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Application of calcium disodium edetate in preparation of medicine for inhibiting connective tissue growth factor and monoamine oxidase of human beings and mammal

A technology of edetate calcium sodium and monoamine oxidase, which is applied in drug delivery, drug combination, and pharmaceutical formulation, etc., can solve problems such as poor therapeutic effect, achieve the effects of reducing total dosage, achieving targeted enrichment, and good therapeutic effect

Inactive Publication Date: 2010-07-21
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above-mentioned CTGF and MAO are all enzymes or factors that play an important role in pulmonary fibrosis. The therapeutic drugs in the prior art have poor therapeutic effect because they cannot target the pathogenic factors of pulmonary fibrosis.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The formula of liposome solution:

[0038] Edetate Calcium Sodium 1g Soy Lecithin 20g Cholesterol 2g α-Tocopherol 1g

[0039] 0.2M Phosphate Buffer with pH=7.0 100ml

[0040] Glucose 50g

[0041] Water for injection to 1000ml

[0042] Preparation:

[0043] Weigh the prescribed amount of phospholipids, cholesterol, α-tocopherol and dissolve them in methylene chloride / methanol (V:V=1:1), add 500ml of water for injection into the prescribed amount of edetate calcium sodium, and use ultrasonic emulsification for 30min. The obtained emulsion was evaporated under reduced pressure at 37°C to remove the solvent, and when the emulsion formed a viscous gel-like liquid, the remaining water for injection, phosphate buffer and glucose were added, and the solvent was continuously evaporated under reduced pressure at 37°C. Ultrasonic emulsification to obtain a liposome solution, the liposome solution was frozen overnight at -20°C, and then completely melted at room temperature; th...

Embodiment 2

[0045] Liposome Solution Formula:

[0046] Edetate Calcium Sodium 2g Dipalmitoyl Phosphatidylglycerol 15g Cholesterol 5g α-Tocopherol 1g

[0047] 0.2M Phosphate Buffer with pH=6.5 100ml

[0048] Sodium chloride 9g

[0049] Water for injection to 1000ml

[0050] prepare

[0051] Weigh 1 g of phospholipids, cholesterol, and α-tocopherol in the prescribed amount and dissolve them in an appropriate amount of absolute ethanol, add 500 ml of water for injection mixed with the prescribed amount of edetate calcium sodium, evaporate under reduced pressure to remove the solvent, add the remaining water for injection and phosphoric acid For salt buffer and sodium chloride, continue to evaporate the solvent under reduced pressure at 37°C, and use a high-pressure homogenizer to process the remaining solution twice at 1200bar, and make up for the evaporated water for injection to obtain 0.2% calcium sodium edetate Liposome injection. Using a Mastersizer 2000 particle size analyzer, usi...

Embodiment 3

[0053] Liposome Solution Formula:

[0054] Edetate Calcium Sodium 5g Dipalmitoylphosphatidylcholine 25g, Cholesterol 1.25g

[0055] 50ml of 0.2M phosphate buffer solution with pH=6.8 Glucose 50g

[0056] Water for injection to 1000ml

[0057] Prepare 0.5% edetate calcium sodium liposome injection as in Example 1. Using a Mastersizer 2000 particle size analyzer, using deionized water as the dispersion medium, the volume average particle size of the samples was measured to be 8.05 μm.

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PUM

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Abstract

The invention relates to the application of calcium disodium edetate in the preparation of medicine for inhibiting connective tissue growth factor and monoamine oxidase of human beings and mammal; the calcium disodium edetate is injection when being applied to prepare the medicine of the diseases, and the injection contains 5-30wt % of calcium disodium edetate and auxiliary material used for the injection; the preferable lung target injection contains 0.1-5wt% of calcium disodium edetate and one or more auxiliary material(s) which is / are applicable to lung target preparation; the lung target injection is microsphere preparation, microcapsule preparation or liposome injection; preferably, the particle sizes of microspheres, microcapsules and liposome are 7-30 mu m; and the lung target preparation is preferably liposome injection liquid.

Description

technical field [0001] The present invention relates to the application of calcium sodium edetate in the preparation of medicines for treating human diseases, an injection of calcium sodium edetate, and a lung-targeted lipid injection. Background technique: [0002] Edetate Calcium Sodium (Ca-Na 2 EDTA) is a kind of metal ion chelating agent, can be used for and can be used for with multiple divalent, trivalent metal chelation, forms stable possible metal complexes, and existing edetate calcium sodium preparation is mainly injection (1g , 5ml) and tablet (0.5g / tablet), mainly used in the clinical treatment of inorganic lead poisoning, for copper, zinc, iron, manganese, cadmium, vanadium, cobalt and certain radioactive elements such as thorium, uranium, radium, Plutonium, etc. also have a certain role in promoting discharge. [0003] Pulmonary fibrosis is the abbreviation of "diffuse interstitial lung disease" or "interstitial lung disease". Pulmonary fibrosis is a large g...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/198A61K9/08A61P11/00
Inventor 李静王虹杨国存程振国于润芳林劼张冬兰吴媛媛肖敏霞张岚刘凯
Owner TIANJIN JINYAO GRP
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