Anti-cancer medicine 23-hydroxy betulic acid fat emulsion and its preparing method

An anti-tumor drug, fat emulsion technology, applied in the direction of anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve problems such as the inability to effectively solve bioavailability, and achieve the advantages of increasing clinical application dosage forms, improving bioavailability, and significant effect. Effect

Inactive Publication Date: 2005-10-19
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] 23-Hydroxybetulinic acid is a strongly hydrophobic drug, and the general formulation method cannot effectively solve the problem of bioavailability
Due to its strong hydrophobicity, only oral tablets are currently available, which will limit its clinical application

Method used

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  • Anti-cancer medicine 23-hydroxy betulic acid fat emulsion and its preparing method
  • Anti-cancer medicine 23-hydroxy betulic acid fat emulsion and its preparing method
  • Anti-cancer medicine 23-hydroxy betulic acid fat emulsion and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] 23-Hydroxybetulinic acid fat emulsion, which consists of:

[0057] 23-Hydroxybetulinic acid 0.5g

[0058] Soy Lecithin for Injection 5g

[0059] Soybean oil for injection 100g

[0060] Glycerin 18g

[0061] Add water for injection to 1000mL

[0062] The preparation method of above-mentioned fat emulsion:

[0063] 1. Grinding 23-hydroxy betulinic acid so that the particle size of 23-hydroxy betulinic acid is less than 75 μm;

[0064] 2. Weigh the crushed 23-hydroxybetulinic acid of the prescribed amount, add the prescribed amount of soybean oil for injection, and mix well to form the oil phase;

[0065] 3. Weigh soybean lecithin for injection, glycerin and appropriate amount of water for injection (at least to completely dissolve the phospholipid into the water phase) of the prescribed amount, and stir at high speed (8000-20000 rpm) after mixing to completely dissolve into the water phase;

[0066] 4. Under the condition of high-speed stirring, add the oil phase in...

Embodiment 2、3、4

[0072] The processing step of embodiment 2,3,4 is exactly the same as embodiment 1, and each component and consumption are as shown in table 1 in its prescription:

[0073] Example

Embodiment 5、6、7、8、9、10

[0075] The processing step of embodiment 5,6,7,8,9,10 is exactly the same as embodiment 1, and each component and consumption are as shown in table 2 in its prescription:

[0076]

Example

active ingredient

(0.5-5g)

vegetable oil

(100-250g)

Emulsifier

(5-20g)

osmotic regulator

(18-25g)

5

23-Hydroxybetulinic acid

Corn oil

Soy lecithin

glucose

6

23-Hydroxybetulinic acid

sesame oil

Lecithin

Mannitol

7

23-Hydroxybetulinic acid

olive oil

Soy lecithin

Sorbitol

8

23-Hydroxybetulinic acid

linseed oil

Lecithin

glucose

9

23-Hydroxybetulinic acid

saffron oil

Soy lecithin

Mannitol

10

23-Hydroxybetulinic acid

fatty acid triglycerides

Lecithin

Sorbitol

[0077] In the foregoing examples, the vegetable oil soybean oil used for injection can also be replaced...

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PUM

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Abstract

The present invention relates to 23-hyroxy betulic acid fat emulsion as anticancer medicine and its preparation process, and belongs to the field of Chinese medicine and medicament preparation technology. The fat emulsion consists of 23-hyroxy betulic acid as active component and medicinal supplementary material, and includes 23-hyroxy betulic acid in 0.5-5 g / L, emulsifier for injection in 5-20 g / L, vegetable oil for injection in 100-250 g / L and osmotic pressure regulator in 18-25 g / L except water for injection. The present invention has simple preparation process, and the prepared 23-hyroxy betulic acid fat emulsion with antitumor effect may be orally taken or intravenously injected. The prepared 23-hyroxy betulic acid fat emulsion has low toxicity, high bioavailability, slow releasing, targeting, and body energy providing effect.

Description

technical field [0001] The invention relates to an antitumor drug 23-hydroxybetulinic acid fat emulsion and a preparation method thereof, belonging to the technical field of traditional Chinese medicine and pharmaceutical preparations. Background technique [0002] With the changes of human living environment, living standard and lifestyle and the advancement of medicine, the spectrum of diseases has undergone significant changes, and malignant tumors have become one of the major diseases that are increasingly common and seriously threaten human life and quality of life. At present, cancer has become the second leading cause of death in the world and even in China. According to statistics from the Ministry of Health, in recent years, there are 2 million new cancer patients in China every year, and more than 1.3 million deaths. At present, the total number of cancer patients in the country is about 4.5 million. Such a large number of cancer patients has formed a huge market ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/56A61P35/00
Inventor 王广基杨敏叶文才项景德曹国宪徐宇平王颂佩
Owner CHINA PHARM UNIV
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