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Antitumor composition

A composition and anti-tumor technology, applied in the direction of anti-tumor drugs, drug combinations, active ingredients of phosphorus compounds, etc., can solve the problems of strong anti-tumor effects, side effects, limited use, and low solubility

Inactive Publication Date: 2007-08-29
SANGI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Platinum, cisplatin (CDDP), carboplatin, and isoproplatin have been used as platinum complexes, but cisplatin with high anti-tumor effect has strong side effects, and its side effects are unbearable for patients, so the use is often limited, and due to Has low solubility in water and is therefore only available in low concentrations
In addition, carboplatin, which has lower side effects than cisplatin, and iproplatin, if the toxicity is reduced, the activity will be reduced, so some satisfactory antitumor effects may not be obtained

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] [Example 1] Adjusted raw materials of platinum tetrachloride 10% hydroxyapatite 90% antitumor agent

[0037] 1. Hydroxyapatite (HAP)

[0038] 2. Platinum tetrachloride (PtCl 4 )

[0039] 3. Sodium hydroxide: pH adjuster

[0040] 4. Citric acid: dispersant

[0041] 1 g of weighed platinum tetrachloride was added to previously distilled water, and after stirring, sodium hydroxide was added to adjust the pH to a neutral range (pH 6.8-7.4). Add 9g of weighed hydroxyapatite to this solution, stir under reduced pressure, add distilled water to this solution, adjust the total amount to 500ml, and carry out about 1 test in a sealed container at a constant temperature of 50-60°C in a dark place. month of stirring.

[0042] Stirring was stopped, concentrated with an evaporator, and freeze-dried to obtain a powder.

[0043]Distilled water was added to the powder to adjust the powder concentration to about 2%, and a dispersant was added to adjust the pH of citric acid to abou...

Embodiment 2

[0057] [Example 2] Adjusted raw materials of platinum hexachloride 10% hydroxyapatite 90% antitumor agent

[0058] 1. Hydroxyapatite (HAP)

[0059] 2. Platinum hexachloride (H 2 PtCl 6 )

[0060] 3. Sodium hydroxide: pH adjuster

[0061] 4. Sodium citrate: dispersant

[0062] 1.005 g of weighed platinum hexachloride was added to previously distilled water, and after stirring, sodium hydroxide was added to adjust the pH to a neutral range (pH6.8-7.4). Add 9 g of weighed hydroxyapatite to this solution, stir under reduced pressure, add distilled water to this solution, adjust the total amount to 200 ml, and stir in a sealed container in a dark place for about 2 months.

[0063] Stirring was stopped and freeze-drying was performed to obtain the powder of platinum hexachloride and hydroxyapatite.

[0064] Distilled water was added to the powder to adjust the powder concentration to about 1%, and sodium citrate was added as a dispersant to make the concentration 10 mM / l.

[...

Embodiment 3

[0072] [Example 3] Raw material for adjustment of sodium hexachloroplatinate 10% hydroxyapatite 90% antitumor agent

[0073] 1. Hydroxyapatite (HAP)

[0074] 2. Sodium hexachloroplatinate (Na 2 PtCl 6 )

[0075] 3. Sodium hydroxide: pH adjuster

[0076] 4. Citric acid: dispersant

[0077] 1 g of weighed sodium hexachloroplatinate was added to previously distilled water, and after stirring, sodium hydroxide was added to adjust the pH to a neutral region (pH 6.8-7.4). Add 9g of weighed hydroxyapatite to the solution, stir under reduced pressure, add distilled water to the solution, adjust the total amount to 500ml, and carry out about 1 hour at a constant temperature of 50-60°C in a sealed container in the dark. months of stirring.

[0078] Stirring was stopped, concentrated with an evaporator, and freeze-dried to obtain a powder.

[0079] Distilled water was added to the powder to adjust the powder concentration to about 2%, and a dispersant was added to adjust the pH of...

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Abstract

Antitumor agents with high antitumor effect have much side-effect, and its activity decreases when the toxicity decreases. Thus, satisfactory antitumor effects are not always obtained. Therefore, development of an antitumor agent having a high antitumor effect, with less side-effect and low toxicity is awaited. The present invention is to provide an antitumor agent of fine particles, wherein platinum chloride, chloroplatinic acids and hydroxyapatite are blend. Platinum chloride and chloroplatinic acids are platinum tetrachloride, tetrachloroplatinate, hexachloroplatinate, disodium platinum tetrachloride, disodium platinum hexachloride, dipotassium platinum tetrachloride, or dipotassium platinum hexachloride. The maximum particle diameter of hydroxyapatite is 1 [mu]m or less.

Description

technical field [0001] The invention relates to an antitumor composition which uses platinum chloride and chloroplatinate as active ingredients, has little side effects, and exhibits particularly excellent anticancer effects on lung cancer. Background technique [0002] Platinum, cisplatin (CDDP), carboplatin, and isoproplatin have been used as platinum complexes, but cisplatin with high anti-tumor effect has strong side effects, and its side effects are unbearable for patients, so the use is often limited, and due to Has low solubility in water and is therefore only available in low concentrations. In addition, carboplatin, iproplatin, which has lower side effects than cisplatin, has lower activity if toxicity is lowered, so some satisfactory antitumor effects may not be obtained. [0003] Therefore, development of antitumor agents with high antitumor effects and low side effects and toxicity is desired. [0004] However, hydroxyapatite is usually composed of Ca 10 (PO ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/24A61K47/04A61P35/00A61K33/243
CPCA61K9/143A61K47/02A61K33/24A61K33/42A61K9/1611A61P35/00A61K33/243A61K2300/00
Inventor 佐久间周治渥美公则菊川馨一郎
Owner SANGI CO LTD
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