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Gemcitabine solid lipid nanospheres, preparation method thereof and use thereof

A technology of solid lipid nanometer and gemcitabine, which is applied in the direction of medical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of toxic and side effects, strong cytotoxicity, and increased adverse reactions. Achieve the effects of reducing toxic and side effects, expanding the scope of clinical application, and good physiological compatibility

Inactive Publication Date: 2010-12-29
苏州特瑞药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Gemcitabine has effective effects on a variety of solid tumors, but as an anti-metabolite anti-tumor drug, it has strong cytotoxicity and is often accompanied by toxic and side effects during clinical application, mainly including bone marrow suppression, digestive system reactions, renal toxicity, and allergic reactions , there are also some reports that gemcitabine can cause adverse reactions such as hypotension, hair loss, drowsiness, deep vein thrombosis, etc. With its clinical application, the reports of adverse reactions of this drug tend to increase

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] A kind of gemcitabine solid lipid nanoparticle is made up of gemcitabine, lipid material, emulsifier, stabilizer:

[0059] Gemcitabine 2g;

[0060] Stearic acid 16g;

[0061] Soy lecithin 10g;

[0062] Pluronic F 68 3g;

[0063] Oleic acid 3g.

[0064] Preparation method: (1) melting the lipid material stearic acid of the prescribed amount in a water bath at 70°C; (2) dispersing gemcitabine and oleic acid in the molten lipid material as an oil phase; (3) dissolving the prescription Amount of emulsifier soybean lecithin, Pluronic F 68 The mixture is dispersed in water for injection and heated to 60°C as the water phase; (4) Add the water phase to the molten oil phase with stirring, and continue to stir for 15 minutes to form a primary suspension; (5) Prepare the primary suspension The suspension was transferred to a high-pressure homogenizer, and high-pressure homogenized 10 times to prepare a gemcitabine nanoparticle suspension. This step was performed und...

Embodiment 2

[0067] A kind of gemcitabine solid lipid nanoparticle is made up of gemcitabine, lipid material, emulsifier, stabilizer:

[0068] Gemcitabine 2g;

[0069] Glyceryl monostearate 15g;

[0070] Lecithin 12g;

[0071] Pluronic F 68 3g;

[0072] Oleic acid 4g.

[0073] Preparation method: (1) melting the lipid material glyceryl monostearate in a prescription amount under a water bath condition of 65°C; (2) dispersing gemcitabine and oleic acid in the molten lipid material as an oil phase; (3 ) the emulsifier lecithin, Pluronic F of prescription amount 68 The mixture is dispersed in water for injection and heated to 60°C as the water phase; (4) Add the water phase to the molten oil phase with stirring, and continue to stir for 15 minutes to form a primary suspension; (5) Prepare the primary suspension The suspension was transferred to a high-pressure homogenizer, and high-pressure homogenized 10 times to prepare a gemcitabine nanoparticle suspension. This step was p...

Embodiment 3

[0076] A kind of gemcitabine solid lipid nanoparticle is made up of gemcitabine, lipid material, emulsifier, stabilizer:

[0077] Gemcitabine 10g;

[0078] Glyceryl monostearate 40g;

[0079] Stearic acid 20g;

[0080] Soy lecithin 20g;

[0081] Pluronic F 68 10g;

[0082] Glycerin 10g;

[0083] Oleic acid 10g.

[0084] Preparation method: (1) melting the mixed lipid material of glyceryl monostearate and stearic acid in a prescription amount under a water bath condition of 70°C; (2) dispersing gemcitabine and oleic acid in the molten lipid material as Oil phase; (3) soybean lecithin, Pluronic F 68 , Glycerin mixed emulsifier is dispersed in water for injection, heated at 65°C, as the water phase; (4) Add the water phase to the molten oil phase under stirring, and continue to stir for 20 minutes to form a primary suspension; (5) Prepare the prepared The primary suspension was transferred to a high-pressure homogenizer, and high-pressure homogenized for 15 tim...

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Abstract

The invention provides gemcitabine solid lipid nanospheres, which comprise the following components in percentage by weight: 5 to 70 percent of lipid material, 5 to 60 percent of emulsifier, 0.1 to 15 percent of stabilizer and 1 to 20 percent of gemcitabine medicament. The gemcitabine solid lipid nanospheres of the invention can be used to prepare gemcitabine solid lipid nanosphere sterile frozen dry preparation with excipient. The gemcitabine solid lipid nanospheres of the invention, which serve as a medicament carrier, have high physiological compatibility and can reduce the side and toxic effects of the medicament, increase the tissue targeting property of the medicament and realize a sustained release function. When the gemcitabine solid lipid nanospheres of the invention are produced industrially, the clinic application range of the gemcitabine can be enlarged.

Description

technical field [0001] The invention relates to a gemcitabine solid lipid nanoparticle and its preparation method and application, in particular to a sterile freeze-dried preparation of an antitumor drug gemcitabine solid lipid nanoparticle and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Tumor has become the second leading cause of population death. According to the report of the World Health Organization, there are 20 million cancer patients in the world's 6 billion population, the incidence rate is about 3.3‰, and the average annual death rate of cancer patients is 12%. According to statistics from the Ministry of Health, cancer has become one of the major diseases that cause death in our country. In recent years, there are more than 2 million new cancer patients and more than 1.3 million deaths in China every year. The total number of cancer patients in the country exceeds 4 million. In addit...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/7068A61K47/12A61K47/14A61K47/24A61K47/26A61K47/36A61K47/34A61P35/00A61K47/10
Inventor 初虹王浩龚金红
Owner 苏州特瑞药业股份有限公司
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