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Docetaxel and vitamin effervescent preparation and preparation method thereof

A technology for docetaxel and effervescent preparations, applied in the field of docetaxel and vitamin effervescent preparations and their preparation, can solve the problems affecting development and clinical application, poor quality stability of injections, poor water solubility of docetaxel, etc. , to achieve great development prospects, low cost, and the effect of reducing gastrointestinal toxicity

Pending Publication Date: 2019-07-19
广州加泰医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Accordingly, in order to improve the deficiencies of the existing preparations of docetaxel, a new effervescent preparation of docetaxel and vitamins will be developed to reduce gastrointestinal toxicity and improve its oral bioavailability, thereby expanding its application range and further To meet the requirements of clinical medication, the dosage form of docetaxel currently on the market is injection, because docetaxel is easily oxidized and hydrolyzed when placed in the solution for a long time, thereby reducing the content of the main drug docetaxel, so the quality of the injection Poor stability; at the same time, the poor water solubility of docetaxel also affects the development and clinical application of oral preparations of docetaxel

Method used

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  • Docetaxel and vitamin effervescent preparation and preparation method thereof
  • Docetaxel and vitamin effervescent preparation and preparation method thereof
  • Docetaxel and vitamin effervescent preparation and preparation method thereof

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preparation example Construction

[0023] A kind of preparation method of quick-release calcium and vitamin effervescent preparation, the preparation method of docetaxel and vitamin effervescent preparation, comprises the following steps:

[0024] (1) Docetaxel and vitamin D were weighed at a weight ratio of 1:1 to 80.

[0025] (2) Dissolving docetaxel and vitamin D in an organic solvent and heating to reflux for 0.5 to 10 hours;

[0026] (3) Concentrate the above solution under reduced pressure at -0.01~0.1Mpa vacuum pressure and temperature below 30~80°C to 5~60% of the original volume, and continue to dry at a temperature of 30~70°C to completely remove the solvent to obtain Dorsey Taxel and vitamin dispersions;

[0027] (4) Take the above dispersion, add excipients and disintegrants, and prepare docetaxel and vitamin effervescent preparations.

[0028] The acid source of the effervescent acid-base pair is any one or more of citric acid, tartaric acid, fumaric acid, citric acid monohydrate, oxalic acid, an...

Embodiment 1

[0044] The screening of embodiment 1 effervescent preparation acid source;

[0045] Three kinds of acid sources were selected, and through the investigation of their properties and phenomena, the results showed that citric acid monohydrate was a hydrate of crystal water, and the phenomenon of moisture absorption was improved, and the phenomenon of sticking and flushing was reduced, and citric acid monohydrate was the best. acid source.

[0046] Table 1 is the acid source screening results table.

[0047]

[0048]

Embodiment 2

[0049] The investigation of embodiment 2 effervescent preparation acid-base weight ratio;

[0050] The total amount of acid and alkali was investigated and selected through the disintegration time after tablet compression, the aesthetics of the surface and the pH value. The results showed that when the total acid and alkali content was 65%, the disintegration time was short, the pH value was moderate, and the surface was smooth and beautiful.

[0051] Table 2 is a table of the investigation results of the proportion of the total amount of acid and alkali.

[0052]

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Abstract

The invention relates to the technical field of effervescent preparations, in particular to a docetaxel and vitamin effervescent preparation and a preparation method thereof. The docetaxel and vitamineffervescent preparation is characterized by comprising the following components in percentage by weight of 1-8% of docetaxel, 10-80% of vitamin D dispersing substances, 1-6% of an effervescent acid-base pair agents and 0.2-2% of a disintegrant. The toxicity of the stomach and the intestine can be reduced, the oral biological availability is increased, the application range of the docetaxel and vitamin effervescent preparation is enlarged, and the clinical medication requirements are further met. The preparation formulation of the docetaxel in the market at present is injection, the docetaxelis easy to oxidize and hydrolyze after being kept in a solution for a long time, so that the content of the docetaxel as a main medicine is reduced, and the quality stability of the injection is poor; and besides, the water solubility of the docetaxel is poor, and development and clinical application of a docetaxel oral preparation are also influenced.

Description

[0001] Technical field: [0002] The invention relates to the technical field of effervescent preparations, in particular to a docetaxel and vitamin effervescent preparation and a preparation method thereof. [0003] Background technique: [0004] Docetaxel (Docetaxel, Docetaxel, C 43 h 53 NO 14 ), is a new anti-cancer drug obtained after structural modification on the basis of the structure of the natural anti-tumor drug paclitaxel. Its anti-cancer spectrum is similar to that of paclitaxel. Thereby inhibiting the mitosis and proliferation of cancer cells, and the drug effect is stronger than paclitaxel. [0005] In vitro studies have shown that its IC50 is 9 times lower than paclitaxel in human breast, colon, bladder and epithelial cell lines. In vivo studies have shown that docetaxel has strong anti-tumor activity, and the tumors and transplanted tumors in mice can completely regress after administration. More importantly, docetaxel-resistant paclitaxel-resistant cell li...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/46A61K47/12A61K47/18A61K31/337A61K31/59A61P35/00
CPCA61K9/0007A61K9/2013A61K31/337A61K31/59A61P35/00A61K2300/00
Inventor 吴鑫欣
Owner 广州加泰医药科技有限公司
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