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Cabazitaxel injection and preparation method thereof

A technology for injections and preparations, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. To ensure the accuracy of clinical dosage and other issues, to achieve the effects of shortening production time, simplifying clinical preparation methods, enhancing stability and dosage accuracy

Inactive Publication Date: 2011-05-25
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation method is quite cumbersome to operate and takes a long time; and the "premix" is a metastable solution with poor physical stability
If too much force is used during the preparation of the 'premix', it will cause precipitation or excessive foaming, which cannot guarantee the accuracy of the clinical dosage; if the force is insufficient during the preparation of the 'premix', Cabazitaxel will not dissolve completely , it is also difficult to ensure the accuracy of clinical dosage
The lifespan of the 'premix solution' is generally only 30 minutes, which is extremely inconvenient for clinical use; if the time is too long, it will cause the degradation of the main drug Cabazitaxel to produce impurities, which will inevitably affect the curative effect and may bring different degrees of toxic and side effects to patients
Although the manufacturer has spent a lot of manpower and material resources on training nurses in large and small hospitals on the preparation of "premixed solution", according to incomplete statistics, among the product quality complaints over the years, cases related to the quality of "premixed solution" still account for all product quality complaints. above 95

Method used

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  • Cabazitaxel injection and preparation method thereof
  • Cabazitaxel injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: prepare Cabazitaxel injection

[0023] (1) Preparation composition:

[0024] Cabazitaxel 0.6g

[0025] Polysorbate 80 15.6g

[0026] Citric acid 0.02g

[0027] Absolute ethanol 11.9g

[0028]

[0029] Total 30ml

[0030] (2) Preparation method:

[0031] Dissolve 0.6 g of cabazitaxel and 0.02 g of citric acid in 10.7 g of absolute ethanol, add 15.6 g of polysorbate 80, stir evenly, add 1.2 g of absolute ethanol to the full amount of 30 ml, continue stirring, and take the intermediate to test the pH, pH Be 4.91; Carry out sterilizing filtration by 0.22 μm microporous membrane, filtrate is aseptically filled in 10ml vial with every 3ml, corkscrew, makes the preparation of cabazitaxel injection (specification 60mg / ).

[0032] The purity of the product detected by HPLC is 99.62% (0.38% of the total impurities of related substances), and the maximum single impurity is 0.18%;

[0033] HPLC detection conditions are:...

Embodiment 2

[0042] Embodiment 2: prepare Cabazitaxel injection

[0043] (1) Preparation composition:

[0044] Cabazitaxel 0.2g

[0045] Polysorbate 80 16g

[0046] Citric acid 1mg

[0047] Absolute ethanol 4g

[0048]

[0049]Total 20ml

[0050] (2) Preparation method:

[0051] Dissolve 0.2 g of cabazitaxel and 1 mg of citric acid in 3.2 g of absolute ethanol, add 16 g of polysorbate 80, stir evenly, add 0.8 g of absolute ethanol to the full amount of 20 ml, continue stirring, take the intermediate to test the pH, pH Be 6.0; Carry out sterilizing filtration by 0.22 μm microporous membrane, filtrate is aseptically filled in 10ml vial with every 2ml, corkscrew, forms the preparation of cabazitaxel injection (specification 20mg / ).

[0052] The purity of the product detected by HPLC is 99.72% (the total impurities of related substances are 0.28%), and the maximum simple impurity is 0.09%; the HPLC detection conditions are the same as in Example 1.

Embodiment 3

[0053] Embodiment 3: prepare Cabazitaxel injection

[0054] (1) Preparation composition:

[0055] Cabazitaxel 1.2g

[0056] Polysorbate 80 6g

[0057] Citric acid 0.1g

[0058] Absolute ethanol 11.3g

[0059]

[0060] Total 20ml

[0061] (2) Preparation method:

[0062] Dissolve 1.2 g of cabazitaxel and 0.1 g of citric acid in 9 g of absolute ethanol, add 6 g of polysorbate 80, stir evenly, add 2.3 g of absolute ethanol to the full amount of 20 ml, continue stirring, and take the intermediate to test the pH, pH Be 4.43; Carry out sterilizing filtration by 0.22 μm sterilizing filter ball, filtrate is aseptically filled in the 10ml vial with every 2ml, corkscrew, forms the preparation of cabazitaxel injection (specification 120mg / ).

[0063] The purity of the product detected by HPLC is 99.65% (0.35% of the total impurities of related substances), and the maximum simple impurity is 0.12%; the HPLC detection conditions ...

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Abstract

The invention provides cabazitaxel injection. The injection of each milliliter comprises the following components by weight: 10 to 100 milligrams of cabazitaxel, 250 to 800 milligrams of polysorbate 80, 200 to 600 milligrams of absolute ethanol, and 0.05 to 20 milligrams of citric acid. The cabazitaxel injection is a single preparation, does not need to be previously dissolved and prepared by using a special solvent, and can be directly diluted for administration; compared with the conventional preparation technology, the preparation has simple preparation process, low cost and good stability; meanwhile, the preparation shortens the time for preparing the medicinal liquor, improves the stability of clinical medicinal liquor, enhances the accuracy of administration dose, and reduces toxic or side reaction; and the preparation simplifies the preparation process of medicinal personnel, and reduces the risks of the preparation process on harm to the medicinal personnel and environmental pollution.

Description

technical field [0001] The invention relates to a cabazitaxel injection and a preparation method thereof, belonging to the technical field of medicinal chemistry. Background technique [0002] Cabazitaxel is a microtubule inhibitor antineoplastic drug developed by Sanofi-aventis. The US Food and Drug Administration approved Cabazitaxel injection (trade name: Jevtana) in June 2010. , combined with prednisone (Prednisone) for the treatment of male prostate cancer, the drug is the first choice for the treatment of advanced, hormone-resistant prostate cancer drugs when the advanced prostate cancer drug docetaxel is ineffective or even aggravated. [0003] In the prior art, Chinese patents CN1152870 and CN1213042 disclose the preparation of Cabazitaxel; Chinese patent CN1200707 discloses new uses of Cabazitaxel; US2005 / 0065138 discloses a new crystal form of acetone solvate of Cabazitaxel and its preparation method. International Patent Publication WO2009 / 115655 discloses other ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/337A61K47/34A61P35/00A61K47/26
CPCA61K9/0019A61K31/337A61K47/10A61K47/12A61K47/26
Inventor 赵俊宗在伟赵砚荣
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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