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

A solid lipid nanometer and vinorelbine technology, applied in the field of medicine, can solve the problems of strong blood vessel irritation, high operation temperature, and poor patient compliance, and achieve the goal of avoiding drug degradation, instability, and direct contact Effect

Inactive Publication Date: 2008-02-27
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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

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

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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 14 mg

[0065] Glyceryl monostearate 200mg

[0066] Lecithin 90mg

[0067] Oleic acid 14mg

[0068] Preparation method: (1) Melt the prescription amount of lipid material glycerol monostearate under 60℃ water bath conditions; (2) Dissolve the prescription amount of phospholipid, oleic acid, and vinorelbine in ethanol, and then add dropwise Into the molten lipid material; (3) After the ethanol is completely removed under vacuum and reduced pressure, it is quickly placed in liquid nitrogen to cool; (4) When it is completely frozen, it is taken out, pulverized with a mortar, and dispersed in an appropriate amount of containing 1% F 68 In the aqueous phase, the pH of the aqueous phase is 4; (5) The tissue masher is mashed, 3000rpm, 6000rpm, 15min each to prepare the primary suspension; (6) The prepared primar...

Embodiment 2

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

[0072] Glyceryl monostearate 200mg

[0073] Lecithin 90mg

[0074] Oleic acid 14mg

[0075] Preparation method: (1) Melt the prescription amount of lipid material glycerol monostearate under 60℃ water bath conditions; (2) Dissolve the prescription amount of phospholipid, oleic acid, and vinorelbine in ethanol, and then add dropwise Into the molten lipid material; (3) After the ethanol is completely removed under vacuum and reduced pressure, it is quickly placed in liquid nitrogen to cool; (4) When it is completely frozen, it is taken out, pulverized with a mortar, and dispersed in an appropriate amount of 1% F 68 In the aqueous phase, the pH of the aqueous phase is 3.7; (5) The tissue masher is mashed, 3000rpm, 6000rpm, 15min each to prepare the primary suspension; (6) The prepared primary suspe...

Embodiment 3

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

[0079] Glyceryl monostearate 150mg

[0080] Lecithin 140mg

[0081] Oleic acid 10mg

[0082] Preparation method: (1) Put the prescription amount of lipid material glyceryl monostearate at 60. Melt in a water bath at ℃; (2) Dissolve the prescribed amount of phospholipids, oleic acid, and vinorelbine in ethanol, and then add them dropwise to the molten lipid material; (3) After the ethanol is completely removed under vacuum and reduced pressure , Quickly place it in liquid nitrogen to cool; (4) Take it out after it is 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) The tissue masher is mashed, 3000rpm, 6000rpm, 15min each to prepare the primary suspension; (6) The prepared primary suspension...

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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 to a vinorelbine solid lipid nanoparticle, a freeze-dried vinorelbine solid lipid nanoparticle preparation and their preparation methods. Background technique [0002] With the development and advancement of medical technology, humans have basically controlled the infectious diseases that mainly threatened human health in the past, while non-communicable diseases such as tumors and cardiovascular and cerebrovascular diseases have gradually become the main enemies of human health. According to a report by the World Health Organization in 1997, 6.3 million people died of cancer in 1996, accounting for about 12% of the total deaths of 5.8 billion people worldwide, and nearly 60% of them died of lung cancer, stomach cancer, breast cancer, colorectal cancer, Oral cancer, liver cancer, cervical cancer and esophageal cancer are the second leading causes of death after cardiovascular di...

Claims

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Application Information

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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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