Vinorelbine solid lipid nano granule, freeze drying formulated product and method of preparing the same

A solid lipid nanotechnology, vinorelbine technology, applied in the field of medicine, can solve the problems of high operating temperature, strong blood vessel irritation, poor patient compliance, etc., to avoid instability, avoid drug degradation, and reduce encapsulation efficiency Effect

Inactive Publication Date: 2010-12-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has obvious deficiencies: the obtained nanoparticles have a large particle size; a large amount of organic solvents are introduced in the preparation process, which is not suitable for clinical application; the process is not suitable for large-scale industrial production; Nanoparticles have certain difficulties
But there are also some shortcomings: part of the drug will be released from the nanoparticles during the ultrasonic process, and the encapsulation rate of the drug will be affected
The advantages of this method are: it is suitable for industrialized large-scale production; the prepared nanoparticles have uniform particle size and small particle size, etc., but it also has obvious shortcomings: the operating temperature is high, and it is not suitable for preparing temperature-sensitive Drugs; higher temperature is prone to drug degradation; it is also not suitable for encapsulating hydrophilic drugs
At the same time, vinorelbine has a strong irritation to blood vessels, and the patient's compliance is poor.
Seriously affect its clinical use, clinical safety and clinical efficacy

Method used

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  • Vinorelbine solid lipid nano granule, freeze drying formulated product and method of preparing the same
  • Vinorelbine solid lipid nano granule, freeze drying formulated product and method of preparing the same
  • Vinorelbine solid lipid nano granule, freeze drying formulated product and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064]The vinorelbine solid lipid nanoparticles provided by the present invention are composed of vinorelbine, lipid materials, phospholipids, and oleic acid: vinorelbine 14mg

[0065] Glyceryl monostearate 200mg

[0066] Lecithin 90mg

[0067] Oleic acid 14mg

[0068] Preparation method: (1) melt the lipid material glyceryl monostearate in the prescribed amount in a water bath at 60°C; (2) dissolve the prescribed amount of phospholipids, oleic acid, and vinorelbine in ethanol, and then add dropwise (3) After completely removing ethanol under vacuum and decompression conditions, quickly place it in liquid nitrogen to cool; (4) Take it out after being completely frozen, grind it with a mortar and disperse it in an appropriate amount of 1%F 68 In the aqueous phase, the pH of the aqueous phase is 4; (5) mash under the tissue masher, 3000rpm, 6000rpm, each 15min, to prepare the primary suspension; (6) transfer the prepared primary suspension to the high-pressu...

Embodiment 2

[0071] The vinorelbine solid lipid nanoparticles provided by the present invention are composed of vinorelbine, lipid materials, phospholipids, and oleic acid: vinorelbine 42mg

[0072] Glyceryl monostearate 200mg

[0073] Lecithin 90mg

[0074] Oleic acid 14mg

[0075] Preparation method: (1) melt the lipid material glyceryl monostearate in the prescribed amount in a water bath at 60°C; (2) dissolve the prescribed amount of phospholipids, oleic acid, and vinorelbine in ethanol, and then add dropwise (3) After completely removing ethanol under vacuum and decompression conditions, quickly place it in liquid nitrogen to cool; (4) Take it out after being completely frozen, grind it with a mortar, and disperse it in an appropriate amount of 1%F 68 In the aqueous phase, the pH of the aqueous phase is 3.7; (5) mash under the tissue masher, 3000rpm, 6000rpm, each for 15min, to prepare the primary suspension; (6) transfer the prepared primary suspension to a high-...

Embodiment 3

[0078] The vinorelbine solid lipid nanoparticles provided by the present invention are composed of vinorelbine, lipid materials, phospholipids, and oleic acid: vinorelbine 100mg

[0079] Glyceryl monostearate 150mg

[0080] Lecithin 140mg

[0081] Oleic acid 10mg

[0082] Preparation method: (1) melt the lipid material glyceryl monostearate in the prescribed amount in a water bath at 60°C; (2) dissolve the prescribed amount of phospholipids, oleic acid, and vinorelbine in ethanol, and then add dropwise (3) After completely removing ethanol under vacuum and decompression conditions, quickly place it in liquid nitrogen to cool; (4) Take it out after being completely frozen, grind it with a mortar, and disperse it in an appropriate amount of 1%F 68 In the aqueous phase, the pH of the aqueous phase is 4; (5) mash under the tissue masher, 3000rpm, 6000rpm, each 15min, to prepare the primary suspension; (6) transfer the prepared primary suspension to the high-pr...

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Abstract

Disclosed is kind of Vinorelbine solid lipid nanoparticles which comprise (by weight percent) vinorelbine 1-25%, grease material 30-90%, phospholipids 5-50% oleinic acid 0-20%. The preparing process consists of melting liposome material through water-bath, dissolving phosphatides, oleic acid and Vnorelbine with ethanol, dropping into the liposome material, removing ethanol under decompression condition, cooling down and freezing, placing into pH 2-5 aqueous phase, triturating and homogenizing the turbid liquor to obtain the freeze-dried preparation with improved anticancer reactivity of Vinorelbine.

Description

technical field [0001] The invention relates to the technical field of medicine, and more specifically relates to a vinorelbine solid lipid nanoparticle, a freeze-dried preparation of vinorelbine solid lipid nanoparticle and a preparation method thereof. Background technique [0002] With the development and progress of medical technology, human beings have basically controlled the infectious diseases that threatened human health in the past, while non-communicable diseases such as tumors and cardiovascular and cerebrovascular diseases have gradually become the main enemy of human health. According to the report of the World Health Organization in 1997, in 1996, 6.3 million people died of cancer in the world's 5.8 billion people, accounting for about 12% of the total number of deaths, of which nearly 60% died of lung cancer, gastric cancer, breast cancer, colorectal cancer, Oral cancer, liver cancer, cervical cancer and esophageal cancer are the second leading causes of deat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/475A61K9/10A61K9/19A61K9/127A61K9/14A61K47/24A61P35/00
Inventor 游剑胡富强袁弘杜永忠
Owner ZHEJIANG UNIV
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