Nano-level emulsion containing taxine or hard-soluble medicine

A technology of insoluble drugs and nanoemulsions, applied in medical preparations containing active ingredients, drug combinations, antineoplastic drugs, etc.

Inactive Publication Date: 2005-10-05
张昊
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But no matter what, there is no large-volume taxane preparation for infusion due t

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1 Nanoemulsion of Paclitaxel

[0020] Composition W / V%

[0021] Paclitaxel 0.1%

[0022] Soybean oil for injection 5%

[0023] Soy Lecithin 2%

[0024] VE 0.1%

[0025] Propylene Glycol 1%

[0026] Glycerin 2.5%

[0027] Add 0.003% EDTA-2Na aqueous solution to 100%

[0028] Combine soy lecithin, VE, soybean oil, and N 2 , heated to dissolve under stirring conditions, add paclitaxel to dissolve and let cool to form an oil phase, and mix propylene glycol, glycerin and 0.003% EDTA-2Na aqueous solution for injection to form a water phase, stir the oil-water two-phase into colostrum, and use high-pressure The homogenizer (Mcrofluidizer) is used to make paclitaxel nano-emulsion, filter with 0.22μm filter membrane, pack in 50ml-500ml infusion bottle, pass N 2 , Sterilize at 100°C for 10-15 minutes after plugging and capping.

Embodiment 2

[0029] Example 2 Nanoemulsion of Paclitaxel

[0030] Composition W / V%

[0031] Paclitaxel 0.1%

[0032] Soybean Oil for Injection 2.5%

[0033] Medium Chain Triglycerides (MCT) 2.5%

[0034] Soyphospholipids for Injection 2%

[0035] VE 0.1%

[0036] PEG 400 1%

[0037] Glycerin 2.5%

[0038]Add water for injection to 10%

[0039] Paclitaxel, soybean oil, MCT, soybean lecithin, V E After dissolving with an appropriate amount of ethanol, use a rotary evaporator to remove the ethanol to obtain an oily phase, and dissolve the PEG 400 , Glycerin and water for injection are mixed to obtain an aqueous phase, and the subsequent operation is the same as in Example 1.

Embodiment 3

[0040] Example 3 Nanoemulsion of Paclitaxel

[0041] Composition W / V%

[0042] Paclitaxel 0.1%

[0043] Safflower Oil for Injection 5%

[0044] Soyphospholipids for Injection 2%

[0045] Pluronic F68 0.1%

[0046] VE 0.1%

[0047] Glycerin 2.5%

[0048] Ethanol 1%

[0049] Add water for injection to 100%

[0050] Method of making is the same as embodiment 1

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Abstract

The invention relates to a composition containing taxine compounds, which including taxine compounds, oil, water, surfactant, cosurfactant, stability, and an osmotic pressure regulator. The inventive composition is used in an emulsion form of oil-in-water, and the taxine grain diameter in the emulsion is nano-size, so it is called as nano-emulsion.

Description

field of invention [0001] The present invention relates to taxoid-containing compositions comprising a taxoid, oil, water, a surfactant and a co-surfactant. The composition of the present invention is used in the form of an oil-in-water emulsion, and the particle size of the taxine in the emulsion is nanoscale, so it can also be called a nanoemulsion. Background of the invention [0002] Paclitaxel (paclitaxel, I), as a member of taxine compounds, is extracted and isolated from Taxus plants of the family Taxaceae, and is an effective drug for treating various tumors. Paclitaxel itself is almost insoluble in water, so currently clinically used preparations such as Taxol (U.S. Bristol-Myers-squibb company), Anzatax® (Australian Faulding company) and domestic percolin®, Taxol® and other commodities are all polyoxygen compounds of I. Ethylene castor oil (Cremophor EL) and ethanol (50:50 (V / V)) mixed solution. The Cremophor EL in the prescription has a good solubilizing effect ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61P35/00
Inventor 张钧寿
Owner 张昊
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