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Taxol lipid preparation and method for preparing same

A paclitaxel lipid and paclitaxel technology, applied in the field of medicine, can solve the problems of poor stability of liposome targeting system, difficult industrialized production, unsatisfactory targeting distribution, etc., to avoid toxic and side effects, improve safety and compliance, and prepare The effect of simple and easy process

Inactive Publication Date: 2010-01-27
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] ③ Compatibility changes: Compatibility of 60 commonly used clinical drugs with paclitaxel will cause infusion turbidity, and some drugs compete with paclitaxel for binding to plasma proteins, increasing toxicity
[0012] However, most paclitaxel-targeted preparations are still in the stage of experimental research, and there are still many problems to be solved in their development, such as poor stability, unsatisfactory target distribution, and difficulties in industrial production in liposome-targeted systems.

Method used

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  • Taxol lipid preparation and method for preparing same
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1. Preparation of paclitaxel lipid formulation

[0041] 1. Preparation of paclitaxel lipid preparation

[0042] 1. Weigh 5 g of phospholipid (Lipoid, Germany) and 10 g of propylene glycol, and heat to dissolve in a water bath at 45° C. to obtain solution A.

[0043] 2. Weigh 0.6g paclitaxel, 15g HS15 (German BASF company), 5g glycerin, 0.18g anhydrous citric acid, 65g anhydrous ethanol, and dissolve at room temperature to obtain solution B.

[0044] 3. Mix solution A and solution B, stir at room temperature, mix evenly, and filter to obtain a paclitaxel lipid preparation, which is protected by nitrogen gas and sealed for storage.

[0045] 2. Preparation of paclitaxel nano preparation

[0046] The paclitaxel lipid preparation prepared in step 1 is diluted with 20 times the volume of normal saline to obtain a paclitaxel nano preparation.

[0047] 3. The particle size determination of paclitaxel nano preparation

[0048] The particle size of the paclitaxel nano-preparation was ...

Embodiment 2

[0049] Example 2. Preparation of paclitaxel lipid formulation

[0050] 1. Preparation of paclitaxel lipid preparation

[0051] 1. Weigh 20 g of phospholipids and 10 g of absolute ethanol, and heat to dissolve in a water bath at 55°C to obtain solution A.

[0052] 2. Weigh 0.6g paclitaxel, 50g HS15, 0.18g anhydrous citric acid, 20g anhydrous ethanol, and dissolve at room temperature to obtain solution B.

[0053] 3. Mix solution A and solution B, stir at room temperature, mix evenly, and filter to obtain a paclitaxel lipid preparation, which is protected by nitrogen gas and sealed for storage.

[0054] 2. Preparation of paclitaxel nano preparation

[0055] The paclitaxel lipid preparation prepared in step 1 is diluted with 20 times the volume of water for injection to obtain paclitaxel nano preparation.

[0056] 3. The particle size determination of paclitaxel nano preparation

[0057] The particle size of the paclitaxel nano-preparation was measured with the ZetaPALS laser dynamic light sc...

Embodiment 3

[0058] Example 3. Preparation of paclitaxel lipid formulation

[0059] 1. Preparation of paclitaxel lipid preparation

[0060] 1. Weigh 10g of phospholipid and 10g of propylene glycol, and heat to dissolve in a water bath at 50°C to obtain solution A.

[0061] 2. Weigh 0.6g paclitaxel, 36g HS15, 15g glycerol, 0.18g anhydrous citric acid, 29g anhydrous ethanol, and dissolve at room temperature to obtain solution B.

[0062] 3. Mix solution A and solution B, stir at room temperature, mix evenly, and filter to obtain a paclitaxel lipid preparation, which is protected by nitrogen gas and sealed for storage.

[0063] 2. Preparation of paclitaxel nano preparation

[0064] The paclitaxel lipid preparation prepared in step 1 is diluted with 20 times the volume of normal saline to obtain a paclitaxel nano preparation.

[0065] 3. The particle size determination of paclitaxel nano preparation

[0066] The particle size of the paclitaxel nano-preparation was measured with the ZetaPALS laser dynamic l...

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Abstract

The invention discloses a taxol lipid preparation and a method for preparing the same. The taxol lipid preparation comprises the following components of taxol, polyethylene glycol-12-hydroxyl stearate and phospholipid. The taxol lipid preparation improves the safety and compliance of the taxol preparation; and after being diluted, the taxol lipid preparation can be automatically emulsified into nano particles for intravenous injection so as to enhance the in vivo absorption of the taxol and fulfill the tumor targeting aim. Moreover, the method has the advantages of simple and convenient preparation process and the suitability for industrialized production.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a paclitaxel lipid preparation and a preparation method thereof. Background technique [0002] In the late 1960s, American scientists isolated and extracted a drug with a novel chemical structure (monomeric diterpenoids) from the bark of Pacific yew, and named it Paclitaxel. In the early 1980s, paclitaxel was discovered to have a unique anti-tumor effect (that is, to promote the accumulation of tubulin in the process of cancer cell division, stabilize microtubules, and ultimately cause cancer cell apoptosis), and thus received widespread attention from the international medical community. Paclitaxel was officially approved by the US FDA in 1992 for the treatment of advanced ovarian cancer, lung cancer, and uterine cancer. The product name is It is one of the best anti-cancer drugs in the world. my country succeeded in imitating in the early 1990s, purple In the clinical treatment...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/337A61K47/34A61P35/00A61K47/14
Inventor 张小宁郝艳丽邰文邬月明王晚
Owner TSINGHUA UNIV
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