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Stable stored composite emulsion carrier in even dimension for hydrophilicity medication and preparation method

A hydrophilic drug, homogeneous technology for emulsion delivery, oil/fat/wax non-active ingredients, etc.

Inactive Publication Date: 2005-03-30
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, about 15% of the drug was still released after 30 days of storage

Method used

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  • Stable stored composite emulsion carrier in even dimension for hydrophilicity medication and preparation method
  • Stable stored composite emulsion carrier in even dimension for hydrophilicity medication and preparation method
  • Stable stored composite emulsion carrier in even dimension for hydrophilicity medication and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 (add the mixture of lecithin and cholesterol in the oil phase)

[0034] The microporous membrane with a pore size of 7 μm is soaked in a hydrophilic substance to fully wet the porous membrane. 2.5 ml of glucose aqueous solution of mitomycin C was prepared, the glucose concentration was 5.8 wt %, and the amount of mitomycin C added was 2.67 mg / ml water. The aqueous solution is mixed with 5.0 ml of lipiodol (cholesterol content: 0.1-2.0 wt %) dissolved with lecithin and cholesterol at a molar ratio of 1:1, and the volume ratio of the oil-water phase is 2:1. Emulsify with a homogeneous emulsifier for 3 minutes to obtain W / O colostrum. Add the water-soluble suspension stabilizer and emulsifier into 100ml of water, stir until completely dissolved as the external water phase. Use 0.085Kgf / cm of 8.0g of W / O type colostrum 2 The constant pressure is pressed into the outer water phase through the hydrophilic microporous membrane with uniform pore size to obtain t...

Embodiment 2

[0039] Embodiment 2 (add the mixture of lecithin and cholesterol in the oil phase)

[0040] The microporous membrane with a pore size of 7 μm is soaked in a hydrophilic substance to fully wet the porous membrane. An aqueous glucose solution of mitomycin C was prepared, the glucose concentration was 5.8 wt%, and the amount of mitomycin C added was 2.4 mg / ml water. This aqueous solution is mixed with 5 ml of super liquefied iodized oil (dissolved with oil-soluble emulsifier) ​​that is dissolved in lecithin and cholesterol (cholesterol content 0.4%) with a molar ratio of 2:1, and the volume ratio of the oil-water phase is 3:1. Emulsify with a homogeneous emulsifier for 3 minutes to obtain W / O colostrum. Add the water-soluble suspension stabilizer and emulsifier into 100ml of water, stir until completely dissolved as the external water phase. Use 0.085Kgf / cm of 8.0g of W / O type colostrum 2 The constant pressure is pressed into the outer water phase through the hydrophilic micro...

Embodiment 3

[0042] Embodiment 3 (in the internal aqueous phase, add internal albumin)

[0043] The microporous membrane with a pore size of 7 μm is soaked in a hydrophilic substance to fully wet the porous membrane. The glucose aqueous solution of doxorubicin was prepared, the glucose concentration was 5.8wt%, the added concentration of bovine serum albumin was 0.5wt%, and the added amount of doxorubicin was 12.0mg / ml water. The aqueous solution was mixed with 5 ml of lipiodol (dissolved with an oil-soluble emulsifier), and the volume ratio of the oil-water phase was 3:1. Emulsify with a homogeneous emulsifier for 3 minutes to obtain W / O colostrum. Add 1.0 g of water-soluble suspension stabilizer and emulsifier into 100 ml of water, stir until completely dissolved as the external water phase. Use 0.085Kgf / cm of 8.0g of W / O type colostrum 2 The constant pressure is pressed into the outer water phase through the hydrophilic microporous membrane with uniform pore size to obtain a W / O / W ty...

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Abstract

A composite emulsion as the carrier of hydrophilic medicine for blocking the artery of cancer in order to apply chemicotherapy is prepared through adding albumin to internal water phase or lecithin or cholesterol to oil phase, mixing the aqueous solution containing hydrophilic medicine with the oil substance containing emulsifier, emulsifying the obtain oil-in-water emulsion, and using pressure to make it pass through millipore membrane into external water phase. Its advantages are high size uniformity and high storage stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations of medical engineering. Background technique [0002] Many anticancer drugs, proteins and other biologically active drugs are hydrophilic drugs, for example, mitomycin C, doxorubicin, cisplatin, tumor necrosis factor, etc. are commonly used hydrophilic anticancer drugs, these drugs If it is directly injected into the human body, it will be randomly distributed in various parts of the human body, which will have a serious killing effect on normal cells and cause the body's immunity to decrease. At the same time, these low-molecular drugs will be quickly filtered by the glomerulus and excreted from the body. To keep the drug concentration in the blood above the effective therapeutic concentration, frequent medication is necessary, which causes great side effects on the human body. Therefore, the embedding of highly toxic drugs with large side effects and short half-life, increasing their...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/44
Inventor 马光辉邵辉苏志国
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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