Paclitaxel injection and preparation method thereof

A technology for paclitaxel and injection, applied in the field of paclitaxel injection and preparation thereof, can solve the problems of unsuitability for industrial use, unstable formula, difficult preparation, etc., and achieve the effects of being beneficial to industrial production, good specification, and clear and transparent solution

Inactive Publication Date: 2015-01-07
HAINAN GENERAL & KANGLI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to prevent the occurrence of allergic reactions, at present, antihistamines such as diphenhydramine and dexamethasone are taken several hours before the infusion, which is very inconvenient to use
[0005] The prior art also introduces a variety of other preparation methods of paclitaxel injection, such as preparing into emulsion, liposome, etc. The formulations of these preparations are somewhat unstable, some are not suitable for industrial use, and some are difficult to prepare

Method used

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  • Paclitaxel injection and preparation method thereof
  • Paclitaxel injection and preparation method thereof
  • Paclitaxel injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A paclitaxel injection, consisting of paclitaxel, Tween-80, mannitol, glycerin, absolute ethanol and anhydrous citric acid;

[0039] The weight ratio of each component of the paclitaxel injection is as follows:

[0040]

[0041] The appropriate amount of anhydrous citric acid is used to adjust the pH of paclitaxel injection at 3.4.

[0042] A preparation method of paclitaxel injection of above-mentioned formula, its steps are as follows:

[0043] (1) Stir and mix 80g glycerin and 800g absolute ethanol to obtain 880g of composite solvent;

[0044] (2) 6g paclitaxel is added in 60g compound solvent, dissolves, and obtains crude drug solution;

[0045] (3) 90g mannitol and 24g Tween-80 are added to the remaining 820g composite solvent, stirred and dissolved to obtain a co-solvent solution;

[0046] (4) Add the bulk drug solution obtained in step (2) to the co-solvent solution obtained in step (3), stir and mix evenly; add an appropriate amount of anhydrous citric aci...

Embodiment 2

[0052] Compared with Example 1, this embodiment is basically the same, the only difference is: 1. In the (4) step of the preparation method, an appropriate amount of anhydrous citric acid is added to adjust the pH to 3.2; 2. In the (6) step of the preparation method In the step, the filling volume is 10g / piece.

[0053] Then finally get the paclitaxel injection with the specification of 60mg / bottle.

[0054] The paclitaxel injection prepared in this example is a light yellow clear liquid with a pH of 3.2.

Embodiment 3

[0056] Compared with Example 1, the present embodiment is basically the same, the only difference being: in the (6) step of the preparation method, the filling amount is 16.7g / piece.

[0057] Then finally get the paclitaxel injection with the specification of 100mg / bottle.

[0058] The paclitaxel injection prepared in this example is a light yellow clear liquid with a pH of 3.4.

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a paclitaxel injection and a preparation method thereof. The paclitaxel injection contains paclitaxel, a cosolvent, a pH adjusting agent and a solvent system, wherein the cosolvent is a mixture of Tween-80 and mannitol; the pH adjusting agent is anhydrous citric acid; the solvent is a mixture of absolute ethyl alcohol and glycerin. A formula is improved, and a preparation technology is improved, so that during intravenous drip of the paclitaxel injection after dilution, liquid insoluble particles can meet requirements of the intravenous drip, and the dosage risk is reduced; cosolvents such as polyoxyethylenated castor oil and the like are not used, so that side effects of the injection are reduced, the safety of the injection is improved, and the injection is good in stability and wide in application prospect.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a paclitaxel injection and a preparation method thereof. Background technique [0002] Paclitaxel, an alkaloid extracted from the bark of the yew tree, promotes the formation of microtubules from tubulin dimers. It is also used as an anti-microtubule agent, which stabilizes microtubules by preventing depolymerization, which shows excellent anticancer effects against ovarian cancer, breast cancer, head and neck cancer, and non-small cell lung cancer. [0003] Since paclitaxel has a very low water solubility of 30 μg / ml and is practically unstable, studies on paclitaxel have been ongoing. In particular, it is difficult to use as an injectable solution due to its insolubility. In addition, paclitaxel injections have various problems such as low stability and toxicity due to solubilizers, and various studies are underway to overcome such problems. [0004] At p...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/337A61K47/34A61K47/12A61K47/10A61P35/00
Inventor 余修祥熊景辉方征远李旻李瑛江强
Owner HAINAN GENERAL & KANGLI PHARMA
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