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Medicament composition for water-soluble injection of paclitaxel, preparation method and uses thereof

A technology for injection and composition, which is applied in the directions of drug combination, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of complex preparation process, complex production process, harsh storage conditions, etc. The preparation process is simple, the production cost is low, and the effect is favorable for storage and transportation

Active Publication Date: 2012-04-11
姚定全
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Paclitaxel liposomes for injection do not contain polyoxyethylated castor oil, which reduces toxic and side effects and is welcomed by patients. However, the production process of this product is relatively complicated, the production cost is high, and its storage conditions are harsh. Clinical application The convenience of the doctor to use the medicine is poor, which greatly limits the clinical application
[0003] In recent years, in view of the problems existing in paclitaxel injection, there have been many reports in the literature that it has been prepared into emulsions, microemulsions, cyclodextrin inclusion complexes, liposomes, nanoparticles and other preparations. However, these preparations have complex preparation processes, Defects such as high cost and poor stability

Method used

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  • Medicament composition for water-soluble injection of paclitaxel, preparation method and uses thereof
  • Medicament composition for water-soluble injection of paclitaxel, preparation method and uses thereof
  • Medicament composition for water-soluble injection of paclitaxel, preparation method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Paclitaxel 30mg

[0032] Solutol HS 15 (manufactured by BASF) 1.5g

[0033] Ethanol 400mg

[0034] Mannitol 550mg

[0035] Dilute hydrochloric acid (adjust the pH value to 3.5) appropriate amount

[0036] Water for injection to 6ml

[0037] Dissolve paclitaxel in ethanol according to the above formula, add Solutol HS 15, mix and stir to dissolve; dissolve mannitol with water for injection, then add to the above paclitaxel-dissolved ethanol solution, stir and mix, adjust the pH value to 3.5 with dilute hydrochloric acid; Dilute the solution to 6 ml with water; add 0.1% (w / v) activated carbon and stir for 20 minutes. The above solution was decarburized through a 0.8 μm filter membrane, then sterilized by filtration through a 0.22 μm filter membrane, distributed into vials, and freeze-dried.

[0038] The freeze-drying process is:

[0039] a. Pre-freezing: The temperature of the product drops to -45°C, and it can be sublimated and dried after 3 hours of heat preservat...

Embodiment 2

[0044] Paclitaxel 30mg

[0045] Solutol HS 15 5.5g

[0046] Ethanol 1.5g

[0047] Mannitol 500mg

[0048] Dilute lactic acid (adjust pH 4.0) appropriate amount

[0049] Water for injection to 6ml

[0050] Dissolve paclitaxel in ethanol, add Solutol HS 15, mix and stir to dissolve; then dissolve mannitol in water, add to the above mixed solution, mix well, and adjust the pH value to 4.0 with lactic acid; the subsequent steps are the same as in Example 1.

Embodiment 3

[0052] Paclitaxel 30mg

[0053] Solutol HS 15 3.5g

[0054] Ethanol 200mg

[0055] Glycerol 50mg

[0056] Mannitol 800mg

[0057] Dilute hydrochloric acid (adjust the pH value to 4.0) appropriate amount

[0058] Water for injection to 8ml

[0059] Dissolve paclitaxel in ethanol, add Solutol HS 15 and glycerin, mix and stir to dissolve; add mannitol aqueous solution, mix, and adjust the pH value to 4.0 with hydrochloric acid; the subsequent steps are the same as in Example 1.

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Abstract

The invention discloses a water-soluble drug composition of taxol for injection. The drug composition comprises taxol as an active component, polyethyleneglycol 15- hydroxy stearic acid ester as a solubilizer, alcohol as a latent solvent and injection water as a solvent. Polysorbate, cyclodextrin derivatives, poloxamer, polyethylene glycol (PEG) and reducing sugar are also added and are favorablefor improving the solubility and stability of the taxol in the composition. The composition is prepared to freeze-dried powder injection for injection, can not produce serious anaphylactic reaction, has small simulation, remarkably improves the clinical compliance of patients and has good water solubility and high convenience for medication by clinicians. The powder injection has good stability, can be stored at room temperature and is favorable for storage and transportation. The powder injection is simple in preparation process, easy to control quality, low in production cost and convenientfor industrialized production and also greatly reduces the economic burden of the patients for medication. The invention also discloses a method for preparing the drug composition and clinical application thereof.

Description

(1) Technical field [0001] The invention relates to a pharmaceutical composition of water-soluble freeze-dried powder injection with paclitaxel as an active ingredient, as well as a preparation method and application of the composition. (2) Background technology [0002] At present, paclitaxel is the first choice of anti-tumor drug in hospitals all over the world. It has good anti-cancer activity, especially for advanced and metastatic ovarian cancer, breast cancer, lung cancer, prostate cancer and melanoma and other tumor diseases. Its mechanism of action is unique, and its side effects are small. It mainly inhibits the microtubule synthesis of cancer cells, prevents its division and proliferation, and thus exerts its anticancer effect. Due to the extremely low solubility of paclitaxel in water, there are many difficulties in the preparation of injections. For example, paclitaxel injection is the mainstream preparation of paclitaxel, but it uses a large amount of non-ionic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/337A61K47/34A61P35/00A61K47/14
Inventor 刘红潘红春姚定全郑薇
Owner 姚定全