Nano-particle containing docetaxel and vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) and preparation method thereof

A technology of docetaxel and nanoparticles, which is applied in the field of nanoparticles containing docetaxel and vitamin E TPGS and its preparation, which can solve the problems that the preparation method needs to be improved, and achieve good chemical and physical stability and production cost Low, high ability effect

Inactive Publication Date: 2014-04-30
SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Thereby, current docetaxel novel preparation and preparation method thereof still need to be improved

Method used

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  • Nano-particle containing docetaxel and vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) and preparation method thereof
  • Nano-particle containing docetaxel and vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) and preparation method thereof
  • Nano-particle containing docetaxel and vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0077] 1. In the method of the present invention for preparing nanoparticles containing docetaxel and vitamin E TPGS, the vitamin E TPGS used can be used not only as an emulsifier, but also to exert a synergistic antitumor effect with docetaxel.

[0078] 2. The method for preparing nanoparticles containing docetaxel and vitamin E TPGS of the present invention uses ethanol, propanol, butanol, isopropanol and tert-butanol as organic solvents that are miscible with water and substantially non-toxic. These substances can be easily removed during freeze-drying, which increases the stability and safety of the nanoparticles containing docetaxel and vitamin E TPGS of the present invention; The preparation process also does not need to remove the organic phase by rotary evaporation and other processes, which greatly reduces the cost and is beneficial to industrial production.

[0079] 3. The prepared nano-particles containing docetaxel and vitamin E TPGS have a good shape, the average ...

Embodiment 1

[0084] Example 1. Preparation of docetaxel and TPGS synergistic anti-tumor albumin nanoparticles with isopropanol as the organic phase

[0085] Weigh 80 mg of multilineage paclitaxel and dissolve it in 30 ml of isopropanol as the organic phase, weigh 600 mg of human serum albumin, 80 mg of TPGS (polyethylene glycol number average molecular weight M n 1000), 200mg mannitol and 60mg sodium acetate were dissolved in 80ml double distilled water, stirred and dissolved as the water phase. Under the condition of high-speed mechanical stirring (2000rpm), the organic phase was slowly added to the water phase, and after stirring for a period of time, it was filtered and sterilized through a 0.22 μm microporous membrane filter. Freeze at -80°C and freeze-dry at -50°C to remove isopropanol and water to obtain a freeze-dried powder with good shape (particle size about 80 nm). The obtained powder can be easily reconstituted into a dispersion before freeze-drying with physiological saline, ...

Embodiment 2

[0086] Example 2. Preparation of docetaxel and TPGS synergistic anti-tumor albumin nanoparticles with isopropanol as the organic phase

[0087] Weigh 80 mg of multilineage paclitaxel dissolved in 30 ml of isopropanol as the organic phase, weigh 1000 mg of human serum albumin, 100 mg of TPGS (polyethylene glycol number average molecular weight M n 1000), 280mg mannitol and 65mg potassium acetate were dissolved in 100ml double distilled water, stirred and dissolved as the water phase. Under the condition of high-speed mechanical stirring (2000rpm), slowly add the organic phase to the water phase, and after stirring for a period of time, filter and sterilize through a 0.22 μm microporous membrane filter. Freeze at -80°C and freeze-dry at -50°C to remove isopropanol and water to obtain a freeze-dried powder with good shape (particle size about 80 nm). The obtained powder can be easily reconstituted into a dispersion before freeze-drying with physiological saline, and its particle...

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Abstract

The invention discloses a nano-particle containing docetaxel and vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) and a preparation method thereof. The nano-particle containing docetaxel and vitamin E TPGS comprises the following components in parts by weight: 2-10 parts of docetaxel, 1-15 parts of vitamin E TPGS, 20-65 parts of albumin, 5-50 parts of cryoprotectant, and 2-20 parts of acidic buffer salt. Relative to an existing docetaxel commercial preparation, the nano-particle containing docetaxel and vitamin E TPGS is good in drug entrapping performance, small in toxic and side effect, high in stability, good in anti-tumor curative effect and convenient to administer; the preparation method is simple, and the production cost is low.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to nanoparticles containing docetaxel and vitamin E TPGS and a preparation method thereof. Background technique [0002] Docetaxel (DTX), also known as docetaxel, is a taxane anticancer drug that was accidentally discovered in the intermediate product of synthetic paclitaxel and was approved by the US FDA in 1998. Docetaxel is a representative of the second-generation taxane anticancer drugs. It not only has good therapeutic effect on ovarian cancer, breast cancer and non-small cell lung cancer, but also has good curative effect on prostate cancer, pancreatic cancer and various soft tissue tumors. In recent years, because of the broad-spectrum anti-cancer properties of docetaxel, people began to pay attention to this new drug product. [0003] However, because the solubility of docetaxel in water is very small (about 10 mg / L), the existing injection (Taxotere, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/337A61K47/34A61P35/00A61P9/00A61K47/14
Inventor 黄来强曾小伟梅林
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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