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Vinorelbine emulsion and its preparing method

A technology of vinorelbine and rebin emulsion, applied in the field of antitumor drug preparations and preparation thereof, can solve the problems affecting clinical safety and clinical efficacy, poor patient compliance, strong vascular irritation and the like

Inactive Publication Date: 2005-07-06
李晓祥
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0030] Take 2g of vinorelbine, 20g of soybean lecithin, 4g of soybean oil, 6g of cholesterol, and 1g of vitamin E, and mix them evenly to obtain an oil phase A solution; take 20g of glycerin and 6g of poloxamer, dissolve them in water, and dissolve them in 800ml to obtain an aqueous phase B. Described water is water for injection (the same below).

[0031] Add the oil phase A to the water phase B, grind and emulsify into colostrum, adjust the pH value to 8 with 1M NaOH, add water to a volume of 1000ml, and then emulsify with a homogenizer to prepare an emulsion. Divide into 100ml volume, and turn into oral emulsion after rotary sterilization. Or pass through a 0.45μm microporous membrane and then pack and sterilize.

[0032] The above-mentioned emulsion is sterilized and filtered through a 0.22 μm microporous membrane, then sub-packaged with a volume of 5 ml, and sterilized by a rotary sterilizer to form an injection emulsion.

example 2

[0034] Take 2g of vinorelbine, 25g of lecithin, 4g of castor oil, 6g of cholesterol, and 1g of vitamin E, and mix them evenly to obtain an oil phase A solution; take 20g of glycerin and 6g of poloxamer, dissolve them in water, and dissolve them in 800ml to obtain an aqueous phase B.

[0035] Add the oil phase A to the water phase B, grind and emulsify into colostrum, adjust the pH value to 8 with 1M NaOH, add water to a volume of 1000ml, and then emulsify with a homogenizer to prepare an emulsion.

[0036] After sterilizing and filtering through a microporous membrane of 0.22 μm, it is divided into 5 ml and sterilized by a rotary sterilizer to form an injection emulsion.

example 3

[0038] Take 5g of vinorelbine, 30g of soybean lecithin, 5g of soybean oil, 1g of cholesterol, and 0.5g of vitamin E, and mix them evenly to obtain an oil phase A solution; take 10g of glycerin and 3g of mannitol, dissolve them in water, and dissolve them in 800ml to obtain an aqueous phase B.

[0039] Add the oil phase A to the water phase B, grind and emulsify into colostrum, adjust the pH value to 8 with 1M NaOH, add water to a volume of 1000ml, and then emulsify with a homogenizer to prepare an emulsion.

[0040] After being sterilized and filtered through a microporous membrane of 0.22 μm, it is divided into 2 ml and freeze-dried to form a freeze-dried injection emulsion.

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Abstract

The invention relates to a vinorelbine emulsion which comprises (by weight ratio) vinorelbine 0.001-10%, emulsifying agent 0.1-20%, triglyceride compounds 0.1-30%, osmoregulation agent 0.1-10%, stabilizing agent 0.05-5%, anti-oxidant 0.01-5%, and balancing water for injection. The invention has the advantages of increased medicament stability and improved curative effect.

Description

1. Technical field [0001] The invention relates to an antitumor drug preparation and a preparation method thereof, specifically a vinorelbine emulsion and a preparation method thereof. 2. Background technology [0002] Vinorelbine is a semi-synthetic vinblastine antitumor drug with high anticancer activity and broad antitumor spectrum. Its mechanism of action is basically the same as that of vinblastine (VLB) and vincristine (VCR). Antineoplastic drugs that inhibit cell division, act directly on the dynamic balance of tubulin / microtubules, inhibit the polymerization of tubulin, and disintegrate microtubules during division, and only affect axonal microtubules at high concentrations. The effect of tubulin helicalization is lower than that of vincristine, by blocking the mitosis of G2 and M phase cells, leading to cell death in interphase or anaphase; after intravenous administration, the pharmacokinetics show a three-compartment model, and the terminal phase is averaged The ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/475A61P35/00
Inventor 李德刚李爱玲万贺蕾
Owner 李晓祥
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