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Novel nano-lipid carrier for injection embodying paclitaxel series substances and preparation method thereof

A nano-lipid carrier, paclitaxel technology, applied in the field of medicine, can solve problems such as limited patents, and achieve the effects of improving release properties, increasing drug loading, and reducing costs

Inactive Publication Date: 2009-02-18
李淑斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many patents on emulsions, microemulsions and liposomes, but the lipid nanoparticles prepared by mixing solid lipids, especially solid lipids and liquid lipids, have very limited patents

Method used

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  • Novel nano-lipid carrier for injection embodying paclitaxel series substances and preparation method thereof
  • Novel nano-lipid carrier for injection embodying paclitaxel series substances and preparation method thereof
  • Novel nano-lipid carrier for injection embodying paclitaxel series substances and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] (1) Weigh 10 g of triolein, 90 g of safflower oil, 20 g of soybean lecithin, and 5 g of docetaxel in a water bath, heat and stir to melt, and keep the temperature at 70°C as the oil phase; (2) add 4 g of Poloxamer188 to Add an appropriate amount of water for injection, heat and stir to dissolve it, and keep the temperature at 70°C as the water phase. Under stirring, the water phase is dropped into the oil phase, and the stirring is continued to form colostrum; (3) the colostrum is homogenized 6 times through 750bar high-pressure emulsification, and the docetaxel nano-lipid carrier suspension can be obtained by rapid cooling and solidification. 0.2% citric acid to adjust the pH to 5.5; or (4) adding 20% ​​glucose to the suspension of docetaxel nano-lipid carrier, and freeze-drying to obtain solid powder of docetaxel nano-lipid carrier for injection.

Embodiment 2

[0058] (1) Weigh 40g of glyceryl trilaurate, 40g of medium-chain oil, 30g of egg yolk phospholipid, 10g of paclitaxel, heat and stir in a water bath to melt, and keep the temperature at 75°C as the oil phase; (2) Weigh polyoxyethylene-8 - Add 7.5 g of caprylic acid / capric glyceride (Labrasol) into an appropriate amount of water for injection, heat and stir to dissolve, and keep the temperature at 75° C. as the water phase. Under stirring, the water phase is dropped into the oil phase, and the stirring is continued to form colostrum; (3) the colostrum is homogenized 5 times through 1000bar high-pressure emulsification, and rapidly cooled and solidified to obtain the docetaxel nano-lipid carrier suspension. Adjust the pH to 4.0 with 0.1 mol / L hydrochloric acid; or (4) add 10% sucrose to the paclitaxel nano-lipid carrier suspension, and freeze-dry to obtain the docetaxel nano-lipid carrier solid powder for injection.

Embodiment 3

[0060] (1) Weigh 62.5g of glyceryl monostearate, 12.5g of soybean oil, 45g of TPGS, 75g of HS-15, 0.1g of oleic acid, and 5g of paclitaxel, heat and stir in a water bath to melt, and keep the temperature at 75°C as the oil phase (2) Weigh 5.0 g of sodium deoxycholate and add it to an appropriate amount of water for injection, heat and stir to dissolve it, and keep the temperature at 75° C. as the water phase. Under stirring, drop the water phase into the oil phase, and continue to stir to form colostrum; (3) the colostrum is homogenized 6 times through 1200bar high-pressure milk, and the paclitaxel nano-lipid carrier suspension can be obtained by rapid cooling and solidification. / L NaOH to adjust the pH to 7.0; or (4) adding 15% mannitol to the paclitaxel nano lipid carrier suspension and spray drying to obtain the paclitaxel nano lipid carrier solid powder for injection. Spray drying conditions: inlet temperature 160°C, outlet temperature 91°C, air volume 100%, flow rate 0.0...

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Abstract

The invention provides a novel nanometer lipid carrier containing a taxol substance for injection and a method for preparing the same. Mixed lipids are used as materials; liquid lipid and solid lipid with different physical states are mixed according to the proportion of between 0 and 100 percent to obtain the nanometer lipid carrier (NLC) which is prepared by a mixed solid-liquid substrate and has different crystalline states; and microemulsion (ME) prepared by a full liquid substrate and solid lipid nanoparticles (SLC) prepared by a full solid substrate are also obtained. The new nanometer lipid carrier can increase or improve the encapsulation efficiency and the release property of drug and has the characteristics of high drug-loading amount, good stability and low toxicity. The taxol substance, a carrier material, a surfactant and injection water are respectively stirred to form two phases of oil and water; the oil phase and the water phase are mixed and emulsified to obtain primary emulsion; further taxol substance nanometer lipid carrier injection or suspension type injection which meets the requirement of intravenous injection is prepared by a high-pressure homogenization process; or a protective agent is added into the injection to prepare solid powder for injection by vacuum freeze drying or spray drying; before use, normal saline, a glucose solution or a Ringer solution is used for dilution; and the solid powder can be rapidly dissolved. Experiments show that the prepared nanometer lipid carrier containing the taxol substance for injection can improve targeting property to tumor cells, improve curative effect, greatly reduce toxic and side effects, has simple preparation process and low cost and is suitable for large-scaled industrialized production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a novel nano-lipid carrier containing paclitaxel for injection and a preparation method thereof. Background technique [0002] Paclitaxel is an important cytotoxic drug, which has a unique role in stabilizing microtubules and promoting their polymerization and assembly. Clinically, it is effective in the treatment of metastatic ovarian cancer and breast cancer, especially for cisplatin-resistant or uncontrolled ovarian cancer, and also has a certain effect on esophageal cancer and lung cancer. It is known as the biggest discovery of anti-tumor drug research in the latter part of the 20th century. Due to the extremely poor water solubility of paclitaxel substances, a large amount of solubilizer polyoxyethylene castor oil (cremophor EL) is used in the paclitaxel injection currently used clinically, which can cause severe acute allergic reactions in the body; although the solubili...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/337A61P35/00
Inventor 李淑斌刘丹宋健鲍洁宁红李明慧郭志福王宏遇娜李雷
Owner 李淑斌
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