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A kind of injectable paclitaxel gel with high drug load and its preparation method and application

A high-drug-loading, paclitaxel-based technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the loss of drug activity, reduce drug loading, increase system complexity, etc. problems, achieve high drug loading, avoid high manufacturing difficulty, and retain drug activity

Active Publication Date: 2020-10-09
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Summarizing the above-mentioned many existing technologies related to paclitaxel gel, the current gel sustained-release system for paclitaxel often needs a certain carrier, which not only increases the complexity of the system, reduces the drug loading, but also considers the carrier. Toxic side effects and biocompatibility, while gels based on paclitaxel drug modification face the risk of loss of drug activity
All in all, there is no satisfactory research report of paclitaxel gel with high drug load.

Method used

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  • A kind of injectable paclitaxel gel with high drug load and its preparation method and application
  • A kind of injectable paclitaxel gel with high drug load and its preparation method and application
  • A kind of injectable paclitaxel gel with high drug load and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Weigh 8.8mg, 20mg, 40mg, 80mg, and 135mg of paclitaxel respectively, and dissolve them in turn in screw bottles containing 1mL of PEG400. After ultrasonically dissolving at room temperature, slowly add 0.75mL, 0.70mL, and 0.55mL to each screw bottle, respectively. , 0.33mL, 0.10mL of PBS phosphate-buffered saline, after ultrasonic dispersion again, let stand at room temperature for a period of time, the paclitaxel content is respectively 0.522% (5mg / mL), 1.22% (10mg / mL), 2.44% (25mg / mL), 5.63% (60mg / mL), and 11.33% (120mg / mL) paclitaxel gels, the gel formation photos of the inverted observation method are as follows figure 1 shown.

Embodiment 2

[0053] Weigh 50 mg of paclitaxel and add it to a screw bottle of 1 mL of ethanol. After ultrasonic dispersion at room temperature, add 0.1 mL of PBS phosphate-buffered saline solution dropwise. (45mg / mL) gel, paclitaxel gel SEM photo as figure 2 shown.

Embodiment 3

[0055] Weigh 60 mg of paclitaxel and add it to a threaded bottle containing 1 mL PEG200. After ultrasonic dispersion at room temperature, slowly add 0.3 mL of 5% glucose injection. 3.99% (42 mg / mL) gel.

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Abstract

The invention discloses injectable paclitaxel gel with high drug loading capacity as well as a preparation method and an application of the injectable paclitaxel gel. The gel is prepared from paclitaxel, an organic good solvent and an aqueous poor solvent; when the gel is prepared, paclitaxel is weighed according to the formula amount, dissolved in the organic good solvent and subjected to ultrasonic dissolution at 10-80 DEG C, then the aqueous poor solvent is added, ultrasonic dispersion is performed again, a product is left to stand for a time, and the paclitaxel gel with high drug loading capacity is obtained. The preparation method of the gel is simple, modification of paclitaxel is not needed, other gel carriers are not needed, so that the problems of drug activity reduction as well as toxic and side effects brought by a carrier are solved, drug administration times can be reduced by means of high drug loading capacity, and the paclitaxel gel has better application prospects.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an injectable paclitaxel gel with high drug loading and a preparation method and application thereof. Background technique [0002] Paclitaxel is a new generation of broad-spectrum anticancer drug used clinically in the 1990s. Its water solubility is poor. The earliest paclitaxel preparation (Taxol) used clinically is a mixture of polyoxyethylene castor oil and absolute ethanol (1:1) As a solubilizer, it is diluted with physiological saline or 5% glucose solution before administration and used for injection. Cosolvents can cause a variety of adverse reactions, including allergic reactions and neurotoxicity. The incidence of allergic reactions is 39%, and the incidence of severe allergic reactions is 2%. Once it occurs, it will seriously endanger the lives of patients. In order to prevent allergic reactions to paclitaxel, anti-allergic pretreatment must be d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/10A61K31/337A61K45/06A61K33/243A61K31/4745A61K31/704A61K31/12A61P35/00
CPCA61K9/0024A61K9/06A61K31/12A61K31/337A61K31/4745A61K31/704A61K33/24A61K45/06A61K47/10A61P35/00A61K2300/00
Inventor 罗祥林张奎
Owner SICHUAN UNIV
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