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Dry docetaxel elixir, and preparation method and application thereof

A docetaxel and dry elixir technology, applied in the field of medicine, can solve the problems of poor drug compliance, complicated production process, inconvenient use, etc., and achieve high drug loading and encapsulation efficiency, easy operation, and improved solubility Effect

Active Publication Date: 2014-12-03
上海市第八人民医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to overcome the extremely poor water solubility of docetaxel in the prior art, the bioavailability of oral administration is almost zero, while the production process of the existing intravenous injection is complicated, the patient's medication compliance is poor, and it is inconvenient to use. There are defects such as pain during injection, and a docetaxel dry elixir and its preparation method and application are provided

Method used

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  • Dry docetaxel elixir, and preparation method and application thereof
  • Dry docetaxel elixir, and preparation method and application thereof
  • Dry docetaxel elixir, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] (1) Preparation of capsule material solution and docetaxel alcohol solution

[0039] Disperse chitosan in dilute acetic acid aqueous solution (0.5%, V / V), swell overnight after stirring, and prepare a 0.01g / mL chitosan solution; dissolve docetaxel in absolute ethanol to prepare docetaxel Alcohol solution, docetaxel in alcohol solution;

[0040] The weight ratio of docetaxel to ethanol is 0.0125:1; the weight ratio of docetaxel to capsule material is 0.5:1;

[0041] (2) Preparation of elixir solution

[0042] Under magnetic stirring (450rpm), the alcohol solution of docetaxel was quickly dropped (10mL / min) into the solution of the capsule material, and mixed evenly under magnetic stirring (450rpm, 10min), then, a small amount of Tween 80 ( Tween80), the amount of Tween80 (Tween80) added is 2% of the sum of the mass of docetaxel and capsule material, and the stirring is continued until a clear and uniformly dispersed elixir solution is formed.

[0043] (3) Preparation ...

Embodiment 2

[0051] (1) Preparation of capsule material solution and docetaxel alcohol solution

[0052] Disperse chitosan in dilute acetic acid aqueous solution (0.5%, V / V), swell overnight after stirring, and prepare a 0.02g / mL chitosan solution; dissolve docetaxel in absolute ethanol to prepare docetaxel Alcohol solution, docetaxel in alcohol solution;

[0053] The weight ratio of docetaxel to ethanol is 0.00125:1; the weight ratio of docetaxel to capsule material is 0.1:1.

[0054] (2) Preparation of elixir solution

[0055] Under magnetic stirring (450rpm), the alcohol solution of docetaxel was quickly dropped (10mL / min) into the solution of the capsule material, and mixed evenly under magnetic stirring (600rpm, 20min), then, a small amount of Tween 80 ( Tween80), the amount of Tween80 (Tween80) added is 2% of the sum of the mass of docetaxel and capsule material, and the stirring is continued until a clear and uniformly dispersed elixir solution is formed.

[0056] (3) Preparation...

Embodiment 3

[0061] (1) Preparation of capsule material solution and docetaxel alcohol solution

[0062] Disperse chitosan in dilute acetic acid aqueous solution (0.5%, V / V), swell overnight after stirring, and prepare a 0.01g / mL chitosan solution; dissolve docetaxel in absolute ethanol to prepare docetaxel Alcohol solution of docetaxel in alcohol solution of docetaxel; the weight ratio of docetaxel to ethanol is 0.0125:1; the weight ratio of docetaxel to capsule material is 1.0:1.

[0063] (2) Preparation of elixir solution

[0064] Under magnetic stirring (500rpm), the alcohol solution of docetaxel was quickly dropped (15mL / min) into the solution of the capsule material, and mixed evenly under magnetic stirring (400rpm, 15min), then, a small amount of poloxamer was added The amount of poloxamer added is 2% of the sum of the mass of docetaxel and capsule material, and the stirring is continued until a clear and uniformly dispersed elixir solution is formed.

[0065] (3) Preparation of d...

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Abstract

The invention discloses a dry docetaxel elixir and a preparation method and application thereof. The preparation method comprises the following steps: adding an alcoholic solution of docetaxel into a solution of a capsule wall material at a speed of 10 to 20 mL / min drop by drop and then carrying out uniform mixing and spray drying, wherein the capsule wall material is one or more selected from the group consisting of chitosan, dextrin, gelatin and starch, the alcoholic solution of docetaxel comprises docetaxel and ethanol, a weight ratio of docetaxel to ethanol is 0.00125-0.0125: 1, and a weight ratio of docetaxel to the capsule wall material is 0.1-1.0: 1. The preparation method for the dry docetaxel elixir provided by the invention has simple process, is easy to operate and applicable to large scale production in the industry of preparations and can substantially improve solubility and bioavailability of docetaxel and compliance of a patient; and the prepared dry docetaxel elixir has the advantages of uniform particle size distribution, high drug loading capacity and encapsulation efficiency and fast drug release.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a docetaxel dry elixir and a preparation method and application thereof. Background technique [0002] Docetaxel (DTX) is a new generation of broad-spectrum taxane antineoplastic drugs. Clinical studies have confirmed that docetaxel has a wide range of cytotoxic effects on a variety of solid tumors, including breast cancer, ovarian cancer, small cell and non-small cell lung cancer, brain cancer, neck cancer, and prostate cancer, with unique curative effects. Docetaxel has extremely poor water solubility, and its oral bioavailability is almost zero. It is usually administered intravenously, but its injections often contain a large amount of ethanol and surfactants. The production process is complicated, and the patient's medication compliance is poor. Inconvenient to use and painful when injected. The above defects have restricted the application of docetaxel as an antitumor dr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K31/337A61K47/36A61K47/42A61P35/00
Inventor 李凤前董文凤杜丽漏德宝
Owner 上海市第八人民医院