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Paclitaxel pharmaceutical composition and preparation method thereof

A composition, paclitaxel technology, applied in the direction of drug combination, pharmaceutical formula, antineoplastic drugs, etc., can solve the problems of easy spray bottle forming, difficult reconstitution, poor stability, etc.

Active Publication Date: 2012-09-19
姚定全
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a new paclitaxel pharmaceutical composition, through the innovative composition of excipients and optimized proportion of excipients, successfully solve the problem of insoluble paclitaxel in water, difficulty in reconstitution after freeze-drying, poor stability during storage, and difficulty in processing. Due to technical problems such as easy spray bottle and poor forming, paclitaxel injection with good water solubility and stability, no allergies, no hemolysis and no irritation, and good forming has been prepared

Method used

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  • Paclitaxel pharmaceutical composition and preparation method thereof
  • Paclitaxel pharmaceutical composition and preparation method thereof
  • Paclitaxel pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] 1. 1,000 bottles of paclitaxel freeze-dried preparation, the specification is that each bottle contains 30 mg of paclitaxel, and the formula composition is as follows:

[0055] Paclitaxel 30g,

[0056] Solutol HS15 2500g,

[0057] Polysorbate 80 200g,

[0058] Glucose 60g,

[0059] Mannitol 1500g,

[0060] Sorbitol 200g,

[0061] phosphoric acid to adjust the pH to 3.0,

[0062] Add water for injection to 6000g.

[0063] 2. Prepare the paclitaxel freeze-dried preparation as follows:

[0064] 1) Weigh Solutol HS15 and polysorbate 80 respectively, and stir at 40-45°C to obtain a clear and transparent solubilizer mixture, which is set aside;

[0065] 2) Add paclitaxel into the solubilizer mixture, stir at 40-45°C for 30 minutes to dissolve until a clear and transparent solution I is obtained, and set aside;

[0066] 3) Weigh glucose, mannitol, and sorbitol respectively, dissolve them in water for injection, keep the temperature at 40-45°C, add 0.1% activated carbon...

Embodiment 2

[0071] 1. 1,000 bottles of paclitaxel freeze-dried preparation, the specification is that each bottle contains 30 mg of paclitaxel, and the formula composition is as follows:

[0072] Paclitaxel 30g,

[0073] Solutol HS15 800g,

[0074] Polysorbate 80 1300g,

[0075] Glucose 750g,

[0076] Mannitol 400g,

[0077] Sorbitol 1300g,

[0078] Citric acid to adjust the pH to 5.0,

[0079]Add water for injection to 8000g.

[0080] 2. Prepare the paclitaxel freeze-dried preparation as follows:

[0081] 1) Weigh Solutol HS15 and polysorbate 80 respectively, and stir at 55-60°C to obtain a clear and transparent solubilizer mixture for later use;

[0082] 2) Add paclitaxel into the solubilizer mixture, stir at 55-60°C for 30 minutes to dissolve until a clear and transparent solution I is obtained, and set aside;

[0083] 3) Weigh glucose, mannitol, and sorbitol respectively, dissolve them in water for injection, keep the temperature at 55-60°C, add 0.2% activated carbon for injec...

Embodiment 3

[0088] 1. 1,000 bottles of paclitaxel freeze-dried preparation, the specification is that each bottle contains 30 mg of paclitaxel, and the formula composition is as follows:

[0089] Paclitaxel 30g,

[0090] Solutol HS15 1200g,

[0091] Polysorbate 80 700g,

[0092] Glucose 500g,

[0093] Mannitol 1200g,

[0094] Sorbitol 800g,

[0095] hydrochloric acid to adjust the pH to 3.5,

[0096] Add water for injection to 10000g.

[0097] 2. Prepare the paclitaxel freeze-dried preparation as follows:

[0098] 1) Weigh Solutol HS15 and polysorbate 80 respectively, stir at 50-55°C to obtain a clear and transparent solubilizer mixture, and set aside;

[0099] 2) Add paclitaxel into the solubilizer mixture, stir at 50-55°C for 30 minutes to dissolve until a clear and transparent solution I is obtained, and set aside;

[0100] 3) Weigh glucose, mannitol, and sorbitol respectively, dissolve them in water for injection, keep the temperature at 50-55°C, add 0.05% activated carbon for...

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Abstract

The invention discloses a paclitaxel pharmaceutical composition and a preparation method thereof. The paclitaxel pharmaceutical composition consists of paclitaxel, a solubilizing agent, a stabilizing agent, an excipient, an acidity regulator and water for injection. A paclitaxel injection is prepared by adopting a freeze drying method. Compared with the prior art, the paclitaxel pharmaceutical composition disclosed by the invention is different in solubilizing process, solubilizing effect and stability. The composition does not contain an organic solvent, thus, the paclitaxel injection has the characteristics of simpler production process, more perfect appearance, shorter freeze drying time and lower equipment requirement. The composition does not contain polyoxyethylenated castor oil, so that the paclitaxel composition has no anaphylactic reaction or hemolysis or irritation. By detection, the paclitaxel injection prepared by adopting the composition and the preparation method disclosed by the invention is high in dissolvability and stability and is suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical composition containing paclitaxel and a preparation method thereof. Background technique [0002] Currently, paclitaxel is the preferred antineoplastic drug in hospitals all over the world. It has good anticancer activity and is effective against advanced ovarian cancer, breast cancer, lung cancer, head and neck cancer, esophageal cancer, germ cell tumor, endometrial cancer, lymphoma, Bladder cancer has a certain effect. Combined with other commonly used anti-tumor drugs, the curative effect can be further improved. 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. However, paclitaxel is extremely poor in water solubility. Currently, paclitaxel injections for clinical use are polyoxy...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K47/34A61P35/00
Inventor 刘红潘红春
Owner 姚定全
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