chromatography to detect the paclitaxel concentration to determine its solubility.

Embodiment 3

[0029] Paclitaxel 20 mg (relatively excessive), was added to 1000 μL of absolute ethanol, and dissolved to form a paclitaxel ethanol solution; in addition, 85 mg of glycyrrhizic acid was ultrasonically dissolved in 9 ml of distilled water to prepare a glycyrrhizic acid aqueous solution. Under ultrasonic conditions with a power of 360W, the ethanol solution of paclitaxel was added dropwise into the aqueous solution of glycyrrhizic acid in a syringe to form a solvent-like solution, and the pH of the solution was adjusted to 4, ultrasonicated for 30 minutes, sealed and placed at 25°C for incubation and shaking. Bed, shaken for 48h to achieve dissolution equilibrium. After the finally obtained sample is filtered through a 0.45 μm microporous membrane, take 0.1 mL and add 0.9 mL of methanol, dilute 10 times (in case precipitation occurs), and take a certain amount into high performance liquid chromatography to detect the paclitaxel concentration to determine its solubility.

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Abstract

The invention relates to a method capable of increasing the solubility of paclitaxel. The method capable of increasing the solubility of the paclitaxel comprises the steps that functional compounds and short-chain alcohol are added into the paclitaxel, and the acidity and alkalinity range of a solution is adjusted to range from pH 2 to pH 7.4; specifically, the method comprises the following steps that 1 part to 2 parts of the paclitaxel is dissolved into 0.5 part to 3 parts of the short-chain alcohol, and an inner phase is prepared; 5 parts to 20 parts of the functional compounds are dissolved into 7 parts to 10 parts of the deionized water, and an outer phase is prepared; the inner phase is added to the outer phase drop by drop, the pH of the solution is adjusted to 2 to 704, ultrasonic treatment is carried out for 30 minutes, the solution is sealed and placed in an incubation shaking bed at the temperature ranging from 25 DEG C to 60 DEG C to be shaken for 1 hour to 48 hours, and therefore solubility equilibrium is achieved. According to the method capable of increasing the solubility of the paclitaxel, an amphipathy medicinal compound with the characteristics of a surface active agent directly serves as a carrier capable of increasing the solubility of the paclitaxel, and meanwhile a certain amount of the short-chain alcohol is added to generate the synergistic effect, so that the solubility of the paclitaxel can be effectively improved, and finally the oral bioavailability of the paclitaxel is expected to be increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a method for increasing the solubility of paclitaxel, in particular to a method for directly using an amphiphilic medicinal compound with the characteristics of a surfactant as a carrier for increasing the solubility of the drug, while adding a certain amount of short-chain alcohol to produce Synergistic effect finally achieves the method of significantly improving the solubility of paclitaxel. Background technique [0002] Paclitaxel (PTX) is a natural tetracyclic diterpene antineoplastic drug extracted from the bark of the Pacific yew tree. Paclitaxel has antitumor activity against a variety of solid tumors, including ovarian cancer, breast cancer and non-small tumors. cell lung cancer. This natural compound exhibits poor water solubility (<1 μg / mL) due to the lack of ionizable groups. Paclitaxel has low oral bioavailability (<2%), so it is commonly administered...

Claims

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Application Information

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IPC IPC(8): A61K47/10A61K47/28A61K31/337A61P35/00
Inventor 李国锋腊蕾杨富恒王春霞任非赵博欣
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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