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Stable medicament lipid complexes

A lipid complex and drug technology, applied in the field of medicine, can solve problems such as nephrotoxicity and vascular stimulation

Inactive Publication Date: 2008-12-17
广州瑞济生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs usually have problems such as vascular stimulation and nephrotoxicity, which cannot be solved by solubilization. The purpose of the present invention is to overcome the defects in the above-mentioned prior art and provide a stable lipoplex and its preparation method

Method used

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  • Stable medicament lipid complexes
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] formula:

[0016] Sodium cholesteryl sulfate 0.35g (about 0.71mmol)

[0017] Clarithromycin 0.5g (about 0.66mmol)

[0018] Egg yolk lecithin 0.75g (about 0.96mmol)

[0019] Weigh cholesterol sodium sulfate and clarithromycin respectively according to the formula and put them in a 100ml beaker, add 15ml of dimethyl sulfoxide, keep warm in a water bath at 45°C, stir continuously to dissolve; and weigh egg yolk lecithin according to the formula and put them in a 50ml beaker , add 12ml of ethanol, stir continuously to dissolve, keep warm in 45°C water bath. Slowly pour the ethanol solution of phospholipids into the above dimethyl sulfoxide solution, stir gently to mix evenly, keep warm in a water bath at 45°C for later use. Draw the above drug solution with a syringe, and put it into the pH7.2 tris buffer solution at a speed of 5 ml / min until all the drug solution is injected to obtain the clarithromycin lipoplex suspension. During injection, the buffer should be stirre...

Embodiment 2

[0022] formula:

[0023] Sodium cholesteryl sulfate 0.2g (about 0.41mmol)

[0024] Sodium cholesteryl phosphate 0.15g (about 0.291mmol)

[0025] Clarithromycin 0.5g (about 0.67mmol)

[0026] Egg yolk lecithin 0.5g (about 0.64mmol)

[0027] Soy lecithin 0.25g (about 0.32mmol)

[0028]Weigh cholesterol sodium sulfate, cholesterol sodium phosphate, and clarithromycin according to the formula respectively, put them in a 100ml beaker, add 15ml of dimethyl sulfoxide, keep warm in a water bath at 45°C, stir continuously to dissolve; and weigh egg yolk lecithin according to the formula Put soybean lecithin and soybean lecithin in a 50ml beaker, add 12ml ethanol, stir continuously to dissolve, and keep warm in a water bath at 45°C. Slowly pour the ethanol solution of phospholipids into the above dimethyl sulfoxide solution, stir gently to mix evenly, keep warm in a water bath at 45°C for later use. Draw the above drug solution with a syringe, and inject / inject it into the pH7.2 bu...

Embodiment 3

[0031] formula:

[0032] Amphotericin B 0.5g (about 0.54mmol)

[0033] Sodium Cholesterol Phosphate 0.3g (about 0.58mmol)

[0034] Egg yolk lecithin 0.5g (about 0.64mmol)

[0035] Weigh amphotericin B and cholesteryl sodium phosphate according to the formula, put them in a 100ml beaker, add 15ml of dimethyl sulfoxide, keep warm in a water bath at 45°C, and stir continuously to dissolve; in addition, weigh egg yolk lecithin according to the formula and dissolve it in 10ml In slightly hot ethanol, slowly add the dimethyl sulfoxide solution of the above drug, and stir to mix evenly. Keep warm in a 45°C water bath for later use. Use a syringe to draw the above drug solution and slowly inject it into the pH7.2 buffer solution. This process should be stirred slowly to accelerate the diffusion of the organic phase. After the drug solution is injected, the amphotericin B lipoplex suspension is obtained, the organic solvent and a small amount of free drug are removed, and concentra...

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Abstract

The invention relates to a stable medical lipid composite; the drug molecules which are insoluble or slightly water-soluble under physiological conditions and the amphiphatic molecules of cholesterin derivant and phospholipid are caused to form the lipid composite and further prepare the drug preparation.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a stable drug lipid complex and a preparation method thereof. Background technique [0002] Insoluble drugs are insoluble in water during parenteral administration, so it is often necessary to make the drug into a water-soluble salt or use non-aqueous solvents, compound solvents, and surfactants to increase the solubility of the drug. Although these methods can solve the problem of drug solubility However, it usually does not reduce the irritation and toxicity of the drug, but instead increases it. In clinical application, it will cause serious side effects such as vascular irritation, and there are many restrictions when using it: there is pain when it is used in high concentrations, and it is difficult to use other intravenous fluids Dilution also produces drug precipitation; if the injection speed is too fast, the drug will precipitate in the blood vessel. [0003] In order ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/28A61K47/24A61K45/00A61K9/14
Inventor 关世侠李海刚
Owner 广州瑞济生物技术有限公司
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